JPS6338037B2 - - Google Patents
Info
- Publication number
- JPS6338037B2 JPS6338037B2 JP55162723A JP16272380A JPS6338037B2 JP S6338037 B2 JPS6338037 B2 JP S6338037B2 JP 55162723 A JP55162723 A JP 55162723A JP 16272380 A JP16272380 A JP 16272380A JP S6338037 B2 JPS6338037 B2 JP S6338037B2
- Authority
- JP
- Japan
- Prior art keywords
- thio
- lincosaminide
- methyl
- substituted
- acid
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired
Links
- 150000001875 compounds Chemical class 0.000 claims description 100
- 239000002253 acid Substances 0.000 claims description 34
- -1 amine compound Chemical class 0.000 claims description 27
- 125000000217 alkyl group Chemical group 0.000 claims description 19
- 150000003839 salts Chemical class 0.000 claims description 19
- 125000001997 phenyl group Chemical class [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 9
- 229910052736 halogen Inorganic materials 0.000 claims description 8
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 7
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 7
- 125000000547 substituted alkyl group Chemical group 0.000 claims description 7
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical group C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims description 6
- 125000004432 carbon atom Chemical group C* 0.000 claims description 6
- 150000002367 halogens Chemical class 0.000 claims description 6
- 229910052760 oxygen Inorganic materials 0.000 claims description 6
- 229910052739 hydrogen Inorganic materials 0.000 claims description 5
- 239000001301 oxygen Substances 0.000 claims description 5
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims description 5
- 229910019142 PO4 Inorganic materials 0.000 claims description 4
- 239000010452 phosphate Substances 0.000 claims description 4
- 239000001257 hydrogen Substances 0.000 claims description 3
- 229910052757 nitrogen Inorganic materials 0.000 claims description 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 3
- 150000002829 nitrogen Chemical class 0.000 claims description 3
- 150000002926 oxygen Chemical class 0.000 claims description 3
- 125000000524 functional group Chemical group 0.000 claims description 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 2
- 150000002431 hydrogen Chemical class 0.000 claims 2
- 239000000203 mixture Substances 0.000 description 54
- 238000000034 method Methods 0.000 description 33
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 28
- 239000004615 ingredient Substances 0.000 description 23
- 239000003826 tablet Substances 0.000 description 21
- 239000000243 solution Substances 0.000 description 20
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 19
- 229910001868 water Inorganic materials 0.000 description 19
- 235000019271 petrolatum Nutrition 0.000 description 17
- 238000011282 treatment Methods 0.000 description 17
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 15
- 235000001014 amino acid Nutrition 0.000 description 15
- 150000001413 amino acids Chemical class 0.000 description 15
- 239000002775 capsule Substances 0.000 description 14
- 239000012458 free base Substances 0.000 description 13
- 239000007788 liquid Substances 0.000 description 13
- 239000000463 material Substances 0.000 description 13
- 238000006467 substitution reaction Methods 0.000 description 13
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 12
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 12
- 239000004264 Petrolatum Substances 0.000 description 11
- 239000002674 ointment Substances 0.000 description 11
- 229940066842 petrolatum Drugs 0.000 description 11
- 241001465754 Metazoa Species 0.000 description 10
- XLOMVQKBTHCTTD-UHFFFAOYSA-N Zinc monoxide Chemical compound [Zn]=O XLOMVQKBTHCTTD-UHFFFAOYSA-N 0.000 description 10
- 238000003756 stirring Methods 0.000 description 10
- 239000000725 suspension Substances 0.000 description 10
- DPVJWUUBZWFDPG-XEDDUELXSA-N (2s,4r)-n-[(1s,2s)-2-chloro-1-[(2r,3r,4s,5r,6r)-3,4,5-trihydroxy-6-methylsulfanyloxan-2-yl]propyl]-4-ethylpiperidine-2-carboxamide;hydrochloride Chemical compound Cl.C1[C@H](CC)CCN[C@@H]1C(=O)N[C@H]([C@H](C)Cl)[C@@H]1[C@H](O)[C@H](O)[C@@H](O)[C@@H](SC)O1 DPVJWUUBZWFDPG-XEDDUELXSA-N 0.000 description 9
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 description 9
- 208000015181 infectious disease Diseases 0.000 description 9
- 230000000844 anti-bacterial effect Effects 0.000 description 8
- 239000002552 dosage form Substances 0.000 description 8
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 8
- LXCFILQKKLGQFO-UHFFFAOYSA-N methylparaben Chemical compound COC(=O)C1=CC=C(O)C=C1 LXCFILQKKLGQFO-UHFFFAOYSA-N 0.000 description 8
- 239000000047 product Substances 0.000 description 8
- 239000011787 zinc oxide Substances 0.000 description 8
- 235000014692 zinc oxide Nutrition 0.000 description 8
- 241000700159 Rattus Species 0.000 description 7
- 241000191967 Staphylococcus aureus Species 0.000 description 7
- 239000003814 drug Substances 0.000 description 7
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 description 6
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 6
- ZMANZCXQSJIPKH-UHFFFAOYSA-N Triethylamine Chemical compound CCN(CC)CC ZMANZCXQSJIPKH-UHFFFAOYSA-N 0.000 description 6
- 239000004480 active ingredient Substances 0.000 description 6
- 238000004458 analytical method Methods 0.000 description 6
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 description 6
- 229960002227 clindamycin Drugs 0.000 description 6
- KDLRVYVGXIQJDK-AWPVFWJPSA-N clindamycin Chemical compound CN1C[C@H](CCC)C[C@H]1C(=O)N[C@H]([C@H](C)Cl)[C@@H]1[C@H](O)[C@H](O)[C@@H](O)[C@@H](SC)O1 KDLRVYVGXIQJDK-AWPVFWJPSA-N 0.000 description 6
- 229940079593 drug Drugs 0.000 description 6
- 239000000546 pharmaceutical excipient Substances 0.000 description 6
- 239000007787 solid Substances 0.000 description 6
- 230000009885 systemic effect Effects 0.000 description 6
- 238000012360 testing method Methods 0.000 description 6
- 239000003871 white petrolatum Substances 0.000 description 6
- VHRSUDSXCMQTMA-PJHHCJLFSA-N 6alpha-methylprednisolone Chemical compound C([C@@]12C)=CC(=O)C=C1[C@@H](C)C[C@@H]1[C@@H]2[C@@H](O)C[C@]2(C)[C@@](O)(C(=O)CO)CC[C@H]21 VHRSUDSXCMQTMA-PJHHCJLFSA-N 0.000 description 5
- 229920001817 Agar Polymers 0.000 description 5
- 241000894006 Bacteria Species 0.000 description 5
- SBKRTALNRRAOJP-BWSIXKJUSA-N N-[(2S)-4-amino-1-[[(2S,3R)-1-[[(2S)-4-amino-1-oxo-1-[[(3S,6S,9S,12S,15R,18R,21S)-6,9,18-tris(2-aminoethyl)-15-benzyl-3-[(1R)-1-hydroxyethyl]-12-(2-methylpropyl)-2,5,8,11,14,17,20-heptaoxo-1,4,7,10,13,16,19-heptazacyclotricos-21-yl]amino]butan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-1-oxobutan-2-yl]-6-methylheptanamide (6S)-N-[(2S)-4-amino-1-[[(2S,3R)-1-[[(2S)-4-amino-1-oxo-1-[[(3S,6S,9S,12S,15R,18R,21S)-6,9,18-tris(2-aminoethyl)-15-benzyl-3-[(1R)-1-hydroxyethyl]-12-(2-methylpropyl)-2,5,8,11,14,17,20-heptaoxo-1,4,7,10,13,16,19-heptazacyclotricos-21-yl]amino]butan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-1-oxobutan-2-yl]-6-methyloctanamide sulfuric acid Polymers OS(O)(=O)=O.CC(C)CCCCC(=O)N[C@@H](CCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CCN)C(=O)N[C@H]1CCNC(=O)[C@@H](NC(=O)[C@H](CCN)NC(=O)[C@H](CCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CCN)NC1=O)[C@@H](C)O.CC[C@H](C)CCCCC(=O)N[C@@H](CCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CCN)C(=O)N[C@H]1CCNC(=O)[C@@H](NC(=O)[C@H](CCN)NC(=O)[C@H](CCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CCN)NC1=O)[C@@H](C)O SBKRTALNRRAOJP-BWSIXKJUSA-N 0.000 description 5
- 108010093965 Polymyxin B Proteins 0.000 description 5
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 description 5
- 239000008272 agar Substances 0.000 description 5
- 150000001412 amines Chemical class 0.000 description 5
- 239000003242 anti bacterial agent Substances 0.000 description 5
- 229940088710 antibiotic agent Drugs 0.000 description 5
- 239000000706 filtrate Substances 0.000 description 5
- 239000007903 gelatin capsule Substances 0.000 description 5
- 230000002401 inhibitory effect Effects 0.000 description 5
- 239000003921 oil Substances 0.000 description 5
- 235000019198 oils Nutrition 0.000 description 5
- 229960003548 polymyxin b sulfate Drugs 0.000 description 5
- 239000000843 powder Substances 0.000 description 5
- 238000002360 preparation method Methods 0.000 description 5
- 239000007858 starting material Substances 0.000 description 5
- 239000000126 substance Substances 0.000 description 5
- 229960004306 sulfadiazine Drugs 0.000 description 5
- SEEPANYCNGTZFQ-UHFFFAOYSA-N sulfadiazine Chemical compound C1=CC(N)=CC=C1S(=O)(=O)NC1=NC=CC=N1 SEEPANYCNGTZFQ-UHFFFAOYSA-N 0.000 description 5
- 229960002597 sulfamerazine Drugs 0.000 description 5
- QPPBRPIAZZHUNT-UHFFFAOYSA-N sulfamerazine Chemical compound CC1=CC=NC(NS(=O)(=O)C=2C=CC(N)=CC=2)=N1 QPPBRPIAZZHUNT-UHFFFAOYSA-N 0.000 description 5
- 229910052717 sulfur Inorganic materials 0.000 description 5
- 239000011593 sulfur Substances 0.000 description 5
- 239000000829 suppository Substances 0.000 description 5
- 239000006188 syrup Substances 0.000 description 5
- 235000020357 syrup Nutrition 0.000 description 5
- 230000001225 therapeutic effect Effects 0.000 description 5
- HEDRZPFGACZZDS-UHFFFAOYSA-N Chloroform Chemical compound ClC(Cl)Cl HEDRZPFGACZZDS-UHFFFAOYSA-N 0.000 description 4
- DGMPVYSXXIOGJY-UHFFFAOYSA-N Fusaric acid Chemical compound CCCCC1=CC=C(C(O)=O)N=C1 DGMPVYSXXIOGJY-UHFFFAOYSA-N 0.000 description 4
- 229930006000 Sucrose Natural products 0.000 description 4
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 description 4
- 239000004098 Tetracycline Substances 0.000 description 4
- 150000007513 acids Chemical class 0.000 description 4
- 239000003054 catalyst Substances 0.000 description 4
- 238000006243 chemical reaction Methods 0.000 description 4
- 238000004587 chromatography analysis Methods 0.000 description 4
- 238000011049 filling Methods 0.000 description 4
- 238000001914 filtration Methods 0.000 description 4
- 210000002196 fr. b Anatomy 0.000 description 4
- 239000008187 granular material Substances 0.000 description 4
- 235000019359 magnesium stearate Nutrition 0.000 description 4
- 239000002609 medium Substances 0.000 description 4
- 239000004292 methyl p-hydroxybenzoate Substances 0.000 description 4
- 235000010270 methyl p-hydroxybenzoate Nutrition 0.000 description 4
- 229960002216 methylparaben Drugs 0.000 description 4
- 229960004584 methylprednisolone Drugs 0.000 description 4
- 239000000244 polyoxyethylene sorbitan monooleate Substances 0.000 description 4
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 description 4
- 229940068968 polysorbate 80 Drugs 0.000 description 4
- 229920000053 polysorbate 80 Polymers 0.000 description 4
- 230000002829 reductive effect Effects 0.000 description 4
- 238000001228 spectrum Methods 0.000 description 4
- UCSJYZPVAKXKNQ-HZYVHMACSA-N streptomycin Chemical compound CN[C@H]1[C@H](O)[C@@H](O)[C@H](CO)O[C@H]1O[C@@H]1[C@](C=O)(O)[C@H](C)O[C@H]1O[C@@H]1[C@@H](NC(N)=N)[C@H](O)[C@@H](NC(N)=N)[C@H](O)[C@H]1O UCSJYZPVAKXKNQ-HZYVHMACSA-N 0.000 description 4
- 239000005720 sucrose Substances 0.000 description 4
- 229960002135 sulfadimidine Drugs 0.000 description 4
- ASWVTGNCAZCNNR-UHFFFAOYSA-N sulfamethazine Chemical compound CC1=CC(C)=NC(NS(=O)(=O)C=2C=CC(N)=CC=2)=N1 ASWVTGNCAZCNNR-UHFFFAOYSA-N 0.000 description 4
- 239000003760 tallow Substances 0.000 description 4
- 235000019364 tetracycline Nutrition 0.000 description 4
- 150000003522 tetracyclines Chemical class 0.000 description 4
- 230000000699 topical effect Effects 0.000 description 4
- 239000008215 water for injection Substances 0.000 description 4
- XGBFWQUQYQIFLB-MTTMTQIXSA-N 23312-56-3 Chemical compound OS(O)(=O)=O.O([C@@H]1[C@@H](NC)[C@@H](O)[C@H]([C@@H]([C@H]1O1)O)NC)[C@]2(O)[C@H]1O[C@H](C)CC2=O XGBFWQUQYQIFLB-MTTMTQIXSA-N 0.000 description 3
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 3
- 241000416162 Astragalus gummifer Species 0.000 description 3
- 108010001478 Bacitracin Proteins 0.000 description 3
- 239000005711 Benzoic acid Substances 0.000 description 3
- 229920002261 Corn starch Polymers 0.000 description 3
- WSFSSNUMVMOOMR-UHFFFAOYSA-N Formaldehyde Chemical compound O=C WSFSSNUMVMOOMR-UHFFFAOYSA-N 0.000 description 3
- 241000282412 Homo Species 0.000 description 3
- 206010061218 Inflammation Diseases 0.000 description 3
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 3
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 3
- 241000193996 Streptococcus pyogenes Species 0.000 description 3
- 229920001615 Tragacanth Polymers 0.000 description 3
- 239000011149 active material Substances 0.000 description 3
- 230000000845 anti-microbial effect Effects 0.000 description 3
- 239000007864 aqueous solution Substances 0.000 description 3
- 125000003118 aryl group Chemical group 0.000 description 3
- 229960003071 bacitracin Drugs 0.000 description 3
- 229930184125 bacitracin Natural products 0.000 description 3
- CLKOFPXJLQSYAH-ABRJDSQDSA-N bacitracin A Chemical compound C1SC([C@@H](N)[C@@H](C)CC)=N[C@@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](CCC(O)=O)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H]1C(=O)N[C@H](CCCN)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@H](CC=2C=CC=CC=2)C(=O)N[C@@H](CC=2N=CNC=2)C(=O)N[C@H](CC(O)=O)C(=O)N[C@@H](CC(N)=O)C(=O)NCCCC1 CLKOFPXJLQSYAH-ABRJDSQDSA-N 0.000 description 3
- 229960005274 benzocaine Drugs 0.000 description 3
- BLFLLBZGZJTVJG-UHFFFAOYSA-N benzocaine Chemical compound CCOC(=O)C1=CC=C(N)C=C1 BLFLLBZGZJTVJG-UHFFFAOYSA-N 0.000 description 3
- 235000010233 benzoic acid Nutrition 0.000 description 3
- 230000003115 biocidal effect Effects 0.000 description 3
- 229940105847 calamine Drugs 0.000 description 3
- OSASVXMJTNOKOY-UHFFFAOYSA-N chlorobutanol Chemical compound CC(C)(O)C(Cl)(Cl)Cl OSASVXMJTNOKOY-UHFFFAOYSA-N 0.000 description 3
- 239000008120 corn starch Substances 0.000 description 3
- 239000006071 cream Substances 0.000 description 3
- 238000002425 crystallisation Methods 0.000 description 3
- 230000008025 crystallization Effects 0.000 description 3
- 239000008367 deionised water Substances 0.000 description 3
- 229910021641 deionized water Inorganic materials 0.000 description 3
- 239000006185 dispersion Substances 0.000 description 3
- 239000003937 drug carrier Substances 0.000 description 3
- 239000012530 fluid Substances 0.000 description 3
- 125000005843 halogen group Chemical group 0.000 description 3
- 229910052864 hemimorphite Inorganic materials 0.000 description 3
- 125000004435 hydrogen atom Chemical class [H]* 0.000 description 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 3
- 230000004054 inflammatory process Effects 0.000 description 3
- 238000007912 intraperitoneal administration Methods 0.000 description 3
- 239000007937 lozenge Substances 0.000 description 3
- 208000004396 mastitis Diseases 0.000 description 3
- 244000005700 microbiome Species 0.000 description 3
- 239000008024 pharmaceutical diluent Substances 0.000 description 3
- 229940057838 polyethylene glycol 4000 Drugs 0.000 description 3
- 239000000741 silica gel Substances 0.000 description 3
- 229910002027 silica gel Inorganic materials 0.000 description 3
- 239000002904 solvent Substances 0.000 description 3
- 239000012177 spermaceti Substances 0.000 description 3
- 229940084106 spermaceti Drugs 0.000 description 3
- 239000000454 talc Substances 0.000 description 3
- 235000012222 talc Nutrition 0.000 description 3
- 229910052623 talc Inorganic materials 0.000 description 3
- 229960002180 tetracycline Drugs 0.000 description 3
- 229930101283 tetracycline Natural products 0.000 description 3
- ZMZDMBWJUHKJPS-UHFFFAOYSA-N thiocyanic acid Chemical compound SC#N ZMZDMBWJUHKJPS-UHFFFAOYSA-N 0.000 description 3
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 3
- 239000003981 vehicle Substances 0.000 description 3
- CPYIZQLXMGRKSW-UHFFFAOYSA-N zinc;iron(3+);oxygen(2-) Chemical compound [O-2].[O-2].[O-2].[O-2].[Fe+3].[Fe+3].[Zn+2] CPYIZQLXMGRKSW-UHFFFAOYSA-N 0.000 description 3
- NGGMYCMLYOUNGM-UHFFFAOYSA-N (-)-fumagillin Natural products O1C(CC=C(C)C)C1(C)C1C(OC)C(OC(=O)C=CC=CC=CC=CC(O)=O)CCC21CO2 NGGMYCMLYOUNGM-UHFFFAOYSA-N 0.000 description 2
- FRPZMMHWLSIFAZ-UHFFFAOYSA-N 10-undecenoic acid Chemical compound OC(=O)CCCCCCCCC=C FRPZMMHWLSIFAZ-UHFFFAOYSA-N 0.000 description 2
- XJMMNTGIMDZPMU-UHFFFAOYSA-N 3-methylglutaric acid Chemical compound OC(=O)CC(C)CC(O)=O XJMMNTGIMDZPMU-UHFFFAOYSA-N 0.000 description 2
- 244000215068 Acacia senegal Species 0.000 description 2
- 241000272517 Anseriformes Species 0.000 description 2
- 239000004099 Chlortetracycline Substances 0.000 description 2
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 description 2
- ULGZDMOVFRHVEP-RWJQBGPGSA-N Erythromycin Chemical compound O([C@@H]1[C@@H](C)C(=O)O[C@@H]([C@@]([C@H](O)[C@@H](C)C(=O)[C@H](C)C[C@@](C)(O)[C@H](O[C@H]2[C@@H]([C@H](C[C@@H](C)O2)N(C)C)O)[C@H]1C)(C)O)CC)[C@H]1C[C@@](C)(OC)[C@@H](O)[C@H](C)O1 ULGZDMOVFRHVEP-RWJQBGPGSA-N 0.000 description 2
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 description 2
- AEMRFAOFKBGASW-UHFFFAOYSA-N Glycolic acid Chemical compound OCC(O)=O AEMRFAOFKBGASW-UHFFFAOYSA-N 0.000 description 2
- 229920000084 Gum arabic Polymers 0.000 description 2
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 2
- 235000019501 Lemon oil Nutrition 0.000 description 2
- OJMMVQQUTAEWLP-UHFFFAOYSA-N Lincomycin Natural products CN1CC(CCC)CC1C(=O)NC(C(C)O)C1C(O)C(O)C(O)C(SC)O1 OJMMVQQUTAEWLP-UHFFFAOYSA-N 0.000 description 2
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 description 2
- 241000699670 Mus sp. Species 0.000 description 2
- YJQPYGGHQPGBLI-UHFFFAOYSA-N Novobiocin Natural products O1C(C)(C)C(OC)C(OC(N)=O)C(O)C1OC1=CC=C(C(O)=C(NC(=O)C=2C=C(CC=C(C)C)C(O)=CC=2)C(=O)O2)C2=C1C YJQPYGGHQPGBLI-UHFFFAOYSA-N 0.000 description 2
- 239000004100 Oxytetracycline Substances 0.000 description 2
- 241001494479 Pecora Species 0.000 description 2
- 229930182555 Penicillin Natural products 0.000 description 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 description 2
- OFOBLEOULBTSOW-UHFFFAOYSA-N Propanedioic acid Natural products OC(=O)CC(O)=O OFOBLEOULBTSOW-UHFFFAOYSA-N 0.000 description 2
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 2
- PPBRXRYQALVLMV-UHFFFAOYSA-N Styrene Chemical compound C=CC1=CC=CC=C1 PPBRXRYQALVLMV-UHFFFAOYSA-N 0.000 description 2
- KDYFGRWQOYBRFD-UHFFFAOYSA-N Succinic acid Natural products OC(=O)CCC(O)=O KDYFGRWQOYBRFD-UHFFFAOYSA-N 0.000 description 2
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 description 2
- QAOWNCQODCNURD-UHFFFAOYSA-N Sulfuric acid Chemical compound OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 description 2
- 239000000205 acacia gum Substances 0.000 description 2
- 235000010489 acacia gum Nutrition 0.000 description 2
- MGVGMXLGOKTYKP-ZFOBEOMCSA-N acetic acid;(6s,8s,9s,10r,11s,13s,14s,17r)-11,17-dihydroxy-17-(2-hydroxyacetyl)-6,10,13-trimethyl-7,8,9,11,12,14,15,16-octahydro-6h-cyclopenta[a]phenanthren-3-one Chemical compound CC(O)=O.C([C@@]12C)=CC(=O)C=C1[C@@H](C)C[C@@H]1[C@@H]2[C@@H](O)C[C@]2(C)[C@@](O)(C(=O)CO)CC[C@H]21 MGVGMXLGOKTYKP-ZFOBEOMCSA-N 0.000 description 2
- 125000002252 acyl group Chemical group 0.000 description 2
- 230000010933 acylation Effects 0.000 description 2
- 238000005917 acylation reaction Methods 0.000 description 2
- 239000004599 antimicrobial Substances 0.000 description 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 description 2
- 239000002585 base Substances 0.000 description 2
- CJZGTCYPCWQAJB-UHFFFAOYSA-L calcium stearate Chemical compound [Ca+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O CJZGTCYPCWQAJB-UHFFFAOYSA-L 0.000 description 2
- 239000008116 calcium stearate Substances 0.000 description 2
- 235000013539 calcium stearate Nutrition 0.000 description 2
- OSGAYBCDTDRGGQ-UHFFFAOYSA-L calcium sulfate Chemical compound [Ca+2].[O-]S([O-])(=O)=O OSGAYBCDTDRGGQ-UHFFFAOYSA-L 0.000 description 2
- KHAVLLBUVKBTBG-UHFFFAOYSA-N caproleic acid Natural products OC(=O)CCCCCCCC=C KHAVLLBUVKBTBG-UHFFFAOYSA-N 0.000 description 2
- XMEVHPAGJVLHIG-FMZCEJRJSA-N chembl454950 Chemical compound [Cl-].C1=CC=C2[C@](O)(C)[C@H]3C[C@H]4[C@H]([NH+](C)C)C(O)=C(C(N)=O)C(=O)[C@@]4(O)C(O)=C3C(=O)C2=C1O XMEVHPAGJVLHIG-FMZCEJRJSA-N 0.000 description 2
- 239000003795 chemical substances by application Substances 0.000 description 2
- 229960005091 chloramphenicol Drugs 0.000 description 2
- WIIZWVCIJKGZOK-RKDXNWHRSA-N chloramphenicol Chemical compound ClC(Cl)C(=O)N[C@H](CO)[C@H](O)C1=CC=C([N+]([O-])=O)C=C1 WIIZWVCIJKGZOK-RKDXNWHRSA-N 0.000 description 2
- CYDMQBQPVICBEU-UHFFFAOYSA-N chlorotetracycline Natural products C1=CC(Cl)=C2C(O)(C)C3CC4C(N(C)C)C(O)=C(C(N)=O)C(=O)C4(O)C(O)=C3C(=O)C2=C1O CYDMQBQPVICBEU-UHFFFAOYSA-N 0.000 description 2
- 229960004475 chlortetracycline Drugs 0.000 description 2
- CYDMQBQPVICBEU-XRNKAMNCSA-N chlortetracycline Chemical compound C1=CC(Cl)=C2[C@](O)(C)[C@H]3C[C@H]4[C@H](N(C)C)C(O)=C(C(N)=O)C(=O)[C@@]4(O)C(O)=C3C(=O)C2=C1O CYDMQBQPVICBEU-XRNKAMNCSA-N 0.000 description 2
- 235000019365 chlortetracycline Nutrition 0.000 description 2
- 239000000084 colloidal system Substances 0.000 description 2
- 239000000645 desinfectant Substances 0.000 description 2
- POULHZVOKOAJMA-UHFFFAOYSA-N dodecanoic acid Chemical compound CCCCCCCCCCCC(O)=O POULHZVOKOAJMA-UHFFFAOYSA-N 0.000 description 2
- 230000000694 effects Effects 0.000 description 2
- 238000006345 epimerization reaction Methods 0.000 description 2
- 239000003885 eye ointment Substances 0.000 description 2
- 235000003599 food sweetener Nutrition 0.000 description 2
- 210000003918 fraction a Anatomy 0.000 description 2
- 229960000936 fumagillin Drugs 0.000 description 2
- NGGMYCMLYOUNGM-CSDLUJIJSA-N fumagillin Chemical compound C([C@H]([C@H]([C@@H]1[C@]2(C)[C@H](O2)CC=C(C)C)OC)OC(=O)\C=C\C=C\C=C\C=C\C(O)=O)C[C@@]21CO2 NGGMYCMLYOUNGM-CSDLUJIJSA-N 0.000 description 2
- 239000000499 gel Substances 0.000 description 2
- 239000001963 growth medium Substances 0.000 description 2
- 125000001475 halogen functional group Chemical group 0.000 description 2
- 229940025294 hemin Drugs 0.000 description 2
- BXWNKGSJHAJOGX-UHFFFAOYSA-N hexadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCO BXWNKGSJHAJOGX-UHFFFAOYSA-N 0.000 description 2
- IPCSVZSSVZVIGE-UHFFFAOYSA-N hexadecanoic acid Chemical compound CCCCCCCCCCCCCCCC(O)=O IPCSVZSSVZVIGE-UHFFFAOYSA-N 0.000 description 2
- JYGXADMDTFJGBT-VWUMJDOOSA-N hydrocortisone Chemical compound O=C1CC[C@]2(C)[C@H]3[C@@H](O)C[C@](C)([C@@](CC4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 JYGXADMDTFJGBT-VWUMJDOOSA-N 0.000 description 2
- 238000007918 intramuscular administration Methods 0.000 description 2
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 description 2
- 239000008101 lactose Substances 0.000 description 2
- 239000010501 lemon oil Substances 0.000 description 2
- 230000000670 limiting effect Effects 0.000 description 2
- OJMMVQQUTAEWLP-KIDUDLJLSA-N lincomycin Chemical compound CN1C[C@H](CCC)C[C@H]1C(=O)N[C@H]([C@@H](C)O)[C@@H]1[C@H](O)[C@H](O)[C@@H](O)[C@@H](SC)O1 OJMMVQQUTAEWLP-KIDUDLJLSA-N 0.000 description 2
- 229960005287 lincomycin Drugs 0.000 description 2
- 239000008176 lyophilized powder Substances 0.000 description 2
- 239000011976 maleic acid Substances 0.000 description 2
- 238000004519 manufacturing process Methods 0.000 description 2
- 238000005649 metathesis reaction Methods 0.000 description 2
- 229920000609 methyl cellulose Polymers 0.000 description 2
- 239000001923 methylcellulose Substances 0.000 description 2
- 235000010981 methylcellulose Nutrition 0.000 description 2
- 229960001293 methylprednisolone acetate Drugs 0.000 description 2
- 238000002156 mixing Methods 0.000 description 2
- 230000004048 modification Effects 0.000 description 2
- 238000012986 modification Methods 0.000 description 2
- 210000000214 mouth Anatomy 0.000 description 2
- 229960002950 novobiocin Drugs 0.000 description 2
- YJQPYGGHQPGBLI-KGSXXDOSSA-N novobiocin Chemical compound O1C(C)(C)[C@H](OC)[C@@H](OC(N)=O)[C@@H](O)[C@@H]1OC1=CC=C(C(O)=C(NC(=O)C=2C=C(CC=C(C)C)C(O)=CC=2)C(=O)O2)C2=C1C YJQPYGGHQPGBLI-KGSXXDOSSA-N 0.000 description 2
- 229940069265 ophthalmic ointment Drugs 0.000 description 2
- 239000007935 oral tablet Substances 0.000 description 2
- 229960000625 oxytetracycline Drugs 0.000 description 2
- IWVCMVBTMGNXQD-PXOLEDIWSA-N oxytetracycline Chemical compound C1=CC=C2[C@](O)(C)[C@H]3[C@H](O)[C@H]4[C@H](N(C)C)C(O)=C(C(N)=O)C(=O)[C@@]4(O)C(O)=C3C(=O)C2=C1O IWVCMVBTMGNXQD-PXOLEDIWSA-N 0.000 description 2
- 235000019366 oxytetracycline Nutrition 0.000 description 2
- 238000007911 parenteral administration Methods 0.000 description 2
- 239000003182 parenteral nutrition solution Substances 0.000 description 2
- 239000000312 peanut oil Substances 0.000 description 2
- 230000026731 phosphorylation Effects 0.000 description 2
- 238000006366 phosphorylation reaction Methods 0.000 description 2
- XNGIFLGASWRNHJ-UHFFFAOYSA-N phthalic acid Chemical compound OC(=O)C1=CC=CC=C1C(O)=O XNGIFLGASWRNHJ-UHFFFAOYSA-N 0.000 description 2
- 239000011772 phylloquinone Substances 0.000 description 2
- 239000006187 pill Substances 0.000 description 2
- 230000003389 potentiating effect Effects 0.000 description 2
- 239000002243 precursor Substances 0.000 description 2
- 229960005205 prednisolone Drugs 0.000 description 2
- OIGNJSKKLXVSLS-VWUMJDOOSA-N prednisolone Chemical compound O=C1C=C[C@]2(C)[C@H]3[C@@H](O)C[C@](C)([C@@](CC4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 OIGNJSKKLXVSLS-VWUMJDOOSA-N 0.000 description 2
- 239000003755 preservative agent Substances 0.000 description 2
- 230000001681 protective effect Effects 0.000 description 2
- 239000011541 reaction mixture Substances 0.000 description 2
- YGSDEFSMJLZEOE-UHFFFAOYSA-N salicylic acid Chemical compound OC(=O)C1=CC=CC=C1O YGSDEFSMJLZEOE-UHFFFAOYSA-N 0.000 description 2
- 229920006395 saturated elastomer Polymers 0.000 description 2
- 239000002002 slurry Substances 0.000 description 2
- PNGLEYLFMHGIQO-UHFFFAOYSA-M sodium;3-(n-ethyl-3-methoxyanilino)-2-hydroxypropane-1-sulfonate;dihydrate Chemical compound O.O.[Na+].[O-]S(=O)(=O)CC(O)CN(CC)C1=CC=CC(OC)=C1 PNGLEYLFMHGIQO-UHFFFAOYSA-M 0.000 description 2
- 238000000638 solvent extraction Methods 0.000 description 2
- 239000008174 sterile solution Substances 0.000 description 2
- 229960005322 streptomycin Drugs 0.000 description 2
- 229960002673 sulfacetamide Drugs 0.000 description 2
- SKIVFJLNDNKQPD-UHFFFAOYSA-N sulfacetamide Chemical compound CC(=O)NS(=O)(=O)C1=CC=C(N)C=C1 SKIVFJLNDNKQPD-UHFFFAOYSA-N 0.000 description 2
- 239000003765 sweetening agent Substances 0.000 description 2
- IWVCMVBTMGNXQD-UHFFFAOYSA-N terramycin dehydrate Natural products C1=CC=C2C(O)(C)C3C(O)C4C(N(C)C)C(O)=C(C(N)=O)C(=O)C4(O)C(O)=C3C(=O)C2=C1O IWVCMVBTMGNXQD-UHFFFAOYSA-N 0.000 description 2
- 238000010998 test method Methods 0.000 description 2
- 229960004989 tetracycline hydrochloride Drugs 0.000 description 2
- 231100000419 toxicity Toxicity 0.000 description 2
- 230000001988 toxicity Effects 0.000 description 2
- 239000000196 tragacanth Substances 0.000 description 2
- 235000010487 tragacanth Nutrition 0.000 description 2
- 229940116362 tragacanth Drugs 0.000 description 2
- 229960002703 undecylenic acid Drugs 0.000 description 2
- 235000012431 wafers Nutrition 0.000 description 2
- 238000005303 weighing Methods 0.000 description 2
- BHQCQFFYRZLCQQ-UHFFFAOYSA-N (3alpha,5alpha,7alpha,12alpha)-3,7,12-trihydroxy-cholan-24-oic acid Natural products OC1CC2CC(O)CCC2(C)C2C1C1CCC(C(CCC(O)=O)C)C1(C)C(O)C2 BHQCQFFYRZLCQQ-UHFFFAOYSA-N 0.000 description 1
- WBYWAXJHAXSJNI-VOTSOKGWSA-M .beta-Phenylacrylic acid Natural products [O-]C(=O)\C=C\C1=CC=CC=C1 WBYWAXJHAXSJNI-VOTSOKGWSA-M 0.000 description 1
- DTOUUUZOYKYHEP-UHFFFAOYSA-N 1,3-bis(2-ethylhexyl)-5-methyl-1,3-diazinan-5-amine Chemical compound CCCCC(CC)CN1CN(CC(CC)CCCC)CC(C)(N)C1 DTOUUUZOYKYHEP-UHFFFAOYSA-N 0.000 description 1
- 125000001478 1-chloroethyl group Chemical group [H]C([H])([H])C([H])(Cl)* 0.000 description 1
- 125000004776 1-fluoroethyl group Chemical group [H]C([H])([H])C([H])(F)* 0.000 description 1
- RTBFRGCFXZNCOE-UHFFFAOYSA-N 1-methylsulfonylpiperidin-4-one Chemical compound CS(=O)(=O)N1CCC(=O)CC1 RTBFRGCFXZNCOE-UHFFFAOYSA-N 0.000 description 1
- 229940078693 1-myristylpicolinium Drugs 0.000 description 1
- XACKAZKMZQZZDT-MDZDMXLPSA-N 2-[(e)-octadec-9-enyl]butanedioic acid Chemical compound CCCCCCCC\C=C\CCCCCCCCC(C(O)=O)CC(O)=O XACKAZKMZQZZDT-MDZDMXLPSA-N 0.000 description 1
- 125000001340 2-chloroethyl group Chemical group [H]C([H])(Cl)C([H])([H])* 0.000 description 1
- 125000004182 2-chlorophenyl group Chemical group [H]C1=C([H])C(Cl)=C(*)C([H])=C1[H] 0.000 description 1
- 125000004777 2-fluoroethyl group Chemical group [H]C([H])(F)C([H])([H])* 0.000 description 1
- ZJWUEJOPKFYFQD-UHFFFAOYSA-N 2-hydroxy-3-phenylbenzoic acid Chemical compound OC(=O)C1=CC=CC(C=2C=CC=CC=2)=C1O ZJWUEJOPKFYFQD-UHFFFAOYSA-N 0.000 description 1
- LGERKUYJCZOBTB-UHFFFAOYSA-N 2-hydroxy-5-phenylbenzoic acid Chemical compound C1=C(O)C(C(=O)O)=CC(C=2C=CC=CC=2)=C1 LGERKUYJCZOBTB-UHFFFAOYSA-N 0.000 description 1
- YOETUEMZNOLGDB-UHFFFAOYSA-N 2-methylpropyl carbonochloridate Chemical compound CC(C)COC(Cl)=O YOETUEMZNOLGDB-UHFFFAOYSA-N 0.000 description 1
- ZRPLANDPDWYOMZ-UHFFFAOYSA-N 3-cyclopentylpropionic acid Chemical compound OC(=O)CCC1CCCC1 ZRPLANDPDWYOMZ-UHFFFAOYSA-N 0.000 description 1
- 125000006305 3-iodophenyl group Chemical group [H]C1=C([H])C(I)=C([H])C(*)=C1[H] 0.000 description 1
- WRFYIYOXJWKONR-UHFFFAOYSA-N 4-bromo-2-methoxyaniline Chemical compound COC1=CC(Br)=CC=C1N WRFYIYOXJWKONR-UHFFFAOYSA-N 0.000 description 1
- 125000004800 4-bromophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Br 0.000 description 1
- ZCTSINFCZHUVLI-UHFFFAOYSA-M 4-methyl-1-tetradecylpyridin-1-ium;chloride Chemical compound [Cl-].CCCCCCCCCCCCCC[N+]1=CC=C(C)C=C1 ZCTSINFCZHUVLI-UHFFFAOYSA-M 0.000 description 1
- BSYNRYMUTXBXSQ-UHFFFAOYSA-N Aspirin Chemical compound CC(=O)OC1=CC=CC=C1C(O)=O BSYNRYMUTXBXSQ-UHFFFAOYSA-N 0.000 description 1
- 241000283690 Bos taurus Species 0.000 description 1
- JJYCENBZIMIWTM-KGSXXDOSSA-N CO[C@@H]1[C@@H](OC(N)=O)[C@@H](O)[C@H](Oc2ccc3c(O)c(NC(=O)c4ccc(O)c(CCC(C)C)c4)c(=O)oc3c2C)OC1(C)C Chemical compound CO[C@@H]1[C@@H](OC(N)=O)[C@@H](O)[C@H](Oc2ccc3c(O)c(NC(=O)c4ccc(O)c(CCC(C)C)c4)c(=O)oc3c2C)OC1(C)C JJYCENBZIMIWTM-KGSXXDOSSA-N 0.000 description 1
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical class [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 description 1
- LSPHULWDVZXLIL-UHFFFAOYSA-N Camphoric acid Natural products CC1(C)C(C(O)=O)CCC1(C)C(O)=O LSPHULWDVZXLIL-UHFFFAOYSA-N 0.000 description 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 description 1
- 241000700198 Cavia Species 0.000 description 1
- 229920000623 Cellulose acetate phthalate Polymers 0.000 description 1
- DBAKFASWICGISY-BTJKTKAUSA-N Chlorpheniramine maleate Chemical compound OC(=O)\C=C/C(O)=O.C=1C=CC=NC=1C(CCN(C)C)C1=CC=C(Cl)C=C1 DBAKFASWICGISY-BTJKTKAUSA-N 0.000 description 1
- 239000004380 Cholic acid Substances 0.000 description 1
- WBYWAXJHAXSJNI-SREVYHEPSA-N Cinnamic acid Chemical compound OC(=O)\C=C/C1=CC=CC=C1 WBYWAXJHAXSJNI-SREVYHEPSA-N 0.000 description 1
- KRKNYBCHXYNGOX-UHFFFAOYSA-K Citrate Chemical compound [O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-K 0.000 description 1
- 208000003322 Coinfection Diseases 0.000 description 1
- 229940126062 Compound A Drugs 0.000 description 1
- 241000699800 Cricetinae Species 0.000 description 1
- 235000019739 Dicalciumphosphate Nutrition 0.000 description 1
- 241000194033 Enterococcus Species 0.000 description 1
- 241000588724 Escherichia coli Species 0.000 description 1
- IAYPIBMASNFSPL-UHFFFAOYSA-N Ethylene oxide Chemical compound C1CO1 IAYPIBMASNFSPL-UHFFFAOYSA-N 0.000 description 1
- 229930183931 Filipin Natural products 0.000 description 1
- 235000019733 Fish meal Nutrition 0.000 description 1
- 241000287828 Gallus gallus Species 0.000 description 1
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 1
- NLDMNSXOCDLTTB-UHFFFAOYSA-N Heterophylliin A Natural products O1C2COC(=O)C3=CC(O)=C(O)C(O)=C3C3=C(O)C(O)=C(O)C=C3C(=O)OC2C(OC(=O)C=2C=C(O)C(O)=C(O)C=2)C(O)C1OC(=O)C1=CC(O)=C(O)C(O)=C1 NLDMNSXOCDLTTB-UHFFFAOYSA-N 0.000 description 1
- 101000619542 Homo sapiens E3 ubiquitin-protein ligase parkin Proteins 0.000 description 1
- PWWVAXIEGOYWEE-UHFFFAOYSA-N Isophenergan Chemical compound C1=CC=C2N(CC(C)N(C)C)C3=CC=CC=C3SC2=C1 PWWVAXIEGOYWEE-UHFFFAOYSA-N 0.000 description 1
- 241000588747 Klebsiella pneumoniae Species 0.000 description 1
- ODKSFYDXXFIFQN-BYPYZUCNSA-N L-arginine Chemical compound OC(=O)[C@@H](N)CCCN=C(N)N ODKSFYDXXFIFQN-BYPYZUCNSA-N 0.000 description 1
- 229930064664 L-arginine Natural products 0.000 description 1
- 235000014852 L-arginine Nutrition 0.000 description 1
- JVTAAEKCZFNVCJ-UHFFFAOYSA-M Lactate Chemical compound CC(O)C([O-])=O JVTAAEKCZFNVCJ-UHFFFAOYSA-M 0.000 description 1
- 239000004166 Lanolin Substances 0.000 description 1
- 239000005639 Lauric acid Substances 0.000 description 1
- 229920000715 Mucilage Polymers 0.000 description 1
- 229910002651 NO3 Inorganic materials 0.000 description 1
- 229930193140 Neomycin Natural products 0.000 description 1
- NHNBFGGVMKEFGY-UHFFFAOYSA-N Nitrate Chemical compound [O-][N+]([O-])=O NHNBFGGVMKEFGY-UHFFFAOYSA-N 0.000 description 1
- 235000021314 Palmitic acid Nutrition 0.000 description 1
- 235000019483 Peanut oil Nutrition 0.000 description 1
- JGSARLDLIJGVTE-MBNYWOFBSA-N Penicillin G Chemical compound N([C@H]1[C@H]2SC([C@@H](N2C1=O)C(O)=O)(C)C)C(=O)CC1=CC=CC=C1 JGSARLDLIJGVTE-MBNYWOFBSA-N 0.000 description 1
- 241000192035 Peptostreptococcus anaerobius Species 0.000 description 1
- 241000286209 Phasianidae Species 0.000 description 1
- 206010035664 Pneumonia Diseases 0.000 description 1
- 108010040201 Polymyxins Proteins 0.000 description 1
- 241000589517 Pseudomonas aeruginosa Species 0.000 description 1
- SKZKKFZAGNVIMN-UHFFFAOYSA-N Salicilamide Chemical compound NC(=O)C1=CC=CC=C1O SKZKKFZAGNVIMN-UHFFFAOYSA-N 0.000 description 1
- 229920001800 Shellac Polymers 0.000 description 1
- DWAQJAXMDSEUJJ-UHFFFAOYSA-M Sodium bisulfite Chemical compound [Na+].OS([O-])=O DWAQJAXMDSEUJJ-UHFFFAOYSA-M 0.000 description 1
- 240000006394 Sorghum bicolor Species 0.000 description 1
- 235000011684 Sorghum saccharatum Nutrition 0.000 description 1
- 229920002472 Starch Polymers 0.000 description 1
- 235000021355 Stearic acid Nutrition 0.000 description 1
- 241000193998 Streptococcus pneumoniae Species 0.000 description 1
- HVWGGPRWKSHASF-UHFFFAOYSA-N Sulfuric acid, monooctadecyl ester Chemical compound CCCCCCCCCCCCCCCCCCOS(O)(=O)=O HVWGGPRWKSHASF-UHFFFAOYSA-N 0.000 description 1
- FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 description 1
- ZMZDMBWJUHKJPS-UHFFFAOYSA-M Thiocyanate anion Chemical compound [S-]C#N ZMZDMBWJUHKJPS-UHFFFAOYSA-M 0.000 description 1
- 206010046914 Vaginal infection Diseases 0.000 description 1
- 229930003448 Vitamin K Natural products 0.000 description 1
- YFESKAUSWQXQGO-UHFFFAOYSA-M [Na+].OC1=CC=CC=C1C([O-])=O.CC(=O)OC1=CC=CC=C1C(=O)OC(=O)C1=CC=CC=C1OC(C)=O Chemical compound [Na+].OC1=CC=CC=C1C([O-])=O.CC(=O)OC1=CC=CC=C1C(=O)OC(=O)C1=CC=CC=C1OC(C)=O YFESKAUSWQXQGO-UHFFFAOYSA-M 0.000 description 1
- 150000001242 acetic acid derivatives Chemical class 0.000 description 1
- 229960001138 acetylsalicylic acid Drugs 0.000 description 1
- 230000009471 action Effects 0.000 description 1
- 230000001154 acute effect Effects 0.000 description 1
- 239000000853 adhesive Substances 0.000 description 1
- 239000002671 adjuvant Substances 0.000 description 1
- 241001148470 aerobic bacillus Species 0.000 description 1
- XAGFODPZIPBFFR-UHFFFAOYSA-N aluminium Chemical compound [Al] XAGFODPZIPBFFR-UHFFFAOYSA-N 0.000 description 1
- 229910052782 aluminium Inorganic materials 0.000 description 1
- 229910000147 aluminium phosphate Inorganic materials 0.000 description 1
- SNAAJJQQZSMGQD-UHFFFAOYSA-N aluminum magnesium Chemical compound [Mg].[Al] SNAAJJQQZSMGQD-UHFFFAOYSA-N 0.000 description 1
- 239000003708 ampul Substances 0.000 description 1
- 229940035676 analgesics Drugs 0.000 description 1
- JFCQEDHGNNZCLN-UHFFFAOYSA-N anhydrous glutaric acid Natural products OC(=O)CCCC(O)=O JFCQEDHGNNZCLN-UHFFFAOYSA-N 0.000 description 1
- 238000010171 animal model Methods 0.000 description 1
- 229940069428 antacid Drugs 0.000 description 1
- 239000003159 antacid agent Substances 0.000 description 1
- 239000000730 antalgic agent Substances 0.000 description 1
- 230000001458 anti-acid effect Effects 0.000 description 1
- 230000003110 anti-inflammatory effect Effects 0.000 description 1
- 229940125715 antihistaminic agent Drugs 0.000 description 1
- 239000000739 antihistaminic agent Substances 0.000 description 1
- 239000003096 antiparasitic agent Substances 0.000 description 1
- 229940125687 antiparasitic agent Drugs 0.000 description 1
- 239000007900 aqueous suspension Substances 0.000 description 1
- 239000008135 aqueous vehicle Substances 0.000 description 1
- 238000003556 assay Methods 0.000 description 1
- 239000012298 atmosphere Substances 0.000 description 1
- 230000001580 bacterial effect Effects 0.000 description 1
- 230000003385 bacteriostatic effect Effects 0.000 description 1
- 239000011324 bead Substances 0.000 description 1
- 230000008901 benefit Effects 0.000 description 1
- IYNDLOXRXUOGIU-LQDWTQKMSA-M benzylpenicillin potassium Chemical compound [K+].N([C@H]1[C@H]2SC([C@@H](N2C1=O)C([O-])=O)(C)C)C(=O)CC1=CC=CC=C1 IYNDLOXRXUOGIU-LQDWTQKMSA-M 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 210000004556 brain Anatomy 0.000 description 1
- 229910052794 bromium Inorganic materials 0.000 description 1
- 238000002815 broth microdilution Methods 0.000 description 1
- 239000000872 buffer Substances 0.000 description 1
- 239000006172 buffering agent Substances 0.000 description 1
- KDYFGRWQOYBRFD-NUQCWPJISA-N butanedioic acid Chemical compound O[14C](=O)CC[14C](O)=O KDYFGRWQOYBRFD-NUQCWPJISA-N 0.000 description 1
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 239000001506 calcium phosphate Substances 0.000 description 1
- LSPHULWDVZXLIL-QUBYGPBYSA-N camphoric acid Chemical compound CC1(C)[C@H](C(O)=O)CC[C@]1(C)C(O)=O LSPHULWDVZXLIL-QUBYGPBYSA-N 0.000 description 1
- 229940041514 candida albicans extract Drugs 0.000 description 1
- 229910052799 carbon Inorganic materials 0.000 description 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 description 1
- 150000001244 carboxylic acid anhydrides Chemical class 0.000 description 1
- 210000004027 cell Anatomy 0.000 description 1
- 239000006285 cell suspension Substances 0.000 description 1
- 229940081734 cellulose acetate phthalate Drugs 0.000 description 1
- 229960000541 cetyl alcohol Drugs 0.000 description 1
- 235000013330 chicken meat Nutrition 0.000 description 1
- 229910052801 chlorine Inorganic materials 0.000 description 1
- FOCAUTSVDIKZOP-UHFFFAOYSA-N chloroacetic acid Chemical compound OC(=O)CCl FOCAUTSVDIKZOP-UHFFFAOYSA-N 0.000 description 1
- 229960004926 chlorobutanol Drugs 0.000 description 1
- WORJEOGGNQDSOE-UHFFFAOYSA-N chloroform;methanol Chemical compound OC.ClC(Cl)Cl WORJEOGGNQDSOE-UHFFFAOYSA-N 0.000 description 1
- BHQCQFFYRZLCQQ-OELDTZBJSA-N cholic acid Chemical compound C([C@H]1C[C@H]2O)[C@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H]([C@@H](CCC(O)=O)C)[C@@]2(C)[C@@H](O)C1 BHQCQFFYRZLCQQ-OELDTZBJSA-N 0.000 description 1
- 235000019416 cholic acid Nutrition 0.000 description 1
- 229960002471 cholic acid Drugs 0.000 description 1
- 235000013985 cinnamic acid Nutrition 0.000 description 1
- 229930016911 cinnamic acid Natural products 0.000 description 1
- 238000000576 coating method Methods 0.000 description 1
- 239000013066 combination product Substances 0.000 description 1
- 229940127555 combination product Drugs 0.000 description 1
- 238000013329 compounding Methods 0.000 description 1
- 239000007891 compressed tablet Substances 0.000 description 1
- 238000009833 condensation Methods 0.000 description 1
- 230000005494 condensation Effects 0.000 description 1
- 229920001577 copolymer Polymers 0.000 description 1
- 230000008878 coupling Effects 0.000 description 1
- 238000010168 coupling process Methods 0.000 description 1
- 238000005859 coupling reaction Methods 0.000 description 1
- 239000013078 crystal Substances 0.000 description 1
- 239000002178 crystalline material Substances 0.000 description 1
- 238000012136 culture method Methods 0.000 description 1
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 description 1
- 125000000582 cycloheptyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 description 1
- QSAWQNUELGIYBC-UHFFFAOYSA-N cyclohexane-1,2-dicarboxylic acid Chemical compound OC(=O)C1CCCCC1C(O)=O QSAWQNUELGIYBC-UHFFFAOYSA-N 0.000 description 1
- NZNMSOFKMUBTKW-UHFFFAOYSA-N cyclohexanecarboxylic acid Chemical compound OC(=O)C1CCCCC1 NZNMSOFKMUBTKW-UHFFFAOYSA-N 0.000 description 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 description 1
- 125000000640 cyclooctyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 description 1
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 description 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 description 1
- 235000013365 dairy product Nutrition 0.000 description 1
- 230000003247 decreasing effect Effects 0.000 description 1
- 238000007872 degassing Methods 0.000 description 1
- KXGVEGMKQFWNSR-UHFFFAOYSA-N deoxycholic acid Natural products C1CC2CC(O)CCC2(C)C2C1C1CCC(C(CCC(O)=O)C)C1(C)C(O)C2 KXGVEGMKQFWNSR-UHFFFAOYSA-N 0.000 description 1
- 239000008121 dextrose Substances 0.000 description 1
- 229940061607 dibasic sodium phosphate Drugs 0.000 description 1
- NEFBYIFKOOEVPA-UHFFFAOYSA-K dicalcium phosphate Chemical compound [Ca+2].[Ca+2].[O-]P([O-])([O-])=O NEFBYIFKOOEVPA-UHFFFAOYSA-K 0.000 description 1
- 229940038472 dicalcium phosphate Drugs 0.000 description 1
- 229910000390 dicalcium phosphate Inorganic materials 0.000 description 1
- 238000010790 dilution Methods 0.000 description 1
- 239000012895 dilution Substances 0.000 description 1
- MZGNSEAPZQGJRB-UHFFFAOYSA-N dimethyldithiocarbamic acid Chemical compound CN(C)C(S)=S MZGNSEAPZQGJRB-UHFFFAOYSA-N 0.000 description 1
- ZZVUWRFHKOJYTH-UHFFFAOYSA-N diphenhydramine Chemical compound C=1C=CC=CC=1C(OCCN(C)C)C1=CC=CC=C1 ZZVUWRFHKOJYTH-UHFFFAOYSA-N 0.000 description 1
- 230000008034 disappearance Effects 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- BNIILDVGGAEEIG-UHFFFAOYSA-L disodium hydrogen phosphate Chemical compound [Na+].[Na+].OP([O-])([O-])=O BNIILDVGGAEEIG-UHFFFAOYSA-L 0.000 description 1
- FVKLXKOXTMCACB-VJWYNRERSA-L disodium;[2-[(6s,8s,9s,10r,11s,13s,14s,17r)-11,17-dihydroxy-6,10,13-trimethyl-3-oxo-7,8,9,11,12,14,15,16-octahydro-6h-cyclopenta[a]phenanthren-17-yl]-2-oxoethyl] phosphate Chemical compound [Na+].[Na+].C([C@@]12C)=CC(=O)C=C1[C@@H](C)C[C@@H]1[C@@H]2[C@@H](O)C[C@]2(C)[C@@](O)(C(=O)COP([O-])([O-])=O)CC[C@H]21 FVKLXKOXTMCACB-VJWYNRERSA-L 0.000 description 1
- 239000012153 distilled water Substances 0.000 description 1
- 238000009826 distribution Methods 0.000 description 1
- 239000006196 drop Substances 0.000 description 1
- 210000001198 duodenum Anatomy 0.000 description 1
- 239000003221 ear drop Substances 0.000 description 1
- 229940047652 ear drops Drugs 0.000 description 1
- 210000005069 ears Anatomy 0.000 description 1
- 230000001804 emulsifying effect Effects 0.000 description 1
- 239000000839 emulsion Substances 0.000 description 1
- 238000005538 encapsulation Methods 0.000 description 1
- 229950007432 endomycin Drugs 0.000 description 1
- 230000007613 environmental effect Effects 0.000 description 1
- 229960003276 erythromycin Drugs 0.000 description 1
- DZGCGKFAPXFTNM-UHFFFAOYSA-N ethanol;hydron;chloride Chemical compound Cl.CCO DZGCGKFAPXFTNM-UHFFFAOYSA-N 0.000 description 1
- BEFDCLMNVWHSGT-UHFFFAOYSA-N ethenylcyclopentane Chemical compound C=CC1CCCC1 BEFDCLMNVWHSGT-UHFFFAOYSA-N 0.000 description 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 238000000605 extraction Methods 0.000 description 1
- 239000003889 eye drop Substances 0.000 description 1
- 229940012356 eye drops Drugs 0.000 description 1
- 229950000152 filipin Drugs 0.000 description 1
- IMQSIXYSKPIGPD-NKYUYKLDSA-N filipin Chemical compound CCCCC[C@H](O)[C@@H]1[C@@H](O)C[C@@H](O)C[C@@H](O)C[C@@H](O)C[C@@H](O)C[C@@H](O)C[C@H](O)\C(C)=C\C=C\C=C\C=C\C=C\[C@H](O)[C@@H](C)OC1=O IMQSIXYSKPIGPD-NKYUYKLDSA-N 0.000 description 1
- IMQSIXYSKPIGPD-UHFFFAOYSA-N filipin III Natural products CCCCCC(O)C1C(O)CC(O)CC(O)CC(O)CC(O)CC(O)CC(O)C(C)=CC=CC=CC=CC=CC(O)C(C)OC1=O IMQSIXYSKPIGPD-UHFFFAOYSA-N 0.000 description 1
- 239000004467 fishmeal Substances 0.000 description 1
- 235000013312 flour Nutrition 0.000 description 1
- 229910052731 fluorine Inorganic materials 0.000 description 1
- 125000001153 fluoro group Chemical group F* 0.000 description 1
- 239000011888 foil Substances 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- PGBHMTALBVVCIT-VCIWKGPPSA-N framycetin Chemical compound N[C@@H]1[C@@H](O)[C@H](O)[C@H](CN)O[C@@H]1O[C@H]1[C@@H](O)[C@H](O[C@H]2[C@@H]([C@@H](N)C[C@@H](N)[C@@H]2O)O[C@@H]2[C@@H]([C@@H](O)[C@H](O)[C@@H](CN)O2)N)O[C@@H]1CO PGBHMTALBVVCIT-VCIWKGPPSA-N 0.000 description 1
- 239000001530 fumaric acid Substances 0.000 description 1
- 239000000417 fungicide Substances 0.000 description 1
- 238000007429 general method Methods 0.000 description 1
- 125000003976 glyceryl group Chemical group [H]C([*])([H])C(O[H])([H])C(O[H])([H])[H] 0.000 description 1
- 150000002337 glycosamines Chemical class 0.000 description 1
- 150000003278 haem Chemical class 0.000 description 1
- BTIJJDXEELBZFS-UHFFFAOYSA-K hemin Chemical compound [Cl-].[Fe+3].[N-]1C(C=C2C(=C(C)C(C=C3C(=C(C)C(=C4)[N-]3)C=C)=N2)C=C)=C(C)C(CCC(O)=O)=C1C=C1C(CCC(O)=O)=C(C)C4=N1 BTIJJDXEELBZFS-UHFFFAOYSA-K 0.000 description 1
- BTIJJDXEELBZFS-QDUVMHSLSA-K hemin Chemical compound CC1=C(CCC(O)=O)C(C=C2C(CCC(O)=O)=C(C)\C(N2[Fe](Cl)N23)=C\4)=N\C1=C/C2=C(C)C(C=C)=C3\C=C/1C(C)=C(C=C)C/4=N\1 BTIJJDXEELBZFS-QDUVMHSLSA-K 0.000 description 1
- 125000003187 heptyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 150000002391 heterocyclic compounds Chemical class 0.000 description 1
- ARBOVOVUTSQWSS-UHFFFAOYSA-N hexadecanoyl chloride Chemical compound CCCCCCCCCCCCCCCC(Cl)=O ARBOVOVUTSQWSS-UHFFFAOYSA-N 0.000 description 1
- LPTIRUACFKQDHZ-UHFFFAOYSA-N hexadecyl sulfate;hydron Chemical compound CCCCCCCCCCCCCCCCOS(O)(=O)=O LPTIRUACFKQDHZ-UHFFFAOYSA-N 0.000 description 1
- 229960004867 hexetidine Drugs 0.000 description 1
- 125000004051 hexyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 description 1
- 150000003840 hydrochlorides Chemical class 0.000 description 1
- 229960000890 hydrocortisone Drugs 0.000 description 1
- 238000005984 hydrogenation reaction Methods 0.000 description 1
- 230000007062 hydrolysis Effects 0.000 description 1
- 238000006460 hydrolysis reaction Methods 0.000 description 1
- KCYQMQGPYWZZNJ-BQYQJAHWSA-N hydron;2-[(e)-oct-1-enyl]butanedioate Chemical compound CCCCCC\C=C\C(C(O)=O)CC(O)=O KCYQMQGPYWZZNJ-BQYQJAHWSA-N 0.000 description 1
- 125000004356 hydroxy functional group Chemical group O* 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- 238000001727 in vivo Methods 0.000 description 1
- 238000001802 infusion Methods 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 238000011081 inoculation Methods 0.000 description 1
- 239000002054 inoculum Substances 0.000 description 1
- 229910052740 iodine Inorganic materials 0.000 description 1
- 229960000318 kanamycin Drugs 0.000 description 1
- 229930027917 kanamycin Natural products 0.000 description 1
- SBUJHOSQTJFQJX-NOAMYHISSA-N kanamycin Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CN)O[C@@H]1O[C@H]1[C@H](O)[C@@H](O[C@@H]2[C@@H]([C@@H](N)[C@H](O)[C@@H](CO)O2)O)[C@H](N)C[C@@H]1N SBUJHOSQTJFQJX-NOAMYHISSA-N 0.000 description 1
- 229930182823 kanamycin A Natural products 0.000 description 1
- 239000004310 lactic acid Substances 0.000 description 1
- 235000014655 lactic acid Nutrition 0.000 description 1
- 229940039717 lanolin Drugs 0.000 description 1
- 235000019388 lanolin Nutrition 0.000 description 1
- 229960004393 lidocaine hydrochloride Drugs 0.000 description 1
- YECIFGHRMFEPJK-UHFFFAOYSA-N lidocaine hydrochloride monohydrate Chemical compound O.[Cl-].CC[NH+](CC)CC(=O)NC1=C(C)C=CC=C1C YECIFGHRMFEPJK-UHFFFAOYSA-N 0.000 description 1
- 238000000622 liquid--liquid extraction Methods 0.000 description 1
- 239000003589 local anesthetic agent Substances 0.000 description 1
- 229960005015 local anesthetics Drugs 0.000 description 1
- 239000006210 lotion Substances 0.000 description 1
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 description 1
- 239000011159 matrix material Substances 0.000 description 1
- 238000005259 measurement Methods 0.000 description 1
- 239000000155 melt Substances 0.000 description 1
- 238000002844 melting Methods 0.000 description 1
- 230000008018 melting Effects 0.000 description 1
- 229940098779 methanesulfonic acid Drugs 0.000 description 1
- WBYWAXJHAXSJNI-UHFFFAOYSA-N methyl p-hydroxycinnamate Natural products OC(=O)C=CC1=CC=CC=C1 WBYWAXJHAXSJNI-UHFFFAOYSA-N 0.000 description 1
- 229960001426 methylprednisolone sodium phosphate Drugs 0.000 description 1
- 230000002906 microbiologic effect Effects 0.000 description 1
- 238000003801 milling Methods 0.000 description 1
- 235000013379 molasses Nutrition 0.000 description 1
- WQEPLUUGTLDZJY-UHFFFAOYSA-N n-Pentadecanoic acid Natural products CCCCCCCCCCCCCCC(O)=O WQEPLUUGTLDZJY-UHFFFAOYSA-N 0.000 description 1
- 229960004927 neomycin Drugs 0.000 description 1
- 229940053050 neomycin sulfate Drugs 0.000 description 1
- 238000006386 neutralization reaction Methods 0.000 description 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 description 1
- 229960000988 nystatin Drugs 0.000 description 1
- VQOXZBDYSJBXMA-NQTDYLQESA-N nystatin A1 Chemical compound O[C@H]1[C@@H](N)[C@H](O)[C@@H](C)O[C@H]1O[C@H]1/C=C/C=C/C=C/C=C/CC/C=C/C=C/[C@H](C)[C@@H](O)[C@@H](C)[C@H](C)OC(=O)C[C@H](O)C[C@H](O)C[C@H](O)CC[C@@H](O)[C@H](O)C[C@](O)(C[C@H](O)[C@H]2C(O)=O)O[C@H]2C1 VQOXZBDYSJBXMA-NQTDYLQESA-N 0.000 description 1
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 1
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 description 1
- HHMAJEQKYRNURJ-UHFFFAOYSA-N octadecylsulfamic acid Chemical compound CCCCCCCCCCCCCCCCCC[NH2+]S([O-])(=O)=O HHMAJEQKYRNURJ-UHFFFAOYSA-N 0.000 description 1
- 125000002347 octyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 239000003883 ointment base Substances 0.000 description 1
- WLJNZVDCPSBLRP-UHFFFAOYSA-N pamoic acid Chemical compound C1=CC=C2C(CC=3C4=CC=CC=C4C=C(C=3O)C(=O)O)=C(O)C(C(O)=O)=CC2=C1 WLJNZVDCPSBLRP-UHFFFAOYSA-N 0.000 description 1
- FJKROLUGYXJWQN-UHFFFAOYSA-N papa-hydroxy-benzoic acid Natural products OC(=O)C1=CC=C(O)C=C1 FJKROLUGYXJWQN-UHFFFAOYSA-N 0.000 description 1
- 102000045222 parkin Human genes 0.000 description 1
- 239000002245 particle Substances 0.000 description 1
- 239000008188 pellet Substances 0.000 description 1
- 229940049954 penicillin Drugs 0.000 description 1
- 150000002960 penicillins Chemical class 0.000 description 1
- 125000001147 pentyl group Chemical group C(CCCC)* 0.000 description 1
- 229940074571 peptostreptococcus anaerobius Drugs 0.000 description 1
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 description 1
- MBWXNTAXLNYFJB-LKUDQCMESA-N phylloquinone Chemical compound C1=CC=C2C(=O)C(C/C=C(C)/CCCC(C)CCCC(C)CCCC(C)C)=C(C)C(=O)C2=C1 MBWXNTAXLNYFJB-LKUDQCMESA-N 0.000 description 1
- SHUZOJHMOBOZST-UHFFFAOYSA-N phylloquinone Natural products CC(C)CCCCC(C)CCC(C)CCCC(=CCC1=C(C)C(=O)c2ccccc2C1=O)C SHUZOJHMOBOZST-UHFFFAOYSA-N 0.000 description 1
- 230000000704 physical effect Effects 0.000 description 1
- 229940075930 picrate Drugs 0.000 description 1
- OXNIZHLAWKMVMX-UHFFFAOYSA-M picrate anion Chemical compound [O-]C1=C([N+]([O-])=O)C=C([N+]([O-])=O)C=C1[N+]([O-])=O OXNIZHLAWKMVMX-UHFFFAOYSA-M 0.000 description 1
- OXNIZHLAWKMVMX-UHFFFAOYSA-N picric acid Chemical compound OC1=C([N+]([O-])=O)C=C([N+]([O-])=O)C=C1[N+]([O-])=O OXNIZHLAWKMVMX-UHFFFAOYSA-N 0.000 description 1
- 125000003386 piperidinyl group Chemical group 0.000 description 1
- 229920001223 polyethylene glycol Polymers 0.000 description 1
- 229940068917 polyethylene glycols Drugs 0.000 description 1
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
- 244000144977 poultry Species 0.000 description 1
- 235000013594 poultry meat Nutrition 0.000 description 1
- 239000012254 powdered material Substances 0.000 description 1
- 238000004321 preservation Methods 0.000 description 1
- 229960003910 promethazine Drugs 0.000 description 1
- 238000011321 prophylaxis Methods 0.000 description 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 125000006239 protecting group Chemical group 0.000 description 1
- 238000000746 purification Methods 0.000 description 1
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 description 1
- 150000003222 pyridines Chemical class 0.000 description 1
- 210000000664 rectum Anatomy 0.000 description 1
- 230000009467 reduction Effects 0.000 description 1
- 239000005871 repellent Substances 0.000 description 1
- 230000002940 repellent Effects 0.000 description 1
- 239000012260 resinous material Substances 0.000 description 1
- 229960000581 salicylamide Drugs 0.000 description 1
- WKEDVNSFRWHDNR-UHFFFAOYSA-N salicylanilide Chemical compound OC1=CC=CC=C1C(=O)NC1=CC=CC=C1 WKEDVNSFRWHDNR-UHFFFAOYSA-N 0.000 description 1
- 229950000975 salicylanilide Drugs 0.000 description 1
- 229960004889 salicylic acid Drugs 0.000 description 1
- 239000007259 schaedler broth Substances 0.000 description 1
- 201000000980 schizophrenia Diseases 0.000 description 1
- 238000007789 sealing Methods 0.000 description 1
- 235000013874 shellac Nutrition 0.000 description 1
- 229960005480 sodium caprylate Drugs 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- 239000001509 sodium citrate Substances 0.000 description 1
- NLJMYIDDQXHKNR-UHFFFAOYSA-K sodium citrate Chemical compound O.O.[Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O NLJMYIDDQXHKNR-UHFFFAOYSA-K 0.000 description 1
- 235000010267 sodium hydrogen sulphite Nutrition 0.000 description 1
- BYKRNSHANADUFY-UHFFFAOYSA-M sodium octanoate Chemical compound [Na+].CCCCCCCC([O-])=O BYKRNSHANADUFY-UHFFFAOYSA-M 0.000 description 1
- JXKPEJDQGNYQSM-UHFFFAOYSA-M sodium propionate Chemical compound [Na+].CCC([O-])=O JXKPEJDQGNYQSM-UHFFFAOYSA-M 0.000 description 1
- 239000004324 sodium propionate Substances 0.000 description 1
- 235000010334 sodium propionate Nutrition 0.000 description 1
- 229960003212 sodium propionate Drugs 0.000 description 1
- DAEPDZWVDSPTHF-UHFFFAOYSA-M sodium pyruvate Chemical compound [Na+].CC(=O)C([O-])=O DAEPDZWVDSPTHF-UHFFFAOYSA-M 0.000 description 1
- 239000008247 solid mixture Substances 0.000 description 1
- 239000011877 solvent mixture Substances 0.000 description 1
- 239000004334 sorbic acid Substances 0.000 description 1
- 235000010199 sorbic acid Nutrition 0.000 description 1
- 229940075582 sorbic acid Drugs 0.000 description 1
- UNFWWIHTNXNPBV-WXKVUWSESA-N spectinomycin Chemical compound O([C@@H]1[C@@H](NC)[C@@H](O)[C@H]([C@@H]([C@H]1O1)O)NC)[C@]2(O)[C@H]1O[C@H](C)CC2=O UNFWWIHTNXNPBV-WXKVUWSESA-N 0.000 description 1
- 229960000268 spectinomycin Drugs 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 239000008117 stearic acid Substances 0.000 description 1
- 239000008227 sterile water for injection Substances 0.000 description 1
- 230000001954 sterilising effect Effects 0.000 description 1
- 238000004659 sterilization and disinfection Methods 0.000 description 1
- 150000003431 steroids Chemical class 0.000 description 1
- 210000002784 stomach Anatomy 0.000 description 1
- 229940044603 styrene Drugs 0.000 description 1
- 125000003107 substituted aryl group Chemical group 0.000 description 1
- 229960005158 sulfamethizole Drugs 0.000 description 1
- VACCAVUAMIDAGB-UHFFFAOYSA-N sulfamethizole Chemical compound S1C(C)=NN=C1NS(=O)(=O)C1=CC=C(N)C=C1 VACCAVUAMIDAGB-UHFFFAOYSA-N 0.000 description 1
- 229960001363 sulfamoxole Drugs 0.000 description 1
- CYFLXLSBHQBMFT-UHFFFAOYSA-N sulfamoxole Chemical compound O1C(C)=C(C)N=C1NS(=O)(=O)C1=CC=C(N)C=C1 CYFLXLSBHQBMFT-UHFFFAOYSA-N 0.000 description 1
- 239000004094 surface-active agent Substances 0.000 description 1
- 239000000375 suspending agent Substances 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 230000002195 synergetic effect Effects 0.000 description 1
- 238000003786 synthesis reaction Methods 0.000 description 1
- 239000011975 tartaric acid Substances 0.000 description 1
- 235000002906 tartaric acid Nutrition 0.000 description 1
- 229940095064 tartrate Drugs 0.000 description 1
- 229940040944 tetracyclines Drugs 0.000 description 1
- NQRYJNQNLNOLGT-UHFFFAOYSA-N tetrahydropyridine hydrochloride Natural products C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 description 1
- 239000004753 textile Substances 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 229940100615 topical ointment Drugs 0.000 description 1
- 231100000331 toxic Toxicity 0.000 description 1
- 230000002588 toxic effect Effects 0.000 description 1
- 108010050327 trypticase-soy broth Proteins 0.000 description 1
- 208000019206 urinary tract infection Diseases 0.000 description 1
- 229940044959 vaginal cream Drugs 0.000 description 1
- 239000000522 vaginal cream Substances 0.000 description 1
- 235000015112 vegetable and seed oil Nutrition 0.000 description 1
- 239000008158 vegetable oil Substances 0.000 description 1
- 229930003231 vitamin Natural products 0.000 description 1
- 239000011782 vitamin Substances 0.000 description 1
- 235000013343 vitamin Nutrition 0.000 description 1
- 229940088594 vitamin Drugs 0.000 description 1
- 239000011712 vitamin K Substances 0.000 description 1
- 235000019168 vitamin K Nutrition 0.000 description 1
- 150000003721 vitamin K derivatives Chemical class 0.000 description 1
- 150000003722 vitamin derivatives Chemical class 0.000 description 1
- 229940046010 vitamin k Drugs 0.000 description 1
- 238000005406 washing Methods 0.000 description 1
- 239000000080 wetting agent Substances 0.000 description 1
- 239000010497 wheat germ oil Substances 0.000 description 1
- 238000010626 work up procedure Methods 0.000 description 1
- 238000002424 x-ray crystallography Methods 0.000 description 1
- 239000012138 yeast extract Substances 0.000 description 1
- 229960001296 zinc oxide Drugs 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
- C07H15/02—Acyclic radicals, not substituted by cyclic structures
- C07H15/14—Acyclic radicals, not substituted by cyclic structures attached to a sulfur, selenium or tellurium atom of a saccharide radical
- C07H15/16—Lincomycin; Derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Oncology (AREA)
- Animal Behavior & Ethology (AREA)
- Communicable Diseases (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Crystallography & Structural Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Biochemistry (AREA)
- Biotechnology (AREA)
- Genetics & Genomics (AREA)
- Molecular Biology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Saccharide Compounds (AREA)
Description
æçç©è³ªãªã³ã³ãã€ã·ã³ã®ç¹æ§åã³èª¿è£œã¯åè¡
åœç¹èš±ç¬¬3086912å·ã§æããã«ãããŠãããã¯ãª
ã³ããã€ã·ã³ã¯åè¡åœç¹èš±ç¬¬3496163å·ã§æãã
ã«ãããŠããããããã®æçç©è³ªã¯äººéåã³åç©
ã®å»è¬ãšããŠåºç¯å²ã«çšããããŠããããããã®
æçç©è³ªããã®ããŸããŸãªèªå°äœé¡ã«ã€ããŠäžç
çãªå€æ°ã®ç¹èš±ãå ¬åžãããã ãªã³ã³ãã€ã·ã³ã¯æ¬¡ã®æ§é åŒããã€ãŠããã ã¯ãªã³ããã€ã·ã³ã¯æ¬¡ã®æ§é åŒããã€ãŠããã æ¬åºé¡ã¯ åŒ ã®æ°èŠã§æçšãªååç©åã¯è£œè¬åŠçã«åå ¥ããã
ããã®é žä»å å¡©ã«é¢ããã ãåŒäžR1ã¯ããã§ã«R2ã§çœ®æãããŠã¯ããªã
ããªãžã³ç°ã®ä»»æã®äœçœ®ã§ãäžååã¯è€æ°å眮æ
ããããã®ã§ãã€ãŠãæ°ŽçŽ ãã¢ã«ãã«ã眮æãã
ãã¢ã«ãã«ïŒçœ®æã¢ã«ãã«ïŒïŒã¢ã«ãã«éšåã¯ïŒ
ãïŒåã®ççŽ ååïŒåã¯ãã®ç°æ§äœåãã·ã¯ãã¢
ã«ãã«ã眮æãããã·ã¯ãã¢ã«ãã«ïŒçœ®æã·ã¯ã
ã¢ã«ãã«ïŒçœ®æãããé žçŽ ïŒçœ®æé žçŽ ïŒã眮æã
ããçªçŽ ïŒçœ®æçªçŽ ïŒãããã²ã³ãããšãã«ã眮
æãããããšãã«ïŒçœ®æããšãã«ïŒãâïŒCH2ïŒo
âOHãâïŒCH2ïŒoâNR4R5ãåã¯ãã®ç°æ§äœå
ã§ãããïŒããã§ïœã¯ïŒãïŒã®æŽæ°ã§ãããR4ãš
R5ã¯ïŒšåã¯ïŒãïŒåã®ççŽ ååã®ã¢ã«ãã«åã¯
ãã®ç°æ§äœåã§ããïŒãR2ã¯ãã§ã«R1ã§çœ®æãã
ãŠã¯ããªãããªãžã³ç°ã®ä»»æã®äœçœ®ã§ïŒå眮æã
ãããã®ã§ã
åœç¹èš±ç¬¬3086912å·ã§æããã«ãããŠãããã¯ãª
ã³ããã€ã·ã³ã¯åè¡åœç¹èš±ç¬¬3496163å·ã§æãã
ã«ãããŠããããããã®æçç©è³ªã¯äººéåã³åç©
ã®å»è¬ãšããŠåºç¯å²ã«çšããããŠããããããã®
æçç©è³ªããã®ããŸããŸãªèªå°äœé¡ã«ã€ããŠäžç
çãªå€æ°ã®ç¹èš±ãå ¬åžãããã ãªã³ã³ãã€ã·ã³ã¯æ¬¡ã®æ§é åŒããã€ãŠããã ã¯ãªã³ããã€ã·ã³ã¯æ¬¡ã®æ§é åŒããã€ãŠããã æ¬åºé¡ã¯ åŒ ã®æ°èŠã§æçšãªååç©åã¯è£œè¬åŠçã«åå ¥ããã
ããã®é žä»å å¡©ã«é¢ããã ãåŒäžR1ã¯ããã§ã«R2ã§çœ®æãããŠã¯ããªã
ããªãžã³ç°ã®ä»»æã®äœçœ®ã§ãäžååã¯è€æ°å眮æ
ããããã®ã§ãã€ãŠãæ°ŽçŽ ãã¢ã«ãã«ã眮æãã
ãã¢ã«ãã«ïŒçœ®æã¢ã«ãã«ïŒïŒã¢ã«ãã«éšåã¯ïŒ
ãïŒåã®ççŽ ååïŒåã¯ãã®ç°æ§äœåãã·ã¯ãã¢
ã«ãã«ã眮æãããã·ã¯ãã¢ã«ãã«ïŒçœ®æã·ã¯ã
ã¢ã«ãã«ïŒçœ®æãããé žçŽ ïŒçœ®æé žçŽ ïŒã眮æã
ããçªçŽ ïŒçœ®æçªçŽ ïŒãããã²ã³ãããšãã«ã眮
æãããããšãã«ïŒçœ®æããšãã«ïŒãâïŒCH2ïŒo
âOHãâïŒCH2ïŒoâNR4R5ãåã¯ãã®ç°æ§äœå
ã§ãããïŒããã§ïœã¯ïŒãïŒã®æŽæ°ã§ãããR4ãš
R5ã¯ïŒšåã¯ïŒãïŒåã®ççŽ ååã®ã¢ã«ãã«åã¯
ãã®ç°æ§äœåã§ããïŒãR2ã¯ãã§ã«R1ã§çœ®æãã
ãŠã¯ããªãããªãžã³ç°ã®ä»»æã®äœçœ®ã§ïŒå眮æã
ãããã®ã§ã
ãåŒãã§ããããããã§ïŒžã¯ïŒ
ïŒïŒ²ïŒâããããã·âã¡ãã«ïŒâããªâαâãªã³
ã³ãµããããïŒïŒïŒ³ïŒâããããã·âã¡ãã«ïŒâ
ããªâαâãªã³ã³ãµããããïŒïŒïŒ³ïŒâããâã¡
ãã«ïŒâããªâαâãªã³ã³ãµããããïŒïŒïŒ²ïŒâ
ããâã¡ãã«ïŒâããªâαâãªã³ã³ãµããããïŒ
ïŒïŒ³ïŒâã¡ããã·âã¡ãã«ïŒâããªâαâãªã³ã³
ãµããããïŒâããªãã·âïŒïŒïŒ³ïŒâïŒã¡ãã«ã
ãªïŒâã¡ãã«ïŒâããªâαâãªã³ã³ãµããããïŒ
âããªãã·âïŒïŒïŒ³ïŒâïŒïŒâããããã·ãšãã«
ããªïŒã¡ãã«ïŒâããªâαâãªã³ã³ãµãããåã³
ïŒâããªãã·âïŒïŒïŒ³ïŒâïŒïŒâããããã·ãã
ãã«ããªïŒâã¡ãã«ïŒâããªâαâãªã³ã³ãµãã
ããããªã矀ããéžã°ããååç©ã®ã¢ããå®èœåº
ã§ããã æ¬çºæã¯äžåŒã®ååç©ã®åé§ç©è³ªã§ããã åŒäžR1ã¯ç°äžã§ç°ã®åãççŽ åã¯å¥ã®ççŽ äž
ã«ïŒååã¯è€æ°å眮æããããã®ã§ãããåR2
ã¯ç°ã®ïŒïŒïŒïŒïŒïŒïŒïŒïŒïŒïŒïŒïŒåã¯ïŒäœçœ®ã«
ããããŠãäžã«å®çŸ©ããããšããã§ãããR3ã¯
ãCH3ãC2H5åã³âCH2âCH2âOHãããªã
矀ããéžã°ããïœã¯ïŒãïŒã®æŽæ°ã§ããã æ¬æ现æžã«èšèŒã®æ°èŠé¡äŒŒäœé¡ã®åæã¯æ¬¡ã®äŸ
瀺çãªåœ¢ã§ç€ºãããšãã§ããã æ³¢ç·ã¯ïŒ€âã·ã¹åã¯ïŒ¬âã·ã¹ç°æ§äœã®ãã¥ããã
瀺ãã æ³¢ç·ã¯ïŒ€âã·ã¹ãâã·ã¹ãâãã©ã³ã¹åã¯
âãã©ã³ã¹æ§é ã瀺ãã æ¬çºæã®ååç©ãã補é ãããâã·ã¹æ§é ã¯ãå®éšçšã¯ã€ãããã¿ã§é»è²ãããŠçèïŒS.
aureusïŒãšæº¶è¡é£éçèïŒS.hemolyticusïŒã«å¯Ÿ
ãã¯ãªã³ããã€ã·ã³ããïŒã10å掻æ§ã§ããããš
ã瀺ãããã äžã®åå¿ããã®ç°æ§äœãåé¢ã§ãããããã
ã¯ïŒ€âã·ã¹ååç©VAãšæãããããâã·ã¹æ§
é ã¯ïŒ¬âã·ã¹ååç©ã»ã©å¹åã®ããæèå€ã§ã¯ãª
ãã MTLã¯åŒ ã®ã¡ãã«ïŒâããªâαâãªã³ã³ãµãããã§ããã ãšãâMTLã¯åŒ ã®ã¡ãã«ïŒïŒïŒ³ïŒâïŒâããªãã·âïŒâãããã
ã·âïŒâããªâαâãªã³ã³ãµãããã§ããã ïŒâClâMTLã¯åŒ ã®ã¡ãã«ïŒïŒïŒ³ïŒâïŒâããªãã·âïŒâã¯ããâ
ïŒâããªâαâãªã³ã³ãµãããã§ããã ãšãâïŒâClâMTLã¯åŒ ã®ã¡ãã«ïŒïŒïŒ²ïŒâïŒâããªãã·âïŒâã¯ããâ
ïŒâããªâαâãªã³ã³ãµãããã§ããã ïŒïŒïŒ³ïŒâã¡ããã·âã¡ãã«ïŒâããªâαâãª
ã³ã³ãµãããã¯æ¬¡ã®ããã«ç€ºãããšãã§ããã
ïŒåè¡åœç¹èš±ç¬¬3702322å·ãå®æœäŸïŒã®ïŒ¢âïŒéšïŒ 次åŒãåç §ãããšããCH3ã®æã«ïŒâããªã
ã·âïŒïŒïŒ³ïŒâïŒã¡ãã«ããªïŒâã¡ãã«ïŒâããª
âαâãªã³ã³ãµããããååšããããâCH2â
CH2âOHã®æã«ã¯ïŒâããªãã·âïŒïŒïŒ³ïŒâ
ïŒïŒâããããã·ãšãã«ããªïŒâã¡ãã«ïŒâããª
âαâãªã³ã³ãµããããååšããããŸããâ
CH2âCH2âCH2âOHã®æã«ã¯ãïŒâããªãã·
âïŒïŒïŒ³ïŒâïŒïŒâããããã·ãããã«ããªïŒâ
ã¡ãã«ïŒâããªâαâãªã³ã³ãµããããååšã
ããïŒåè¡åœç¹èš±ç¬¬3915954å·ã®å®æœäŸïŒïŒ10åã³
31ãåç §ïŒ äžåŒã®ïŒâäœçœ®ã®ããããã·åã³ããåºã¯æ¬¡ã®
ããã«ç€ºãããšãã§ããã åŒäžïŒ¹ã¯ïŒïŒïŒ²ïŒâããããã·ãïŒïŒïŒ³ïŒâãã
ããã·ãïŒïŒïŒ³ïŒâãããåã³ïŒïŒïŒ²ïŒâãããã
ãªã矀ããéžã°ããã ããªãžã³ã¢ã·ã«åºã䜿çšããŠåèšè£œé ãè¡ãã
çããæ¬çºæã®é¡äŒŒäœãéå ããŠå¯Ÿå¿ãã飜åå
åç©ã®æ··åç©ãçãããã®äžã€ã¯ïŒ¬âã·ã¹ç°æ§äœ
ã§ãããååšããããã®ä»ã®ååç©é¡ã¯ïŒ¬âãã©
ã³ã¹ãâã·ã¹ãåã³ïŒ€âãã©ã³ã¹ç°æ§äœé¡ã§ã
ããäžè¬ã«æ¬æ现æžã«èšèŒã®ä»»æã®ååç©é¡ã«ã€
ããŠã¯ãéå åã¯æ¬çºæã®äžé£œååé§ç©è³ªããæ
è掻æ§ã匷ãããããªãžã³ã¢ã·ã«åºã®äœ¿çšã¯ã
âã·ã¹ãâã·ã¹ãâãã©ã³ã¹åã³ïŒ¬âãã©ã³
ã¹ç°æ§äœãšããŠååšããé¡äŒŒäœãäžãããããã§
ãâã·ã¹ç°æ§äœã¯ãæè掻æ§ããã匷åã§ãã
ããšãããã€ãã æ°èŠé¡äŒŒäœé¡ãã€ããã®ã«æ¬æ现æžã§çšããã
ãäžè¬çãªæ¹æ³ã¯åšç¥ã®æ¹æ³ã§ãã€ãŠãé©åœãªé ž
ãé©åœãªç³ã¢ãã³ãšçµåããããã®ã§ãããïŒãæ··
åã«ã«ãã³é žç¡æ°Žç©æé ïŒMixed Carboxylic
Acid Anbydride ProcednreïŒãã¢ããé žååŠ
ïŒChemistry of The Amino AcidsïŒç¬¬ïŒå·»970
é ããžãšã³ã»ãŠã€ãªãŒã»ã¢ã³ãã»ãµã³ãºç€Ÿã1961
幎ïŒãé žãäžé£œåã®æã«ã¯ãçããäžé£œåé¡äŒŒäœ
ãæšæºæ¡ä»¶äžã«æ¥è§Šéå ããŠã飜åé¡äŒŒäœãã€ã
ããããäŸãã°æ¬¡ã®æ¡ä»¶ã䜿çšããŠéå ãè¡ãã
ãšãã§ããã H2â0.352ã3.52KgïŒcm2ïŒïŒã50psiïŒ è§Šåªâé žåçœéïŒPtO2ïŒ æº¶åªâH2Oåã¯H2OïŒMeOHïŒåã¯H2OïŒ
EtOH HClâ10ïŒ éå°ã æéâ24ã48æé æ¬æ现æžã§äœ¿çšããæã«ãïŒãïŒåã®ççŽ åå
ã®ã¢ã«ãã«ãšãã®ç°æ§äœåã¯ãã¡ãã«ããšãã«ã
ãããã«ãããã«ããã³ãã«ãããã·ã«ãããã
ã«ããªã¯ãã«ãåã³ãã®åæéç°æ§äœé¡ãå å«ã
ãã 眮æã¢ã«ãã«ã¯ãæ°ŽçŽ ååã®äžã€ãŸãã¯ãã以
äžãããã²ã³ããªãã¡ClïŒBrïŒïŒŠåã³ïŒ©ãé žçŽ ã
ããããã·ã«ãã¢ãã³ïŒç¬¬äžçŽïŒãã¢ãã³ïŒç¬¬äº
çŽâäžèšã®ãããªã¢ã«ãã«ã§ã¢ã«ãã«çœ®æãããŠ
ããïŒãã¢ãã³ïŒç¬¬äžçŽâäžèšã®ãããªã¢ã«ãã«
ã§ã¢ã«ãã«çœ®æãããŠããïŒãç¡«é»ãâSHãåã³
ããšãã«ã§çœ®ããããããäžã®ã¢ã«ãã«ååç©ã
æå³ãããååç©ã®äŸã¯ïŒâãã«ãªããšãã«ãïŒ
âã¯ãããšãã«ãïŒâãã«ãªããšãã«ãïŒâã¯ã
ããšãã«ãïŒâããã¢ãããã«ãïŒâãšãŒããã
ãã«ãïŒâã¯ããããã«ãïŒâãã«ãªãããã«ã
åã³ïŒâã¯ããããã«ã§ããã ã·ã¯ãã¢ã«ãã«ã¯ã·ã¯ããããã«ãã·ã¯ããã
ã«ãã·ã¯ããã³ãã«ãã·ã¯ãããã·ã«ãã·ã¯ãã
ããã«ãåã³ã·ã¯ããªã¯ãã«ãæå³ããã 眮æã·ã¯ãã¢ã«ãã«ã¯çœ®æã¢ã«ãã«ã«ã€ããŠäž
ã«èšèŒããããã«çœ®æãããã·ã¯ãã¢ã«ãã«ãæ
å³ãããååç©ã®äŸã¯ïŒâã·ã¯ããããã«ãšã
ã«ãïŒâã·ã¯ãããã«ãããã«ãïŒâã·ã¯ããã³
ãã«ããã«ãåã³ïŒâã·ã¯ãããã·ã«ããã«ã§ã
ãã è³éŠæã¯ããšãã«åã³ãæ°ŽçŽ ååã®äžã€åã¯ã
ã以äžãäžã®ãããªããã²ã³ãããããã·ã«ãã¢
ãã³ïŒç¬¬äžçŽã第äºçŽãåã³ç¬¬äžçŽã§ããããåŸ
ã®äºè ã¯äžã®ããã«ã¢ã«ãã«ã§çœ®æãããŠããã
ã®ïŒãâSHãåã³ããšãã«ã§çœ®ããããããå Žå
ã®çœ®æããšãã«ãæå³ãããååç©ã®äŸã¯ïœâã
ãã¢ããšãã«ãïœâãšãŒãããšãã«ãïœâã¯ãã
ããšãã«ãïœâãšãã«ããšãã«ãïœâãããã«ã
ãšãã«ãïœâã¡ãã«ããšãã«ãåã³ïœâãªã¯ãã«
ããšãã«ã§ããã äžã«è©³ããè¿°ã¹ãããã«ãæ¬çºæååç©é¡ãã
ã¹ããªã«åãããšïŒâãã¹ããšãŒããçããã¢ã·
ã«åãããšïŒâãã«ãããŒããçããäž¡è ãšãç
äœå ã§æè掻æ§ãããã 眮æé žçŽ ã¯ïŒãïŒåã®ççŽ ã®ã¢ã«ãã«ãã¢ãªãŒ
ã«åã³çœ®æã¢ãªãŒã«ã§çœ®æãããé žçŽ ãæå³ã
ãã 眮æçªçŽ ã¯ãïŒã18åã®ççŽ ã®ã¢ã·ã«ãïŒãïŒ
åã®ççŽ ã®ã¢ãã¢ã«ãã«ãåã³ãžã¢ã«ãã«ïŒã¢ã«
ãã«ã¯ïŒãïŒåã®ççŽ ã§ãã¢ã·ã«åºãšã¢ã«ãã«åº
ã¯ããããç°æ§äœåãå«ãïŒã§çœ®æãããçªçŽ ã
æå³ããã ããã¯ã¯ãããããã¢ããšãŒããåã¯ãã«ãªã
ãæå³ããã æ¬æ现æžã®åºçºææãšããŠäœ¿ãããã¢ããé žã®
æš¡ç¯çãªåºå žã¯ä»¥äžã®ãšããã§ããã ïŒ ãè€çŽ ç°åŒååç©ïŒHeterocyclic
CompoundsïŒã第ïŒå·»ããžãšã³ã»ãŠã€ãªãŒã»ã¢
ã³ãã»ãµã³ãºç€Ÿã1950幎ããã®è³æã¯ããã²ã³
åã³ã¢ã«ãã«çœ®æã¢ããé žã®è£œé ãèšèŒããŠã
ãã ïŒ ã±ãã«ã«ã»ã¢ãã¹ãã©ã¯ã 81â105223Aâã¢ã«ãã«åã³ã·ã¯ãã¢ã«ãã«ã 81â152243Sâã¢ã«ãã«åã³ããã²ã³çœ®æã 82â170746âããã²ã³çœ®æã 85â46322Qâãžãã眮æã 85â177258Wâãžãã眮æã 84â116928Xâãžãã眮æã 81â3737dâããšãã«çœ®æã 78â58201tâããšãã«çœ®æã 76â126800yâããã©ãã眮æã 82â11036Kâããã¢çœ®æã 83â27119Wâããã¢çœ®æã 84â16613Xâããã¢çœ®æã 78â123494Gâããã¢çœ®æã ãã®ååç©ã¯ãã®æè¡ã§åšç¥ã®æ段ã«ãã€ãŠ
é žã«å æ°Žå解ã§ãããã®é žããã¯ããã®æè¡ã§
åšç¥ã®æ段ã«ãã€ãŠéå ã§ããã ãã®ååç©ã¯ãã®æè¡ã§åšç¥ã®æ段ã«ãã€ãŠ
é žã«å æ°Žå解ã§ãããçããé žã次ã«åè¡åœç¹
蚱第3583972å·ã«èšèŒã®æé ã«ããâè±ã¡ã
ã«åã§ããã ãã®ååç©ã¯ãã®æè¡ã§åšç¥ã®æ段ã«ãã€ãŠ
é žã«å æ°Žå解ã§ããã ãã®ååç©ã¯ãã®æè¡ã§åšç¥ã®æ段ã«ãã€ãŠ
é žã«å æ°Žå解ã§ããããŸããçããé žããåè¡
åœç¹èš±ç¬¬3583972å·ã§æããã«ãããæé ã«ã
ã€ãŠãâCH3åºã®äžæ¹åã¯åæ¹ãé€å»ã§ã
ãã ãã®ååç©ã¯ãã®æè¡ã§åšç¥ã®æ段ã«ãã€ãŠ
é žã«å æ°Žå解ã§ãããçããé žã¯åè¡åœç¹èš±ç¬¬
3583972å·ã«é瀺ãããæ¹æ³ã«ãã€ãŠæ¬¡ã®åå
ç©ã«è»¢åã§ããã éé¢ã®NH2åã¯OHåºããã€ååç©é¡ã¯ãã¢
ããç³ãšçž®åãããåã«ãããã®åºãä¿è·ããŠ
ãããªããŠã¯ãªããªãããã®ãããªåºã®ä¿è·ã¯
ãã®æè¡ã§åšç¥ã§ããããææ©ååŠã®ä¿è·åº
ïŒProtective Groups in Organic
ChemistryïŒãããžãšã€ã»ãšãããããªãŠãŒã»ã
ã³ããŒïŒJ.F.W.McomieïŒããã¬ãã åºç瀟ã
1973幎ããåç §ã®ããšã ïŒ ãžã€ãŒãã« ãªã ã±ãã«ã« ãœãµãšãã€
ïŒJour.Chem.Soc.ïŒ1969幎ã2134é ã çš®ã ã®ïŒšâã¢ã«ãã«çœ®æããªãžã³é¡ã ïŒåžè²©ã®ãã®ïŒ ïŒã¢ã«ãã«ãåæã¢ã«ãã«ãåã³ã·ã¯ãã¢ã«
ãã«ã ïŒ Joar.Chem.Soc.1969幎934é 以äžã®å®æœäŸã¯æ¬çºææ¹æ³åã³çæç©ã®äŸç€ºã§
ããããéå®ãããã®ãšèããŠã¯ãªããªããä»ã«
泚æããªããã°ãçŸåçã¯ãã¹ãŠééã«ããããŸ
ã溶åªæ··åç©ã®å²åã¯ãã¹ãŠå®¹éã«ããã å®æœäŸïŒ ïŒâClâMTLã®ïŒâã·ã¹âãšãã«â
âãããµããããã³ãªã³é žHClïŒïŒµâ57930E
âååç©ïŒ¶ïŒ ã¢ã»ããããªã«2.5ãªããã«äžã«æº¶è§£ãããã¢
ããé žHClïŒã±ãã«ã«ã»ã¢ãã¹ãã©ã¯ã51å·»
1643aã1957幎ïŒ67ïœïŒ0.357ã¢ã«ïŒãšããªãšãã«
ã¢ãã³71.5ïœïŒ0.714ã¢ã«ïŒã®æº¶æ¶²ã10âã«å·åŽ
ããã€ãœããã«ã¯ããããªã«ã¡ãŒã47.6ïœ
ïŒ0.354ã¢ã«ïŒãäžåºŠã«å ããããã®æ··åç©ïŒæº¶æ¶²
ïŒã10âã§ïŒæéãããŸãããã¢ã»ãã³1500ml
ãšH2O1500mlãšã®æž©ããæ··åç©äžã«ïŒâClâ
MTLïŒJ.Med.Chem.12å·»780é ã1969幎ãããŒã»
ãžãšãŒã»ãã¬ãŒã¬ã€ã³ïŒB.J.MegerleinïŒåã³ãš
ãã»ã«ã¬ã³ïŒF.KaganïŒïŒ97.7ïœïŒ0.357ã¢ã«ïŒã
溶解ããããšã«ãã€ãŠæº¶æ¶²ïŒ¢ãã€ããã溶液ã
30âã«å·åŽãã溶液ã«äžåºŠã«å ãããåå¿æ¶²ã
25âã§18æéãããŸããã¢ã»ãã³åã³ã¢ã»ããã
ãªã«ãç空äžã§é€å»ãããçœãããç¶ã®æ®çç©ã
ãéããçµæ¶ç¶ã®ææãéããŠä¹Ÿç¥ãããšãçŽç²
ãªçæç©95ïœãçãããã液ãä»äžãããšïŒã¯ã
ããã°ã©ãã€ïŒãå¥ã«çæç©10ïœãçãããå šäœ
ã®åç73ïŒ åæïŒ C17H25ClN2O5Sã«å¯Ÿã㊠èšç®å€ïŒïŒ£ïŒ50.42ïŒïŒšïŒ6.22ïŒïŒ®ïŒ6.92ïŒ ïŒ³ïŒ7.92ïŒClïŒ8.76 枬å®å€ïŒïŒ£ïŒ50.67ïŒïŒšïŒ6.40ïŒïŒ®ïŒ6.64ïŒ ïŒ³ïŒ7.90ïŒClïŒ8.70 αCHCl3 D ïŒïŒ£ïŒ1.0ïŒïŒ293ã åºçºææ4.05ïœïŒ0.01ã¢ã«ïŒãæ°Ž40mlãã¡ã¿ã
ãŒã«60mlã37ïŒ HCl1.0mlåã³PtO28.0ïœã®æ··åç©
ãããŒæ°ŽçŽ æ·»å è£ çœ®ã«ãã3.52KgïŒcm2ïŒ50p.s.iïŒ
ã§ïŒæééå ãããCHCl3ïŒã¡ã¿ããŒã«ïŒïŒïŒ
ïŒïŒãããªãç³»ã§ã·ãªã«ã²ã«æ¿äžã®TLCã«ãã€
ãŠåå¿æ··åç©ãåæãããšãåºçºææãå šéšæ¶ã
ãŠã極æ§ã®ãã倧ããäºã€ã®ææãçŽïŒïŒïŒã®æ¯
ã§ååšããããšã瀺ããã觊åªãé€å»ããããã«
åå¿æ¶²ããéããã液ãç空äžã«æ¿çž®ãããšãçœ
ãçµæ¶æ§ã®ãããçãããããããéããã液ã
貯ãããåå¿æ··åç©ã®TLCã«ãã€ãŠèŠ³å¯ããã
äºçæç©ã®ãã¡ã極æ§ã®æã倧ãããã®çœè²åºäœ
ã¯ãæ°Žããåçµæ¶ããããšã25ã35ïŒ ã®åçã§æ
ãã§ããçæç©ïŒµâ57930Eãèç¹222ã224âã
çããã åæïŒ C17H32Cl2N2O5Sã«å¯Ÿã㊠èšç®å€ïŒïŒ£ïŒ45.63ïŒïŒšïŒ7.21ïŒïŒ®ïŒ6.26ïŒ ïŒ³ïŒ7.17ïŒClïŒ15.85 枬å®å€ïŒïŒ£ïŒ45.77ïŒïŒšïŒ7.44ïŒïŒ®ïŒ6.39ïŒ ïŒ³ïŒ7.21ïŒClïŒ16.17 αH2O D ïŒïŒ£ïŒ1.0ïŒïŒ176ã ã®çµ¶å¯Ÿç«äœé 眮åã³ç«äœååŠã¯ãç·çµæ¶åŠ
ã«ãã€ãŠç¢ºå®ãããã ã¯ãªã³ããã€ã·ã³ãšã®æ¯èŒã«ãããŠãè©Šéšãã
ãâ57930Eã¯æ¬¡ã®æèã¹ãã¯ãã«ããã€ãŠã
ãã
ã³ãµããããïŒïŒïŒ³ïŒâããããã·âã¡ãã«ïŒâ
ããªâαâãªã³ã³ãµããããïŒïŒïŒ³ïŒâããâã¡
ãã«ïŒâããªâαâãªã³ã³ãµããããïŒïŒïŒ²ïŒâ
ããâã¡ãã«ïŒâããªâαâãªã³ã³ãµããããïŒ
ïŒïŒ³ïŒâã¡ããã·âã¡ãã«ïŒâããªâαâãªã³ã³
ãµããããïŒâããªãã·âïŒïŒïŒ³ïŒâïŒã¡ãã«ã
ãªïŒâã¡ãã«ïŒâããªâαâãªã³ã³ãµããããïŒ
âããªãã·âïŒïŒïŒ³ïŒâïŒïŒâããããã·ãšãã«
ããªïŒã¡ãã«ïŒâããªâαâãªã³ã³ãµãããåã³
ïŒâããªãã·âïŒïŒïŒ³ïŒâïŒïŒâããããã·ãã
ãã«ããªïŒâã¡ãã«ïŒâããªâαâãªã³ã³ãµãã
ããããªã矀ããéžã°ããååç©ã®ã¢ããå®èœåº
ã§ããã æ¬çºæã¯äžåŒã®ååç©ã®åé§ç©è³ªã§ããã åŒäžR1ã¯ç°äžã§ç°ã®åãççŽ åã¯å¥ã®ççŽ äž
ã«ïŒååã¯è€æ°å眮æããããã®ã§ãããåR2
ã¯ç°ã®ïŒïŒïŒïŒïŒïŒïŒïŒïŒïŒïŒïŒïŒåã¯ïŒäœçœ®ã«
ããããŠãäžã«å®çŸ©ããããšããã§ãããR3ã¯
ãCH3ãC2H5åã³âCH2âCH2âOHãããªã
矀ããéžã°ããïœã¯ïŒãïŒã®æŽæ°ã§ããã æ¬æ现æžã«èšèŒã®æ°èŠé¡äŒŒäœé¡ã®åæã¯æ¬¡ã®äŸ
瀺çãªåœ¢ã§ç€ºãããšãã§ããã æ³¢ç·ã¯ïŒ€âã·ã¹åã¯ïŒ¬âã·ã¹ç°æ§äœã®ãã¥ããã
瀺ãã æ³¢ç·ã¯ïŒ€âã·ã¹ãâã·ã¹ãâãã©ã³ã¹åã¯
âãã©ã³ã¹æ§é ã瀺ãã æ¬çºæã®ååç©ãã補é ãããâã·ã¹æ§é ã¯ãå®éšçšã¯ã€ãããã¿ã§é»è²ãããŠçèïŒS.
aureusïŒãšæº¶è¡é£éçèïŒS.hemolyticusïŒã«å¯Ÿ
ãã¯ãªã³ããã€ã·ã³ããïŒã10å掻æ§ã§ããããš
ã瀺ãããã äžã®åå¿ããã®ç°æ§äœãåé¢ã§ãããããã
ã¯ïŒ€âã·ã¹ååç©VAãšæãããããâã·ã¹æ§
é ã¯ïŒ¬âã·ã¹ååç©ã»ã©å¹åã®ããæèå€ã§ã¯ãª
ãã MTLã¯åŒ ã®ã¡ãã«ïŒâããªâαâãªã³ã³ãµãããã§ããã ãšãâMTLã¯åŒ ã®ã¡ãã«ïŒïŒïŒ³ïŒâïŒâããªãã·âïŒâãããã
ã·âïŒâããªâαâãªã³ã³ãµãããã§ããã ïŒâClâMTLã¯åŒ ã®ã¡ãã«ïŒïŒïŒ³ïŒâïŒâããªãã·âïŒâã¯ããâ
ïŒâããªâαâãªã³ã³ãµãããã§ããã ãšãâïŒâClâMTLã¯åŒ ã®ã¡ãã«ïŒïŒïŒ²ïŒâïŒâããªãã·âïŒâã¯ããâ
ïŒâããªâαâãªã³ã³ãµãããã§ããã ïŒïŒïŒ³ïŒâã¡ããã·âã¡ãã«ïŒâããªâαâãª
ã³ã³ãµãããã¯æ¬¡ã®ããã«ç€ºãããšãã§ããã
ïŒåè¡åœç¹èš±ç¬¬3702322å·ãå®æœäŸïŒã®ïŒ¢âïŒéšïŒ 次åŒãåç §ãããšããCH3ã®æã«ïŒâããªã
ã·âïŒïŒïŒ³ïŒâïŒã¡ãã«ããªïŒâã¡ãã«ïŒâããª
âαâãªã³ã³ãµããããååšããããâCH2â
CH2âOHã®æã«ã¯ïŒâããªãã·âïŒïŒïŒ³ïŒâ
ïŒïŒâããããã·ãšãã«ããªïŒâã¡ãã«ïŒâããª
âαâãªã³ã³ãµããããååšããããŸããâ
CH2âCH2âCH2âOHã®æã«ã¯ãïŒâããªãã·
âïŒïŒïŒ³ïŒâïŒïŒâããããã·ãããã«ããªïŒâ
ã¡ãã«ïŒâããªâαâãªã³ã³ãµããããååšã
ããïŒåè¡åœç¹èš±ç¬¬3915954å·ã®å®æœäŸïŒïŒ10åã³
31ãåç §ïŒ äžåŒã®ïŒâäœçœ®ã®ããããã·åã³ããåºã¯æ¬¡ã®
ããã«ç€ºãããšãã§ããã åŒäžïŒ¹ã¯ïŒïŒïŒ²ïŒâããããã·ãïŒïŒïŒ³ïŒâãã
ããã·ãïŒïŒïŒ³ïŒâãããåã³ïŒïŒïŒ²ïŒâãããã
ãªã矀ããéžã°ããã ããªãžã³ã¢ã·ã«åºã䜿çšããŠåèšè£œé ãè¡ãã
çããæ¬çºæã®é¡äŒŒäœãéå ããŠå¯Ÿå¿ãã飜åå
åç©ã®æ··åç©ãçãããã®äžã€ã¯ïŒ¬âã·ã¹ç°æ§äœ
ã§ãããååšããããã®ä»ã®ååç©é¡ã¯ïŒ¬âãã©
ã³ã¹ãâã·ã¹ãåã³ïŒ€âãã©ã³ã¹ç°æ§äœé¡ã§ã
ããäžè¬ã«æ¬æ现æžã«èšèŒã®ä»»æã®ååç©é¡ã«ã€
ããŠã¯ãéå åã¯æ¬çºæã®äžé£œååé§ç©è³ªããæ
è掻æ§ã匷ãããããªãžã³ã¢ã·ã«åºã®äœ¿çšã¯ã
âã·ã¹ãâã·ã¹ãâãã©ã³ã¹åã³ïŒ¬âãã©ã³
ã¹ç°æ§äœãšããŠååšããé¡äŒŒäœãäžãããããã§
ãâã·ã¹ç°æ§äœã¯ãæè掻æ§ããã匷åã§ãã
ããšãããã€ãã æ°èŠé¡äŒŒäœé¡ãã€ããã®ã«æ¬æ现æžã§çšããã
ãäžè¬çãªæ¹æ³ã¯åšç¥ã®æ¹æ³ã§ãã€ãŠãé©åœãªé ž
ãé©åœãªç³ã¢ãã³ãšçµåããããã®ã§ãããïŒãæ··
åã«ã«ãã³é žç¡æ°Žç©æé ïŒMixed Carboxylic
Acid Anbydride ProcednreïŒãã¢ããé žååŠ
ïŒChemistry of The Amino AcidsïŒç¬¬ïŒå·»970
é ããžãšã³ã»ãŠã€ãªãŒã»ã¢ã³ãã»ãµã³ãºç€Ÿã1961
幎ïŒãé žãäžé£œåã®æã«ã¯ãçããäžé£œåé¡äŒŒäœ
ãæšæºæ¡ä»¶äžã«æ¥è§Šéå ããŠã飜åé¡äŒŒäœãã€ã
ããããäŸãã°æ¬¡ã®æ¡ä»¶ã䜿çšããŠéå ãè¡ãã
ãšãã§ããã H2â0.352ã3.52KgïŒcm2ïŒïŒã50psiïŒ è§Šåªâé žåçœéïŒPtO2ïŒ æº¶åªâH2Oåã¯H2OïŒMeOHïŒåã¯H2OïŒ
EtOH HClâ10ïŒ éå°ã æéâ24ã48æé æ¬æ现æžã§äœ¿çšããæã«ãïŒãïŒåã®ççŽ åå
ã®ã¢ã«ãã«ãšãã®ç°æ§äœåã¯ãã¡ãã«ããšãã«ã
ãããã«ãããã«ããã³ãã«ãããã·ã«ãããã
ã«ããªã¯ãã«ãåã³ãã®åæéç°æ§äœé¡ãå å«ã
ãã 眮æã¢ã«ãã«ã¯ãæ°ŽçŽ ååã®äžã€ãŸãã¯ãã以
äžãããã²ã³ããªãã¡ClïŒBrïŒïŒŠåã³ïŒ©ãé žçŽ ã
ããããã·ã«ãã¢ãã³ïŒç¬¬äžçŽïŒãã¢ãã³ïŒç¬¬äº
çŽâäžèšã®ãããªã¢ã«ãã«ã§ã¢ã«ãã«çœ®æãããŠ
ããïŒãã¢ãã³ïŒç¬¬äžçŽâäžèšã®ãããªã¢ã«ãã«
ã§ã¢ã«ãã«çœ®æãããŠããïŒãç¡«é»ãâSHãåã³
ããšãã«ã§çœ®ããããããäžã®ã¢ã«ãã«ååç©ã
æå³ãããååç©ã®äŸã¯ïŒâãã«ãªããšãã«ãïŒ
âã¯ãããšãã«ãïŒâãã«ãªããšãã«ãïŒâã¯ã
ããšãã«ãïŒâããã¢ãããã«ãïŒâãšãŒããã
ãã«ãïŒâã¯ããããã«ãïŒâãã«ãªãããã«ã
åã³ïŒâã¯ããããã«ã§ããã ã·ã¯ãã¢ã«ãã«ã¯ã·ã¯ããããã«ãã·ã¯ããã
ã«ãã·ã¯ããã³ãã«ãã·ã¯ãããã·ã«ãã·ã¯ãã
ããã«ãåã³ã·ã¯ããªã¯ãã«ãæå³ããã 眮æã·ã¯ãã¢ã«ãã«ã¯çœ®æã¢ã«ãã«ã«ã€ããŠäž
ã«èšèŒããããã«çœ®æãããã·ã¯ãã¢ã«ãã«ãæ
å³ãããååç©ã®äŸã¯ïŒâã·ã¯ããããã«ãšã
ã«ãïŒâã·ã¯ãããã«ãããã«ãïŒâã·ã¯ããã³
ãã«ããã«ãåã³ïŒâã·ã¯ãããã·ã«ããã«ã§ã
ãã è³éŠæã¯ããšãã«åã³ãæ°ŽçŽ ååã®äžã€åã¯ã
ã以äžãäžã®ãããªããã²ã³ãããããã·ã«ãã¢
ãã³ïŒç¬¬äžçŽã第äºçŽãåã³ç¬¬äžçŽã§ããããåŸ
ã®äºè ã¯äžã®ããã«ã¢ã«ãã«ã§çœ®æãããŠããã
ã®ïŒãâSHãåã³ããšãã«ã§çœ®ããããããå Žå
ã®çœ®æããšãã«ãæå³ãããååç©ã®äŸã¯ïœâã
ãã¢ããšãã«ãïœâãšãŒãããšãã«ãïœâã¯ãã
ããšãã«ãïœâãšãã«ããšãã«ãïœâãããã«ã
ãšãã«ãïœâã¡ãã«ããšãã«ãåã³ïœâãªã¯ãã«
ããšãã«ã§ããã äžã«è©³ããè¿°ã¹ãããã«ãæ¬çºæååç©é¡ãã
ã¹ããªã«åãããšïŒâãã¹ããšãŒããçããã¢ã·
ã«åãããšïŒâãã«ãããŒããçããäž¡è ãšãç
äœå ã§æè掻æ§ãããã 眮æé žçŽ ã¯ïŒãïŒåã®ççŽ ã®ã¢ã«ãã«ãã¢ãªãŒ
ã«åã³çœ®æã¢ãªãŒã«ã§çœ®æãããé žçŽ ãæå³ã
ãã 眮æçªçŽ ã¯ãïŒã18åã®ççŽ ã®ã¢ã·ã«ãïŒãïŒ
åã®ççŽ ã®ã¢ãã¢ã«ãã«ãåã³ãžã¢ã«ãã«ïŒã¢ã«
ãã«ã¯ïŒãïŒåã®ççŽ ã§ãã¢ã·ã«åºãšã¢ã«ãã«åº
ã¯ããããç°æ§äœåãå«ãïŒã§çœ®æãããçªçŽ ã
æå³ããã ããã¯ã¯ãããããã¢ããšãŒããåã¯ãã«ãªã
ãæå³ããã æ¬æ现æžã®åºçºææãšããŠäœ¿ãããã¢ããé žã®
æš¡ç¯çãªåºå žã¯ä»¥äžã®ãšããã§ããã ïŒ ãè€çŽ ç°åŒååç©ïŒHeterocyclic
CompoundsïŒã第ïŒå·»ããžãšã³ã»ãŠã€ãªãŒã»ã¢
ã³ãã»ãµã³ãºç€Ÿã1950幎ããã®è³æã¯ããã²ã³
åã³ã¢ã«ãã«çœ®æã¢ããé žã®è£œé ãèšèŒããŠã
ãã ïŒ ã±ãã«ã«ã»ã¢ãã¹ãã©ã¯ã 81â105223Aâã¢ã«ãã«åã³ã·ã¯ãã¢ã«ãã«ã 81â152243Sâã¢ã«ãã«åã³ããã²ã³çœ®æã 82â170746âããã²ã³çœ®æã 85â46322Qâãžãã眮æã 85â177258Wâãžãã眮æã 84â116928Xâãžãã眮æã 81â3737dâããšãã«çœ®æã 78â58201tâããšãã«çœ®æã 76â126800yâããã©ãã眮æã 82â11036Kâããã¢çœ®æã 83â27119Wâããã¢çœ®æã 84â16613Xâããã¢çœ®æã 78â123494Gâããã¢çœ®æã ãã®ååç©ã¯ãã®æè¡ã§åšç¥ã®æ段ã«ãã€ãŠ
é žã«å æ°Žå解ã§ãããã®é žããã¯ããã®æè¡ã§
åšç¥ã®æ段ã«ãã€ãŠéå ã§ããã ãã®ååç©ã¯ãã®æè¡ã§åšç¥ã®æ段ã«ãã€ãŠ
é žã«å æ°Žå解ã§ãããçããé žã次ã«åè¡åœç¹
蚱第3583972å·ã«èšèŒã®æé ã«ããâè±ã¡ã
ã«åã§ããã ãã®ååç©ã¯ãã®æè¡ã§åšç¥ã®æ段ã«ãã€ãŠ
é žã«å æ°Žå解ã§ããã ãã®ååç©ã¯ãã®æè¡ã§åšç¥ã®æ段ã«ãã€ãŠ
é žã«å æ°Žå解ã§ããããŸããçããé žããåè¡
åœç¹èš±ç¬¬3583972å·ã§æããã«ãããæé ã«ã
ã€ãŠãâCH3åºã®äžæ¹åã¯åæ¹ãé€å»ã§ã
ãã ãã®ååç©ã¯ãã®æè¡ã§åšç¥ã®æ段ã«ãã€ãŠ
é žã«å æ°Žå解ã§ãããçããé žã¯åè¡åœç¹èš±ç¬¬
3583972å·ã«é瀺ãããæ¹æ³ã«ãã€ãŠæ¬¡ã®åå
ç©ã«è»¢åã§ããã éé¢ã®NH2åã¯OHåºããã€ååç©é¡ã¯ãã¢
ããç³ãšçž®åãããåã«ãããã®åºãä¿è·ããŠ
ãããªããŠã¯ãªããªãããã®ãããªåºã®ä¿è·ã¯
ãã®æè¡ã§åšç¥ã§ããããææ©ååŠã®ä¿è·åº
ïŒProtective Groups in Organic
ChemistryïŒãããžãšã€ã»ãšãããããªãŠãŒã»ã
ã³ããŒïŒJ.F.W.McomieïŒããã¬ãã åºç瀟ã
1973幎ããåç §ã®ããšã ïŒ ãžã€ãŒãã« ãªã ã±ãã«ã« ãœãµãšãã€
ïŒJour.Chem.Soc.ïŒ1969幎ã2134é ã çš®ã ã®ïŒšâã¢ã«ãã«çœ®æããªãžã³é¡ã ïŒåžè²©ã®ãã®ïŒ ïŒã¢ã«ãã«ãåæã¢ã«ãã«ãåã³ã·ã¯ãã¢ã«
ãã«ã ïŒ Joar.Chem.Soc.1969幎934é 以äžã®å®æœäŸã¯æ¬çºææ¹æ³åã³çæç©ã®äŸç€ºã§
ããããéå®ãããã®ãšèããŠã¯ãªããªããä»ã«
泚æããªããã°ãçŸåçã¯ãã¹ãŠééã«ããããŸ
ã溶åªæ··åç©ã®å²åã¯ãã¹ãŠå®¹éã«ããã å®æœäŸïŒ ïŒâClâMTLã®ïŒâã·ã¹âãšãã«â
âãããµããããã³ãªã³é žHClïŒïŒµâ57930E
âååç©ïŒ¶ïŒ ã¢ã»ããããªã«2.5ãªããã«äžã«æº¶è§£ãããã¢
ããé žHClïŒã±ãã«ã«ã»ã¢ãã¹ãã©ã¯ã51å·»
1643aã1957幎ïŒ67ïœïŒ0.357ã¢ã«ïŒãšããªãšãã«
ã¢ãã³71.5ïœïŒ0.714ã¢ã«ïŒã®æº¶æ¶²ã10âã«å·åŽ
ããã€ãœããã«ã¯ããããªã«ã¡ãŒã47.6ïœ
ïŒ0.354ã¢ã«ïŒãäžåºŠã«å ããããã®æ··åç©ïŒæº¶æ¶²
ïŒã10âã§ïŒæéãããŸãããã¢ã»ãã³1500ml
ãšH2O1500mlãšã®æž©ããæ··åç©äžã«ïŒâClâ
MTLïŒJ.Med.Chem.12å·»780é ã1969幎ãããŒã»
ãžãšãŒã»ãã¬ãŒã¬ã€ã³ïŒB.J.MegerleinïŒåã³ãš
ãã»ã«ã¬ã³ïŒF.KaganïŒïŒ97.7ïœïŒ0.357ã¢ã«ïŒã
溶解ããããšã«ãã€ãŠæº¶æ¶²ïŒ¢ãã€ããã溶液ã
30âã«å·åŽãã溶液ã«äžåºŠã«å ãããåå¿æ¶²ã
25âã§18æéãããŸããã¢ã»ãã³åã³ã¢ã»ããã
ãªã«ãç空äžã§é€å»ãããçœãããç¶ã®æ®çç©ã
ãéããçµæ¶ç¶ã®ææãéããŠä¹Ÿç¥ãããšãçŽç²
ãªçæç©95ïœãçãããã液ãä»äžãããšïŒã¯ã
ããã°ã©ãã€ïŒãå¥ã«çæç©10ïœãçãããå šäœ
ã®åç73ïŒ åæïŒ C17H25ClN2O5Sã«å¯Ÿã㊠èšç®å€ïŒïŒ£ïŒ50.42ïŒïŒšïŒ6.22ïŒïŒ®ïŒ6.92ïŒ ïŒ³ïŒ7.92ïŒClïŒ8.76 枬å®å€ïŒïŒ£ïŒ50.67ïŒïŒšïŒ6.40ïŒïŒ®ïŒ6.64ïŒ ïŒ³ïŒ7.90ïŒClïŒ8.70 αCHCl3 D ïŒïŒ£ïŒ1.0ïŒïŒ293ã åºçºææ4.05ïœïŒ0.01ã¢ã«ïŒãæ°Ž40mlãã¡ã¿ã
ãŒã«60mlã37ïŒ HCl1.0mlåã³PtO28.0ïœã®æ··åç©
ãããŒæ°ŽçŽ æ·»å è£ çœ®ã«ãã3.52KgïŒcm2ïŒ50p.s.iïŒ
ã§ïŒæééå ãããCHCl3ïŒã¡ã¿ããŒã«ïŒïŒïŒ
ïŒïŒãããªãç³»ã§ã·ãªã«ã²ã«æ¿äžã®TLCã«ãã€
ãŠåå¿æ··åç©ãåæãããšãåºçºææãå šéšæ¶ã
ãŠã極æ§ã®ãã倧ããäºã€ã®ææãçŽïŒïŒïŒã®æ¯
ã§ååšããããšã瀺ããã觊åªãé€å»ããããã«
åå¿æ¶²ããéããã液ãç空äžã«æ¿çž®ãããšãçœ
ãçµæ¶æ§ã®ãããçãããããããéããã液ã
貯ãããåå¿æ··åç©ã®TLCã«ãã€ãŠèŠ³å¯ããã
äºçæç©ã®ãã¡ã極æ§ã®æã倧ãããã®çœè²åºäœ
ã¯ãæ°Žããåçµæ¶ããããšã25ã35ïŒ ã®åçã§æ
ãã§ããçæç©ïŒµâ57930Eãèç¹222ã224âã
çããã åæïŒ C17H32Cl2N2O5Sã«å¯Ÿã㊠èšç®å€ïŒïŒ£ïŒ45.63ïŒïŒšïŒ7.21ïŒïŒ®ïŒ6.26ïŒ ïŒ³ïŒ7.17ïŒClïŒ15.85 枬å®å€ïŒïŒ£ïŒ45.77ïŒïŒšïŒ7.44ïŒïŒ®ïŒ6.39ïŒ ïŒ³ïŒ7.21ïŒClïŒ16.17 αH2O D ïŒïŒ£ïŒ1.0ïŒïŒ176ã ã®çµ¶å¯Ÿç«äœé 眮åã³ç«äœååŠã¯ãç·çµæ¶åŠ
ã«ãã€ãŠç¢ºå®ãããã ã¯ãªã³ããã€ã·ã³ãšã®æ¯èŒã«ãããŠãè©Šéšãã
ãâ57930Eã¯æ¬¡ã®æèã¹ãã¯ãã«ããã€ãŠã
ãã
ãè¡šã
ãè¡šã
äžã®è©Šéšã®æé ã¯æ¬¡ã®ãšããã§ããã
奜æ°èã«å¯Ÿããäž¡ååç©ã®æå°é»æ¢æ¿åºŠ
ïŒTICïŒã¯æšæºãã€ã¯ããã¬ãŒãã»ããã¹åžéæ³
ãçšããŠæ±ºå®ããããè³å¿æµžåºæ¶²ïŒBHIâãã€
ãã³è£œïŒã®ããã¹å¹å°ã䜿çšãããã¬ãŒãã37â
ã§20æéå¹é€ããã é»è²ãããŠçèUC6685ã6696ã¯ãåžè²©ã®äžçš®
åã¯ãã以äžã®æçç©è³ªã«èæ§ã®ããèšåºåé¢è
ã§ããã ãUCã¯ã¢ãããžãšã³ç€Ÿã®ä¿åå¹é€åºã®ç»é²å
æšã§ããããããã®å¹é€æ³ã¯ãè«æ±ããã°ãã·ã¬
ã³å·ã«ã©ããºãŒã®ã¢ãããžãšã³ç€Ÿããå ¥æã§ã
ãã
ïŒTICïŒã¯æšæºãã€ã¯ããã¬ãŒãã»ããã¹åžéæ³
ãçšããŠæ±ºå®ããããè³å¿æµžåºæ¶²ïŒBHIâãã€
ãã³è£œïŒã®ããã¹å¹å°ã䜿çšãããã¬ãŒãã37â
ã§20æéå¹é€ããã é»è²ãããŠçèUC6685ã6696ã¯ãåžè²©ã®äžçš®
åã¯ãã以äžã®æçç©è³ªã«èæ§ã®ããèšåºåé¢è
ã§ããã ãUCã¯ã¢ãããžãšã³ç€Ÿã®ä¿åå¹é€åºã®ç»é²å
æšã§ããããããã®å¹é€æ³ã¯ãè«æ±ããã°ãã·ã¬
ã³å·ã«ã©ããºãŒã®ã¢ãããžãšã³ç€Ÿããå ¥æã§ã
ãã
ãè¡šã
ãè¡šã
ãè¡šã
ãã«ã¹ã»ã¢ããšãã
ãŠã¹
(Peptostreptococcus
anaerobius)
äžã®è©Šéšã«å¯Ÿããæé ã¯æ¬¡ã®ãšããã§ãããè¬
å€ã®æ®µéçïŒååžéãã·ãšãã©ãŒã»ããã¹
ïŒSchaedler BrothïŒïŒml容éã§ã€ããã溶èã
ãïŒ47âïŒãŠã€ã«ã±ã³ã¹âãã€ã«ã°ã¬ã³
ïŒWilkensâChalgrenïŒå¯å€©å¹å°ïŒåŸè¿°ïŒ9.0mlã
æçç©è³ªãè¿œå ãããããã¹ã«å ãããæçç©è³ª
ãšæ··åããŠãããå¯å€©ã100mmÃ20mmã®ãããªç¿
ã«æ³šããç¿ãæ¥çš®ã«å ç«ã€ãŠäžå€å®éšå°äžã«æŸçœ®
ããŠããã å¹é€åºããŠã€ã«ã±ã³ã¹ã»ãã€ã³ã°ã¬ã³å¯å€©äžã«
æ¡çãã€ãBBLç¡æ°æ§ã®ãžã€ãŒäžã§37âã§48æ
éçè²ãããããã¬ãŒãããã®çè²ç©ãåãå ¥
ããã·ãšãã©ãŒããã¹äžã§0.5ãã¯ãã¢ãŒã©ã³
ãã»ã¹ã¿ã³ããŒãïŒMcFaeland StandardïŒã®æ··
æ¿åºŠïŒmlåœã108åã®èäœïŒã«çããèäœæžæ¿æ¶²
ãã€ãããã¹ãã€ã¢ãŒãºã»ã¬ããªã±ãŒã¿ãŒ
ïŒSteers repliâcatorïŒã®ããŒã¿ã«æžæ¿æ¶²ããã
ããã§æ³šããçŽïŒã2ÎŒãå¯å€©ãã¬ãŒãè¡šé¢ã«
åé ãããæ¥çš®ç©ã也ç¥ãããŸã§ïŒãïŒåæŸçœ®ã
ãŠåŸãBBLç¡æ°æ§ãžã€ãŒïŒ85ïŒ ïŒ® 10ïŒ ïŒš ïŒ
ïŒ CO2ã®é°å²æ°ïŒäžã«ãã¬ãŒããå ¥ãã37âã§72
æéå¹é€ããã çè²ãæããè¬å€ã®æå°éãšããŠæå°é»æ¢æ¿åºŠ
ïŒMICïŒãèªã¿ãšããçè²ã®ããèãèç¶ã®ã
ã®ãåã¯ïŒåæªæºã®éèœã¯é°æ§ãšèããã ãŠã€ã«ãã³ã¹ã»ãã€ã«ã°ã¬ã³å¯å€©å¹å° 次ã®æåã調åããèžçæ°Ž1000mlã«æº¶è§£ããã
PHã7.0ã7.2ã«ãã¹ãã§ããã ããªããã«ãŒãŒ 10ïœ ã²ãªã»ãŒã 10ïœ é µæ¯ãšãã¹ ïŒïœ ã¶ã©ãç³ ïŒïœ NaCl ïŒïœ âã¢ã«ã®ãã³âéé¢å¡©åº ïŒïœ ãã«ãã³é žãããªãŠã å¡© ïŒïœ å¯å€© 15ïœ ãã ïŒããšãããããããã€ãªã³ïŒåã³ïŒãã¿
ãã³K1ã®æº¶æ¶²ãå ããããã³ïŒã¯ããããã³ïŒ
5ÎŒïœïŒmlåã³K10.5ïœïŒmlã®æçµæ¿åºŠãšãããæ
æ°çã«121âã10åã®ãªãŒãã¯ã¬ãŒãåŠçããã
ã¹ããã¯âããã³0.5ïœïŒ1N NaOH10mlïŒ
H2O990mlã 121âã§12åã®ãªãŒãã¯ã¬ãŒãåŠçã å¹å°åœãã¹ããã¯10mlãå ããã ïŒãã¿ãã³ïŒ«ã¹ããã¯âãã¿ãã³K1溶液0.05ml
ïŒ95ïŒ ãšã¿ããŒã«20mlã æ» èãéããã å¹å°åœãã¹ããã¯0.2mlãå ããã ã¯ã€ãããã¿ã§ïŒµâ57930Eã®è ¹è å æäžïŒI.
P.ïŒLD50ã¯592mgïŒKgã§ããã®ãããã€ãããã®
å€ã¯ãå¥åã®åæ§ãªLD50枬å®ïŒåã®å¹³åã§ããã
ãã®å€ã¯ãã¯ãªã³ããã€ã·ã³HClã®LD50ã®çŽïŒ
åã§ãããLD50ã®å€ã¯ãâ57930Eã®æ¥æ§è ¹è
å æäžæ¯æ§ãã¯ãªã³ããã€ã·ã³HClã®æ¯æ§ã®çŽå
åã§ããããšã瀺ããã®ãšããŠè§£éãããã¹ãã§
ããã
ãŠã¹
(Peptostreptococcus
anaerobius)
äžã®è©Šéšã«å¯Ÿããæé ã¯æ¬¡ã®ãšããã§ãããè¬
å€ã®æ®µéçïŒååžéãã·ãšãã©ãŒã»ããã¹
ïŒSchaedler BrothïŒïŒml容éã§ã€ããã溶èã
ãïŒ47âïŒãŠã€ã«ã±ã³ã¹âãã€ã«ã°ã¬ã³
ïŒWilkensâChalgrenïŒå¯å€©å¹å°ïŒåŸè¿°ïŒ9.0mlã
æçç©è³ªãè¿œå ãããããã¹ã«å ãããæçç©è³ª
ãšæ··åããŠãããå¯å€©ã100mmÃ20mmã®ãããªç¿
ã«æ³šããç¿ãæ¥çš®ã«å ç«ã€ãŠäžå€å®éšå°äžã«æŸçœ®
ããŠããã å¹é€åºããŠã€ã«ã±ã³ã¹ã»ãã€ã³ã°ã¬ã³å¯å€©äžã«
æ¡çãã€ãBBLç¡æ°æ§ã®ãžã€ãŒäžã§37âã§48æ
éçè²ãããããã¬ãŒãããã®çè²ç©ãåãå ¥
ããã·ãšãã©ãŒããã¹äžã§0.5ãã¯ãã¢ãŒã©ã³
ãã»ã¹ã¿ã³ããŒãïŒMcFaeland StandardïŒã®æ··
æ¿åºŠïŒmlåœã108åã®èäœïŒã«çããèäœæžæ¿æ¶²
ãã€ãããã¹ãã€ã¢ãŒãºã»ã¬ããªã±ãŒã¿ãŒ
ïŒSteers repliâcatorïŒã®ããŒã¿ã«æžæ¿æ¶²ããã
ããã§æ³šããçŽïŒã2ÎŒãå¯å€©ãã¬ãŒãè¡šé¢ã«
åé ãããæ¥çš®ç©ã也ç¥ãããŸã§ïŒãïŒåæŸçœ®ã
ãŠåŸãBBLç¡æ°æ§ãžã€ãŒïŒ85ïŒ ïŒ® 10ïŒ ïŒš ïŒ
ïŒ CO2ã®é°å²æ°ïŒäžã«ãã¬ãŒããå ¥ãã37âã§72
æéå¹é€ããã çè²ãæããè¬å€ã®æå°éãšããŠæå°é»æ¢æ¿åºŠ
ïŒMICïŒãèªã¿ãšããçè²ã®ããèãèç¶ã®ã
ã®ãåã¯ïŒåæªæºã®éèœã¯é°æ§ãšèããã ãŠã€ã«ãã³ã¹ã»ãã€ã«ã°ã¬ã³å¯å€©å¹å° 次ã®æåã調åããèžçæ°Ž1000mlã«æº¶è§£ããã
PHã7.0ã7.2ã«ãã¹ãã§ããã ããªããã«ãŒãŒ 10ïœ ã²ãªã»ãŒã 10ïœ é µæ¯ãšãã¹ ïŒïœ ã¶ã©ãç³ ïŒïœ NaCl ïŒïœ âã¢ã«ã®ãã³âéé¢å¡©åº ïŒïœ ãã«ãã³é žãããªãŠã å¡© ïŒïœ å¯å€© 15ïœ ãã ïŒããšãããããããã€ãªã³ïŒåã³ïŒãã¿
ãã³K1ã®æº¶æ¶²ãå ããããã³ïŒã¯ããããã³ïŒ
5ÎŒïœïŒmlåã³K10.5ïœïŒmlã®æçµæ¿åºŠãšãããæ
æ°çã«121âã10åã®ãªãŒãã¯ã¬ãŒãåŠçããã
ã¹ããã¯âããã³0.5ïœïŒ1N NaOH10mlïŒ
H2O990mlã 121âã§12åã®ãªãŒãã¯ã¬ãŒãåŠçã å¹å°åœãã¹ããã¯10mlãå ããã ïŒãã¿ãã³ïŒ«ã¹ããã¯âãã¿ãã³K1溶液0.05ml
ïŒ95ïŒ ãšã¿ããŒã«20mlã æ» èãéããã å¹å°åœãã¹ããã¯0.2mlãå ããã ã¯ã€ãããã¿ã§ïŒµâ57930Eã®è ¹è å æäžïŒI.
P.ïŒLD50ã¯592mgïŒKgã§ããã®ãããã€ãããã®
å€ã¯ãå¥åã®åæ§ãªLD50枬å®ïŒåã®å¹³åã§ããã
ãã®å€ã¯ãã¯ãªã³ããã€ã·ã³HClã®LD50ã®çŽïŒ
åã§ãããLD50ã®å€ã¯ãâ57930Eã®æ¥æ§è ¹è
å æäžæ¯æ§ãã¯ãªã³ããã€ã·ã³HClã®æ¯æ§ã®çŽå
åã§ããããšã瀺ããã®ãšããŠè§£éãããã¹ãã§
ããã
ãè¡šã
äžèšè©Šéšã®æé ã¯æ¬¡ã®ãšããã§ããã
ã¯ã€ãããã¿ä¿è·è©ŠéšïŒ
äœé18ã20ïœã®æšæºçãªå®éšçšã¯ã€ãããã¿
ïŒCFâïŒã¯ã€ãããã¿ïŒ10å¹ãã€ã®çŸ€ããâ170â
ã§åçµç¶æ ã«ä¿ãããŠããæšæºç现èæžæ¿æ¶²çŽ
100LD50ã§ææãããã䜿çšçŽåã«æžæ¿æ¶²ããã°
ãã解åããé©åœã«åžéãããææã¯è ¹èå çµè·¯
ã§ããã ææ矀ã®åŠçœ®ã¯çŽã¡ã«å§ãŸããïŒæ¥ïŒåã§ïŒæ¥
éç¶ããããïŒæåã®24æéãïŒæ¥ïŒãæªåŠçœ®æ
æã¯ã€ãããã¿ã®çŸ€ãå¹é€åºã®æ¯æ§å¯Ÿç §ãšããŠçš
ããã åŠçœ®ç®¡çãå§ãŸã€ãŠããïŒæ¥åŸã«ãçååç©ã
殺ããåŠçœ®çŸ€ã®ã¯ã€ãããã¿ã®æ»äº¡çã«åºã¥ããŠ
æçç©è³ªã®å¹³åä¿è·æäžéãèšç®ãããã¹ãã¢ã
ã³ïŒSpearmanïŒåã³ã«ãŒããŒïŒKarberïŒã®æ¹æ³
ã«ãã€ãŠã360ããžã¿ã«ã»ã³ã³ããŠãŒã¿ãŒã§ãã
ã°ã©ã åããããšããã«ãå¹³åä¿è·æäžéãšãã®
95ïŒ ä¿¡é ŒåºŠã®ééãèšç®ããã ãŸããå®æœäŸïŒã®ç¬¬éšããååç©ïŒ¡ãåé¢
ãããããã®ææã¯æ¬¡ã®ããã«åŸãããã 第éšããåã€ãŠãããã液ãç空äžã§ä¹Ÿåºã
ããŸã§æ¿çž®ãããæ®çç©ããã®éé¢å¡©åºã«è»¢å
ãã溶é¢æº¶åªãšããŠCHCl3ïŒã¡ã¿ããŒã«ïŒïŒïŒ
ïŒïŒã䜿çšããŠãã·ãªã«ã²ã«äžã®ã¯ãããã°ã©ã
ã€ã«ãããããã®ããæ¹ã§ã第éšã§è¿°ã¹ã極æ§
ã®æãäœãææãåŸããããããããã®HClå¡©ã«
転åããã¢ã»ãã³åã³æ°Žããåçµæ¶ãããããã®
ç°æ§äœã«æ«å®çã«æ§é ãæå®ããŠããã ãšïŒ¡ã®ãããªãžã³ç°ã«çµåãããã«ã«ãã
ã«å®èœåºã®ãšãããŒåã¯ãåœæ¥è ã«åšç¥ã®æ¹æ³ã«
ãã€ãŠéæã§ããããã®ãšãããŒåã§ã€ãããã
ãã©ã³ã¹ç°æ§äœïŒ¢ãšïŒ£ã¯ãçµæ¶ååã¯ã¯ãã
ãã°ã©ãã€ã®ãããªæ £çšæé ã«ãã€ãŠåé¢ã§ã
ãã ãã®ä»£ããã«ãšïŒ¡ãå æ°Žå解ãããšãã¢ã
ãé žïŒ€ãšïŒ¥ãåŸããã次ã«ãããåœæ¥è ã«åš
ç¥ã®æ¹æ³ã«ããããããããšïŒ§ã«ãšãããŒ
åãããã¢ããé žïŒŠåã³ïŒ§ãåã«è¿°ã¹ããªã³
ã³ãµãããé¡ã®ä»»æã®ãã®ãšçµåã§ããã â57930Eã®ïŒ€âã·ã¹ç°æ§äœïŒïŒ¡ïŒã¯ã第
ïŒè¡šã§æ¢è¿°ããBHIããã¹ã§è©Šéšãããšã次ã®
æèã¹ãã¯ãã«ããã€ãŠããã
ïŒCFâïŒã¯ã€ãããã¿ïŒ10å¹ãã€ã®çŸ€ããâ170â
ã§åçµç¶æ ã«ä¿ãããŠããæšæºç现èæžæ¿æ¶²çŽ
100LD50ã§ææãããã䜿çšçŽåã«æžæ¿æ¶²ããã°
ãã解åããé©åœã«åžéãããææã¯è ¹èå çµè·¯
ã§ããã ææ矀ã®åŠçœ®ã¯çŽã¡ã«å§ãŸããïŒæ¥ïŒåã§ïŒæ¥
éç¶ããããïŒæåã®24æéãïŒæ¥ïŒãæªåŠçœ®æ
æã¯ã€ãããã¿ã®çŸ€ãå¹é€åºã®æ¯æ§å¯Ÿç §ãšããŠçš
ããã åŠçœ®ç®¡çãå§ãŸã€ãŠããïŒæ¥åŸã«ãçååç©ã
殺ããåŠçœ®çŸ€ã®ã¯ã€ãããã¿ã®æ»äº¡çã«åºã¥ããŠ
æçç©è³ªã®å¹³åä¿è·æäžéãèšç®ãããã¹ãã¢ã
ã³ïŒSpearmanïŒåã³ã«ãŒããŒïŒKarberïŒã®æ¹æ³
ã«ãã€ãŠã360ããžã¿ã«ã»ã³ã³ããŠãŒã¿ãŒã§ãã
ã°ã©ã åããããšããã«ãå¹³åä¿è·æäžéãšãã®
95ïŒ ä¿¡é ŒåºŠã®ééãèšç®ããã ãŸããå®æœäŸïŒã®ç¬¬éšããååç©ïŒ¡ãåé¢
ãããããã®ææã¯æ¬¡ã®ããã«åŸãããã 第éšããåã€ãŠãããã液ãç空äžã§ä¹Ÿåºã
ããŸã§æ¿çž®ãããæ®çç©ããã®éé¢å¡©åºã«è»¢å
ãã溶é¢æº¶åªãšããŠCHCl3ïŒã¡ã¿ããŒã«ïŒïŒïŒ
ïŒïŒã䜿çšããŠãã·ãªã«ã²ã«äžã®ã¯ãããã°ã©ã
ã€ã«ãããããã®ããæ¹ã§ã第éšã§è¿°ã¹ã極æ§
ã®æãäœãææãåŸããããããããã®HClå¡©ã«
転åããã¢ã»ãã³åã³æ°Žããåçµæ¶ãããããã®
ç°æ§äœã«æ«å®çã«æ§é ãæå®ããŠããã ãšïŒ¡ã®ãããªãžã³ç°ã«çµåãããã«ã«ãã
ã«å®èœåºã®ãšãããŒåã¯ãåœæ¥è ã«åšç¥ã®æ¹æ³ã«
ãã€ãŠéæã§ããããã®ãšãããŒåã§ã€ãããã
ãã©ã³ã¹ç°æ§äœïŒ¢ãšïŒ£ã¯ãçµæ¶ååã¯ã¯ãã
ãã°ã©ãã€ã®ãããªæ £çšæé ã«ãã€ãŠåé¢ã§ã
ãã ãã®ä»£ããã«ãšïŒ¡ãå æ°Žå解ãããšãã¢ã
ãé žïŒ€ãšïŒ¥ãåŸããã次ã«ãããåœæ¥è ã«åš
ç¥ã®æ¹æ³ã«ããããããããšïŒ§ã«ãšãããŒ
åãããã¢ããé žïŒŠåã³ïŒ§ãåã«è¿°ã¹ããªã³
ã³ãµãããé¡ã®ä»»æã®ãã®ãšçµåã§ããã â57930Eã®ïŒ€âã·ã¹ç°æ§äœïŒïŒ¡ïŒã¯ã第
ïŒè¡šã§æ¢è¿°ããBHIããã¹ã§è©Šéšãããšã次ã®
æèã¹ãã¯ãã«ããã€ãŠããã
ãè¡šã
å®æœäŸïŒ 7ClâMTLã®ãã®ä»é¡äŒŒäœ
å®æœäŸïŒã®æé ã«åŸããããã®ã¢ããé
žã®ä»£ã
ãã«æ¬¡ã®ã¢ããé žã䜿çšããŠã察å¿ããæ°èŠãªæ
è掻æ§é¡äŒŒäœé¡ããããã®éé¢å¡©åºåã¯é žä»å å¡©
ãšããŠã€ãããããåŸè ã¯åœæ¥è ã«åšç¥ã®æ¹æ³ã«
ãã€ãŠã€ããããšãã§ããã
ãã«æ¬¡ã®ã¢ããé žã䜿çšããŠã察å¿ããæ°èŠãªæ
è掻æ§é¡äŒŒäœé¡ããããã®éé¢å¡©åºåã¯é žä»å å¡©
ãšããŠã€ãããããåŸè ã¯åœæ¥è ã«åšç¥ã®æ¹æ³ã«
ãã€ãŠã€ããããšãã§ããã
ãè¡šã
ãè¡šã
å®æœäŸïŒ MTLã®é¡äŒŒäœé¡
å®æœäŸïŒã®æé ã«åŸããããã®ã¢ããé
žã®ä»£ã
ãã«ã¢ããé žé¡ã䜿çšãããŸãïŒâClâMTLã®
代ããã«MTLïŒJ.Am.Chem.Soc.89å·»2448é ã
1967幎ããããªãŠãŒã»ã·ãŠã¬ãŒããŒïŒW.
SchroederïŒãããŒã»ããã¹ã¿ãŒïŒB.BannisterïŒ
åã³ãšããã»ããŒã¯ã»ãïŒH.HoeksemaïŒïŒã䜿
çšããŠã察å¿ããæ°èŠãªæè掻æ§é¡äŒŒäœé¡ãã€ã
ãããã
ãã«ã¢ããé žé¡ã䜿çšãããŸãïŒâClâMTLã®
代ããã«MTLïŒJ.Am.Chem.Soc.89å·»2448é ã
1967幎ããããªãŠãŒã»ã·ãŠã¬ãŒããŒïŒW.
SchroederïŒãããŒã»ããã¹ã¿ãŒïŒB.BannisterïŒ
åã³ãšããã»ããŒã¯ã»ãïŒH.HoeksemaïŒïŒã䜿
çšããŠã察å¿ããæ°èŠãªæè掻æ§é¡äŒŒäœé¡ãã€ã
ãããã
ãè¡šã
å®æœäŸïŒ ãšãâMTLã®é¡äŒŒäœé¡
å®æœäŸïŒã®æé ã«åŸããããã®ã¢ããé
žã®ä»£ã
ãã«æ¬¡ã®ã¢ããé žé¡ã䜿çšããåïŒâClâMTL
ã®ä»£ããã«ãšãâMTLïŒJ.Chem.Soc.ããŒãã³ã»
ã¢ã€ïŒPerkin I.ïŒã1974幎360âé ãããã¹ã¿
ãŒïŒã䜿çšããŠã察å¿ããæ°èŠãªæè掻æ§é¡äŒŒäœ
é¡ãã€ããããã
ãã«æ¬¡ã®ã¢ããé žé¡ã䜿çšããåïŒâClâMTL
ã®ä»£ããã«ãšãâMTLïŒJ.Chem.Soc.ããŒãã³ã»
ã¢ã€ïŒPerkin I.ïŒã1974幎360âé ãããã¹ã¿
ãŒïŒã䜿çšããŠã察å¿ããæ°èŠãªæè掻æ§é¡äŒŒäœ
é¡ãã€ããããã
ãè¡šã
å®æœäŸïŒ ãšãâïŒâClâMTLã®é¡äŒŒäœé¡
å®æœäŸïŒã®æé ã«åŸããããã®ã¢ããé
žã®ä»£ã
ãã«æ¬¡ã®ã¢ããé žé¡ã䜿çšããïŒâClâMTLã®
代ããã«ãšãâïŒâClâMTLã䜿çšããŠã察å¿
ããæ°èŠãªæè掻æ§é¡äŒŒäœé¡ãã€ããããã
ãã«æ¬¡ã®ã¢ããé žé¡ã䜿çšããïŒâClâMTLã®
代ããã«ãšãâïŒâClâMTLã䜿çšããŠã察å¿
ããæ°èŠãªæè掻æ§é¡äŒŒäœé¡ãã€ããããã
ãè¡šã
ïŒâClâMTLãã€ããã®ã«çšããæé ã«ãã€
ãŠãšãâïŒâClâMTlãã€ããããããäœãåº
çºææã¯MTLã®ä»£ããã«ãšãâMTLã§ããã å®æœäŸïŒãïŒã®ååç©é¡ã®ã»ãšãã©ã®ãã®ã®å
åŠçåã³ç©ççæ§ç¶ã¯æ¬¡ã®ãšããã§ããã
ãŠãšãâïŒâClâMTlãã€ããããããäœãåº
çºææã¯MTLã®ä»£ããã«ãšãâMTLã§ããã å®æœäŸïŒãïŒã®ååç©é¡ã®ã»ãšãã©ã®ãã®ã®å
åŠçåã³ç©ççæ§ç¶ã¯æ¬¡ã®ãšããã§ããã
ãè¡šã
å®æœäŸïŒ ïŒâã¯ããâMTLã®ãã¶ãªã³é
žã¢ã
ã å®æœäŸïŒã®æé ã«åŸããããã®ã¢ããé žã®ä»£ã
ãã«æ¬¡ã®ãã¶ãªã³é žã䜿çšããŠãâ55581ãåŸ
ãããã åæïŒ C19H29ClN2O5Sã«å¯Ÿã㊠èšç®å€ïŒïŒ£ïŒ52.70ïŒïŒšïŒ6.75ïŒïŒ®ïŒ6.47ïŒ ïŒ³ïŒ7.41ïŒClïŒ9.19 枬å®å€ïŒïŒ£ïŒ52.15ïŒïŒšïŒ6.65ïŒïŒ®ïŒ6.36ïŒ ïŒ³ïŒ7.21ïŒClïŒ7.94 åèäŸïŒ ïŒâClâMTLã®ïŒâã·ã¹âïœâãã
ã«ââãããµããããã³ãªã³é žã¢ããåã¯ïŒµ
â60970E åºçºææ4.0ïœïŒ0.0093ã¢ã«ïŒãæ°Ž40mlãã¡ã¿ã
ãŒã«40mlã37ïŒ HCl2mlãåã³Pto2觊åª8.0ïœã®æ··
åç©ãããŒæ°ŽçŽ æ·»å è£ çœ®ã«ããã3.52KgïŒcm2
ïŒ50psiïŒã§18æééå ããã觊åªãé€ãããã«å
å¿æ¶²ããéããã液ãç空äžã§æ¿çž®ãããšããã¯
ãè²ã®æ²¹ãçãããCHCl3âã¡ã¿ããŒã«ïŒïŒïŒ
ïŒïŒæº¶æ¶²20mlã«æ²¹ã溶解ããååšããå¡©é žãäžå
ããã«ååãªããªãšãã«ã¢ãã³ãå ãããCHCl3
âã¡ã¿ããŒã«ïŒïŒïŒïŒïŒãããªã溶åªç³»ã䜿çšã
ãŠããã®æº¶æ¶²ãã·ãªã«ã²ã«äžã®ã¯ãããã°ã©ãã€
ã«ããããäž»çæç©ã®äºã€ã®ãã©ã¯ã·ãšã³ãåŸã
ãããæ©ã移åããæ¹ã®ææãå«æãããã©ã¯ã·
ãšã³ãäžç·ã«ããŠç空äžã§èžçºããããšãçœè²åº
äœã®ãã©ã¯ã·ãšã³ïŒ¡ãçããã移åã®ãããææ
ãå«æãããã©ã¯ã·ãšã³ãäžç·ã«ããŠç空äžã§èž
çºããããšãçœè²åºäœã®ãã©ã¯ã·ãšã³ïŒ¢ãçã
ãã ãã©ã¯ã·ãšã³ïŒ¢ãå°éã®H2Oã«æº¶è§£ããPHïŒ
ã«ããã«ååãªéã®37ïŒ HClãå ãããçµæ¶åã
èµ·ãããåºäœãéããŠH2Oããåçµæ¶ããããšã
æãã§ããçæç©ïŒµâ60970Eã®çœè²çµæ¶ãïŒèç¹
224ã226âïŒã25ã35ïŒ ã®åçã§çããã åæïŒ C17H32Cl2N2O5Sã«å¯Ÿã㊠èšç®å€ïŒïŒ£ïŒ47.99ïŒïŒšïŒ7.63ïŒïŒ®ïŒ5.89ïŒ ïŒ³ïŒ6.75ïŒClïŒ14.92 枬å®å€ïŒïŒ£ïŒ47.97ïŒïŒšïŒ7.42ïŒïŒ®ïŒ6.23ïŒ ïŒ³ïŒ6.90ïŒClïŒ14.87 αMeOH D ïŒ178ãïŒïŒ£ïŒ1.0ïŒ CMRåæã¯ãææ¡ã®æ§é ãæ¯æããŠããã â60970Eã®ããŸããŸãªçŽ°èã«å¯Ÿããæå°é»
æ¢æ¿åºŠïŒMICïŒã¯ãÎŒïœïŒmlã§ä»¥äžã®ãšããã§
ããã埮çç© UCïŒ MIC é»è²ãããŠçè 6 0.125 é»è²ãããŠçè 570 0.25 746 0.062 è žçè 694 0.25 åè¿é£éçè 152 0.008 èºçåçè 41 0.016 å€§è žè45 31.2 èºçæè 58 7.8 ã·ãšãããŠã©ãŒè 126 31.2 ç·è¿è 95 ïŒ125 è©Šéšæé ã¯å®æœäŸïŒã§æããã«ããããšããã§
ããã å®éšçã«çŽ°èã§ææãããæšæºçãªå®éšçšã¯ã€
ãããã¿ã«ã€ããŠãâ60970Eã®çäœè©Šéšãè¡
ãªã€ããâ57930Eãšæ¯èŒããªããè©Šéšãè¡ãª
ã€ãã次ã®çµæã¯ãååã³åèºçåçèã«å¯Ÿ
ããçäœè©Šéšã§ïŒµâ60970Eãâ57930Eããè
ãã匷ã掻æ§ãããããšã瀺ããŠãããé»è²ãã
ãŠçèãšæº¶è¡é£éçèã«å¯ŸããŠã¯ãâ60970E
ã¯ïŒµâ57930Eãšæ¬è³ªçã«åã掻æ§ã瀺ãã
ã å®æœäŸïŒã®æé ã«åŸããããã®ã¢ããé žã®ä»£ã
ãã«æ¬¡ã®ãã¶ãªã³é žã䜿çšããŠãâ55581ãåŸ
ãããã åæïŒ C19H29ClN2O5Sã«å¯Ÿã㊠èšç®å€ïŒïŒ£ïŒ52.70ïŒïŒšïŒ6.75ïŒïŒ®ïŒ6.47ïŒ ïŒ³ïŒ7.41ïŒClïŒ9.19 枬å®å€ïŒïŒ£ïŒ52.15ïŒïŒšïŒ6.65ïŒïŒ®ïŒ6.36ïŒ ïŒ³ïŒ7.21ïŒClïŒ7.94 åèäŸïŒ ïŒâClâMTLã®ïŒâã·ã¹âïœâãã
ã«ââãããµããããã³ãªã³é žã¢ããåã¯ïŒµ
â60970E åºçºææ4.0ïœïŒ0.0093ã¢ã«ïŒãæ°Ž40mlãã¡ã¿ã
ãŒã«40mlã37ïŒ HCl2mlãåã³Pto2觊åª8.0ïœã®æ··
åç©ãããŒæ°ŽçŽ æ·»å è£ çœ®ã«ããã3.52KgïŒcm2
ïŒ50psiïŒã§18æééå ããã觊åªãé€ãããã«å
å¿æ¶²ããéããã液ãç空äžã§æ¿çž®ãããšããã¯
ãè²ã®æ²¹ãçãããCHCl3âã¡ã¿ããŒã«ïŒïŒïŒ
ïŒïŒæº¶æ¶²20mlã«æ²¹ã溶解ããååšããå¡©é žãäžå
ããã«ååãªããªãšãã«ã¢ãã³ãå ãããCHCl3
âã¡ã¿ããŒã«ïŒïŒïŒïŒïŒãããªã溶åªç³»ã䜿çšã
ãŠããã®æº¶æ¶²ãã·ãªã«ã²ã«äžã®ã¯ãããã°ã©ãã€
ã«ããããäž»çæç©ã®äºã€ã®ãã©ã¯ã·ãšã³ãåŸã
ãããæ©ã移åããæ¹ã®ææãå«æãããã©ã¯ã·
ãšã³ãäžç·ã«ããŠç空äžã§èžçºããããšãçœè²åº
äœã®ãã©ã¯ã·ãšã³ïŒ¡ãçããã移åã®ãããææ
ãå«æãããã©ã¯ã·ãšã³ãäžç·ã«ããŠç空äžã§èž
çºããããšãçœè²åºäœã®ãã©ã¯ã·ãšã³ïŒ¢ãçã
ãã ãã©ã¯ã·ãšã³ïŒ¢ãå°éã®H2Oã«æº¶è§£ããPHïŒ
ã«ããã«ååãªéã®37ïŒ HClãå ãããçµæ¶åã
èµ·ãããåºäœãéããŠH2Oããåçµæ¶ããããšã
æãã§ããçæç©ïŒµâ60970Eã®çœè²çµæ¶ãïŒèç¹
224ã226âïŒã25ã35ïŒ ã®åçã§çããã åæïŒ C17H32Cl2N2O5Sã«å¯Ÿã㊠èšç®å€ïŒïŒ£ïŒ47.99ïŒïŒšïŒ7.63ïŒïŒ®ïŒ5.89ïŒ ïŒ³ïŒ6.75ïŒClïŒ14.92 枬å®å€ïŒïŒ£ïŒ47.97ïŒïŒšïŒ7.42ïŒïŒ®ïŒ6.23ïŒ ïŒ³ïŒ6.90ïŒClïŒ14.87 αMeOH D ïŒ178ãïŒïŒ£ïŒ1.0ïŒ CMRåæã¯ãææ¡ã®æ§é ãæ¯æããŠããã â60970Eã®ããŸããŸãªçŽ°èã«å¯Ÿããæå°é»
æ¢æ¿åºŠïŒMICïŒã¯ãÎŒïœïŒmlã§ä»¥äžã®ãšããã§
ããã埮çç© UCïŒ MIC é»è²ãããŠçè 6 0.125 é»è²ãããŠçè 570 0.25 746 0.062 è žçè 694 0.25 åè¿é£éçè 152 0.008 èºçåçè 41 0.016 å€§è žè45 31.2 èºçæè 58 7.8 ã·ãšãããŠã©ãŒè 126 31.2 ç·è¿è 95 ïŒ125 è©Šéšæé ã¯å®æœäŸïŒã§æããã«ããããšããã§
ããã å®éšçã«çŽ°èã§ææãããæšæºçãªå®éšçšã¯ã€
ãããã¿ã«ã€ããŠãâ60970Eã®çäœè©Šéšãè¡
ãªã€ããâ57930Eãšæ¯èŒããªããè©Šéšãè¡ãª
ã€ãã次ã®çµæã¯ãååã³åèºçåçèã«å¯Ÿ
ããçäœè©Šéšã§ïŒµâ60970Eãâ57930Eããè
ãã匷ã掻æ§ãããããšã瀺ããŠãããé»è²ãã
ãŠçèãšæº¶è¡é£éçèã«å¯ŸããŠã¯ãâ60970E
ã¯ïŒµâ57930Eãšæ¬è³ªçã«åã掻æ§ã瀺ãã
ãè¡šã
åèäŸïŒ ïŒâClâMTLã®ïŒâã·ã¹âïœâãã
ã«ââãããµããããã³ãªã³é žã¢ããåã¯ïŒµ
â61734E åã®å®éšããã®ãã©ã¯ã·ãšã³ïŒ¡ãããã©ã¯ã·ãš
ã³ïŒ¢ã«å¯ŸããŠè¿°ã¹ããã®ãšåãæ¹æ³ã§ããã®HCl
å¡©ã«è»¢åãããçæç©ã®åç25ã35ïŒ ãåŸããã
ãã®CMRã¹ãã¯ãã«ã¯ãã©ã¯ã·ãšã³ïŒ¢ããåŸã
ãããã®ãšæ¬è³ªçã«åãã§ãã€ãã å®æœäŸïŒ ïŒâãã¹ããšãŒãé¡äŒŒäœ å®æœäŸïŒãïŒã§ã€ããããååç©é¡ã®ïŒâãã¹
ããšãŒãé¡äŒŒäœã¯ãåœæ¥è ã«åšç¥ã®æé ã«ãã€ãŠ
ã€ãããããæçœã§é©åãªå€æŽã«ãããåè¡åœç¹
蚱第3487068å·ã§æããã«ãããæé ã䜿çšã§ã
ããåºæ¬çã«ã¯ãä»»æã®æé ã¯åœ±é¿ãåãããã
åºããŸãåœæ¥è ã«åšç¥ã®æé ã«ãã€ãŠä¿è·ããã
ãšãå«ãã次ã«ãããã¯ãã¹ããªã«åã®å®æãã
åŸã«é€å»ãããã å®æœäŸïŒ ïŒâãã«ãããŒãé¡äŒŒäœ å®æœäŸïŒãïŒã§ã€ããããååç©é¡ã®ïŒâãã«
ãããŒãé¡äŒŒäœã¯ãåœæ¥è ã«åšç¥ã®æé ã«ãã€ãŠ
ã€ãããããæçœã§é©åãªå€æŽã«ãããåè¡åœç¹
蚱第3580904å·ã§æããã«ãããæé ã䜿çšã§ã
ããåºæ¬çã«ã¯ãä»»æã®æé ã¯ãŸã圱é¿ãåãã
ããåºãåœæ¥è ã«åšç¥ã®æé ã«ãã€ãŠä¿è·ããã
ãšãå«ãã次ã«ãããã¯ãå¡©åãã«ããã€ã«ãšã®
ã¢ã·ã«åã®çµäºã®ããšã§é€å»ãããã å®æœäŸïŒãïŒã§ã€ããããååç©é¡ã®ä»£è¡šçãª
ããã€ãã®æå°é»æ¢æ¿åºŠïŒMICïŒã次ã«è¿°ã¹ãã
è©Šéšæé ã¯äžè¿°ã®ãšããã§ããã
ã«ââãããµããããã³ãªã³é žã¢ããåã¯ïŒµ
â61734E åã®å®éšããã®ãã©ã¯ã·ãšã³ïŒ¡ãããã©ã¯ã·ãš
ã³ïŒ¢ã«å¯ŸããŠè¿°ã¹ããã®ãšåãæ¹æ³ã§ããã®HCl
å¡©ã«è»¢åãããçæç©ã®åç25ã35ïŒ ãåŸããã
ãã®CMRã¹ãã¯ãã«ã¯ãã©ã¯ã·ãšã³ïŒ¢ããåŸã
ãããã®ãšæ¬è³ªçã«åãã§ãã€ãã å®æœäŸïŒ ïŒâãã¹ããšãŒãé¡äŒŒäœ å®æœäŸïŒãïŒã§ã€ããããååç©é¡ã®ïŒâãã¹
ããšãŒãé¡äŒŒäœã¯ãåœæ¥è ã«åšç¥ã®æé ã«ãã€ãŠ
ã€ãããããæçœã§é©åãªå€æŽã«ãããåè¡åœç¹
蚱第3487068å·ã§æããã«ãããæé ã䜿çšã§ã
ããåºæ¬çã«ã¯ãä»»æã®æé ã¯åœ±é¿ãåãããã
åºããŸãåœæ¥è ã«åšç¥ã®æé ã«ãã€ãŠä¿è·ããã
ãšãå«ãã次ã«ãããã¯ãã¹ããªã«åã®å®æãã
åŸã«é€å»ãããã å®æœäŸïŒ ïŒâãã«ãããŒãé¡äŒŒäœ å®æœäŸïŒãïŒã§ã€ããããååç©é¡ã®ïŒâãã«
ãããŒãé¡äŒŒäœã¯ãåœæ¥è ã«åšç¥ã®æé ã«ãã€ãŠ
ã€ãããããæçœã§é©åãªå€æŽã«ãããåè¡åœç¹
蚱第3580904å·ã§æããã«ãããæé ã䜿çšã§ã
ããåºæ¬çã«ã¯ãä»»æã®æé ã¯ãŸã圱é¿ãåãã
ããåºãåœæ¥è ã«åšç¥ã®æé ã«ãã€ãŠä¿è·ããã
ãšãå«ãã次ã«ãããã¯ãå¡©åãã«ããã€ã«ãšã®
ã¢ã·ã«åã®çµäºã®ããšã§é€å»ãããã å®æœäŸïŒãïŒã§ã€ããããååç©é¡ã®ä»£è¡šçãª
ããã€ãã®æå°é»æ¢æ¿åºŠïŒMICïŒã次ã«è¿°ã¹ãã
è©Šéšæé ã¯äžè¿°ã®ãšããã§ããã
ãè¡šã
â â â
X
ïŒCâ7âClâMTL YïŒCâMTL ZïŒCâepiâMTL
RïŒCïŒHïŒâ
â â â
X
ïŒCâ7âClâMTL YïŒCâMTL ZïŒCâepiâMTL
RïŒCïŒHïŒâ
ãè¡šã
æ¬çºæååç©é¡ã¯çš®ã
ã®ã°ã©ã éœæ§åã³ã°ã©ã
é°æ§åŸ®çç©ã«å¯ŸããŠæŽ»æ§ãããããããã®ãããª
埮çç©ãæå¶ãããããããŸããŸãªç°å¢ã§äœ¿çšã§
ãããäŸãã°ãé»è²ãããŠçèã§æ±æãããé£åš
ã®æŽã€ãŠç©ã¿éãããã®ã«ãã®èãæå¶ãããã
ã®æ®ºèå€ãšããŠäœ¿çšã§ããããŸããé»è²ãããŠç
èã§æ±æãããæ¯ç§åã³å»ç§çšèšåã®æ¶æ¯å€ãšã
ãŠäœ¿çšã§ãããæŽã«ãæ¬çºæååç©é¡ã¯ãæŽæ¿¯ã
ãè¡£é¡ã®éèçšãªã³ã¹å€ãšããŠããŸãçŽãç¹ç©ã®
å«æµžçšã«äœ¿çšã§ããããããã¯ãŸãããã¬ãŒãæ€
å®å¹å°ãã®ä»ã®åŸ®çç©åŠçå¹å°äžã«ãããæåæ§
èã®çè²ãæããã«ãæçšã§ããã æ¬çºæååç©é¡ã¯ç°å¢PHã«åŸã€ãŠãããã³åå
ã¯éãããã³å圢ã§ååšããããããã³ååãæ
å³ããŠããæã«ã¯ãååç©ã¯è£œè¬åŠçã«åãå ¥ã
ãããé žä»å å¡©ãšããŠååšããéãããã³ååã
æå³ããæã«ã¯ååç©ã¯éé¢å¡©åºãšããŠååšã
ããéé¢å¡©åºã¯ãé©åœãªé žã§ãããPHçŽ7.0ã«ã
奜ãŸããã¯PHçŽïŒãªããPHïŒã«äžåããããšã«ã
ã€ãŠãå®å®ãªé žä»å å¡©ã«è»¢åã§ããããã®ç®çã«
é©ããé žã¯å¡©é žãç¡«é žãçé žãããªã·ã¢ã³é žãã
ã«ãªãçªé žããããµãã«ãªãç é žããããµãã«ãª
ãçé žãé ¢é žããã¯ãé žããããé žãä¹³é žããã¬
ã€ã³é žããããŒã«é žããã¢ã€ãã¯ã¢ã·ãããã³ãŒ
ã«é žããã«ããã³é žãç²æ¶²é žãã·ãšãŠããŠé žãã°
ã«ã¿ã«é žãã°ãªã³ãŒã«é žããã¿ãŒã«é žãé ç³é žã
ã©ãŠãªã³é žãã¹ãã¢ãªã³é žããµãªãã«é žãïŒâã
ãšãã«ãµãªãã«é žãïŒâããšãã«ãµãªãã«é žãïŒ
âã¡ãã«ã°ã«ã¿ãŒã«é žããªã«ãã¹ã«ãå®æ¯éŠé žã
ã·ã¯ããããµã³ã¹ã«ãã¢ãã³é žãã·ã¯ããã³ã¿ã³
ããããªã³é žãïŒïŒïŒâã·ã¯ããããµã³ãžã«ã«ã
ã³é žãïŒâã·ã¯ããããµã³ã«ã«ãã³é žããªã¯ã¿ã
ã»ãã«ãã¯ãé žããªã¯ããã«ãã¯ãé žãã¡ã¿ã³ã¹
ã«ãã³é žãããªã¢ã³ãã³é žãã©ã€ããã±é žããžã¡
ãã«ãžããªã«ã«ããã³é žããããµãã·ã«ã¹ã«ãã¢
ãã³é žããªã¯ã¿ãã·ã«ã¹ã«ãã¢ãã³é žããœã«ãã³
é žãã¢ãã¯ããé ¢é žããŠã³ãã·ã¬ã³é žã4â²âãã
ããã·ã¢ãŸãã³ãŒã³âïŒâã¹ã«ãã³é žããªã¯ã¿ã
ã·ã«ç¡«é žããã¯ãªã³é žãå®æ¯éŠé žãæ¡ç®é žçãå
å«ããã é žä»å å¡©ã¯éé¢å¡©åºãšåãç®çã«äœ¿çšã§ãã
ããåå¡©åºã®å質åäžã®ãã䜿ãããšãã§ããã
äŸãã°éé¢å¡©åºããã¯ãªã³é žå¡©ã®ãããªæ°Žã«æº¶ã
ãªãå¡©ã«è»¢åããããã粟補æé äŸãã°æº¶åªæœåº
ãšæŽæµãã¯ãããã°ã©ãã€ãåå¥æ¶²â液æœåºãå
ã³çµæ¶åã«ããã次ã«ã¢ã«ã«ãªåŠçã«ãã€ãŠéé¢
å¡©åºåãåçããããåã¯è€å解ã«ãã€ãŠå¥ã®å¡©
ãã€ããã®ã«çšãããããåã¯éé¢å¡©åºãå¡©é žå¡©
ãç¡«é žå¡©ã®ãããªæ°Žæº¶æ§ã®å¡©ã«è»¢åããå¡©ã®æ°Žæº¶
液ãçš®ã ã®æ°Žãšæ··ãããªã溶åªã§æœåºããŠããã
æœåºæº¶æ¶²ã®åŠçã«ãã€ãŠéé¢å¡©åºåãåçãã
ããåã¯è€å解ã«ãã€ãŠå¥ã®å¡©ã«è»¢åããã äžã«æããã«ãããæèçãªçšéã®ã»ããéé¢
å¡©åºã¯ç·©è¡æãšããŠåã¯å¶é žå€ãšããŠäœ¿çšã§ã
ããåè¡åœç¹èš±ç¬¬2425320å·åã³ç¬¬2606155å·ã«ã
ãã°ãããªã·ã¢ã³é žä»å å¡©ã¯ãã«ã ã¢ã«ããããš
çž®åããããšé žæŽæµæå¶å€ãšããŠæçšãªæš¹èç¶æ
æã圢æãããéé¢å¡©åºãææ¯ãªé žã«å¯Ÿããè¯å¥œ
ãªè³Šåœ¢å€ãšãªããäŸãã°åè¡åœç¹èš±ç¬¬1915334å·
ãšç¬¬2075359å·ã«ããã°ããã«ãªãçªé žä»å å¡©ã¯
é²èŸå€ãšããŠæçšã§ããããŸãåè¡åœç¹èš±ç¬¬
3122536å·ãšç¬¬3122552å·ã«ããã°ããããµãã«ãª
ãç é žãšãããµãã«ãªãçé žã®ä»å å¡©ã¯å¯çè«æ²
æ» å€ãšããŠæçšã§ããã æ¬çºæååç©é¡ã¯ãé©åœãªçµæç©ã®åœ¢ã®æèå€
ãšããŠæçšã§ããããããã®çµæç©ã¯ãéé¢å¡©åº
åã¯è¬åŠçã«åå ¥ãããããã®å¡©é¡ã®åœ¢ã®æŽ»æ§å
åç©ã®é©åœéãå«æããé å€ãã«ãã»ã«ãäžžè¬ã
ç²æ«ãç²å€ãç¡èã®éçµå£æº¶æ¶²åã¯æžæ¿æ¶²ãåã³
çµå£æº¶æ¶²åã¯æžæ¿æ¶²ãåã³æ²¹âæ°Žä¹³æ¿æ¶²ã®ãããª
åäœé©é圢åŒã§äººéãšåç©ãžæäžããããã«æäŸ
ãããã®ã奜ãŸããã çµå£æäžã«ã¯ãåºäœåã¯æµäœã®åäœæäžé圢åŒ
ãã€ããããšãã§ãããé å€ã®ãããªåºäœçµæç©
ãã€ããã«ã¯ãåºæ¬æŽ»æ§æåã補è¬åŠçåžéå€å
ã¯æ äœãšããŠã®æ»ç³ãã¹ãã¢ãªã³é žãã°ãã·ãŠ
ã ãçé žäºã«ã«ã·ãŠã ãçªé žã¢ã«ãããŠã ãã°ã
ã·ãŠã ãç¡«é žã«ã«ã·ãŠã ã殿ç²ãä¹³é ãã¢ã©ãã¢
ãŽã ãã¡ãã«ã»ã«ããŒã¹ãåã³æ©èœäžåæ§ãªææ
çã®æ £çšæåãšæ··åãããäœçšãé·ã³ããããé
ããããããå©ç¹ãæã¯å°å ¥è¬ç©ãæå®ã®é åºã§
äœçšãããå©ç¹ãåããæäžéåäœãæäŸããã
ããé å€ãç©å±€ããããåã¯å¥ã®åœ¢ã§ã³ã³ããŠã³
ãããããšãã§ãããäŸãã°ãé å€ãå åŽã®é©é
ãšå€åŽã®é©éæåãããªããåŸè ãåè ãå ã圢
ã«ã§ãããïŒæåãè žæº¶ç®å±€ã«ãã€ãŠåé¢ããã
ã®å±€ã«èå ã§ã®åŽ©å£ã«èããŠå åŽæåãåäºæè ž
ãžç¡å·ã®ãŸãŸééããããããŸãã¯æŸåºãé ãã
ãããã圹ç®ãè¡ãªãããããšãã§ããããã®ã
ããªè žæº¶ç®èã被èŠã«ã¯ãå€æ°ã®éåäœã®é žãå
ã¯éåäœã®é žãšã»ã©ãã¯ãã»ãã«ã¢ã«ã³ãŒã«ãã»
ã«ããŒã¹ã»ã¢ã»ããŒãã»ãã¿ã¬ãŒããã¹ãã¬ã³â
ãã¬ã€ã³é žå ±éåäœçã®ãããªææãšã®æ··åç©ã
å«ããçš®ã ã®ææã䜿çšã§ããã®ä»£ããã«ãäºã€
ãªãããã以äžã®çžå®¹ããªã掻æ§æåãå«æãã
é å€ã®è£œé ã«äºæåç³»ãå©çšã§ãããé å€ãšåã
æ¹æ³ã§ãŠãšãã¢ãŒã¯ã€ãããããã圢ã庶ç³ãã®
ä»ã®çå³å€ãšé¢šå³æãå«ãŸããŠããç¹ãç°ãªãã®
ã¿ã§ãããæãç°¡åãªæ æ§ã®å Žåãã«ãã»ã«ã¯é
å€ã®ããã«ãåŠæ¹å€ã®ååç©ãäžæŽ»æ§ãªè£œè¬åŠç
åžéå€ãšæ··åããé©åœãªå€§ããã®ç¡¬ããŒã©ãã³ã«
ãã»ã«ãžæ··åç©ãå å¡«ããããšã§ã€ãããããå¥
ã®æ æ§ã§ã¯ã掻æ§ååç©ãå«æããéåäœé žã®è¢«
èŠããŒãºã硬ããŒã©ãã³ã«ãã»ã«ã«è©°ããããšã«
ãã€ãŠã«ãã»ã«å€ãã€ãããè»ããŒã©ãã³ã«ãã»
ã«ã¯ã掻æ§æåãšåãå ¥ããããæ€ç©æ²¹ã軜質液
äœãããã©ã¯ã¿ã åã¯ãã®ä»ã®äžæŽ»æ§æ²¹ãšã®ã¹ã©
ãªãŒã®æ©æ¢°ã«ããã«ãã»ã«å°å ¥ã«ãã€ãŠã€ããã
ãã ã·ãããå€ããšãªããžãŒã«å€åã³æžæ¿æ¶²ã®ãã
ãªçµå£æäžåãã®æµäœåäœæäžé圢åŒãã€ããã
ãšãã§ããã掻æ§ååç©ã®æ°Žæº¶åã®ãã®ã¯ç ç³ã
è³éŠæ§é¢šå³æåã³é²è å€ãšå ±ã«æ°Žæ§è³Šåœ¢å€äžã«æº¶
解ããããšã·ãããå€ãã§ããããšãªããžãŒã«å€
ã¯ãè³éŠæ§é¢šå³æãšå ±ã«ç ç³ã®ãããªé©åœãªçå³
æãå ããæ°Žâã¢ã«ã³ãŒã«ïŒãšã¿ããŒã«ïŒã®è³Šåœ¢
å€ã䜿çšããŠã€ãããããæžæ¿æ¶²ã¯ãã¢ã©ãã¢ãŽ
ã ããã©ã¬ã«ã³ããŽã ãã¡ãã«ã»ã«ããŒã¹çã®ã
ããªæžæ¿å€ã®å©ããåããŠãã·ãããçšè³Šåœ¢å€ã«
ããäžæº¶æ§åã«ã€ããããšãã§ããã å±æçšè»ããã¯ããããã©ã¿ã ãã©ããªã³ãã
ãªãšãã¬ã³ã°ãªã³ãŒã«ããããã®æ··åç©çã®é©åœ
ãªè»ããåºæäžã«æŽ»æ§ååç©ãåæ£ãããããšã«
ãã€ãŠã€ãããããè»ããåºæã«åæ£ãããåã«
è»è³ªæ¶²äœãããã©ã¿ã ã磚ç ç©ãšããŠå©çšããã³
ãã€ããã«ã«ãããååç©ã埮ç²ç ããã®ãæå©
ã§ãããå±æçšã¯ãªãŒã åã³ããŒã·ãšã³ã¯ãæ°Žäž
ã«æ²¹çžãä¹³åãããåã«ãæ²¹çžã«ååç©ãåæ£ã
ããããšã«ãã€ãŠã€ããããã éçµå£æäžã«ã¯ãæµäœã®åäœæäžé圢åŒã¯ã掻
æ§ååç©ãšç¡è賊圢å€ïŒæ°Žã奜é©ïŒãå©çšããŠã€
ããããã掻æ§ååç©ã¯ã䜿çšåœ¢åŒåã³æ¿åºŠã«ã
ãããã賊圢å€äžã«æžæ¿ãããããåã¯æº¶è§£ãã
ãããšãã§ããã溶液ãã€ããã«ã¯ã掻æ§ååç©
ã®æ°Žæº¶æ§åã泚å°çšæ°Žã«æº¶è§£ããé©åœãªå°ã³ãå
ã¯ã¢ã³ãã«ã«å å¡«ãå°å ¥ããåã«ãéæ» èããã
å±æ麻é å€ãé²è å€åã³ç·©è¡å€ã®ãããªå©å€ã賊
圢å€äžã«æº¶è§£ããã®ãæå©ã§ãããå®å®æ§ãé«ã
ããããå°ã³ãã«å å¡«åŸãçµæç©ãåçµããç空
äžã§æ°Žãé€å»ãããåçµä¹Ÿç¥ããç²æ«ãå°ã³ãäž
ã«å°å ¥ãã䜿çšçŽåã«æº¶æ¶²ãåæ§æããããæ·»ã
ã泚å°çšæ°Žã®å°ã³ããè£å ãããéçµå£æžæ¿æ¶²ã¯
å®è³ªçã«åãæ¹æ³ã§ã€ããããããäœã掻æ§åå
ç©ã溶解ãã代ããã«è³Šåœ¢å€äžã«æžæ¿ããããé
ã«ããæ» èã¯ã§ããªããç¡èã®è³Šåœ¢å€äžã«æžæ¿ã
ãåã«ã掻æ§ååç©ã¯é žåãšãã¬ã³ã«åœãŠãŠæ» è
ããã掻æ§ååç©ã®åäžååžã容æã«ããããã
çµæç©äžã«è¡šé¢æŽ»æ§å€åã¯æ¹¿æœ€å€ãå«ããã®ãæ
å©ã§ããã æ¬æ现æžåã³ç¹èš±è«æ±ã®ç¯å²ã§äœ¿ãããçšèªã®
åäœæäžéïŒé©éïŒåœ¢åŒãšã¯ã人éã®æ£è åã³å
ç©çšã«åäœæäžéãšããŠé©ããç©ççã«ã°ãã°ã
ã«ãªã€ãåäœã®ããšã§ãããååäœã¯å¿ èŠãªè£œè¬
åŠçåžéå€ãæ äœåã¯è³Šåœ¢å€ãšå ±åããŠæãã§ã
ãæ²»çå¹æãçããããã«èšç®ãããæå®éã®æŽ»
æ§ææãå«æãããæ¬çºæã®æ°èŠãªåäœæäžé圢
åŒã®æ现ã¯ã(a)掻æ§ææã®ãã°ãããæ§è³ªãšãé
æããããšããç¹å®ã®æ²»çå¹æãåã³(b)æ¬æ现æž
ã§è©³çŽ°ã«æããã«ãããŠããããã«ã人éåã³å
ç©ãžã®æ²»ççšã«ãã®ãããªæŽ»æ§ææãã³ã³ããŠã³
ãããæè¡ã«åºæã®å¶éã«ãã€ãŠæå³ãããã€çŽ
æ¥ãããã«ãã€ãŠãããããããã®ä»æ§ã¯æ¬çºæ
ã®ç¹åŸŽã§ãããæ¬çºæã«åŸãé©åœãªåäœæäžé圢
åŒã®äŸã¯ãé å€ãã«ãã»ã«ãäžžè¬ããããŒããå
è¬ãç²æ«è¬å ãç²å€ããŠãšãã¢ãŒãã«ã·ãšãè¶ãµ
ãžéã倧ãµãžéã滎ã³ãéãã¢ã³ãã«ãå°ã³ãã
以äžã®ä»»æã®ãã®ã®å¥ã ã®è€æ°äœ¿çšãåã³æ¬æ现
æžã«èšèŒã®ãã®ä»ã®åœ¢åŒã§ããã æ¬æ现æžã«èšèŒã®çç¶ã®åŠçœ®çšã«çµæç©ã®äž»æŽ»
æ§æåãšããŠãã®æŽ»æ§ååç©ãæäžããã»ããæ
å©ãªçµåãã®æ§ç¶ãåŸãããããã®ã³ã³ããŠã³ã
ã«ä»ã®çš®é¡ã®ååç©ãå«ããããšãã§ããããã®
ãããªçµåãã¯ãæ¬æŽ»æ§ååç©ãšå ±ã«ãã¹ãã¯ã
ããã€ã·ã³ãã¯ãã©ã ããšãã³ãŒã«ãããããªã·
ã³ããžããããããªã·ã³ãããã©ãµã€ã¯ãªã³é¡
ïŒäŸãã°ããã©ãµã€ã¯ãªã³ããªãã·ããã©ãµã€ã¯
ãªã³ãåã³ã¯ãã«ããã©ãµã€ã¯ãªã³ïŒãããã·ãª
ã³é¡ããšãªã¹ããã€ã·ã³ãã«ããã€ã·ã³ãã¹ãã¬
ãããã€ã·ã³ãããªãã€ã·ã³ãããªããã·ã³ãã
ã·ãã©ã·ã³ããã¹ã¿ãã³ããã€ãªãã³ãããã®ãª
ã³åã³ãšã³ããã€ã·ã³ã®ãããªãçµæç©ã®æèã¹
ãã¯ãã«ãåºããç¹å®çŽ°èã«å¯Ÿããçžä¹äœçšãã
ã€æçç©è³ªé¡ïŒãã€ããã³ã«ããŸãŒã³ããã¬ãã
ãœãã³ã6αâã¡ãã«ãã¬ãããœãã³ã6αâãã«
ãªããã¬ãããœãã³çã®ãããªæçç掻æ§ããã€
ã¹ããã€ãé¡ïŒã¢ã¹ããªã³ããµãªãã«é žãããªãŠ
ã ïŒã¢ã»ãã«ãµãªãã«é žïŒç¡æ°Žç©ãâã¢ã»ãã«
âïœâã¢ããããšãã«åã³ãµãªãã«ã¢ããã®ãã
ãªé®çå€ïŒã¯ããããšãã©ãã³ãã¬ãšãŒãããžã
ãšãã«ããã©ãã³ãããã¡ã¿ãžã³ããã©ãã¢ãžã³
çã®ãããªæãã¹ã¿ãã³å€ïŒãµã«ãã¢ãžã¢ãžã³ã
ã«ãã¢ã¡ã¿ãžã³ããµã«ãã¢ã¡ã©ãžã³ããµã«ãã¢ã»
ã¿ããããµã«ãã¢ãžã¡ããããµãŸãŒã«ããµã«ãã¢
ã¡ããŸãŒã«çã®ãããªãµã«ãã¢å€ïŒãŠã³ãã·ã¬ã³
é žãããããªã³é žãããªãŠã ããµãªãã«ã¢ããª
ããã«ããªã«é žãããªãŠã åã³ããã»ããžã³ã®ã
ããªé²ã«ãå€ïŒåã³ãã¿ãã³å€ãå å«ããã 掻æ§ååç©ã®æ²»çã«ãããé©éã¯ãæäžåŸè·¯ã
æ£è ã®å¹Žä»€ãäœéãçç¶ãåã³åŠçœ®ããç¹å®ã®ç
æ°ã«ãã€ãŠæ±ºãŸããçŽ15ã500mgã§ïŒæ¥ïŒãïŒå
ïŒïŒæéæ¯ïŒã®æäžéèšç»ã¯ãçµæç©ãæå¹ã§ã
ãã»ãšãã©ã®çç¶ã®åŠçœ®ã«å¯ŸããŠæå¹ãªç¯å²ãå
å«ããŠãããå°å ã«ã¯ãïŒæ¥Kgåœã15ã30mgã®åº
ç€ã§èšç®ãããæäžéããïŒæéæ¯ã«æäžããã 奜éœåãªåå¹æçãªæäžã®ãããåäœé©é圢åŒ
ã«ããŠæŽ»æ§ååç©ãé©åœãªè£œè¬åŠçæ äœãšã³ã³ã
ãŠã³ããããæ¬çºæã®å¥œãŸããæ æ§ã§ã¯ãé©éå
äœã¯å šèº«çåŠçœ®çšã«15ïŒ30ïŒ50ïŒ125ïŒ250åã³
500mgã§ãããå±æåŠçœ®çšã«ã¯0.25ïŒ0.5ïŒïŒïŒïŒ
åã³ïŒïŒ éã§ããããŸãéçµå£æäžçšã«ã¯ïŒã65
ïŒ ïŒïœïŒïœïŒã®ååç©ãå«æãããæ¬æŽ»æ§ååç©
ãšäžçš®åã¯ãã以äžã®ãã®ä»æŽ»æ§æåãå«æãã
çµæç©é¡ã®æäžéã¯ããã®ãããªåæåã®éåžžæ
äžéãåç §ããªãã決å®ãããã¹ãã§ããã 以äžã®å®æœäŸã¯æ¬çºæãå®æœãããããšæ¬çºæ
è ãèããæãããæ æ§ã®äŸç€ºã§ããããéå®ç
ã«èããããŠã¯ãªããªãã çµæç©å®æœäŸïŒ ã«ãã»ã« ïŒååœãæ¬çºæã®æŽ»æ§ååç©250mgãå«æãã
çµå£çšã®ç¡¬ãäºæ®»ãŒã©ãã³ã«ãã»ã«1000åãã次
ã®çš®é¡åã³éã®ææããã€ããã æ¬çºæã®æŽ»æ§ååç© 250ïœ ãšãããããæ®¿ç² 100ïœ æ» ç³ 75ïœ ã¹ãã¢ãªã³é žãã°ãã·ãŠã 25ïœ ææãå®å šã«æ··åããéåžžã®æ¹æ³ã§ã«ãã»ã«å
ããã äžã®ã«ãã»ã«ã¯ïŒæéæ¯ã«ïŒã«ãã»ã«ã®çµå£æ
äžã§æ人ã®å šèº«çææåŠçœ®ã«æå¹ã§ããã äžã®æé ã䜿çšããŠãäžèšã®250ïœã®ä»£ããã«
15ïŒ30ïŒ50ïŒ125åã³500ïœã®æ¬çºæã®æŽ»æ§ååç©
ã䜿çšããŠã15ïŒ30ïŒ50ïŒ125åã³500mgã®æ¬çºæ
ã®æŽ»æ§ååç©ãå«æããã«ãã»ã«ãåãããã«ã€
ããããã çµæç©å®æœäŸïŒ ã«ãã»ã« ïŒååœãæ¬çºæã®æŽ»æ§ååç©200mgãšããã©ãµ
ã€ã¯ãªã³å¡©é žå¡©250mgãå«æããçµå£çšã®ç¡¬ãäº
æ®»ãŒã©ãã³ã«ãã»ã«1000åã次ã®çš®é¡åã³éã®æ
åããã€ããã æ¬çºæã®æŽ»æ§ååç© 200ïœ ããã©ãµã€ã¯ãªã³å¡©é žå¡© 250ïœ æ» ç³ 75ïœ ã¹ãã¢ãªã³é žãã°ãã·ãŠã 25ïœ æåãå®å šã«æ··åãã次ã«éåžžã®æ¹æ³ã§ã«ãã»
ã«åããã äžã®ã«ãã»ã«ã¯ãïŒæéæ¯ã«ïŒã«ãã»ã«ã®çµå£
æäžã§æ人ã®å šèº«çææåŠçœ®ã«æçšã§ããã äžã®æé ã䜿çšããŠãããã©ãµã€ã¯ãªã³ã®ä»£ã
ã«ã¯ãã©ã ããšãã³ãŒã«ããªãã·ããã©ãµã€ã¯ãª
ã³ãã¯ãã«ããã©ãµã€ã¯ãªã³ãããã®ãªã³ããšã¯
ã¹ããã€ã·ã³ãã¹ãã¬ãããã€ã·ã³ããžãããã
ãããªã·ã³ãåã³ããããªã·ã³250ïœã䜿çšããŠã
æ¬çºæã®æŽ»æ§ååç©ãšãããã®æçç©è³ªã®åã ã
å«æããã«ãã»ã«ãåãããã«ã€ããããã ããã©ãµã€ã¯ãªã³ã®ä»£ããã«ã«ãªãŠã ããã·ãª
ã³ïŒ§ã®ãããªããã·ãªã³ã䜿çšããæã«ã¯ãã«ã
ã»ã«åœã250000åäœã䜿çšããã ãã®ãããªçµåãçæç©ã¯ãïŒæéæ¯ã«ïŒã«ã
ã»ã«ã®çµå£æäžã«ãã€ãŠæ人ã®æ··åææã®å šèº«ç
åŠçœ®ã«æçšã§ããã çµæç©å®æœäŸïŒ é å€ ïŒé åœãæ¬çºæã®æŽ»æ§ååç©500mgãå«æãã
çµå£çšé å€1000åã次ã®çš®é¡åã³éã®ææããã€
ããã æ¬çºæã®æŽ»æ§ååç© 500ïœ ä¹³ ç³ 125ïœ ãšãããããæ®¿ç² 65ïœ ã¹ãã¢ãªã³é žãã°ãã·ãŠã 25ïœ è»œè³ªæ¶²äœãããã©ã¯ã¿ã ïŒïœ æåãå®å šã«æ··åããã¹ã©ãã°ã«ãããã¹ã©ã
ã°ã¯16çªã®ãµããã匷å¶ééãããŠç Žå£ãããç
ããé¡ç²ãé å€ã«å§çž®ããïŒé åœãæ¬çºæã®æŽ»æ§
ååç©500mgãå«æããé å€ã«å§çž®ããã äžã®é å€ã¯ãïŒæéæ¯ã«ïŒé ã®çµå£æäžã«ãã
æ人ã®å šèº«çææåŠçœ®ã«æçšã§ããã æ¬çºæã®æŽ»æ§ååç©ã®éã250ïœã«æžãã以å€
ã¯äžã®æé ã䜿çšããŠãæ¬çºæã®æŽ»æ§ååç©250
mgãå«æããé å€ãã€ããããã çµæç©å®æœäŸïŒ é å€ ïŒé åœãæ¬çºæã®æŽ»æ§ååç©250mgãšãµã«ãã¢
ãžã¢ãžã³ããµã«ãã¢ã¡ã©ãžã³åã³ãµã«ãã¢ã¡ã¿ãž
ã³èš250mgïŒå83.3mgïŒãå«æããçµå£é å€1000
é ãã次ã®çš®é¡åã³éã®ææããã€ããã æ¬çºæã®æŽ»æ§ååç© 250ïœ ãµã«ãã¢ãžã¢ãžã³ 83.3ïœ ãµã«ãã¢ã¡ã©ãžã³ 83.3ïœ ãµã«ãã¢ã¡ã¿ãžã³ 83.3ïœ ä¹³ ç³ 50ïœ ãšãããããæ®¿ç² 50ïœ ã¹ãã¢ãªã³é žã«ã«ã·ãŠã 25ïœ è»œè³ªæ¶²äœãããã©ã¿ã ïŒïœ æåãå®å šã«æ··åãã¹ã©ãã°åãããã¹ã©ãã°
ã¯16çªãµããã匷å¶ééãããŠç Žå£ãããçãã
é¡ç²ããæ¬çºæã®æŽ»æ§ååç©250mgãšãµã«ãã¢ãž
ã¢ãžã³ããµã«ãã¢ã¡ã©ãžã³ãåã³ãµã«ãã¢ã¡ã¿ãž
ã³èš250mgïŒå83.3mgïŒãå«æããé å€ã«å§çž®ã
ãã äžã®é å€ã¯ãŸãïŒé ãçµå£æäžãã次ã«ïŒæé
æ¯ã«ïŒé ã®æäžã«ããå šèº«çææåŠçœ®ã«æçšã§ã
ãã æ³å°¿åšææã®åŠçœ®ã«ã¯ãäžã®åŠæ¹å€ã®äžã€ã®ãµ
ã«ãã¢å€ã®ä»£ããã«ããµã«ãã¢ã¡ãã«ãã¢ãžã¢ãŸ
ãŒã«250ïœåã¯ãµã«ãã¢ã»ã¿ãã250ïœã䜿çšãã
ã®ãæå©ã§ããã çµæç©å®æœäŸïŒ çµå£ã·ãããå€ ååïŒc.c.æäžéäžã«ãµã«ãã¢å€åèš0.5ïœãšæ¬
çºæã®æŽ»æ§ååç©250mgãå«æããçµå£çšæ°Žæ§æž
æ¿æ¶²1000c.c.ã次ã®çš®é¡åã³éã®æåããã€ããã æ¬çºæã®æŽ»æ§ååç© 50ïœ ãµã«ãã¢ãžã¢ãžã³ 33.3ïœ ãµã«ãã¢ã¡ã©ãžã³ 33.3ïœ ãµã«ãã¢ã¡ã¿ãžã³ 33.3ïœ ãããé ž ïŒïœ å®æ¯éŠé ž ïŒïœ 庶 ç³ 700ïœ ãã©ã¬ã«ã³ã ïŒïœ ã¬ã¢ã³æ²¹ ïŒc.c. è±ã€ãªã³æ°Ž 1000c.c.ãšããé 溶液850c.c.ã«ããã«è¶³ãéã®æ°Žã«ãããé žãå®
æ¯éŠé žã庶ç³ããã©ã¬ã«ã³ãåã³ã¬ã¢ã³æ²¹ãåæ£
ããããæ¬çºæã®æŽ»æ§ååç©ãšåŸ®ç²ç ãµã«ãã¢å€
ããåäžã«ååžããããŸã§ã·ãããäžã§ãããŸã
ããå šéã1000c.c.ã«ããã®ã«ååãªæ°Žãå ããã ããããŠã€ããããçµæç©ã¯ãïŒæ¥ã«ïŒåè¶ãµ
ãžïŒæ¯ãã€ã®æäžéã§ãæ人ã®èºçã®å šèº«çåŠçœ®
ã«æçšã§ããã çµæç©å®æœäŸïŒ éçµå£æº¶æ¶² ïŒc.c.äžã«æ¬çºæã®æŽ»æ§ååç©200mgãå«æãã
çèå 䜿çšã®ç¡è氎溶液ã次ã®çš®é¡åã³éã®ææ
ããã€ããã æ¬çºæã®æŽ»æ§ååç© 200ïœ ãªãã«ã€ã³å¡©é žå¡© ïŒïœ ã¡ãã«ãã©ãã³ 2.5ïœ æ³šå°çšæ°Ž 1000c.c.ã«ããé æåãæ°Žã«æº¶è§£ãããéã«ãã€ãŠæº¶æ¶²ãæ» èã
ããç¡è溶液ãå°ã³ãã«å å¡«ããå°ã³ããå¯å°ã
ãã çµæç©å®æœäŸïŒ éçµå£èª¿è£œå€ ïŒc.c.äžã«æ¬çºæã®æŽ»æ§ååç©200mgãšã¹ãã¯ã
ããã€ã·ã³ç¡«é žå¡©400mgãå«æããçèå 䜿çšã®
ç¡è氎溶液ã次ã®çš®é¡åã³éã®æåããã€ããã æ¬çºæã®æŽ»æ§ååç© 200ïœ ã¹ãã¯ãããã€ã·ã³ç¡«é žå¡© 400ïœ ä¹³ é 50ïœ æ³šå°çšæ°Ž 1000c.c.ãšããé æ¬çºæã®æŽ»æ§ååç©ãã¹ãã¯ãããã€ã·ã³ç¡«é ž
å¡©åã³ä¹³é ãæ°Žã«æº¶è§£ãã溶液ããéã«ãã€ãŠæ»
èãããïŒc.c.ã®éã§æ» è溶液ãç¡èçãªå°ã³ãã«
ç¡èçã«å å¡«ããåçµããããé«ç空äžã§æ°Žãé€
å»ããåçµä¹Ÿç¥ããç²æ«ã®å ¥ã€ãå°ã³ããå°å ¥ã
ãã䜿çšçŽåã«æº¶æ¶²ïŒc.c.ãã€ãã泚å°çšç¡èæ°Žã®
ååéãå°ã³ãã«å ããã çµæç©å®æœäŸïŒ å±æçšè»ãã 0.25ïŒ ã®è»ãã1000ïœã次ã®çš®é¡åã³éã®æå
ããã€ããã æ¬çºæã®æŽ»æ§ååç© 2.5ïœ é žåäºé 50ïœ ã«ã©ãã³ 50ïœ æ¶²äœãããã©ã¿ã ïŒééïŒ 250ïœ çŸ è 200ïœ çœè²ãããã©ã¿ã 1000ïœãšããé çœè²ãããã©ã¿ã ãšçŸèã溶èãã液äœããã
ã©ã¿ã 100ïœãããã«å ãããæ¬çºæã®æŽ»æ§åå
ç©ãé žåäºéåã³ã«ã©ãã³ãæ®ãã®æ¶²äœãããã©
ã¿ã ã«å ããç²æ«ã埮ç²ç ãããŠåäžååžããã
ãŸã§æ··åç©ãç²ç ãããç²æ«æ··åç©ãçœè²ããã
ã©ã¿ã æ··åç©äžã«ãããŸããè»ãããåºãŸããŸã§
ãããŸããç¶ããã äžã®è»ããã¯ãææã®åŠçœ®çšã«åºä¹³é¡ã®ç®èã«
å±æçã«å¡åžãããšæçšã§ããã äžã®çµæç©ã¯ãé žåäºéãšã«ã©ãã³ãçç¥ããŠ
ã€ããããšãã§ããã äžã®æé ã«åŸã€ãŠãäžã§çšãã25ïœã®ä»£ããã«
æ¬çºæã®æŽ»æ§ååç©ã®ïŒïŒ10ïŒ20åã³50ïœã䜿çš
ããŠã0.5ïŒïŒïŒïŒïŒåã³ïŒïŒ ã®éã®æ¬çºæã®æŽ»
æ§ååç©ãå«æããè»ãããåãããã«ã€ããã
ãã çµæç©å®æœäŸïŒ ã¯ãªãŒã è çšã¯ãªãŒã 1000ïœã次ã®çš®é¡åã³éã®æåã
ãã€ããã æ¬çºæã®æŽ»æ§ååç© 50ïœ ãã¬ã·ããã»ã¬ã®ãŠã©ãŒ1) 150ïœ é¯šãã 100ïœ ãããã¬ã³ã°ãªã³ãŒã« 50ïœ ããªãœã«ããŒã80 ïŒïœ ã¡ãã«ãã©ãã³ ïŒïœ è±ã€ãªã³æ°Ž 1000ïœãšããé ïŒ ãŽãŒã«ãã·ãŠãããã»ã±ãã«ã«ã»ã³ãŒãã¬ãŒ
ã·ãšã³ïŒããŠãŒãšãŒã¯å·ããŠãŒãšãŒã¯ïŒããã®
èªå·±ä¹³åããã°ãªã»ãªã«ã»ã¢ãã¹ãã¢ã¬ãŒãã ãã¬ã·ãããšé¯šããã70ã80âã®æž©åºŠã§äžç·ã«
溶èãããæ°ŽçŽ500ïœã«ã¡ãã«ãã©ãã³ã溶解ãã
ãããã¬ã³ã°ãªã³ãŒã«ãããªãœã«ããŒã80ãåã³
æ¬çºæã®æŽ»æ§ååç©ãé ã ã«å ãã75ã80âã®æž©
床ãä¿ã€ãã¡ãã«ãã©ãã³æ··åç©ããã¬ã·ãããš
鯚ãããšã®æº¶èç©ã«ãäžå®ã«ãããŸããªããåŸã
ã«å ãããããããããŸããªããã枩床ã40ã45
âã«äœäžãããŸã§ãå°ãªããšã30åéæ·»å ãç¶ã
ããæ°ŽçŽ50ïœã«æº¶è§£ãããããé ž2.5ïœãšäºå¡©åº
æ§çé žãããªãŠã 0.2ïœãæ··å ¥ããããšã«ãã€ãŠã
æçµçãªã¯ãªãŒã ã®PHã3.5ã«èª¿æŽãããæåŸã«ã
æçµééã1000ïœã«ãã€ãŠããååéã®æ°Žãå
ãã調補å€ãå·åŽããŠåºãŸããŸã§å質ã«ä¿ã€ãã
ã«ãããŸããã äžã®çµæç©ã¯äººéã®è å ææã®åŠçœ®ã«æçšã§ã
ãã çµæç©å®æœäŸ10 çŒç§çšè»ãã 0.5ïŒ æ¬çºæã®æŽ»æ§ååç©ãå«æããçŒç§çšè»
ãã1000ïœã次ã®çš®é¡åã³éã®æåããã€ããã æ¬çºæã®æŽ»æ§ååç© ïŒïœ ãã·ãã©ã·ã³ 12.2ïœ ããªããã·ã³ïŒ¢ç¡«é žå¡©ïŒ10000åäœïŒmgïŒ
ïŒïœ 軜質液äœãããã©ã¿ã 250ïœ çŸ è 200ïœ çœè²ãããã©ã¿ã 1000ïœãšããé 空æ°åŒè¶ 埮ç²ç æ©ã«ãã€ãŠåºäœæåã埮ç²ç
ãã軜質液äœãããã©ã¿ã ã«å ãããæ··åç©ãã³
ãã€ããã«ã«ãããŠåŸ®ç²ç ç²åãåäžååžãã
ããçŸèãšçœè²ãããã©ã¿ã ãäžç·ã«æº¶èããã
ãããããŠæž©åºŠã45ã50âã«èª¿æŽããã液äœãã
ãã©ã¿ã ã®ã¹ã©ãªãŒãå ããåºãŸããŸã§è»ããã
ãããŸãããïŒãã©ã ïŒ3.9ïœïŒã®çŒç§çšããŠãŒ
ãã«è»ãããå è£ ããã®ãé©ããŠããã äžã®è»ããã¯ã人éãã®ä»ã®åç©ã®å±æææã®
åŠçœ®ã®ããçŒã«æçšã«é©çšãããã äžã®çµæç©ã¯ççã®åŠçœ®çšã«ã¡ãã«ãã¬ãããœ
ãã³ïŒïœïŒ0.5ïŒ ïŒãå«æããã®ãæå©ã§ãããã
ãã®ä»£ããã«ãã·ãã©ã·ã³ãšããªããã·ã³ïŒ¢ç¡«é ž
å¡©ãçç¥ã§ããã çµæç©å®æœäŸ11 ç¹çŒå€ïŒè³æ»Žå€ ïŒc.c.åœãæ¬çºæã®æŽ»æ§ååç©10mgãšã¡ãã«ãã¬
ãããœãã³ïŒmgãå«æããçŒåã¯è³çšã®ç¡èçæ°Ž
溶液1000c.c.ãã次ã®çš®é¡åã³éã®æåããã€ã
ãã æ¬çºæã®æŽ»æ§ååç© 10ïœ ã¡ãã«ãã¬ãããœãã³çé žãããªãŠã ïŒïœ ãããé žãããªãŠã 4.5ïœ éäºç¡«é žãããªãŠã ïŒïœ ããªãšãã¬ã³ã°ãªã³ãŒã« 4000 120ïœ ããªã¹ãã«âγâãã³ãªããŠã ã¯ãã©ã€ã
0.2ïœ ããªããã«ãããªãã³ ïŒïœ è±ã€ãªã³æ°Ž 1000c.c.ãšããé æåãæ°Žã«æº¶è§£ããçãã溶液ããéã«ãã€ãŠ
æ» èããã溶液ãç¡èã®æ»Žã³ã容åšã«ç¡èçã«å
å¡«ããã ããããŠã€ããããçµæç©ã¯ãçŒãšè³ã䞊ã³ã«
åç©ã®èº«äœã®ãã®ä»ã®ææãªçµç¹ã®ççåã³ææ
ã®å±æåŠçœ®ã«æçšã§ããã çµæç©å®æœäŸ12 ãããŒã 次ã®çš®é¡åã³éã®æåãããããŒã10000åã
ã€ããã æ¬çºæã®æŽ»æ§ååç© 100ïœ ããªãã€ã·ã³ç¡«é žå¡© 50ïœ ããªããã·ã³ïŒ¢ç¡«é žå¡©ïŒ10000åäœïŒmgïŒ
ïŒïœ ã¢ããå®æ¯éŠé žãšãã« 50ïœ ã¹ãã¢ãªã³é žã«ã«ã·ãŠã 150ïœ ç²æ«åº¶ç³ 5000ïœãšããé ç²æ«ææãå®å šã«æ··åããéåžžã®å§çž®é å€ã®è£œ
é æè¡ã«åŸã€ãŠã0.5ïœã®ãããŒãã«å§çž®ããã ãããŒãã¯äººéã®å£è å ã«ä¿æããåŸã ã«æº¶ã
ããŸãã«ããŠäººã®å£ãšã®ã©ã®åŠçœ®ãè¡ãªãããã
ã«ããã çµæç©å®æœäŸ13 çŽè žäœ¿çšã®åè¬ ïŒå2.5ïœã®éãã§ãæ¬çºæã®æŽ»æ§ååç©100mg
ãå«æããåè¬1000åãã次ã®çš®é¡åã³éã®æå
ããã€ããã æ¬çºæã®æŽ»æ§ååç© 100ïœ ããªããã·ã³ïŒ¢ç¡«é žå¡©ïŒ10000åäœïŒmgïŒ
1.25ïœ ã¡ãã«ãã¬ãããœãã³ ïŒïœ ã¢ããå®æ¯éŠé žãšãã« 75ïœ é žåäºé 62.5ïœ ãããã¬ã³ã°ãªã³ãŒã« 162.5ïœ ããªãšãã¬ã³ã°ãªã³ãŒã«4000 2500ïœãšããé æ¬çºæã®æŽ»æ§ååç©ãããªããã·ã³ïŒ¢ç¡«é žå¡©ã
ã¡ãã«ãã¬ãããœãã³ãã¢ããå®æ¯éŠé žãšãã«å
ã³é žåäºéããããã¬ã³ã°ãªã³ãŒã«ã«å ããç²æ«
ã埮ç²ç ãããŠåäžååžããããŸã§æ··åç©ãç·Ž
ããããªãšãã¬ã³ã°ãªã³ãŒã«4000ã溶èãããã
ãã¬ã³ã°ãªã³ãŒã«åæ£æ¶²ããããŸããªããåŸã ã«
å ãããå·åŽããŠããªãéåã«40âã§æžæ¿æ¶²ã泚
ãã çµæç©ãæŸå·ããŠåºåãããéåããåãåºã
ãŠãååè¬ãç®ã§å ãã äžã®åè¬ã¯ççåã³ææã®å±æçåŠçœ®çšãšããŠ
çŽè žã«æ¿å ¥ãããã ãã®ä»£ããã«ãã¹ããã€ããçç¥ããŠäžã®çµæ
ç©ãã€ããããšãã§ããã çµæç©å®æœäŸ14 ä¹³è ºçè»ãã ä¹³çã®ä¹³è ºçåŠçœ®çšè»ãã1000ïœã次ã®çš®é¡å
ã³éã®æåããã€ããã æ¬çºæã®æŽ»æ§ååç© 25ïœ ã¡ãã«ãã¬ãããœãã³ã¢ã»ããŒã 0.5ïœ è»œè³ªæ¶²äœãããã©ã¯ã¿ã 300ïœ ç¡æ°Žã¯ãããã¿ããŒã« ïŒïœ ããªãœã«ããŒã80 ïŒïœ ïŒïŒ ã¢ãã¹ãã¢ãªã³é žã¢ã«ãããŠã âèœè±çæ²¹
ã²ã« 400ïœ çœè²ãããã©ã¯ã¿ã 1000ïœãšããé æ¬çºæã®æŽ»æ§ååç©ãšã¡ãã«ãã¬ãããœãã³ã¢
ã»ããŒããã埮ç²ç ãããŠåäžååžããããŸã§è»œ
質液äœãããã©ã¿ã ãšäžç·ã«ç·Žããã¯ãããã¿ã
ãŒã«ãããªãœã«ããŒã80ãèœè±çæ²¹ã²ã«åã³çœè²
ãããã©ã¿ã ã48.9âïŒ120ãïŒã«å ç±ããŠæº¶è
ç©ã圢æããã液äœãããã©ã¿ã åæ£æ¶²ããã®äž
ã«æ··ã蟌ããããããããŸããªãããåæ£æ¶²ã宀
æž©ãŸã§æŸå·ãåºåããã10ïœã®æåéã§äœ¿ãæšãŠ
ã®ä¹³è ºççšæ³šå°åšã«å å¡«ããã çµæç©å®æœäŸ15 åç©é£Œæ 次ã®çš®é¡åã³éã®æåãã飌æããã¯ã¹1000ïœ
ãã€ããã æ¬çºæã®æŽ»æ§ååç© 10ïœ å€§è±ç² 400ïœ é ç² 400ïœ å°éºŠèèœæ²¹ 50ïœ ããããç³è 140ïœ æåãäžç·ã«æ··åããå§çž®ããŠãã¬ããã«ã
ãããã®çµæç©ã¯ã茞éäžã®äºé²ã®ããå®éšå
ç©ãããªãã¡ã©ããããã€ãããã¿ãã¢ã«ã¢ã
ãããã ã¹ã¿ãŒã«çµŠé€ã§ããã 家犜ãäŸãã°ã«ããšãããã²ããäžé¢é³¥ãã¬ã
ãšãŠã®ãããªãã®ä»ã®åç©ã«ã¯ãæ¬çºæã®æŽ»æ§å
åç©ã®æãã§ããæäžéãäžããèšç®éã®çµæç©
ãåç©ã®é垞飌æã«æ·»å ã§ããã çµæç©å®æœäŸ 16 以äžã®çµæç©å®æœäŸïŒã15ã®åã ã®æé ã«åŸã€
ãŠãæ²»çç¹æ§ãæäŸããããã«ãæ¬çºæã®åã ã®
æè掻æ§ååç©ã¯ãå®æœäŸäžã«ç€ºãããæ¬çºæã®
掻æ§ååç©ã«å¯Ÿãããã®ãšç䟡ã®éã§ä»£æ¿ãã
ãã åæ§ã«ãäžã®éé¢å¡©åºååç©é¡ã®åã ã¯ã補è¬
åŠçã«ïŒåã¯è¬çåŠçã«ïŒåå ¥ããããé žä»å
å¡©ãäŸãã°å¡©é žå¡©ãç¡«é žå¡©ãç¡é žå¡©ãçé žå¡©ãã
ããé žå¡©ãä¹³é žå¡©ãé ¢é žå¡©ãé ç³é žå¡©ãåã³ãã¯
ãé žå¡©ã®åœ¢ã§äœ¿çšã§ããã æŽã«ãäžã®æ¬çºæã®æè掻æ§ååç©é¡ã®åã ã®
ãã®ã®ïŒâãã¹ããšãŒãåã³ïŒåã¯ïŒâãã«ãã
ãŒãã掻æ§æåãšããŠä»£ããã«äœ¿çšãããšãæ²»ç
ç¹æ§ããã€çµæç©é¡ãæäŸãããã
é°æ§åŸ®çç©ã«å¯ŸããŠæŽ»æ§ãããããããã®ãããª
埮çç©ãæå¶ãããããããŸããŸãªç°å¢ã§äœ¿çšã§
ãããäŸãã°ãé»è²ãããŠçèã§æ±æãããé£åš
ã®æŽã€ãŠç©ã¿éãããã®ã«ãã®èãæå¶ãããã
ã®æ®ºèå€ãšããŠäœ¿çšã§ããããŸããé»è²ãããŠç
èã§æ±æãããæ¯ç§åã³å»ç§çšèšåã®æ¶æ¯å€ãšã
ãŠäœ¿çšã§ãããæŽã«ãæ¬çºæååç©é¡ã¯ãæŽæ¿¯ã
ãè¡£é¡ã®éèçšãªã³ã¹å€ãšããŠããŸãçŽãç¹ç©ã®
å«æµžçšã«äœ¿çšã§ããããããã¯ãŸãããã¬ãŒãæ€
å®å¹å°ãã®ä»ã®åŸ®çç©åŠçå¹å°äžã«ãããæåæ§
èã®çè²ãæããã«ãæçšã§ããã æ¬çºæååç©é¡ã¯ç°å¢PHã«åŸã€ãŠãããã³åå
ã¯éãããã³å圢ã§ååšããããããã³ååãæ
å³ããŠããæã«ã¯ãååç©ã¯è£œè¬åŠçã«åãå ¥ã
ãããé žä»å å¡©ãšããŠååšããéãããã³ååã
æå³ããæã«ã¯ååç©ã¯éé¢å¡©åºãšããŠååšã
ããéé¢å¡©åºã¯ãé©åœãªé žã§ãããPHçŽ7.0ã«ã
奜ãŸããã¯PHçŽïŒãªããPHïŒã«äžåããããšã«ã
ã€ãŠãå®å®ãªé žä»å å¡©ã«è»¢åã§ããããã®ç®çã«
é©ããé žã¯å¡©é žãç¡«é žãçé žãããªã·ã¢ã³é žãã
ã«ãªãçªé žããããµãã«ãªãç é žããããµãã«ãª
ãçé žãé ¢é žããã¯ãé žããããé žãä¹³é žããã¬
ã€ã³é žããããŒã«é žããã¢ã€ãã¯ã¢ã·ãããã³ãŒ
ã«é žããã«ããã³é žãç²æ¶²é žãã·ãšãŠããŠé žãã°
ã«ã¿ã«é žãã°ãªã³ãŒã«é žããã¿ãŒã«é žãé ç³é žã
ã©ãŠãªã³é žãã¹ãã¢ãªã³é žããµãªãã«é žãïŒâã
ãšãã«ãµãªãã«é žãïŒâããšãã«ãµãªãã«é žãïŒ
âã¡ãã«ã°ã«ã¿ãŒã«é žããªã«ãã¹ã«ãå®æ¯éŠé žã
ã·ã¯ããããµã³ã¹ã«ãã¢ãã³é žãã·ã¯ããã³ã¿ã³
ããããªã³é žãïŒïŒïŒâã·ã¯ããããµã³ãžã«ã«ã
ã³é žãïŒâã·ã¯ããããµã³ã«ã«ãã³é žããªã¯ã¿ã
ã»ãã«ãã¯ãé žããªã¯ããã«ãã¯ãé žãã¡ã¿ã³ã¹
ã«ãã³é žãããªã¢ã³ãã³é žãã©ã€ããã±é žããžã¡
ãã«ãžããªã«ã«ããã³é žããããµãã·ã«ã¹ã«ãã¢
ãã³é žããªã¯ã¿ãã·ã«ã¹ã«ãã¢ãã³é žããœã«ãã³
é žãã¢ãã¯ããé ¢é žããŠã³ãã·ã¬ã³é žã4â²âãã
ããã·ã¢ãŸãã³ãŒã³âïŒâã¹ã«ãã³é žããªã¯ã¿ã
ã·ã«ç¡«é žããã¯ãªã³é žãå®æ¯éŠé žãæ¡ç®é žçãå
å«ããã é žä»å å¡©ã¯éé¢å¡©åºãšåãç®çã«äœ¿çšã§ãã
ããåå¡©åºã®å質åäžã®ãã䜿ãããšãã§ããã
äŸãã°éé¢å¡©åºããã¯ãªã³é žå¡©ã®ãããªæ°Žã«æº¶ã
ãªãå¡©ã«è»¢åããããã粟補æé äŸãã°æº¶åªæœåº
ãšæŽæµãã¯ãããã°ã©ãã€ãåå¥æ¶²â液æœåºãå
ã³çµæ¶åã«ããã次ã«ã¢ã«ã«ãªåŠçã«ãã€ãŠéé¢
å¡©åºåãåçããããåã¯è€å解ã«ãã€ãŠå¥ã®å¡©
ãã€ããã®ã«çšãããããåã¯éé¢å¡©åºãå¡©é žå¡©
ãç¡«é žå¡©ã®ãããªæ°Žæº¶æ§ã®å¡©ã«è»¢åããå¡©ã®æ°Žæº¶
液ãçš®ã ã®æ°Žãšæ··ãããªã溶åªã§æœåºããŠããã
æœåºæº¶æ¶²ã®åŠçã«ãã€ãŠéé¢å¡©åºåãåçãã
ããåã¯è€å解ã«ãã€ãŠå¥ã®å¡©ã«è»¢åããã äžã«æããã«ãããæèçãªçšéã®ã»ããéé¢
å¡©åºã¯ç·©è¡æãšããŠåã¯å¶é žå€ãšããŠäœ¿çšã§ã
ããåè¡åœç¹èš±ç¬¬2425320å·åã³ç¬¬2606155å·ã«ã
ãã°ãããªã·ã¢ã³é žä»å å¡©ã¯ãã«ã ã¢ã«ããããš
çž®åããããšé žæŽæµæå¶å€ãšããŠæçšãªæš¹èç¶æ
æã圢æãããéé¢å¡©åºãææ¯ãªé žã«å¯Ÿããè¯å¥œ
ãªè³Šåœ¢å€ãšãªããäŸãã°åè¡åœç¹èš±ç¬¬1915334å·
ãšç¬¬2075359å·ã«ããã°ããã«ãªãçªé žä»å å¡©ã¯
é²èŸå€ãšããŠæçšã§ããããŸãåè¡åœç¹èš±ç¬¬
3122536å·ãšç¬¬3122552å·ã«ããã°ããããµãã«ãª
ãç é žãšãããµãã«ãªãçé žã®ä»å å¡©ã¯å¯çè«æ²
æ» å€ãšããŠæçšã§ããã æ¬çºæååç©é¡ã¯ãé©åœãªçµæç©ã®åœ¢ã®æèå€
ãšããŠæçšã§ããããããã®çµæç©ã¯ãéé¢å¡©åº
åã¯è¬åŠçã«åå ¥ãããããã®å¡©é¡ã®åœ¢ã®æŽ»æ§å
åç©ã®é©åœéãå«æããé å€ãã«ãã»ã«ãäžžè¬ã
ç²æ«ãç²å€ãç¡èã®éçµå£æº¶æ¶²åã¯æžæ¿æ¶²ãåã³
çµå£æº¶æ¶²åã¯æžæ¿æ¶²ãåã³æ²¹âæ°Žä¹³æ¿æ¶²ã®ãããª
åäœé©é圢åŒã§äººéãšåç©ãžæäžããããã«æäŸ
ãããã®ã奜ãŸããã çµå£æäžã«ã¯ãåºäœåã¯æµäœã®åäœæäžé圢åŒ
ãã€ããããšãã§ãããé å€ã®ãããªåºäœçµæç©
ãã€ããã«ã¯ãåºæ¬æŽ»æ§æåã補è¬åŠçåžéå€å
ã¯æ äœãšããŠã®æ»ç³ãã¹ãã¢ãªã³é žãã°ãã·ãŠ
ã ãçé žäºã«ã«ã·ãŠã ãçªé žã¢ã«ãããŠã ãã°ã
ã·ãŠã ãç¡«é žã«ã«ã·ãŠã ã殿ç²ãä¹³é ãã¢ã©ãã¢
ãŽã ãã¡ãã«ã»ã«ããŒã¹ãåã³æ©èœäžåæ§ãªææ
çã®æ £çšæåãšæ··åãããäœçšãé·ã³ããããé
ããããããå©ç¹ãæã¯å°å ¥è¬ç©ãæå®ã®é åºã§
äœçšãããå©ç¹ãåããæäžéåäœãæäŸããã
ããé å€ãç©å±€ããããåã¯å¥ã®åœ¢ã§ã³ã³ããŠã³
ãããããšãã§ãããäŸãã°ãé å€ãå åŽã®é©é
ãšå€åŽã®é©éæåãããªããåŸè ãåè ãå ã圢
ã«ã§ãããïŒæåãè žæº¶ç®å±€ã«ãã€ãŠåé¢ããã
ã®å±€ã«èå ã§ã®åŽ©å£ã«èããŠå åŽæåãåäºæè ž
ãžç¡å·ã®ãŸãŸééããããããŸãã¯æŸåºãé ãã
ãããã圹ç®ãè¡ãªãããããšãã§ããããã®ã
ããªè žæº¶ç®èã被èŠã«ã¯ãå€æ°ã®éåäœã®é žãå
ã¯éåäœã®é žãšã»ã©ãã¯ãã»ãã«ã¢ã«ã³ãŒã«ãã»
ã«ããŒã¹ã»ã¢ã»ããŒãã»ãã¿ã¬ãŒããã¹ãã¬ã³â
ãã¬ã€ã³é žå ±éåäœçã®ãããªææãšã®æ··åç©ã
å«ããçš®ã ã®ææã䜿çšã§ããã®ä»£ããã«ãäºã€
ãªãããã以äžã®çžå®¹ããªã掻æ§æåãå«æãã
é å€ã®è£œé ã«äºæåç³»ãå©çšã§ãããé å€ãšåã
æ¹æ³ã§ãŠãšãã¢ãŒã¯ã€ãããããã圢ã庶ç³ãã®
ä»ã®çå³å€ãšé¢šå³æãå«ãŸããŠããç¹ãç°ãªãã®
ã¿ã§ãããæãç°¡åãªæ æ§ã®å Žåãã«ãã»ã«ã¯é
å€ã®ããã«ãåŠæ¹å€ã®ååç©ãäžæŽ»æ§ãªè£œè¬åŠç
åžéå€ãšæ··åããé©åœãªå€§ããã®ç¡¬ããŒã©ãã³ã«
ãã»ã«ãžæ··åç©ãå å¡«ããããšã§ã€ãããããå¥
ã®æ æ§ã§ã¯ã掻æ§ååç©ãå«æããéåäœé žã®è¢«
èŠããŒãºã硬ããŒã©ãã³ã«ãã»ã«ã«è©°ããããšã«
ãã€ãŠã«ãã»ã«å€ãã€ãããè»ããŒã©ãã³ã«ãã»
ã«ã¯ã掻æ§æåãšåãå ¥ããããæ€ç©æ²¹ã軜質液
äœãããã©ã¯ã¿ã åã¯ãã®ä»ã®äžæŽ»æ§æ²¹ãšã®ã¹ã©
ãªãŒã®æ©æ¢°ã«ããã«ãã»ã«å°å ¥ã«ãã€ãŠã€ããã
ãã ã·ãããå€ããšãªããžãŒã«å€åã³æžæ¿æ¶²ã®ãã
ãªçµå£æäžåãã®æµäœåäœæäžé圢åŒãã€ããã
ãšãã§ããã掻æ§ååç©ã®æ°Žæº¶åã®ãã®ã¯ç ç³ã
è³éŠæ§é¢šå³æåã³é²è å€ãšå ±ã«æ°Žæ§è³Šåœ¢å€äžã«æº¶
解ããããšã·ãããå€ãã§ããããšãªããžãŒã«å€
ã¯ãè³éŠæ§é¢šå³æãšå ±ã«ç ç³ã®ãããªé©åœãªçå³
æãå ããæ°Žâã¢ã«ã³ãŒã«ïŒãšã¿ããŒã«ïŒã®è³Šåœ¢
å€ã䜿çšããŠã€ãããããæžæ¿æ¶²ã¯ãã¢ã©ãã¢ãŽ
ã ããã©ã¬ã«ã³ããŽã ãã¡ãã«ã»ã«ããŒã¹çã®ã
ããªæžæ¿å€ã®å©ããåããŠãã·ãããçšè³Šåœ¢å€ã«
ããäžæº¶æ§åã«ã€ããããšãã§ããã å±æçšè»ããã¯ããããã©ã¿ã ãã©ããªã³ãã
ãªãšãã¬ã³ã°ãªã³ãŒã«ããããã®æ··åç©çã®é©åœ
ãªè»ããåºæäžã«æŽ»æ§ååç©ãåæ£ãããããšã«
ãã€ãŠã€ãããããè»ããåºæã«åæ£ãããåã«
è»è³ªæ¶²äœãããã©ã¿ã ã磚ç ç©ãšããŠå©çšããã³
ãã€ããã«ã«ãããååç©ã埮ç²ç ããã®ãæå©
ã§ãããå±æçšã¯ãªãŒã åã³ããŒã·ãšã³ã¯ãæ°Žäž
ã«æ²¹çžãä¹³åãããåã«ãæ²¹çžã«ååç©ãåæ£ã
ããããšã«ãã€ãŠã€ããããã éçµå£æäžã«ã¯ãæµäœã®åäœæäžé圢åŒã¯ã掻
æ§ååç©ãšç¡è賊圢å€ïŒæ°Žã奜é©ïŒãå©çšããŠã€
ããããã掻æ§ååç©ã¯ã䜿çšåœ¢åŒåã³æ¿åºŠã«ã
ãããã賊圢å€äžã«æžæ¿ãããããåã¯æº¶è§£ãã
ãããšãã§ããã溶液ãã€ããã«ã¯ã掻æ§ååç©
ã®æ°Žæº¶æ§åã泚å°çšæ°Žã«æº¶è§£ããé©åœãªå°ã³ãå
ã¯ã¢ã³ãã«ã«å å¡«ãå°å ¥ããåã«ãéæ» èããã
å±æ麻é å€ãé²è å€åã³ç·©è¡å€ã®ãããªå©å€ã賊
圢å€äžã«æº¶è§£ããã®ãæå©ã§ãããå®å®æ§ãé«ã
ããããå°ã³ãã«å å¡«åŸãçµæç©ãåçµããç空
äžã§æ°Žãé€å»ãããåçµä¹Ÿç¥ããç²æ«ãå°ã³ãäž
ã«å°å ¥ãã䜿çšçŽåã«æº¶æ¶²ãåæ§æããããæ·»ã
ã泚å°çšæ°Žã®å°ã³ããè£å ãããéçµå£æžæ¿æ¶²ã¯
å®è³ªçã«åãæ¹æ³ã§ã€ããããããäœã掻æ§åå
ç©ã溶解ãã代ããã«è³Šåœ¢å€äžã«æžæ¿ããããé
ã«ããæ» èã¯ã§ããªããç¡èã®è³Šåœ¢å€äžã«æžæ¿ã
ãåã«ã掻æ§ååç©ã¯é žåãšãã¬ã³ã«åœãŠãŠæ» è
ããã掻æ§ååç©ã®åäžååžã容æã«ããããã
çµæç©äžã«è¡šé¢æŽ»æ§å€åã¯æ¹¿æœ€å€ãå«ããã®ãæ
å©ã§ããã æ¬æ现æžåã³ç¹èš±è«æ±ã®ç¯å²ã§äœ¿ãããçšèªã®
åäœæäžéïŒé©éïŒåœ¢åŒãšã¯ã人éã®æ£è åã³å
ç©çšã«åäœæäžéãšããŠé©ããç©ççã«ã°ãã°ã
ã«ãªã€ãåäœã®ããšã§ãããååäœã¯å¿ èŠãªè£œè¬
åŠçåžéå€ãæ äœåã¯è³Šåœ¢å€ãšå ±åããŠæãã§ã
ãæ²»çå¹æãçããããã«èšç®ãããæå®éã®æŽ»
æ§ææãå«æãããæ¬çºæã®æ°èŠãªåäœæäžé圢
åŒã®æ现ã¯ã(a)掻æ§ææã®ãã°ãããæ§è³ªãšãé
æããããšããç¹å®ã®æ²»çå¹æãåã³(b)æ¬æ现æž
ã§è©³çŽ°ã«æããã«ãããŠããããã«ã人éåã³å
ç©ãžã®æ²»ççšã«ãã®ãããªæŽ»æ§ææãã³ã³ããŠã³
ãããæè¡ã«åºæã®å¶éã«ãã€ãŠæå³ãããã€çŽ
æ¥ãããã«ãã€ãŠãããããããã®ä»æ§ã¯æ¬çºæ
ã®ç¹åŸŽã§ãããæ¬çºæã«åŸãé©åœãªåäœæäžé圢
åŒã®äŸã¯ãé å€ãã«ãã»ã«ãäžžè¬ããããŒããå
è¬ãç²æ«è¬å ãç²å€ããŠãšãã¢ãŒãã«ã·ãšãè¶ãµ
ãžéã倧ãµãžéã滎ã³ãéãã¢ã³ãã«ãå°ã³ãã
以äžã®ä»»æã®ãã®ã®å¥ã ã®è€æ°äœ¿çšãåã³æ¬æ现
æžã«èšèŒã®ãã®ä»ã®åœ¢åŒã§ããã æ¬æ现æžã«èšèŒã®çç¶ã®åŠçœ®çšã«çµæç©ã®äž»æŽ»
æ§æåãšããŠãã®æŽ»æ§ååç©ãæäžããã»ããæ
å©ãªçµåãã®æ§ç¶ãåŸãããããã®ã³ã³ããŠã³ã
ã«ä»ã®çš®é¡ã®ååç©ãå«ããããšãã§ããããã®
ãããªçµåãã¯ãæ¬æŽ»æ§ååç©ãšå ±ã«ãã¹ãã¯ã
ããã€ã·ã³ãã¯ãã©ã ããšãã³ãŒã«ãããããªã·
ã³ããžããããããªã·ã³ãããã©ãµã€ã¯ãªã³é¡
ïŒäŸãã°ããã©ãµã€ã¯ãªã³ããªãã·ããã©ãµã€ã¯
ãªã³ãåã³ã¯ãã«ããã©ãµã€ã¯ãªã³ïŒãããã·ãª
ã³é¡ããšãªã¹ããã€ã·ã³ãã«ããã€ã·ã³ãã¹ãã¬
ãããã€ã·ã³ãããªãã€ã·ã³ãããªããã·ã³ãã
ã·ãã©ã·ã³ããã¹ã¿ãã³ããã€ãªãã³ãããã®ãª
ã³åã³ãšã³ããã€ã·ã³ã®ãããªãçµæç©ã®æèã¹
ãã¯ãã«ãåºããç¹å®çŽ°èã«å¯Ÿããçžä¹äœçšãã
ã€æçç©è³ªé¡ïŒãã€ããã³ã«ããŸãŒã³ããã¬ãã
ãœãã³ã6αâã¡ãã«ãã¬ãããœãã³ã6αâãã«
ãªããã¬ãããœãã³çã®ãããªæçç掻æ§ããã€
ã¹ããã€ãé¡ïŒã¢ã¹ããªã³ããµãªãã«é žãããªãŠ
ã ïŒã¢ã»ãã«ãµãªãã«é žïŒç¡æ°Žç©ãâã¢ã»ãã«
âïœâã¢ããããšãã«åã³ãµãªãã«ã¢ããã®ãã
ãªé®çå€ïŒã¯ããããšãã©ãã³ãã¬ãšãŒãããžã
ãšãã«ããã©ãã³ãããã¡ã¿ãžã³ããã©ãã¢ãžã³
çã®ãããªæãã¹ã¿ãã³å€ïŒãµã«ãã¢ãžã¢ãžã³ã
ã«ãã¢ã¡ã¿ãžã³ããµã«ãã¢ã¡ã©ãžã³ããµã«ãã¢ã»
ã¿ããããµã«ãã¢ãžã¡ããããµãŸãŒã«ããµã«ãã¢
ã¡ããŸãŒã«çã®ãããªãµã«ãã¢å€ïŒãŠã³ãã·ã¬ã³
é žãããããªã³é žãããªãŠã ããµãªãã«ã¢ããª
ããã«ããªã«é žãããªãŠã åã³ããã»ããžã³ã®ã
ããªé²ã«ãå€ïŒåã³ãã¿ãã³å€ãå å«ããã 掻æ§ååç©ã®æ²»çã«ãããé©éã¯ãæäžåŸè·¯ã
æ£è ã®å¹Žä»€ãäœéãçç¶ãåã³åŠçœ®ããç¹å®ã®ç
æ°ã«ãã€ãŠæ±ºãŸããçŽ15ã500mgã§ïŒæ¥ïŒãïŒå
ïŒïŒæéæ¯ïŒã®æäžéèšç»ã¯ãçµæç©ãæå¹ã§ã
ãã»ãšãã©ã®çç¶ã®åŠçœ®ã«å¯ŸããŠæå¹ãªç¯å²ãå
å«ããŠãããå°å ã«ã¯ãïŒæ¥Kgåœã15ã30mgã®åº
ç€ã§èšç®ãããæäžéããïŒæéæ¯ã«æäžããã 奜éœåãªåå¹æçãªæäžã®ãããåäœé©é圢åŒ
ã«ããŠæŽ»æ§ååç©ãé©åœãªè£œè¬åŠçæ äœãšã³ã³ã
ãŠã³ããããæ¬çºæã®å¥œãŸããæ æ§ã§ã¯ãé©éå
äœã¯å šèº«çåŠçœ®çšã«15ïŒ30ïŒ50ïŒ125ïŒ250åã³
500mgã§ãããå±æåŠçœ®çšã«ã¯0.25ïŒ0.5ïŒïŒïŒïŒ
åã³ïŒïŒ éã§ããããŸãéçµå£æäžçšã«ã¯ïŒã65
ïŒ ïŒïœïŒïœïŒã®ååç©ãå«æãããæ¬æŽ»æ§ååç©
ãšäžçš®åã¯ãã以äžã®ãã®ä»æŽ»æ§æåãå«æãã
çµæç©é¡ã®æäžéã¯ããã®ãããªåæåã®éåžžæ
äžéãåç §ããªãã決å®ãããã¹ãã§ããã 以äžã®å®æœäŸã¯æ¬çºæãå®æœãããããšæ¬çºæ
è ãèããæãããæ æ§ã®äŸç€ºã§ããããéå®ç
ã«èããããŠã¯ãªããªãã çµæç©å®æœäŸïŒ ã«ãã»ã« ïŒååœãæ¬çºæã®æŽ»æ§ååç©250mgãå«æãã
çµå£çšã®ç¡¬ãäºæ®»ãŒã©ãã³ã«ãã»ã«1000åãã次
ã®çš®é¡åã³éã®ææããã€ããã æ¬çºæã®æŽ»æ§ååç© 250ïœ ãšãããããæ®¿ç² 100ïœ æ» ç³ 75ïœ ã¹ãã¢ãªã³é žãã°ãã·ãŠã 25ïœ ææãå®å šã«æ··åããéåžžã®æ¹æ³ã§ã«ãã»ã«å
ããã äžã®ã«ãã»ã«ã¯ïŒæéæ¯ã«ïŒã«ãã»ã«ã®çµå£æ
äžã§æ人ã®å šèº«çææåŠçœ®ã«æå¹ã§ããã äžã®æé ã䜿çšããŠãäžèšã®250ïœã®ä»£ããã«
15ïŒ30ïŒ50ïŒ125åã³500ïœã®æ¬çºæã®æŽ»æ§ååç©
ã䜿çšããŠã15ïŒ30ïŒ50ïŒ125åã³500mgã®æ¬çºæ
ã®æŽ»æ§ååç©ãå«æããã«ãã»ã«ãåãããã«ã€
ããããã çµæç©å®æœäŸïŒ ã«ãã»ã« ïŒååœãæ¬çºæã®æŽ»æ§ååç©200mgãšããã©ãµ
ã€ã¯ãªã³å¡©é žå¡©250mgãå«æããçµå£çšã®ç¡¬ãäº
æ®»ãŒã©ãã³ã«ãã»ã«1000åã次ã®çš®é¡åã³éã®æ
åããã€ããã æ¬çºæã®æŽ»æ§ååç© 200ïœ ããã©ãµã€ã¯ãªã³å¡©é žå¡© 250ïœ æ» ç³ 75ïœ ã¹ãã¢ãªã³é žãã°ãã·ãŠã 25ïœ æåãå®å šã«æ··åãã次ã«éåžžã®æ¹æ³ã§ã«ãã»
ã«åããã äžã®ã«ãã»ã«ã¯ãïŒæéæ¯ã«ïŒã«ãã»ã«ã®çµå£
æäžã§æ人ã®å šèº«çææåŠçœ®ã«æçšã§ããã äžã®æé ã䜿çšããŠãããã©ãµã€ã¯ãªã³ã®ä»£ã
ã«ã¯ãã©ã ããšãã³ãŒã«ããªãã·ããã©ãµã€ã¯ãª
ã³ãã¯ãã«ããã©ãµã€ã¯ãªã³ãããã®ãªã³ããšã¯
ã¹ããã€ã·ã³ãã¹ãã¬ãããã€ã·ã³ããžãããã
ãããªã·ã³ãåã³ããããªã·ã³250ïœã䜿çšããŠã
æ¬çºæã®æŽ»æ§ååç©ãšãããã®æçç©è³ªã®åã ã
å«æããã«ãã»ã«ãåãããã«ã€ããããã ããã©ãµã€ã¯ãªã³ã®ä»£ããã«ã«ãªãŠã ããã·ãª
ã³ïŒ§ã®ãããªããã·ãªã³ã䜿çšããæã«ã¯ãã«ã
ã»ã«åœã250000åäœã䜿çšããã ãã®ãããªçµåãçæç©ã¯ãïŒæéæ¯ã«ïŒã«ã
ã»ã«ã®çµå£æäžã«ãã€ãŠæ人ã®æ··åææã®å šèº«ç
åŠçœ®ã«æçšã§ããã çµæç©å®æœäŸïŒ é å€ ïŒé åœãæ¬çºæã®æŽ»æ§ååç©500mgãå«æãã
çµå£çšé å€1000åã次ã®çš®é¡åã³éã®ææããã€
ããã æ¬çºæã®æŽ»æ§ååç© 500ïœ ä¹³ ç³ 125ïœ ãšãããããæ®¿ç² 65ïœ ã¹ãã¢ãªã³é žãã°ãã·ãŠã 25ïœ è»œè³ªæ¶²äœãããã©ã¯ã¿ã ïŒïœ æåãå®å šã«æ··åããã¹ã©ãã°ã«ãããã¹ã©ã
ã°ã¯16çªã®ãµããã匷å¶ééãããŠç Žå£ãããç
ããé¡ç²ãé å€ã«å§çž®ããïŒé åœãæ¬çºæã®æŽ»æ§
ååç©500mgãå«æããé å€ã«å§çž®ããã äžã®é å€ã¯ãïŒæéæ¯ã«ïŒé ã®çµå£æäžã«ãã
æ人ã®å šèº«çææåŠçœ®ã«æçšã§ããã æ¬çºæã®æŽ»æ§ååç©ã®éã250ïœã«æžãã以å€
ã¯äžã®æé ã䜿çšããŠãæ¬çºæã®æŽ»æ§ååç©250
mgãå«æããé å€ãã€ããããã çµæç©å®æœäŸïŒ é å€ ïŒé åœãæ¬çºæã®æŽ»æ§ååç©250mgãšãµã«ãã¢
ãžã¢ãžã³ããµã«ãã¢ã¡ã©ãžã³åã³ãµã«ãã¢ã¡ã¿ãž
ã³èš250mgïŒå83.3mgïŒãå«æããçµå£é å€1000
é ãã次ã®çš®é¡åã³éã®ææããã€ããã æ¬çºæã®æŽ»æ§ååç© 250ïœ ãµã«ãã¢ãžã¢ãžã³ 83.3ïœ ãµã«ãã¢ã¡ã©ãžã³ 83.3ïœ ãµã«ãã¢ã¡ã¿ãžã³ 83.3ïœ ä¹³ ç³ 50ïœ ãšãããããæ®¿ç² 50ïœ ã¹ãã¢ãªã³é žã«ã«ã·ãŠã 25ïœ è»œè³ªæ¶²äœãããã©ã¿ã ïŒïœ æåãå®å šã«æ··åãã¹ã©ãã°åãããã¹ã©ãã°
ã¯16çªãµããã匷å¶ééãããŠç Žå£ãããçãã
é¡ç²ããæ¬çºæã®æŽ»æ§ååç©250mgãšãµã«ãã¢ãž
ã¢ãžã³ããµã«ãã¢ã¡ã©ãžã³ãåã³ãµã«ãã¢ã¡ã¿ãž
ã³èš250mgïŒå83.3mgïŒãå«æããé å€ã«å§çž®ã
ãã äžã®é å€ã¯ãŸãïŒé ãçµå£æäžãã次ã«ïŒæé
æ¯ã«ïŒé ã®æäžã«ããå šèº«çææåŠçœ®ã«æçšã§ã
ãã æ³å°¿åšææã®åŠçœ®ã«ã¯ãäžã®åŠæ¹å€ã®äžã€ã®ãµ
ã«ãã¢å€ã®ä»£ããã«ããµã«ãã¢ã¡ãã«ãã¢ãžã¢ãŸ
ãŒã«250ïœåã¯ãµã«ãã¢ã»ã¿ãã250ïœã䜿çšãã
ã®ãæå©ã§ããã çµæç©å®æœäŸïŒ çµå£ã·ãããå€ ååïŒc.c.æäžéäžã«ãµã«ãã¢å€åèš0.5ïœãšæ¬
çºæã®æŽ»æ§ååç©250mgãå«æããçµå£çšæ°Žæ§æž
æ¿æ¶²1000c.c.ã次ã®çš®é¡åã³éã®æåããã€ããã æ¬çºæã®æŽ»æ§ååç© 50ïœ ãµã«ãã¢ãžã¢ãžã³ 33.3ïœ ãµã«ãã¢ã¡ã©ãžã³ 33.3ïœ ãµã«ãã¢ã¡ã¿ãžã³ 33.3ïœ ãããé ž ïŒïœ å®æ¯éŠé ž ïŒïœ 庶 ç³ 700ïœ ãã©ã¬ã«ã³ã ïŒïœ ã¬ã¢ã³æ²¹ ïŒc.c. è±ã€ãªã³æ°Ž 1000c.c.ãšããé 溶液850c.c.ã«ããã«è¶³ãéã®æ°Žã«ãããé žãå®
æ¯éŠé žã庶ç³ããã©ã¬ã«ã³ãåã³ã¬ã¢ã³æ²¹ãåæ£
ããããæ¬çºæã®æŽ»æ§ååç©ãšåŸ®ç²ç ãµã«ãã¢å€
ããåäžã«ååžããããŸã§ã·ãããäžã§ãããŸã
ããå šéã1000c.c.ã«ããã®ã«ååãªæ°Žãå ããã ããããŠã€ããããçµæç©ã¯ãïŒæ¥ã«ïŒåè¶ãµ
ãžïŒæ¯ãã€ã®æäžéã§ãæ人ã®èºçã®å šèº«çåŠçœ®
ã«æçšã§ããã çµæç©å®æœäŸïŒ éçµå£æº¶æ¶² ïŒc.c.äžã«æ¬çºæã®æŽ»æ§ååç©200mgãå«æãã
çèå 䜿çšã®ç¡è氎溶液ã次ã®çš®é¡åã³éã®ææ
ããã€ããã æ¬çºæã®æŽ»æ§ååç© 200ïœ ãªãã«ã€ã³å¡©é žå¡© ïŒïœ ã¡ãã«ãã©ãã³ 2.5ïœ æ³šå°çšæ°Ž 1000c.c.ã«ããé æåãæ°Žã«æº¶è§£ãããéã«ãã€ãŠæº¶æ¶²ãæ» èã
ããç¡è溶液ãå°ã³ãã«å å¡«ããå°ã³ããå¯å°ã
ãã çµæç©å®æœäŸïŒ éçµå£èª¿è£œå€ ïŒc.c.äžã«æ¬çºæã®æŽ»æ§ååç©200mgãšã¹ãã¯ã
ããã€ã·ã³ç¡«é žå¡©400mgãå«æããçèå 䜿çšã®
ç¡è氎溶液ã次ã®çš®é¡åã³éã®æåããã€ããã æ¬çºæã®æŽ»æ§ååç© 200ïœ ã¹ãã¯ãããã€ã·ã³ç¡«é žå¡© 400ïœ ä¹³ é 50ïœ æ³šå°çšæ°Ž 1000c.c.ãšããé æ¬çºæã®æŽ»æ§ååç©ãã¹ãã¯ãããã€ã·ã³ç¡«é ž
å¡©åã³ä¹³é ãæ°Žã«æº¶è§£ãã溶液ããéã«ãã€ãŠæ»
èãããïŒc.c.ã®éã§æ» è溶液ãç¡èçãªå°ã³ãã«
ç¡èçã«å å¡«ããåçµããããé«ç空äžã§æ°Žãé€
å»ããåçµä¹Ÿç¥ããç²æ«ã®å ¥ã€ãå°ã³ããå°å ¥ã
ãã䜿çšçŽåã«æº¶æ¶²ïŒc.c.ãã€ãã泚å°çšç¡èæ°Žã®
ååéãå°ã³ãã«å ããã çµæç©å®æœäŸïŒ å±æçšè»ãã 0.25ïŒ ã®è»ãã1000ïœã次ã®çš®é¡åã³éã®æå
ããã€ããã æ¬çºæã®æŽ»æ§ååç© 2.5ïœ é žåäºé 50ïœ ã«ã©ãã³ 50ïœ æ¶²äœãããã©ã¿ã ïŒééïŒ 250ïœ çŸ è 200ïœ çœè²ãããã©ã¿ã 1000ïœãšããé çœè²ãããã©ã¿ã ãšçŸèã溶èãã液äœããã
ã©ã¿ã 100ïœãããã«å ãããæ¬çºæã®æŽ»æ§åå
ç©ãé žåäºéåã³ã«ã©ãã³ãæ®ãã®æ¶²äœãããã©
ã¿ã ã«å ããç²æ«ã埮ç²ç ãããŠåäžååžããã
ãŸã§æ··åç©ãç²ç ãããç²æ«æ··åç©ãçœè²ããã
ã©ã¿ã æ··åç©äžã«ãããŸããè»ãããåºãŸããŸã§
ãããŸããç¶ããã äžã®è»ããã¯ãææã®åŠçœ®çšã«åºä¹³é¡ã®ç®èã«
å±æçã«å¡åžãããšæçšã§ããã äžã®çµæç©ã¯ãé žåäºéãšã«ã©ãã³ãçç¥ããŠ
ã€ããããšãã§ããã äžã®æé ã«åŸã€ãŠãäžã§çšãã25ïœã®ä»£ããã«
æ¬çºæã®æŽ»æ§ååç©ã®ïŒïŒ10ïŒ20åã³50ïœã䜿çš
ããŠã0.5ïŒïŒïŒïŒïŒåã³ïŒïŒ ã®éã®æ¬çºæã®æŽ»
æ§ååç©ãå«æããè»ãããåãããã«ã€ããã
ãã çµæç©å®æœäŸïŒ ã¯ãªãŒã è çšã¯ãªãŒã 1000ïœã次ã®çš®é¡åã³éã®æåã
ãã€ããã æ¬çºæã®æŽ»æ§ååç© 50ïœ ãã¬ã·ããã»ã¬ã®ãŠã©ãŒ1) 150ïœ é¯šãã 100ïœ ãããã¬ã³ã°ãªã³ãŒã« 50ïœ ããªãœã«ããŒã80 ïŒïœ ã¡ãã«ãã©ãã³ ïŒïœ è±ã€ãªã³æ°Ž 1000ïœãšããé ïŒ ãŽãŒã«ãã·ãŠãããã»ã±ãã«ã«ã»ã³ãŒãã¬ãŒ
ã·ãšã³ïŒããŠãŒãšãŒã¯å·ããŠãŒãšãŒã¯ïŒããã®
èªå·±ä¹³åããã°ãªã»ãªã«ã»ã¢ãã¹ãã¢ã¬ãŒãã ãã¬ã·ãããšé¯šããã70ã80âã®æž©åºŠã§äžç·ã«
溶èãããæ°ŽçŽ500ïœã«ã¡ãã«ãã©ãã³ã溶解ãã
ãããã¬ã³ã°ãªã³ãŒã«ãããªãœã«ããŒã80ãåã³
æ¬çºæã®æŽ»æ§ååç©ãé ã ã«å ãã75ã80âã®æž©
床ãä¿ã€ãã¡ãã«ãã©ãã³æ··åç©ããã¬ã·ãããš
鯚ãããšã®æº¶èç©ã«ãäžå®ã«ãããŸããªããåŸã
ã«å ãããããããããŸããªããã枩床ã40ã45
âã«äœäžãããŸã§ãå°ãªããšã30åéæ·»å ãç¶ã
ããæ°ŽçŽ50ïœã«æº¶è§£ãããããé ž2.5ïœãšäºå¡©åº
æ§çé žãããªãŠã 0.2ïœãæ··å ¥ããããšã«ãã€ãŠã
æçµçãªã¯ãªãŒã ã®PHã3.5ã«èª¿æŽãããæåŸã«ã
æçµééã1000ïœã«ãã€ãŠããååéã®æ°Žãå
ãã調補å€ãå·åŽããŠåºãŸããŸã§å質ã«ä¿ã€ãã
ã«ãããŸããã äžã®çµæç©ã¯äººéã®è å ææã®åŠçœ®ã«æçšã§ã
ãã çµæç©å®æœäŸ10 çŒç§çšè»ãã 0.5ïŒ æ¬çºæã®æŽ»æ§ååç©ãå«æããçŒç§çšè»
ãã1000ïœã次ã®çš®é¡åã³éã®æåããã€ããã æ¬çºæã®æŽ»æ§ååç© ïŒïœ ãã·ãã©ã·ã³ 12.2ïœ ããªããã·ã³ïŒ¢ç¡«é žå¡©ïŒ10000åäœïŒmgïŒ
ïŒïœ 軜質液äœãããã©ã¿ã 250ïœ çŸ è 200ïœ çœè²ãããã©ã¿ã 1000ïœãšããé 空æ°åŒè¶ 埮ç²ç æ©ã«ãã€ãŠåºäœæåã埮ç²ç
ãã軜質液äœãããã©ã¿ã ã«å ãããæ··åç©ãã³
ãã€ããã«ã«ãããŠåŸ®ç²ç ç²åãåäžååžãã
ããçŸèãšçœè²ãããã©ã¿ã ãäžç·ã«æº¶èããã
ãããããŠæž©åºŠã45ã50âã«èª¿æŽããã液äœãã
ãã©ã¿ã ã®ã¹ã©ãªãŒãå ããåºãŸããŸã§è»ããã
ãããŸãããïŒãã©ã ïŒ3.9ïœïŒã®çŒç§çšããŠãŒ
ãã«è»ãããå è£ ããã®ãé©ããŠããã äžã®è»ããã¯ã人éãã®ä»ã®åç©ã®å±æææã®
åŠçœ®ã®ããçŒã«æçšã«é©çšãããã äžã®çµæç©ã¯ççã®åŠçœ®çšã«ã¡ãã«ãã¬ãããœ
ãã³ïŒïœïŒ0.5ïŒ ïŒãå«æããã®ãæå©ã§ãããã
ãã®ä»£ããã«ãã·ãã©ã·ã³ãšããªããã·ã³ïŒ¢ç¡«é ž
å¡©ãçç¥ã§ããã çµæç©å®æœäŸ11 ç¹çŒå€ïŒè³æ»Žå€ ïŒc.c.åœãæ¬çºæã®æŽ»æ§ååç©10mgãšã¡ãã«ãã¬
ãããœãã³ïŒmgãå«æããçŒåã¯è³çšã®ç¡èçæ°Ž
溶液1000c.c.ãã次ã®çš®é¡åã³éã®æåããã€ã
ãã æ¬çºæã®æŽ»æ§ååç© 10ïœ ã¡ãã«ãã¬ãããœãã³çé žãããªãŠã ïŒïœ ãããé žãããªãŠã 4.5ïœ éäºç¡«é žãããªãŠã ïŒïœ ããªãšãã¬ã³ã°ãªã³ãŒã« 4000 120ïœ ããªã¹ãã«âγâãã³ãªããŠã ã¯ãã©ã€ã
0.2ïœ ããªããã«ãããªãã³ ïŒïœ è±ã€ãªã³æ°Ž 1000c.c.ãšããé æåãæ°Žã«æº¶è§£ããçãã溶液ããéã«ãã€ãŠ
æ» èããã溶液ãç¡èã®æ»Žã³ã容åšã«ç¡èçã«å
å¡«ããã ããããŠã€ããããçµæç©ã¯ãçŒãšè³ã䞊ã³ã«
åç©ã®èº«äœã®ãã®ä»ã®ææãªçµç¹ã®ççåã³ææ
ã®å±æåŠçœ®ã«æçšã§ããã çµæç©å®æœäŸ12 ãããŒã 次ã®çš®é¡åã³éã®æåãããããŒã10000åã
ã€ããã æ¬çºæã®æŽ»æ§ååç© 100ïœ ããªãã€ã·ã³ç¡«é žå¡© 50ïœ ããªããã·ã³ïŒ¢ç¡«é žå¡©ïŒ10000åäœïŒmgïŒ
ïŒïœ ã¢ããå®æ¯éŠé žãšãã« 50ïœ ã¹ãã¢ãªã³é žã«ã«ã·ãŠã 150ïœ ç²æ«åº¶ç³ 5000ïœãšããé ç²æ«ææãå®å šã«æ··åããéåžžã®å§çž®é å€ã®è£œ
é æè¡ã«åŸã€ãŠã0.5ïœã®ãããŒãã«å§çž®ããã ãããŒãã¯äººéã®å£è å ã«ä¿æããåŸã ã«æº¶ã
ããŸãã«ããŠäººã®å£ãšã®ã©ã®åŠçœ®ãè¡ãªãããã
ã«ããã çµæç©å®æœäŸ13 çŽè žäœ¿çšã®åè¬ ïŒå2.5ïœã®éãã§ãæ¬çºæã®æŽ»æ§ååç©100mg
ãå«æããåè¬1000åãã次ã®çš®é¡åã³éã®æå
ããã€ããã æ¬çºæã®æŽ»æ§ååç© 100ïœ ããªããã·ã³ïŒ¢ç¡«é žå¡©ïŒ10000åäœïŒmgïŒ
1.25ïœ ã¡ãã«ãã¬ãããœãã³ ïŒïœ ã¢ããå®æ¯éŠé žãšãã« 75ïœ é žåäºé 62.5ïœ ãããã¬ã³ã°ãªã³ãŒã« 162.5ïœ ããªãšãã¬ã³ã°ãªã³ãŒã«4000 2500ïœãšããé æ¬çºæã®æŽ»æ§ååç©ãããªããã·ã³ïŒ¢ç¡«é žå¡©ã
ã¡ãã«ãã¬ãããœãã³ãã¢ããå®æ¯éŠé žãšãã«å
ã³é žåäºéããããã¬ã³ã°ãªã³ãŒã«ã«å ããç²æ«
ã埮ç²ç ãããŠåäžååžããããŸã§æ··åç©ãç·Ž
ããããªãšãã¬ã³ã°ãªã³ãŒã«4000ã溶èãããã
ãã¬ã³ã°ãªã³ãŒã«åæ£æ¶²ããããŸããªããåŸã ã«
å ãããå·åŽããŠããªãéåã«40âã§æžæ¿æ¶²ã泚
ãã çµæç©ãæŸå·ããŠåºåãããéåããåãåºã
ãŠãååè¬ãç®ã§å ãã äžã®åè¬ã¯ççåã³ææã®å±æçåŠçœ®çšãšããŠ
çŽè žã«æ¿å ¥ãããã ãã®ä»£ããã«ãã¹ããã€ããçç¥ããŠäžã®çµæ
ç©ãã€ããããšãã§ããã çµæç©å®æœäŸ14 ä¹³è ºçè»ãã ä¹³çã®ä¹³è ºçåŠçœ®çšè»ãã1000ïœã次ã®çš®é¡å
ã³éã®æåããã€ããã æ¬çºæã®æŽ»æ§ååç© 25ïœ ã¡ãã«ãã¬ãããœãã³ã¢ã»ããŒã 0.5ïœ è»œè³ªæ¶²äœãããã©ã¯ã¿ã 300ïœ ç¡æ°Žã¯ãããã¿ããŒã« ïŒïœ ããªãœã«ããŒã80 ïŒïœ ïŒïŒ ã¢ãã¹ãã¢ãªã³é žã¢ã«ãããŠã âèœè±çæ²¹
ã²ã« 400ïœ çœè²ãããã©ã¯ã¿ã 1000ïœãšããé æ¬çºæã®æŽ»æ§ååç©ãšã¡ãã«ãã¬ãããœãã³ã¢
ã»ããŒããã埮ç²ç ãããŠåäžååžããããŸã§è»œ
質液äœãããã©ã¿ã ãšäžç·ã«ç·Žããã¯ãããã¿ã
ãŒã«ãããªãœã«ããŒã80ãèœè±çæ²¹ã²ã«åã³çœè²
ãããã©ã¿ã ã48.9âïŒ120ãïŒã«å ç±ããŠæº¶è
ç©ã圢æããã液äœãããã©ã¿ã åæ£æ¶²ããã®äž
ã«æ··ã蟌ããããããããŸããªãããåæ£æ¶²ã宀
æž©ãŸã§æŸå·ãåºåããã10ïœã®æåéã§äœ¿ãæšãŠ
ã®ä¹³è ºççšæ³šå°åšã«å å¡«ããã çµæç©å®æœäŸ15 åç©é£Œæ 次ã®çš®é¡åã³éã®æåãã飌æããã¯ã¹1000ïœ
ãã€ããã æ¬çºæã®æŽ»æ§ååç© 10ïœ å€§è±ç² 400ïœ é ç² 400ïœ å°éºŠèèœæ²¹ 50ïœ ããããç³è 140ïœ æåãäžç·ã«æ··åããå§çž®ããŠãã¬ããã«ã
ãããã®çµæç©ã¯ã茞éäžã®äºé²ã®ããå®éšå
ç©ãããªãã¡ã©ããããã€ãããã¿ãã¢ã«ã¢ã
ãããã ã¹ã¿ãŒã«çµŠé€ã§ããã 家犜ãäŸãã°ã«ããšãããã²ããäžé¢é³¥ãã¬ã
ãšãŠã®ãããªãã®ä»ã®åç©ã«ã¯ãæ¬çºæã®æŽ»æ§å
åç©ã®æãã§ããæäžéãäžããèšç®éã®çµæç©
ãåç©ã®é垞飌æã«æ·»å ã§ããã çµæç©å®æœäŸ 16 以äžã®çµæç©å®æœäŸïŒã15ã®åã ã®æé ã«åŸã€
ãŠãæ²»çç¹æ§ãæäŸããããã«ãæ¬çºæã®åã ã®
æè掻æ§ååç©ã¯ãå®æœäŸäžã«ç€ºãããæ¬çºæã®
掻æ§ååç©ã«å¯Ÿãããã®ãšç䟡ã®éã§ä»£æ¿ãã
ãã åæ§ã«ãäžã®éé¢å¡©åºååç©é¡ã®åã ã¯ã補è¬
åŠçã«ïŒåã¯è¬çåŠçã«ïŒåå ¥ããããé žä»å
å¡©ãäŸãã°å¡©é žå¡©ãç¡«é žå¡©ãç¡é žå¡©ãçé žå¡©ãã
ããé žå¡©ãä¹³é žå¡©ãé ¢é žå¡©ãé ç³é žå¡©ãåã³ãã¯
ãé žå¡©ã®åœ¢ã§äœ¿çšã§ããã æŽã«ãäžã®æ¬çºæã®æè掻æ§ååç©é¡ã®åã ã®
ãã®ã®ïŒâãã¹ããšãŒãåã³ïŒåã¯ïŒâãã«ãã
ãŒãã掻æ§æåãšããŠä»£ããã«äœ¿çšãããšãæ²»ç
ç¹æ§ããã€çµæç©é¡ãæäŸãããã
Claims (1)
- ãç¹èš±è«æ±ã®ç¯å²ã ïŒ åŒ ã®ååç©ããã®ïŒâãã¹ããšãŒããïŒâãã«ãã
ãŒããåã¯è£œè¬åŠçã«åãå ¥ãããããã®é žä»å
å¡©ãR1ã¯ããã§ã«R2ã§çœ®æãããŠã¯ããªãããª
ãžã³ç°ã®ä»»æã®äœçœ®ã§ãäžååã¯è€æ°å眮æãã
ããã®ã§ãã€ãŠãæ°ŽçŽ ãã¢ã«ãã«ã眮æãããã¢
ã«ãã«ïŒã¢ã«ãã«éšåã¯ïŒãïŒåã®ççŽ ååïŒå
ã¯ãã®ç°æ§äœåãã·ã¯ãã¢ã«ãã«ã眮æãããã·
ã¯ãã¢ã«ãã«ã眮æãããé žçŽ ã眮æãããçª
çŽ ãããã²ã³ãããšãã«ã眮æãããããšãã«ã
âïŒCH2ïŒoâOHãâïŒCH2ïŒoâNR4R5ãåã¯ã
ã®ç°æ§äœåïŒããã§ïœã¯ïŒãïŒã®æŽæ°ã§ããã
R4ãšR5ã¯ïŒšåã¯ïŒãïŒåã®ççŽ ååã®ã¢ã«ãã«
åã¯ãã®ç°æ§äœåã§ããïŒãããªã矀ããéžã°
ããR2ã¯ãã§ã«R1ã§çœ®æãããŠã¯ããªãããªãž
ã³ç°ã®ä»»æã®äœçœ®ã§äžå眮æããããã®ã§ã
ãåŒãã§ããããããã§ïŒžã¯ïŒïŒïŒ²ïŒâãã ããã·âã¡ãã«ïŒâããªâαâãªã³ã³ãµãããã
ïŒïŒïŒ³ïŒâããããã·âã¡ãã«ïŒâããªâαâãª
ã³ã³ãµããããïŒïŒïŒ³ïŒâããâã¡ãã«ïŒâããª
âαâãªã³ã³ãµããããïŒïŒïŒ²ïŒâããâã¡ãã«
ïŒâããªâαâãªã³ã³ãµããããïŒïŒïŒ³ïŒâã¡ã
ãã·âã¡ãã«ïŒâããªâαâãªã³ã³ãµããããïŒ
âããªãã·âïŒïŒïŒ³ïŒâïŒã¡ãã«ããªïŒâã¡ãã«
ïŒâããªâαâãªã³ã³ãµããããïŒâããªãã·â
ïŒïŒïŒ³ïŒâïŒïŒâããããã·ãšãã«ããªïŒâã¡ã
ã«ïŒâããªâαâãªã³ã³ãµãããåã³ïŒâããªã
ã·âïŒïŒïŒ³ïŒâïŒïŒâããããã·ãããã«ããªïŒ
âã¡ãã«ïŒâããªâαâãªã³ã³ãµããããããªã
矀ããéžã°ããååç©ã®ã¢ããå®èœåºã§ãããã ïŒ R1ãïŒâäœçœ®ã«ãã€ãŠïŒãïŒåã®ççŽ åå
ã®ã¢ã«ãã«åã¯ãã®ç°æ§äœåã§ãããR2ã¯ïŒå
ã¯ïŒäœçœ®ã«ãããç¹èš±è«æ±ã®ç¯å²ç¬¬ïŒé ã«ããå
åç©ãåã¯è£œè¬åŠçã«åãå ¥ãããããã®é žä»å
å¡©ã ïŒ åŒ ãR1ã¯ããã§ã«R2ã§çœ®æãããŠã¯ããªãããª
ãžã³ç°ã®ä»»æã®äœçœ®ã§ãäžååã¯è€æ°å眮æãã
ããã®ã§ãã€ãŠãæ°ŽçŽ ãã¢ã«ãã«ã眮æãããã¢
ã«ãã«ïŒã¢ã«ãã«éšåã¯ïŒãïŒåã®ççŽ ååïŒå
ã¯ãã®ç°æ§äœåãã·ã¯ãã¢ã«ãã«ã眮æãããã·
ã¯ãã¢ã«ãã«ã眮æãããé žçŽ ã眮æãããçª
çŽ ãããã²ã³ãããšãã«ã眮æãããããšãã«ã
âïŒCH2ïŒoâOHãâïŒCH2ïŒoâNR4R5ãåã¯ã
ã®ç°æ§äœåã§ãããïŒããã§ïœã¯ïŒãïŒã®æŽæ°ã§
ãããR4ãšR5ã¯ïŒšåã¯ïŒãïŒåã®ççŽ ååã®ã¢
ã«ãã«åã¯ãã®ç°æ§äœåã§ããïŒ ãåŒãã¯ãã§ã«R1ã§çœ®æãããŠã¯ããªãã㪠ãžã³ç°ã®ä»»æã®äœçœ®ã§äžå眮æã§ãããã®ã¢ãã
é žããïŒïŒïŒ²ïŒâããããã·âã¡ãã«ïŒâããªâ
αâãªã³ã³ãµããããïŒïŒïŒ³ïŒâããããã·âã¡
ãã«ïŒâããªâαâãªã³ã³ãµããããïŒïŒïŒ³ïŒâ
ããâã¡ãã«ïŒâããªâαâãªã³ã³ãµããããïŒ
ïŒïŒ²ïŒâããâã¡ãã«ïŒâããªâαâãªã³ã³ãµã
ãããïŒïŒïŒ³ïŒâã¡ããã·âã¡ãã«ïŒâããªâα
âãªã³ã³ãµããããïŒâããªãã·âïŒïŒïŒ³ïŒâ
ïŒã¡ãã«ããªïŒâã¡ãã«ïŒâããªâαâãªã³ã³ãµ
ããããïŒâããªãã·âïŒïŒïŒ³ïŒâïŒïŒâããã
ãã·ãšãã«ããªïŒâã¡ãã«ïŒâããªâαâãªã³ã³
ãµãããåã³ïŒâããªãã·âïŒïŒïŒ³ïŒâïŒïŒâã
ãããã·ãããã«ããªïŒâã¡ãã«ïŒâããªâαâ
ãªã³ã³ãµããããããªã矀ããéžã°ããç³ã¢ãã³
ååç©ãšåå¿ãããããšãããªãã åŒ ãåŒäžR1ã¯äžã«å®çŸ©ããããšããã§ãããR2
ã¯ãã§ã«R1ã§çœ®æãããŠã¯ããªãããªãžã³ç°ã®
ä»»æã®äœçœ®ã§äžå眮æãããããã®ã§ã
ãåŒãã§ããããããã§ïŒžã¯ïŒïŒïŒ²ïŒâãã ããã·âã¡ãã«ïŒâããªâαâãªã³ã³ãµãããã
ïŒïŒïŒ³ïŒâããããã·âã¡ãã«ïŒâããªâαâãª
ã³ã³ãµããããïŒïŒïŒ³ïŒâããâã¡ãã«ïŒâããª
âαâãªã³ã³ãµããããïŒïŒïŒ²ïŒâããâã¡ãã«
ïŒâããªâαâãªã³ã³ãµããããïŒïŒïŒ³ïŒâã¡ã
ãã·âã¡ãã«ïŒâããªâαâãªã³ã³ãµããããïŒ
âããªãã·âïŒïŒïŒ³ïŒâïŒã¡ãã«ããªïŒâã¡ãã«
ïŒâããªâαâãªã³ã³ãµããããïŒâããªãã·â
ïŒïŒïŒ³ïŒâïŒïŒâããããã·ãšãã«ããªïŒâã¡ã
ã«ïŒâããªâαâãªã³ã³ãµãããåã³ïŒâããªã
ã·âïŒïŒïŒ³ïŒâïŒïŒâããããã·ãããã«ããªïŒ
âã¡ãã«ïŒâããªâαâãªã³ã³ãµããããããªã
矀ããéžã°ããååç©ã®ã¢ããå®èœåºã§ãããã®
ååç©ã®è£œæ³ã
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US9665279A | 1979-11-23 | 1979-11-23 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPS5687597A JPS5687597A (en) | 1981-07-16 |
| JPS6338037B2 true JPS6338037B2 (ja) | 1988-07-28 |
Family
ID=22258400
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP16272380A Granted JPS5687597A (en) | 1979-11-23 | 1980-11-20 | Analogue of lincomycin and clindamycin |
| JP63026734A Granted JPS63225392A (ja) | 1979-11-23 | 1988-02-09 | ãªã³ã³ãã€ã·ã³ãšã¯ãªã³ããã€ã·ã³ã®é¡äŒŒäœ |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP63026734A Granted JPS63225392A (ja) | 1979-11-23 | 1988-02-09 | ãªã³ã³ãã€ã·ã³ãšã¯ãªã³ããã€ã·ã³ã®é¡äŒŒäœ |
Country Status (4)
| Country | Link |
|---|---|
| JP (2) | JPS5687597A (ja) |
| BE (1) | BE886301A (ja) |
| ES (2) | ES8206547A1 (ja) |
| ZA (1) | ZA806438B (ja) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2007528360A (ja) * | 2003-06-17 | 2007-10-11 | ããã¥ãã³ã»ãã¡ãŒãã·ã¥ãŒãã£ã«ã«ãºã»ã€ã³ã³ãŒãã¬ã€ããã | æè掻æ§ãæãããªã³ã³ãã€ã·ã³èªå°äœ |
-
1980
- 1980-10-20 ZA ZA00806438A patent/ZA806438B/xx unknown
- 1980-11-20 JP JP16272380A patent/JPS5687597A/ja active Granted
- 1980-11-21 BE BE0/202901A patent/BE886301A/fr not_active IP Right Cessation
-
1981
- 1981-11-20 ES ES507345A patent/ES8206547A1/es not_active Expired
- 1981-11-20 ES ES507346A patent/ES507346A0/es active Granted
-
1988
- 1988-02-09 JP JP63026734A patent/JPS63225392A/ja active Granted
Also Published As
| Publication number | Publication date |
|---|---|
| JPS63225392A (ja) | 1988-09-20 |
| ES507345A0 (es) | 1982-09-01 |
| ES8206547A1 (es) | 1982-09-01 |
| ES8206548A1 (es) | 1982-08-16 |
| ES507346A0 (es) | 1982-08-16 |
| ZA806438B (en) | 1981-10-28 |
| JPH0141157B2 (ja) | 1989-09-04 |
| JPS5687597A (en) | 1981-07-16 |
| BE886301A (fr) | 1981-05-21 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| DE69726577T2 (de) | Kristallin form i von clarithromycin | |
| US4278789A (en) | Lincomycin compounds | |
| CH677495A5 (ja) | ||
| KR100191989B1 (ko) | ì ê·í ê²°ì íì 묎ì7-((1ìí,5ìí,6ìí)-6-ìë¯žë ž-3-ììë¹ì¬ìŽíŽë¡(3.1.0)í¥ì€-3-ìŒ)-6-í룚ì€ë¡-1-(2,4-ëí룚ì€ë¡íë)-1,4-ëíìŽëë¡-4-ì¥ì-1,8-ëíí°ëŠ¬ë-3-칎복ì€ì° ë©íì€í°ì° ìŒ | |
| DE3876174T2 (de) | 2',3'-dideoxy-3'-fluorothymidin und verwandte verbindungen zur behandlung von adenovirus-infektionen. | |
| JPH0340030B2 (ja) | ||
| US3632768A (en) | Therapeutic composition and method for treating infections with actinospectacin | |
| US4310660A (en) | Lincomycin compounds | |
| DE68922127T2 (de) | Zinkceftiofurkomplexe. | |
| US4309533A (en) | Lincomycin compounds | |
| US3764672A (en) | Composition and process of treatment using lincomycin derivatives | |
| US3920630A (en) | 2,2{40 -Anhydro-ara-cytidine compounds and process of preparation | |
| US3539689A (en) | 7-halo-lincomycin composition and process of treatment | |
| US3155580A (en) | Antibiotic composition | |
| NZ213741A (en) | Crystalline cephalosporin hydrohalide compounds and pharmaceutical compositions | |
| JPS6338037B2 (ja) | ||
| CH640236A5 (en) | 3-(2-Aminoethylthio)-6-ethyl-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2 -carboxylic acid and process for its preparation | |
| KR0132671B1 (ko) | 9-r-ììì¬ìŽíŽëŠ ì늬ížë¡ë§ìŽì íìì | |
| JPH0216758B2 (ja) | ||
| US3597415A (en) | Erythromycin amides and process for preparing same | |
| CA1165316A (en) | Analogs of lincomycin and clindamycin | |
| CA1164864A (en) | Analogs of lincomycin and clindamycin | |
| JPS5931796A (ja) | ïœïœã®ïœâïŒïŒâ修食èªå°äœ | |
| US3661891A (en) | Erythromycin ureides and process of preparation | |
| US3689645A (en) | Erythromycin amides as antibacterial agents |