JP4284474B2 - Endothermic composition for external use and use as sleep-inducing agent - Google Patents
Endothermic composition for external use and use as sleep-inducing agent Download PDFInfo
- Publication number
- JP4284474B2 JP4284474B2 JP05028698A JP5028698A JP4284474B2 JP 4284474 B2 JP4284474 B2 JP 4284474B2 JP 05028698 A JP05028698 A JP 05028698A JP 5028698 A JP5028698 A JP 5028698A JP 4284474 B2 JP4284474 B2 JP 4284474B2
- Authority
- JP
- Japan
- Prior art keywords
- composition
- patch
- weight
- parts
- present
- 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 - Lifetime
Links
- 239000000203 mixture Substances 0.000 title claims description 130
- 230000001939 inductive effect Effects 0.000 title description 4
- UWKAYLJWKGQEPM-LBPRGKRZSA-N linalyl acetate Chemical compound CC(C)=CCC[C@](C)(C=C)OC(C)=O UWKAYLJWKGQEPM-LBPRGKRZSA-N 0.000 claims description 32
- 244000178870 Lavandula angustifolia Species 0.000 claims description 30
- 235000010663 Lavandula angustifolia Nutrition 0.000 claims description 30
- 229920002125 Sokalan® Polymers 0.000 claims description 30
- 239000001102 lavandula vera Substances 0.000 claims description 28
- 235000018219 lavender Nutrition 0.000 claims description 28
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 27
- CDOSHBSSFJOMGT-UHFFFAOYSA-N linalool Chemical compound CC(C)=CCCC(C)(O)C=C CDOSHBSSFJOMGT-UHFFFAOYSA-N 0.000 claims description 24
- UWKAYLJWKGQEPM-UHFFFAOYSA-N linalool acetate Natural products CC(C)=CCCC(C)(C=C)OC(C)=O UWKAYLJWKGQEPM-UHFFFAOYSA-N 0.000 claims description 23
- 150000003839 salts Chemical class 0.000 claims description 21
- 239000001490 (3R)-3,7-dimethylocta-1,6-dien-3-ol Substances 0.000 claims description 18
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims description 12
- 239000000758 substrate Substances 0.000 claims description 11
- 150000005846 sugar alcohols Polymers 0.000 claims description 11
- 229910052751 metal Inorganic materials 0.000 claims description 10
- 239000002184 metal Substances 0.000 claims description 10
- FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 claims description 9
- 150000002739 metals Chemical class 0.000 claims description 9
- 239000011975 tartaric acid Substances 0.000 claims description 9
- 235000002906 tartaric acid Nutrition 0.000 claims description 9
- CDOSHBSSFJOMGT-JTQLQIEISA-N (R)-linalool Natural products CC(C)=CCC[C@@](C)(O)C=C CDOSHBSSFJOMGT-JTQLQIEISA-N 0.000 claims description 8
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 claims description 8
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 claims description 8
- 229930007744 linalool Natural products 0.000 claims description 8
- 239000000463 material Substances 0.000 claims description 8
- 229920001282 polysaccharide Polymers 0.000 claims description 7
- 239000005017 polysaccharide Substances 0.000 claims description 7
- 229920002678 cellulose Polymers 0.000 claims description 6
- 239000001913 cellulose Substances 0.000 claims description 6
- KCXVZYZYPLLWCC-UHFFFAOYSA-N EDTA Chemical compound OC(=O)CN(CC(O)=O)CCN(CC(O)=O)CC(O)=O KCXVZYZYPLLWCC-UHFFFAOYSA-N 0.000 claims description 4
- 229910000147 aluminium phosphate Inorganic materials 0.000 claims description 4
- 239000000411 inducer Substances 0.000 claims description 2
- 150000004676 glycans Chemical class 0.000 claims 1
- 239000004584 polyacrylic acid Substances 0.000 description 22
- -1 lavandol Chemical compound 0.000 description 17
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 16
- 230000000694 effects Effects 0.000 description 16
- 239000000341 volatile oil Substances 0.000 description 16
- 230000000284 resting effect Effects 0.000 description 12
- 230000002093 peripheral effect Effects 0.000 description 11
- 230000036760 body temperature Effects 0.000 description 10
- 238000001816 cooling Methods 0.000 description 10
- 238000009826 distribution Methods 0.000 description 10
- 210000001061 forehead Anatomy 0.000 description 10
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 9
- 229940083980 lavender extract Drugs 0.000 description 9
- 235000020723 lavender extract Nutrition 0.000 description 9
- 239000004094 surface-active agent Substances 0.000 description 9
- 230000009471 action Effects 0.000 description 8
- 235000011187 glycerol Nutrition 0.000 description 8
- 230000001965 increasing effect Effects 0.000 description 8
- 239000000171 lavandula angustifolia l. flower oil Substances 0.000 description 8
- 229910052782 aluminium Inorganic materials 0.000 description 7
- 238000010586 diagram Methods 0.000 description 7
- 238000002474 experimental method Methods 0.000 description 7
- 230000033764 rhythmic process Effects 0.000 description 7
- 238000000222 aromatherapy Methods 0.000 description 6
- 239000003205 fragrance Substances 0.000 description 6
- 238000004519 manufacturing process Methods 0.000 description 6
- 150000004804 polysaccharides Chemical class 0.000 description 6
- 238000003756 stirring Methods 0.000 description 6
- XAGFODPZIPBFFR-UHFFFAOYSA-N aluminium Chemical compound [Al] XAGFODPZIPBFFR-UHFFFAOYSA-N 0.000 description 5
- 239000003795 chemical substances by application Substances 0.000 description 5
- 238000011156 evaluation Methods 0.000 description 5
- 238000009472 formulation Methods 0.000 description 5
- 230000000147 hypnotic effect Effects 0.000 description 5
- 230000003340 mental effect Effects 0.000 description 5
- 229920001495 poly(sodium acrylate) polymer Polymers 0.000 description 5
- NNMHYFLPFNGQFZ-UHFFFAOYSA-M sodium polyacrylate Chemical compound [Na+].[O-]C(=O)C=C NNMHYFLPFNGQFZ-UHFFFAOYSA-M 0.000 description 5
- 238000012360 testing method Methods 0.000 description 5
- GLZPCOQZEFWAFX-UHFFFAOYSA-N Geraniol Chemical compound CC(C)=CCCC(C)=CCO GLZPCOQZEFWAFX-UHFFFAOYSA-N 0.000 description 4
- 239000004698 Polyethylene Substances 0.000 description 4
- 208000013738 Sleep Initiation and Maintenance disease Diseases 0.000 description 4
- PPBRXRYQALVLMV-UHFFFAOYSA-N Styrene Chemical compound C=CC1=CC=CC=C1 PPBRXRYQALVLMV-UHFFFAOYSA-N 0.000 description 4
- WNROFYMDJYEPJX-UHFFFAOYSA-K aluminium hydroxide Chemical compound [OH-].[OH-].[OH-].[Al+3] WNROFYMDJYEPJX-UHFFFAOYSA-K 0.000 description 4
- 229940024545 aluminum hydroxide Drugs 0.000 description 4
- 210000004556 brain Anatomy 0.000 description 4
- 239000008367 deionised water Substances 0.000 description 4
- 229910021641 deionized water Inorganic materials 0.000 description 4
- 229940079593 drug Drugs 0.000 description 4
- 239000003814 drug Substances 0.000 description 4
- 239000000499 gel Substances 0.000 description 4
- 238000005259 measurement Methods 0.000 description 4
- 238000000034 method Methods 0.000 description 4
- LXCFILQKKLGQFO-UHFFFAOYSA-N methylparaben Chemical compound COC(=O)C1=CC=C(O)C=C1 LXCFILQKKLGQFO-UHFFFAOYSA-N 0.000 description 4
- 210000003928 nasal cavity Anatomy 0.000 description 4
- 239000003921 oil Substances 0.000 description 4
- 235000019198 oils Nutrition 0.000 description 4
- 229920000573 polyethylene Polymers 0.000 description 4
- 230000001624 sedative effect Effects 0.000 description 4
- PUPZLCDOIYMWBV-UHFFFAOYSA-N (+/-)-1,3-Butanediol Chemical compound CC(O)CCO PUPZLCDOIYMWBV-UHFFFAOYSA-N 0.000 description 3
- LUEWUZLMQUOBSB-FSKGGBMCSA-N (2s,3s,4s,5s,6r)-2-[(2r,3s,4r,5r,6s)-6-[(2r,3s,4r,5s,6s)-4,5-dihydroxy-2-(hydroxymethyl)-6-[(2r,4r,5s,6r)-4,5,6-trihydroxy-2-(hydroxymethyl)oxan-3-yl]oxyoxan-3-yl]oxy-4,5-dihydroxy-2-(hydroxymethyl)oxan-3-yl]oxy-6-(hydroxymethyl)oxane-3,4,5-triol Chemical compound O[C@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@@H](O[C@@H]2[C@H](O[C@@H](OC3[C@H](O[C@@H](O)[C@@H](O)[C@H]3O)CO)[C@@H](O)[C@H]2O)CO)[C@H](O)[C@H]1O LUEWUZLMQUOBSB-FSKGGBMCSA-N 0.000 description 3
- 229920002134 Carboxymethyl cellulose Polymers 0.000 description 3
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 description 3
- 229920002581 Glucomannan Polymers 0.000 description 3
- 244000178860 Lavandula latifolia Species 0.000 description 3
- 229920000161 Locust bean gum Polymers 0.000 description 3
- 239000004743 Polypropylene Substances 0.000 description 3
- 239000002585 base Substances 0.000 description 3
- 235000010948 carboxy methyl cellulose Nutrition 0.000 description 3
- 150000001875 compounds Chemical class 0.000 description 3
- MTHSVFCYNBDYFN-UHFFFAOYSA-N diethylene glycol Chemical compound OCCOCCO MTHSVFCYNBDYFN-UHFFFAOYSA-N 0.000 description 3
- 239000000835 fiber Substances 0.000 description 3
- 229940046240 glucomannan Drugs 0.000 description 3
- 210000003128 head Anatomy 0.000 description 3
- 239000004615 ingredient Substances 0.000 description 3
- 206010022437 insomnia Diseases 0.000 description 3
- 235000010420 locust bean gum Nutrition 0.000 description 3
- 239000000711 locust bean gum Substances 0.000 description 3
- VLKZOEOYAKHREP-UHFFFAOYSA-N n-Hexane Chemical compound CCCCCC VLKZOEOYAKHREP-UHFFFAOYSA-N 0.000 description 3
- 239000004745 nonwoven fabric Substances 0.000 description 3
- 239000002674 ointment Substances 0.000 description 3
- 229920000058 polyacrylate Polymers 0.000 description 3
- 229920000139 polyethylene terephthalate Polymers 0.000 description 3
- 239000005020 polyethylene terephthalate Substances 0.000 description 3
- 229920001155 polypropylene Polymers 0.000 description 3
- 230000008326 skin blood flow Effects 0.000 description 3
- GRWFGVWFFZKLTI-IUCAKERBSA-N (-)-α-pinene Chemical compound CC1=CC[C@@H]2C(C)(C)[C@H]1C2 GRWFGVWFFZKLTI-IUCAKERBSA-N 0.000 description 2
- NIXOWILDQLNWCW-UHFFFAOYSA-N 2-Propenoic acid Natural products OC(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-N 0.000 description 2
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 description 2
- 244000025254 Cannabis sativa Species 0.000 description 2
- 235000012766 Cannabis sativa ssp. sativa var. sativa Nutrition 0.000 description 2
- 235000012765 Cannabis sativa ssp. sativa var. spontanea Nutrition 0.000 description 2
- 229920000742 Cotton Polymers 0.000 description 2
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 2
- WEEGYLXZBRQIMU-UHFFFAOYSA-N Eucalyptol Chemical compound C1CC2CCC1(C)OC2(C)C WEEGYLXZBRQIMU-UHFFFAOYSA-N 0.000 description 2
- 241000282412 Homo Species 0.000 description 2
- FYYHWMGAXLPEAU-UHFFFAOYSA-N Magnesium Chemical compound [Mg] FYYHWMGAXLPEAU-UHFFFAOYSA-N 0.000 description 2
- PXHVJJICTQNCMI-UHFFFAOYSA-N Nickel Chemical compound [Ni] PXHVJJICTQNCMI-UHFFFAOYSA-N 0.000 description 2
- 239000004677 Nylon Substances 0.000 description 2
- 239000004372 Polyvinyl alcohol Substances 0.000 description 2
- 229910052783 alkali metal Inorganic materials 0.000 description 2
- DIZPMCHEQGEION-UHFFFAOYSA-H aluminium sulfate (anhydrous) Chemical compound [Al+3].[Al+3].[O-]S([O-])(=O)=O.[O-]S([O-])(=O)=O.[O-]S([O-])(=O)=O DIZPMCHEQGEION-UHFFFAOYSA-H 0.000 description 2
- VSCWAEJMTAWNJL-UHFFFAOYSA-K aluminium trichloride Chemical compound Cl[Al](Cl)Cl VSCWAEJMTAWNJL-UHFFFAOYSA-K 0.000 description 2
- 125000000129 anionic group Chemical group 0.000 description 2
- 239000011575 calcium Substances 0.000 description 2
- 229910052791 calcium Inorganic materials 0.000 description 2
- 235000009120 camo Nutrition 0.000 description 2
- CRPUJAZIXJMDBK-UHFFFAOYSA-N camphene Chemical compound C1CC2C(=C)C(C)(C)C1C2 CRPUJAZIXJMDBK-UHFFFAOYSA-N 0.000 description 2
- 239000001768 carboxy methyl cellulose Substances 0.000 description 2
- 239000008112 carboxymethyl-cellulose Substances 0.000 description 2
- 125000002091 cationic group Chemical group 0.000 description 2
- 230000008859 change Effects 0.000 description 2
- 235000005607 chanvre indien Nutrition 0.000 description 2
- 239000001926 citrus aurantium l. subsp. bergamia wright et arn. oil Substances 0.000 description 2
- 239000006071 cream Substances 0.000 description 2
- 239000012530 fluid Substances 0.000 description 2
- 230000017525 heat dissipation Effects 0.000 description 2
- 239000011487 hemp Substances 0.000 description 2
- 230000006698 induction Effects 0.000 description 2
- 238000004898 kneading Methods 0.000 description 2
- 239000011777 magnesium Substances 0.000 description 2
- 229910052749 magnesium Inorganic materials 0.000 description 2
- 230000007246 mechanism Effects 0.000 description 2
- 235000010270 methyl p-hydroxybenzoate Nutrition 0.000 description 2
- 239000004292 methyl p-hydroxybenzoate Substances 0.000 description 2
- 229960002216 methylparaben Drugs 0.000 description 2
- 238000002156 mixing Methods 0.000 description 2
- 229920001778 nylon Polymers 0.000 description 2
- 239000002304 perfume Substances 0.000 description 2
- 230000035699 permeability Effects 0.000 description 2
- 229920002451 polyvinyl alcohol Polymers 0.000 description 2
- 239000011148 porous material Substances 0.000 description 2
- 238000002360 preparation method Methods 0.000 description 2
- 230000001737 promoting effect Effects 0.000 description 2
- 239000008213 purified water Substances 0.000 description 2
- 230000002040 relaxant effect Effects 0.000 description 2
- 208000019116 sleep disease Diseases 0.000 description 2
- 159000000000 sodium salts Chemical group 0.000 description 2
- 230000002936 tranquilizing effect Effects 0.000 description 2
- 239000002759 woven fabric Substances 0.000 description 2
- NPNUFJAVOOONJE-ZIAGYGMSSA-N β-(E)-Caryophyllene Chemical compound C1CC(C)=CCCC(=C)[C@H]2CC(C)(C)[C@@H]21 NPNUFJAVOOONJE-ZIAGYGMSSA-N 0.000 description 2
- HDTRYLNUVZCQOY-UHFFFAOYSA-N α-D-glucopyranosyl-α-D-glucopyranoside Natural products OC1C(O)C(O)C(CO)OC1OC1C(O)C(O)C(O)C(CO)O1 HDTRYLNUVZCQOY-UHFFFAOYSA-N 0.000 description 1
- XMGQYMWWDOXHJM-SNVBAGLBSA-N (-)-α-limonene Chemical compound CC(=C)[C@H]1CCC(C)=CC1 XMGQYMWWDOXHJM-SNVBAGLBSA-N 0.000 description 1
- CDOSHBSSFJOMGT-SNVBAGLBSA-N (S)-linalool Chemical compound CC(C)=CCC[C@](C)(O)C=C CDOSHBSSFJOMGT-SNVBAGLBSA-N 0.000 description 1
- SVUOLADPCWQTTE-UHFFFAOYSA-N 1h-1,2-benzodiazepine Chemical compound N1N=CC=CC2=CC=CC=C12 SVUOLADPCWQTTE-UHFFFAOYSA-N 0.000 description 1
- SMZOUWXMTYCWNB-UHFFFAOYSA-N 2-(2-methoxy-5-methylphenyl)ethanamine Chemical compound COC1=CC=C(C)C=C1CCN SMZOUWXMTYCWNB-UHFFFAOYSA-N 0.000 description 1
- HZAXFHJVJLSVMW-UHFFFAOYSA-N 2-Aminoethan-1-ol Chemical compound NCCO HZAXFHJVJLSVMW-UHFFFAOYSA-N 0.000 description 1
- SHDIPWPAGQDYTH-UHFFFAOYSA-N 2-[bis(2-hydroxyethyl)amino]ethanol;prop-2-enoic acid Chemical compound OC(=O)C=C.OCCN(CCO)CCO SHDIPWPAGQDYTH-UHFFFAOYSA-N 0.000 description 1
- NVEQFIOZRFFVFW-UHFFFAOYSA-N 9-epi-beta-caryophyllene oxide Natural products C=C1CCC2OC2(C)CCC2C(C)(C)CC21 NVEQFIOZRFFVFW-UHFFFAOYSA-N 0.000 description 1
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 description 1
- 208000019901 Anxiety disease Diseases 0.000 description 1
- 240000007436 Cananga odorata Species 0.000 description 1
- 235000002566 Capsicum Nutrition 0.000 description 1
- 244000205754 Colocasia esculenta Species 0.000 description 1
- 235000006481 Colocasia esculenta Nutrition 0.000 description 1
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 description 1
- 241000360590 Erythrites Species 0.000 description 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 1
- 235000001242 French lavender Nutrition 0.000 description 1
- 229920002148 Gellan gum Polymers 0.000 description 1
- GLZPCOQZEFWAFX-YFHOEESVSA-N Geraniol Natural products CC(C)=CCC\C(C)=C/CO GLZPCOQZEFWAFX-YFHOEESVSA-N 0.000 description 1
- 239000005792 Geraniol Substances 0.000 description 1
- 239000004354 Hydroxyethyl cellulose Substances 0.000 description 1
- 229920000663 Hydroxyethyl cellulose Polymers 0.000 description 1
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 description 1
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 1
- 206010022035 Initial insomnia Diseases 0.000 description 1
- 241000207923 Lamiaceae Species 0.000 description 1
- 235000002997 Lavandula Nutrition 0.000 description 1
- 241001529749 Lavandula Species 0.000 description 1
- 235000010658 Lavandula latifolia Nutrition 0.000 description 1
- 244000041506 Lavandula officinalis Species 0.000 description 1
- 241001227551 Lavandula x intermedia Species 0.000 description 1
- 235000019501 Lemon oil Nutrition 0.000 description 1
- 241000101960 Linyphia hortensis Species 0.000 description 1
- 229930195725 Mannitol Natural products 0.000 description 1
- 235000005135 Micromeria juliana Nutrition 0.000 description 1
- GLZPCOQZEFWAFX-JXMROGBWSA-N Nerol Natural products CC(C)=CCC\C(C)=C\CO GLZPCOQZEFWAFX-JXMROGBWSA-N 0.000 description 1
- 239000006002 Pepper Substances 0.000 description 1
- 235000016761 Piper aduncum Nutrition 0.000 description 1
- 240000003889 Piper guineense Species 0.000 description 1
- 235000017804 Piper guineense Nutrition 0.000 description 1
- 235000008184 Piper nigrum Nutrition 0.000 description 1
- 239000002202 Polyethylene glycol Substances 0.000 description 1
- ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 description 1
- PXRCIOIWVGAZEP-UHFFFAOYSA-N Primaeres Camphenhydrat Natural products C1CC2C(O)(C)C(C)(C)C1C2 PXRCIOIWVGAZEP-UHFFFAOYSA-N 0.000 description 1
- HDSBZMRLPLPFLQ-UHFFFAOYSA-N Propylene glycol alginate Chemical compound OC1C(O)C(OC)OC(C(O)=O)C1OC1C(O)C(O)C(C)C(C(=O)OCC(C)O)O1 HDSBZMRLPLPFLQ-UHFFFAOYSA-N 0.000 description 1
- 239000004373 Pullulan Substances 0.000 description 1
- 229920001218 Pullulan Polymers 0.000 description 1
- 229920000297 Rayon Polymers 0.000 description 1
- 240000002114 Satureja hortensis Species 0.000 description 1
- 235000007315 Satureja hortensis Nutrition 0.000 description 1
- RTAQQCXQSZGOHL-UHFFFAOYSA-N Titanium Chemical compound [Ti] RTAQQCXQSZGOHL-UHFFFAOYSA-N 0.000 description 1
- HDTRYLNUVZCQOY-WSWWMNSNSA-N Trehalose Natural products O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@@H]1O[C@@H]1[C@H](O)[C@@H](O)[C@@H](O)[C@@H](CO)O1 HDTRYLNUVZCQOY-WSWWMNSNSA-N 0.000 description 1
- BZHJMEDXRYGGRV-UHFFFAOYSA-N Vinyl chloride Chemical compound ClC=C BZHJMEDXRYGGRV-UHFFFAOYSA-N 0.000 description 1
- 229920002978 Vinylon Polymers 0.000 description 1
- HCHKCACWOHOZIP-UHFFFAOYSA-N Zinc Chemical compound [Zn] HCHKCACWOHOZIP-UHFFFAOYSA-N 0.000 description 1
- HDYRYUINDGQKMC-UHFFFAOYSA-M acetyloxyaluminum;dihydrate Chemical compound O.O.CC(=O)O[Al] HDYRYUINDGQKMC-UHFFFAOYSA-M 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- 150000007513 acids Chemical class 0.000 description 1
- 230000006978 adaptation Effects 0.000 description 1
- 239000002390 adhesive tape Substances 0.000 description 1
- 235000010443 alginic acid Nutrition 0.000 description 1
- 239000000783 alginic acid Substances 0.000 description 1
- 229920000615 alginic acid Polymers 0.000 description 1
- 229960001126 alginic acid Drugs 0.000 description 1
- 150000004781 alginic acids Chemical class 0.000 description 1
- HDTRYLNUVZCQOY-LIZSDCNHSA-N alpha,alpha-trehalose Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@@H]1O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 HDTRYLNUVZCQOY-LIZSDCNHSA-N 0.000 description 1
- FAMPSKZZVDUYOS-UHFFFAOYSA-N alpha-Caryophyllene Natural products CC1=CCC(C)(C)C=CCC(C)=CCC1 FAMPSKZZVDUYOS-UHFFFAOYSA-N 0.000 description 1
- XCPQUQHBVVXMRQ-UHFFFAOYSA-N alpha-Fenchene Natural products C1CC2C(=C)CC1C2(C)C XCPQUQHBVVXMRQ-UHFFFAOYSA-N 0.000 description 1
- MVNCAPSFBDBCGF-UHFFFAOYSA-N alpha-pinene Natural products CC1=CCC23C1CC2C3(C)C MVNCAPSFBDBCGF-UHFFFAOYSA-N 0.000 description 1
- AZDRQVAHHNSJOQ-UHFFFAOYSA-N alumane Chemical class [AlH3] AZDRQVAHHNSJOQ-UHFFFAOYSA-N 0.000 description 1
- 150000004645 aluminates Chemical class 0.000 description 1
- CEGOLXSVJUTHNZ-UHFFFAOYSA-K aluminium tristearate Chemical compound [Al+3].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O CEGOLXSVJUTHNZ-UHFFFAOYSA-K 0.000 description 1
- 229940009827 aluminum acetate Drugs 0.000 description 1
- 229940063656 aluminum chloride Drugs 0.000 description 1
- 229940024546 aluminum hydroxide gel Drugs 0.000 description 1
- 229940063655 aluminum stearate Drugs 0.000 description 1
- 229940010048 aluminum sulfate Drugs 0.000 description 1
- ANBBXQWFNXMHLD-UHFFFAOYSA-N aluminum;sodium;oxygen(2-) Chemical compound [O-2].[O-2].[Na+].[Al+3] ANBBXQWFNXMHLD-UHFFFAOYSA-N 0.000 description 1
- SMYKVLBUSSNXMV-UHFFFAOYSA-K aluminum;trihydroxide;hydrate Chemical compound O.[OH-].[OH-].[OH-].[Al+3] SMYKVLBUSSNXMV-UHFFFAOYSA-K 0.000 description 1
- 150000001412 amines Chemical class 0.000 description 1
- 150000003863 ammonium salts Chemical class 0.000 description 1
- 230000000954 anitussive effect Effects 0.000 description 1
- 208000004793 anterograde amnesia Diseases 0.000 description 1
- 239000003242 anti bacterial agent Substances 0.000 description 1
- 230000000844 anti-bacterial effect Effects 0.000 description 1
- 230000003110 anti-inflammatory effect Effects 0.000 description 1
- 229940124584 antitussives Drugs 0.000 description 1
- 230000036506 anxiety Effects 0.000 description 1
- 230000037007 arousal Effects 0.000 description 1
- 239000012752 auxiliary agent Substances 0.000 description 1
- 235000001053 badasse Nutrition 0.000 description 1
- 229940049706 benzodiazepine Drugs 0.000 description 1
- NPNUFJAVOOONJE-UHFFFAOYSA-N beta-cariophyllene Natural products C1CC(C)=CCCC(=C)C2CC(C)(C)C21 NPNUFJAVOOONJE-UHFFFAOYSA-N 0.000 description 1
- 239000011230 binding agent Substances 0.000 description 1
- 230000017531 blood circulation Effects 0.000 description 1
- 230000003925 brain function Effects 0.000 description 1
- 229910052793 cadmium Inorganic materials 0.000 description 1
- BDOSMKKIYDKNTQ-UHFFFAOYSA-N cadmium atom Chemical compound [Cd] BDOSMKKIYDKNTQ-UHFFFAOYSA-N 0.000 description 1
- 229930006739 camphene Natural products 0.000 description 1
- ZYPYEBYNXWUCEA-UHFFFAOYSA-N camphenilone Natural products C1CC2C(=O)C(C)(C)C1C2 ZYPYEBYNXWUCEA-UHFFFAOYSA-N 0.000 description 1
- 235000010418 carrageenan Nutrition 0.000 description 1
- 239000000679 carrageenan Substances 0.000 description 1
- 229920001525 carrageenan Polymers 0.000 description 1
- 229940113118 carrageenan Drugs 0.000 description 1
- 229940117948 caryophyllene Drugs 0.000 description 1
- NPNUFJAVOOONJE-UONOGXRCSA-N caryophyllene Natural products C1CC(C)=CCCC(=C)[C@@H]2CC(C)(C)[C@@H]21 NPNUFJAVOOONJE-UONOGXRCSA-N 0.000 description 1
- 210000003169 central nervous system Anatomy 0.000 description 1
- 239000013522 chelant Substances 0.000 description 1
- 230000027288 circadian rhythm Effects 0.000 description 1
- 239000011248 coating agent Substances 0.000 description 1
- 238000000576 coating method Methods 0.000 description 1
- 229910017052 cobalt Inorganic materials 0.000 description 1
- 239000010941 cobalt Substances 0.000 description 1
- GUTLYIVDDKVIGB-UHFFFAOYSA-N cobalt atom Chemical compound [Co] GUTLYIVDDKVIGB-UHFFFAOYSA-N 0.000 description 1
- 230000000052 comparative effect Effects 0.000 description 1
- 239000010636 coriander oil Substances 0.000 description 1
- 230000002939 deleterious effect Effects 0.000 description 1
- 239000000645 desinfectant Substances 0.000 description 1
- ZBCBWPMODOFKDW-UHFFFAOYSA-N diethanolamine Chemical compound OCCNCCO ZBCBWPMODOFKDW-UHFFFAOYSA-N 0.000 description 1
- PCHPORCSPXIHLZ-UHFFFAOYSA-N diphenhydramine hydrochloride Chemical compound [Cl-].C=1C=CC=CC=1C(OCC[NH+](C)C)C1=CC=CC=C1 PCHPORCSPXIHLZ-UHFFFAOYSA-N 0.000 description 1
- 239000002612 dispersion medium Substances 0.000 description 1
- 230000000517 effect on sleep Effects 0.000 description 1
- 230000001804 emulsifying effect Effects 0.000 description 1
- 239000000839 emulsion Substances 0.000 description 1
- UNXHWFMMPAWVPI-ZXZARUISSA-N erythritol Chemical compound OC[C@H](O)[C@H](O)CO UNXHWFMMPAWVPI-ZXZARUISSA-N 0.000 description 1
- 238000001704 evaporation Methods 0.000 description 1
- 230000008020 evaporation Effects 0.000 description 1
- 238000000605 extraction Methods 0.000 description 1
- 239000010408 film Substances 0.000 description 1
- 239000000796 flavoring agent Substances 0.000 description 1
- 235000019634 flavors Nutrition 0.000 description 1
- 235000013305 food Nutrition 0.000 description 1
- 235000012041 food component Nutrition 0.000 description 1
- 239000005417 food ingredient Substances 0.000 description 1
- 235000010492 gellan gum Nutrition 0.000 description 1
- 239000000216 gellan gum Substances 0.000 description 1
- 239000003349 gelling agent Substances 0.000 description 1
- 229940113087 geraniol Drugs 0.000 description 1
- 210000004209 hair Anatomy 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-M hydroxide Chemical compound [OH-] XLYOFNOQVPJJNP-UHFFFAOYSA-M 0.000 description 1
- 235000019447 hydroxyethyl cellulose Nutrition 0.000 description 1
- 229920003063 hydroxymethyl cellulose Polymers 0.000 description 1
- 229940031574 hydroxymethyl cellulose Drugs 0.000 description 1
- 239000001863 hydroxypropyl cellulose Substances 0.000 description 1
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 description 1
- 239000010656 jasmine oil Substances 0.000 description 1
- 238000010030 laminating Methods 0.000 description 1
- 244000056931 lavandin Species 0.000 description 1
- 235000009606 lavandin Nutrition 0.000 description 1
- 239000010501 lemon oil Substances 0.000 description 1
- 235000001964 liazer and helhal Nutrition 0.000 description 1
- 125000000396 limonene group Chemical group 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 239000006210 lotion Substances 0.000 description 1
- 230000014759 maintenance of location Effects 0.000 description 1
- WPBNNNQJVZRUHP-UHFFFAOYSA-L manganese(2+);methyl n-[[2-(methoxycarbonylcarbamothioylamino)phenyl]carbamothioyl]carbamate;n-[2-(sulfidocarbothioylamino)ethyl]carbamodithioate Chemical compound [Mn+2].[S-]C(=S)NCCNC([S-])=S.COC(=O)NC(=S)NC1=CC=CC=C1NC(=S)NC(=O)OC WPBNNNQJVZRUHP-UHFFFAOYSA-L 0.000 description 1
- 239000000594 mannitol Substances 0.000 description 1
- 235000010355 mannitol Nutrition 0.000 description 1
- 150000002736 metal compounds Chemical class 0.000 description 1
- 229920000609 methyl cellulose Polymers 0.000 description 1
- 239000001923 methylcellulose Substances 0.000 description 1
- 235000010981 methylcellulose Nutrition 0.000 description 1
- 150000007522 mineralic acids Chemical class 0.000 description 1
- 230000003020 moisturizing effect Effects 0.000 description 1
- 238000000465 moulding Methods 0.000 description 1
- 229920001206 natural gum Polymers 0.000 description 1
- 210000005036 nerve Anatomy 0.000 description 1
- 210000002569 neuron Anatomy 0.000 description 1
- 229910052759 nickel Inorganic materials 0.000 description 1
- 239000002736 nonionic surfactant Substances 0.000 description 1
- 210000001331 nose Anatomy 0.000 description 1
- 150000007524 organic acids Chemical class 0.000 description 1
- 229920001277 pectin Polymers 0.000 description 1
- 239000001814 pectin Substances 0.000 description 1
- 235000010987 pectin Nutrition 0.000 description 1
- 239000003208 petroleum Substances 0.000 description 1
- 230000000144 pharmacologic effect Effects 0.000 description 1
- 239000011505 plaster Substances 0.000 description 1
- 229920000728 polyester Polymers 0.000 description 1
- 229920001223 polyethylene glycol Polymers 0.000 description 1
- 229920000642 polymer Polymers 0.000 description 1
- 230000000379 polymerizing effect Effects 0.000 description 1
- 229910052700 potassium Inorganic materials 0.000 description 1
- 239000011591 potassium Substances 0.000 description 1
- 229920005614 potassium polyacrylate Polymers 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 230000002335 preservative effect Effects 0.000 description 1
- 235000010409 propane-1,2-diol alginate Nutrition 0.000 description 1
- 239000000770 propane-1,2-diol alginate Substances 0.000 description 1
- 235000019423 pullulan Nutrition 0.000 description 1
- GRWFGVWFFZKLTI-UHFFFAOYSA-N rac-alpha-Pinene Natural products CC1=CCC2C(C)(C)C1C2 GRWFGVWFFZKLTI-UHFFFAOYSA-N 0.000 description 1
- 239000002964 rayon Substances 0.000 description 1
- 230000003578 releasing effect Effects 0.000 description 1
- 238000011160 research Methods 0.000 description 1
- 235000019719 rose oil Nutrition 0.000 description 1
- 239000010666 rose oil Substances 0.000 description 1
- 239000000932 sedative agent Substances 0.000 description 1
- 208000022925 sleep disturbance Diseases 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
- 229910001388 sodium aluminate Inorganic materials 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 235000001966 spaanse laventel Nutrition 0.000 description 1
- 238000003892 spreading Methods 0.000 description 1
- 230000007480 spreading Effects 0.000 description 1
- 230000006641 stabilisation Effects 0.000 description 1
- 238000011105 stabilization Methods 0.000 description 1
- 238000001256 steam distillation Methods 0.000 description 1
- 230000004936 stimulating effect Effects 0.000 description 1
- 238000003860 storage Methods 0.000 description 1
- 235000000346 sugar Nutrition 0.000 description 1
- 150000008163 sugars Chemical class 0.000 description 1
- 229920002994 synthetic fiber Polymers 0.000 description 1
- 239000012209 synthetic fiber Substances 0.000 description 1
- 235000010491 tara gum Nutrition 0.000 description 1
- 239000000213 tara gum Substances 0.000 description 1
- KKEYFWRCBNTPAC-UHFFFAOYSA-L terephthalate(2-) Chemical compound [O-]C(=O)C1=CC=C(C([O-])=O)C=C1 KKEYFWRCBNTPAC-UHFFFAOYSA-L 0.000 description 1
- 125000002282 terpinolene group Chemical group 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 229910052719 titanium Inorganic materials 0.000 description 1
- 239000010936 titanium Substances 0.000 description 1
- 239000003204 tranquilizing agent Substances 0.000 description 1
- 238000013519 translation Methods 0.000 description 1
- ZIBGPFATKBEMQZ-UHFFFAOYSA-N triethylene glycol Chemical compound OCCOCCOCCO ZIBGPFATKBEMQZ-UHFFFAOYSA-N 0.000 description 1
- 238000009834 vaporization Methods 0.000 description 1
- 230000008016 vaporization Effects 0.000 description 1
- 210000002268 wool Anatomy 0.000 description 1
- 229920001285 xanthan gum Polymers 0.000 description 1
- 235000010493 xanthan gum Nutrition 0.000 description 1
- 239000000230 xanthan gum Substances 0.000 description 1
- 229940082509 xanthan gum Drugs 0.000 description 1
- 229910052725 zinc Inorganic materials 0.000 description 1
- 239000011701 zinc Substances 0.000 description 1
- UHVMMEOXYDMDKI-JKYCWFKZSA-L zinc;1-(5-cyanopyridin-2-yl)-3-[(1s,2s)-2-(6-fluoro-2-hydroxy-3-propanoylphenyl)cyclopropyl]urea;diacetate Chemical compound [Zn+2].CC([O-])=O.CC([O-])=O.CCC(=O)C1=CC=C(F)C([C@H]2[C@H](C2)NC(=O)NC=2N=CC(=CC=2)C#N)=C1O UHVMMEOXYDMDKI-JKYCWFKZSA-L 0.000 description 1
- 239000002888 zwitterionic surfactant Substances 0.000 description 1
Images
Landscapes
- Medicinal Preparation (AREA)
- Medicines Containing Plant Substances (AREA)
- Thermotherapy And Cooling Therapy Devices (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Description
【０００１】
【発明の属する技術分野】
本発明は、リナロール又はリナリルアセテートの少なくとも１種を吸熱性組成物に含有する外用組成物及びそれを含有する貼付剤に関する。
【０００２】
また本発明は、上記外用組成物及び貼付剤の睡眠導入剤としての用途に関する。
【０００３】
【従来の技術】
従来、不眠症の治療には、トランキライザーなどの睡眠導入薬が使用されるが、これらの薬剤は劇物であり、連用による耐性や反跳性不眠などの副作用も多い。副作用が比較的少ないとされるベンゾジアゼピン系の薬剤さえも、前向性健忘や服用後にもうろう状態を生じやすい等の副作用が報告されており、このような副作用がなく、安心して服用できる睡眠薬の開発が求められている。
【０００４】
ところで、ヨーロッパ地方を中心に古くから知られているアロマテラピーによると、様々な精油の香りによる薬理的・心理的療法が広く伝えられており（「実践アロマテラピー」：シャーリ・プライス著、高山林太郎訳、1987年）（「アロマテラピー」：ロバート・ティスランド著、高山林太郎訳、1985年）、各研究分野においても、香りが生理・心理状態に与える影響に関する報告が数多く出されている〔化学技術誌、1990年８月；フレグランス・ジャーナル、No.86、1987年；フレグランス・ジャーナル、No.77、16、1986年；日本神経精神薬理学雑誌、Vol.15、39-42、1995；FOOD & FOOD INGREDIENTS JOURNAL No.156, 1993等〕。また、アロマテラピーで用いられる精油による安眠効果に関して、特開平４−１２８２３４号、特開平４−１４９１３６号の報告がある。
【０００５】
このようなアロマテラピー（芳香療法）には、その鎮静効果、殺菌効果、抗炎症効果、鎮咳効果及びリラックス効果等といった効用に加えて、安全性が高いこと等からラベンダー精油がよく用いられている。
【０００６】
しかしながら、特開平４−１４９１３６号（特許公開公報第１３頁、実施例２）にはラベンダー精油には安眠促進効果が殆どないことが記載されており、また今までラベンダー精油に催眠作用があるという報告はない。
【０００７】
【発明が解決しようとする課題】
本発明は、かかる事情に鑑みて開発されたもので、ラベンダー精油等に含まれるリナロール又はリナリルアセテートの少なくとも１種を吸熱性組成物中に含有する冷却作用及び鎮静作用のある外用組成物を提供することを目的とする。該外用組成物は、ヒトの額部や胸部に適用されることにより催眠効果を発揮する入眠補助剤若しくは睡眠導入剤として有用である。
【０００８】
また本発明は、上記外用組成物をシート状基材に積層してなる貼付剤を提供することを目的とする。
【０００９】
【課題を解決するための手段】
本発明者らは、上記従来技術の問題点を解決すべく、鎮静効果があって安全性の高いラベンダー抽出物に注目して種々研究をすすめていたところ、ラベンダー抽出物又はその揮発成分を吸熱性組成物に配合して外用剤とし、これを上半身、特に頭・顔部又は胸部に適用すると、体温によってラベンダーの揮発成分が効果的に鼻腔から作用して、該外用剤の冷却作用と相俟って、入眠がスムーズに導かれることを見いだした。本発明はかかる知見に基づいて開発されたものである。
【００１０】
すなわち、本発明は下記（１）〜（８）に掲げる外用組成物である。
【００１１】
（１）リナロール又はリナリルアセテートの少なくとも１種を吸熱性組成物中に含有する外用組成物。
【００１２】
（２）最終組成物１００重量部に含まれるリナロールの配合量が０．０００５〜０．６重量部であり、またリナリルアセテートの配合量が０．０００５〜０．８重量部である（１）記載の外用組成物。
【００１３】
（３）ラベンダーの抽出物を吸熱性組成物中に含有する（１）又は（２）記載の外用組成物。
【００１４】
（４）最終組成物が３０〜９５％の割合で水分を含有していることを特徴とする（１）乃至（３）のいずれかに記載の外用組成物。
【００１５】
（５）吸熱性組成物が、多糖類及び水を含有する組成物であることを特徴とする（１）乃至（４）のいずれかに記載の外用組成物。
【００１６】
（６）吸熱組成物が、ポリアクリル酸類、多価金属類及び水を含有する組成物である（１）乃至（４）のいずれかに記載の外用組成物。
【００１７】
（７）吸熱組成物が更に多価アルコールを含む組成物である（５）又は（６）に記載の外用組成物。
【００１８】
（８）吸熱組成物が、更に(i)酒石酸，クエン酸，リン酸，エチレンジアミン四酢酸またはそれらの塩の少なくとも１種，または(ii)セルロース誘導体のいずれか少なくとも１方を含む組成物である（６）又は（７）記載の外用組成物。
【００１９】
これらの外用組成物は、睡眠導入剤として用いることができる。
【００２０】
更に本発明は、上記いずれかに記載の外用組成物を有する貼付剤である。
【００２１】
前述するように、従来、ラベンダー精油ならびにそれに含まれている揮発成分に睡眠導入作用や催眠作用があるという報告はない。
【００２２】
本発明者らの更なる研究によると、本発明の外用組成物は、ラベンダー油に含まれている揮発成分を効果的に鼻腔から吸入させることにより中枢神経をリラックスさせ、さらに末梢の皮膚血流量を増加させて末梢皮膚温を上げ、体内深部からの放熱を助長することが判明した。
【００２３】
従来から、体温と睡眠リズムとの間に一定の相関関係があることが知られている。すなわち、就眠に先だって末梢皮膚温が上昇し始め、それにやや遅れて直腸温が下降し、睡眠中はこの状態が続く（綜合臨床 Vol.34 増刊号(1985),14-16）。また、かかる就眠時の体温リズムの発現には、皮膚血流量を増加させて体内深部の熱を放散する機構が関与していることが指摘されている（Damm,F.,Doring,G.,ら、「体温とサーカディアンリズム」1973年）。
【００２４】
本発明の外用組成物は、ヒトの生体リズムを、このような就眠時の自然の体温リズムに人為的に近づけることによって、自然により近い睡眠を導くものである。また本発明の外用組成物は、皮膚表面を冷却することによって生体の熱放散機構を補助するものであり、これによって就眠時の生体リズムに一層近づけて睡眠をスムーズに導くことができる。更に本発明の外用組成物によれば、体温によって揮散されたリナロール等のラベンダーの揮発成分の働きによってヒトに鎮静作用を与え、精神的な面からも安らかな睡眠をもたらすことができる。
【００２５】
【発明の実施の形態】
本発明の外用組成物は、リナロール又はリナリルアセテートの少なくとも１種を吸熱性組成物に含有することを特徴とする。
【００２６】
本発明で用いられるリナロールは、天然に広く存在するリナロールであればよく、テルピノレン形，リモネン形といった構造異性体の別やｄ体及びｌ体の別を問うものではない。好ましくは、ラベンダー油に存在するリナロールと同一のｌ−リナロールを挙げることができる。リナリルアセテートも、同様に、天然に広く存在するリナリルアセテートであればよい。なお、これらは取得の由来によって何ら限定されるものではない。
【００２７】
本発明の外用組成物に含まれるリナロールの割合は、最終組成物１００重量部あたり０．０００５〜０．６重量部、好ましくは０．００２〜０．４５重量部、より好ましくは０．００３〜０．４重量部である。
【００２８】
本発明の外用組成物に含まれるリナリルアセテートの割合は、最終組成物１００重量部あたり０．０００５〜０．８重量部、好ましくは０．００２〜０．７重量部、より好ましくは０．００３〜０．６重量部である。
【００２９】
本発明の組成物には、これらの成分が各種単独で配合されていても、また２種を組み合わせて配合されていてもよい。
【００３０】
リナロールのうち、ｄ−リナロールは、一般にメキシコ産リナロエ油、ボアドローズ油、コリアンダー油、オヤイヌコウジュの精油に、またｌ−リナロールは、一般にホウショウ油、ラベンダー油、ベルガモット油等の精油に含まれており、さらにリナリルアセテートは、一般にラベンダー油、ベルガモット油、プチグレン油、ジャスミン油、イランイラン油、レモン油等の精油に含まれている。従って、本発明においては、本発明の効果を阻害しない限り、上記リナロール及び／又はリナリルアセテートとしてこれらの精油を用いることもできる。
【００３１】
かかる精油としては好適にはラベンダー油を挙げることができる。ラベンダー油にはリナリルアセテート及びｌ−リナロールに加えて、ゲラニオール、ラバンズロール、ネロール、α−ピネン、カリオフィレン、１，８−シネオール、カンフェン、ｌ−リモネン、ジペンネンなど約数百の成分が含まれている。これらラベンダー油の成分は本発明の効果に対して協同的に働くことはあっても本発明の効果を阻害するものではないと認識される。
【００３２】
ラベンダー油は、一般に、例えばラベンダーの花穂を水蒸気蒸留するか、又はヘキサン、石油エーテル、アルコール等の溶媒を用いて抽出することによって得ることができる。
【００３３】
従って、本発明の外用組成物は、上記のようにして抽出されるラベンダーの抽出物を単独若しくは２種以上組み合わせて、吸熱性組成物に含有する組成物であってもよい。
【００３４】
本発明で用いられるラベンダーには、シソ科のラベンダー属に属するもの及びそれらの変種等が広く包含される。一般にラベンダーは葉や苞葉の形状により（１）スパイカラベンダー・グループ（Spica-type lavender group）、（２）フレンチラベンダー・グループ（Stoechas-type lavender group）及び（３）ファーンラベンンダー・グループ（Fern-like lavender group, Pterostachys lavender）に分類され、さらに（１）はコモンラベンダー系（Lavandula angustifolia Mill.及びその栽培品種等）、ラバンディン系（L.x intermedia Emeric ex Loisel.(Lavandula hybrida Reverchon ex Briq.,L.hortensis Hy)）及びその他の系統（例えば、スパイクラベンダー（L.latifolia Medik.(L.spica auct.,non L.)）等）のものに分類される。本発明はこれらのラベンダーのいずれをも使用することができる。
【００３５】
また、ラベンダーの由来及び産地も特に制限されず、フランス、イタリア、イギリス、ロシア、オーストラリア、北アメリカ、北海道などのいずれのものであってもよい。
【００３６】
ラベンダーの抽出物は、リナロールを５〜６０重量％、好ましくは２０〜４５重量％の範囲で含むか、又はリナリルアセテートを５〜８０重量％、好ましくは２０〜７０重量％の範囲で含むものであれば、それに含まれる他の成分及びそれらの配合割合等は特に制限されるものではない。
【００３７】
本発明の外用組成物は、特に制限されないが、かかるラベンダーの抽出物を、０．０１〜１重量％、好ましくは０．０５〜０．５重量％、より好ましくは０．１〜０．３重量％の割合で含有していることが望ましい。
【００３８】
本発明で吸熱性組成物とは、水を必須の成分として含有する組成物であって、水分が蒸発する際の潜熱放出に基づいて吸熱作用を発揮する含水組成物を広く意味する。かかる組成物に基づいて本発明の組成物は、常に室温よりも低い温度に保たれており、被験物を冷却する作用を有する。
【００３９】
吸熱性組成物に含まれる水分含量は、特に限定はされないが、本発明の最終組成物１００重量部に含まれる水分含量として、３０〜９５重量部、好ましくは４０〜９５重量部、より好ましくは５０〜９５重量部、一層好ましくは７５〜９５重量部を例示することができる。
【００４０】
本発明で用いられる吸熱性組成物の成分は、上記特性を有するものであれば特に制限されないが、本発明の外用組成物をクリーム、ゲル、軟膏、硬膏、ローション、乳液等の外用剤、好ましくはクリーム、ゲル又は軟膏として調製できるものであることが望ましい。好ましくは、本発明の外用組成物を、抱水性、放湿性、自己保形性又は粘着性を有するゲル状物として調製できる成分を有することが望ましい。
【００４１】
なお、ここで「抱水性」とは、内部に水を安定的に含む性質を意味するが、より好ましくはさらに圧縮しても含有水分を滲出しない性質を意味する。
【００４２】
また「自己保形性」とは、流動性や崩壊性を顕著には生じず形状を保持している性質を意味する。
【００４３】
水を含んでかかる性質を奏し得る成分としては、第一に、一般にゲル化剤として用いられる多糖類を例示することができる。
【００４４】
具体的には、カラギーナン、アルギン酸、アルギン酸プロピレングリコールエステル、タラガム、ローカストビーンガム、グルコマンナン、キサンタンガム、ジェランガム、ペクチン、プルラン等の天然ガム類を挙げることができる。これらは単独若しくは２種以上の組み合わせて用いることができる。好ましくはグルコマンナン、ローカストビーンガムを例示することができる。
【００４５】
これらの多糖類は、本発明の外用組成物１００重量部当たりに換算して、通常０．１〜１０重量部、好ましくは０．２〜５重量部、より好ましくは０．５〜３重量部の割合で配合されることが望ましい。
【００４６】
吸熱性組成物は、上記多糖類に加えて多価アルコールを含有していてもよい。
【００４７】
多価アルコールは、ラベンダー精油等の油性成分を水に分散・乳化させるときのバインダーにもなり、さらに湿潤性の付与、使用感向上に寄与する。
【００４８】
多価アルコールとしては、直鎖状や分枝状等の形状及び分子量等によって特に制限されず、被着体（冷却対象体）又は被着物（冷却対象物）に対して安全なものであれば通常使用されるもののいずれをも使用することができる。具体的にはグリセリン、エチレングリコール、ジエチレングリコール、トリエチレングリコール、ポリエチレングリコール、プロピレングリコール、ブチレングリコール、等が例示され、中でもグリセリン（濃グリセリンを含む。）、プロピレングリコール、ブチレングリコールが好適に挙げられる。
【００４９】
これらの多価アルコールは、本発明の外用組成物１００重量部当たりに換算して、通常０．１〜３０重量部、好ましくは５〜２０重量部の割合で配合されることが望ましい。
【００５０】
更に、必要に応じてマンニット、エリトリット等の糖アルコール、又はトレハロース等の糖類を配合することもできる。
【００５１】
また必要に応じて界面活性剤を配合してもよい。界面活性剤は、その種類の別を問わず、本発明の外用組成物に配合されるリナロール又はリナリルアセテートや、精油に含まれる各種香料成分の種類に応じて、陽イオン系，陰イオン系，両性イオン系及び非イオン系といった界面活性剤の中から適宜選択して用いることができる。なお、これらの界面活性剤は１種を単独で使用しても２種以上を組み合わせて用いてもよい。
【００５２】
水を含んで、抱水性、放湿性、自己保形性を奏し得る成分として、第二に、ポリアクリル酸類及び多価金属類を挙げることができる。
【００５３】
なお、ここでポリアクリル酸類とは、ポリアクリル酸のみならずその塩を包含する趣旨で用いられる。
【００５４】
ポリアクリル酸又はポリアクリル酸塩としては、直鎖状又は分枝状の別を問わず、またその分子量も特に制限されないが、通常分子量１万〜１０００万のものが用いられる。ゲル強度を高めてより多くの水分を安定的に保持させるという観点からは、特に１００万〜７００万の分子量のものが望ましい。
【００５５】
なお、ポリアクリル酸として、通常のアクリル酸を重合して得られる重合体のほか、カルボキシビニルポリマー（例えば、カーボポール（登録商標）等）等のアクリル酸重合体を一部架橋したものや、ポリビニルアルコール等も好適に使用し得る。
【００５６】
ポリアクリル酸の塩としては、特に制限はないが、好適にはポリアクリル酸ナトリウム、ポリアクリル酸カリウムなどのポリアクリル酸の一価金属塩、ポリアクリル酸モノエタノールアミン、ポリアクリル酸ジエタノールアミン、ポリアクリル酸トリエタノールアミン等のポリアクリル酸のアミン類、ポリアクリル酸のアンモニウム塩等が例示される。これらは単独で使用してもよいし、２種以上組み合わせて用いることもできる。より好ましくは、ナトリウム塩である。
【００５７】
上記ポリアクリル酸及びポリアクリル酸の塩は、それぞれ単独で使用しても、またそれらを組み合わせて用いることもできる。分子量が１００万以上のポリアクリル酸は一般的に入手が困難であることから、ポリアクリル酸とポリアクリル酸の塩（例えば、ナトリウム塩）を併用して用いる方が望ましい。但し、将来分子量１００万以上のポリアクリル酸の入手が容易になれば、この限りではない。
【００５８】
ポリアクリル酸とポリアクリル酸の塩とを併用する場合のそれらの配合比は、平均分子量が２００万以上、好適には４００万以上になるように調整されれば特に制限されないが、具体的には０：１０〜９：１（重量比）好ましくは２：１〜１：２（重量比）の割合が例示される。
【００５９】
ポリアクリル酸及び／又はポリアクリル酸の塩は、本発明の外用組成物１００重量部あたりに換算して、通常１〜２０重量部、好ましくは３〜１０重量部の割合で配合されることが望ましい。
【００６０】
また、本発明で多価金属類とは、多価金属、その塩及び多価金属化合物を広く包含する趣旨で用いられる。
【００６１】
これらの多価金属類としては、二価以上であって上記ポリアクリル酸又はポリアクリル酸の塩を架橋せしめるものであれば特に制限されず、また一種のみならず二種以上を組み合わせて使用することもできる。
【００６２】
好適にはマグネシウム、カルシウム、亜鉛、カドミウム、アルミニウム、チタン、マンガン、コバルト、ニッケルなどの多価金属、それらの塩又はそれらの化合物が例示されるが、皮膚に対する安全性、生産性、ゲル特性の観点からより好ましくはアルミニウム、マグネシウム、カルシウム又はそれらの化合物であり、とりわけアルミニウム化合物が望ましい。
【００６３】
例えばアルミニウム化合物としては、具体的には水酸化アルミニウムのような水酸化物、あるいは塩化アルミニウム、硫酸アルミニウム、酢酸アルミニウム、ステアリン酸アルミニウムのような無機酸又は有機酸の正塩、もしくはそれらの塩基性塩、アルミニウムみょうばんのような複塩、アルミン酸ナトリウムのようなアルミン酸塩、無機性アルミニウム錯塩及び有機性アルミニウムキレート化合物などが例示される。これらのアルミニウム化合物は、水溶性、難溶性の別を問わない。
【００６４】
これらの多価金属類は、本発明の外用組成物１００重量部あたりに換算し、通常０．０１〜１０重量部、好ましくは０．０５〜１重量部、より好ましくは０．１〜０．５重量部の割合で配合されることが望ましい。
【００６５】
上記吸熱性組成物は、上記成分を含有するものであればよいが、さらに(i)酒石酸，クエン酸，リン酸，エチレンジアミン四酢酸又はそれらの塩の少なくとも１種、(ii)多価アルコール及び(iii)セルロース誘導体からなる群から選択されるいずれか少なくとも１種を含んでいてもよい。
【００６６】
酒石酸，クエン酸，リン酸，エチレンジアミン四酢酸の塩としては、ナトリウムやカリウム等のアルカリ金属塩を好適に例示することができる。好適には酒石酸である。
【００６７】
これらの酸又はその塩は、本発明の外用組成物１００重量部あたりに換算して、０．０１〜２重量部、好ましくは０．０５〜１重量部、より好ましくは０．１〜０．５重量部の範囲から適宜選択して用いられる。
【００６８】
多価アルコールとしては、多糖類と組み合わせて用いられるものを同様に挙げることができる。好適には、グリセリン（濃グリセリンを含む。）、プロピレングリコール及びブチレングリコールが挙げられる。これらの多価アルコールは、湿潤性の付与や使用感向上に寄与するとともに、ポリアクリル酸又はその塩等の分散媒として有用である。
【００６９】
これらの多価アルコールは、最終組成物１００重量部あたりに換算して、０〜３０重量部、好ましくは１０〜２０重量部の範囲から適宜選択して用いられる。
【００７０】
セルロース誘導体は、非ニュートン流体を示す本発明の組成物の加工性を良好にし、ゲルの安定化を向上させ、また粘度の調整を簡便にする点で有用である。
【００７１】
使用されるセルロース誘導体としては特に制限されないが、具体的には、カルボキシメチルセルロースのアルカリ金属塩、ヒドロキシメチルセルロース、ヒドロキシエチルセルロース、ヒドロキシプロピルセルロース、メチルセルロース等が挙げられ、これらを１種又は２種以上組み合わせて用いることもできる。好適には、カルボキシメチルセルロース（以下、ＣＭＣともいう。）が挙げられる。
【００７２】
これらセルロース誘導体は、最終組成物１００重量部当たり、０．０１〜１０重量部、好ましくは０．１〜５重量部の範囲から適宜選択して用いられる。
【００７３】
また必要に応じて界面活性剤を配合することができる。界面活性剤は、前述するようにその種類の別を問わず、本発明の外用組成物に配合される各種香料成分の種類に応じて、陽イオン系，陰イオン系，両性イオン系及び非イオン系といった界面活性剤の中から適宜選択して用いることができる。これらの界面活性剤は１種を単独で使用しても２種以上を組み合わせて用いてもよい。
【００７４】
なお、本発明の外用組成物には、前述する各成分に加えて必要に応じて、更に防腐剤、保湿剤、刺激緩和剤、除菌剤、抗菌剤等を配合することができる。
【００７５】
前述する多糖類またはポリアクリル酸類及び多価金属類を吸熱性組成物の成分として用いて調製される本発明の外用組成物は、とりわけ、組成物１００重量部あたり７５重量部以上、好ましくは７５〜９５重量部という高い含水率で水分を有することができる。組成物に含まれる水分は冷却作用の本源であることから、このような高含水性の本発明組成物は吸熱効果、冷却効果に優れるものである。
【００７６】
さらに当該組成物は、多量の水分を安定的に保持することができ、このため圧縮しても含有水分を滲出することがないうえ、９５重量部という高含水率を有していても、稠度の低下により流動状態になるということがなく、この点で自己保形性に優れるという特性を有している。また、高い含水状態であっても適度な弾力性を有し、またそれ自体強い粘着性を有しているため、他の粘着テープ等の補助材を使用することなく簡便に被着体に貼付できる。また、被着体を問わず簡便に剥がすことができ、しかも被着体に剥がし残りを残さず、また安全性が高いという点で有用である。
【００７７】
本発明の外用組成物を身体に直接若しくは間接的に塗布若しくは貼付すると、体温によって組成物中に含まれるリナロール、リナリルアセテートといったラベンダー類抽出物に含まれる成分が揮散して鼻腔に効果的に作用し、神経をリラックスさせるとともに、末梢皮膚血流量を増加させて皮膚からの放熱を促進し、これにより体内深部の体温が下降する入眠時の生体リズムに導いて入眠を促すことができる。また、本発明の外用組成物は、経時的に表面から含有水分が蒸発するため、該蒸発時の潜熱放出に基づいて吸熱作用を有する。よってかかる組成物を就寝時に皮膚に塗布若しくは貼付すれば、被着皮膚から気化潜熱の形で熱を奪うことにより上記の体内放熱作用を補助・促進して、スムーズな入眠を促すことができる。
【００７８】
本発明の外用組成物は、特に不安、過労、憂鬱、興奮などといった精神的原因に基づく不眠若しくは入眠障害、生体リズムの変調に基づく不眠若しくは入眠障害等に有用である。
【００７９】
本発明の外用組成物の適用部位は、特に制限されるものではないが、ラベンダーの揮発成分を鼻腔に作用させて効果を生じさせるという目的からは、好ましくは鼻に近い上半身の領域部であり、より好ましくは胸部または顔面・頭部、特に額部である。
【００８０】
かかる特性に基づいて、本発明はさらに、上記外用組成物を一定形態に成形してなる貼付剤を提供する。
【００８１】
形態は特に限定されないが、取扱い易さ、携帯、保管等の面からシート状が好ましい。かかるシート状の貼付剤は、上記外用組成物そのものをシート状に展延したり、また液状の組成物をシート状基材に含浸したり、軟膏状、クリーム状若しくはゲル状の組成物をシート状基材に塗布・展延することによって調製することができる。
【００８２】
ここでシート状の基材としては、本発明の外用組成物を担持できるものであって、ラベンダー抽出物等の揮発成分の透過及び外用組成物の放湿性を妨げないように適度な透過・透湿性を有するものであれば特に制限はなく、種々の織布、不織布及びフィルム等を使用することができる。上記性質を有する限り、シート状基材の開孔径については特に制限はないが、通常０．００１〜５ｍｍ程度、好ましくは０．０１〜１ｍｍ程度を挙げることができる。
【００８３】
基材として織布もしくは不織布を使用する場合、その素材は特に制限されず、綿、麻、羊毛などの天然繊維、レーヨン、アセテート等のセルロース系繊維、ナイロン、ビニロン、スチロール、ポリプロピレン、ポリエチレン、ポリエチレンテレフタレート、アクリル等の合成繊維、綿、麻、毛等の天然繊維等を挙げることができる。
【００８４】
基材としてフィルムを使用する場合も、その素材は特に制限されないが、具体的にはスチロール、ポリプロピレン、ポリエチレンテレフタレート、ポリエチレン等が挙げられる。この場合、適度な透過・透湿性を担保するためにメッシュ状のフィルムを用いることもできる。メッシュの孔径は特に制限されないが、上述するように通常０．００１〜５ｍｍ、好ましくは０．０１〜１ｍｍの孔径を挙げることができる。
【００８５】
上記シート状基材の厚みについても、外用組成物の放湿性等を妨げない限りにおいて特に制限はないが、使用感、貼付部位への馴染み易さ等の観点から、通常１〜１０００μ、好ましくは１０〜５００μである。
【００８６】
また、当該基材は、貼付剤を皮膚に貼着した場合に貼着部位の外形状になじむように、適度な伸縮性を有することが好ましい。
【００８７】
かかるシート状基材の上に塗布・展延されて積層されてなる外用組成物の厚みは特に制限されないが、使用感、吸熱量等の観点から、通常１〜７ｍｍ、好ましくは４〜５ｍｍである。
【００８８】
本発明の貼付剤は、基本的には、外用組成物、又は外用組成物及びシート状基材からなるが、取り扱い性や衛生上の観点から、更に必要に応じて、使用時に剥離除去される剥離フィルムを外用組成物表面に積層しておくこともできる。
【００８９】
かかる剥離フィルムとしては、ポリエステル、ポリプロピレン、ポリエチレン、ナイロン、塩化ビニル、ポリエチレンテレフタレートなどを使用することができる。
【００９０】
また、本発明の貼付剤は、大きさも特に制限されず、貼着場所等に応じて適宜選択・調製することができる。
【００９１】
本発明の貼付剤は、前述の外用組成物を用いて、従来公知の方法に従って製造することができ、例えば本発明組成物を剥離シートの上に均一に展延塗布し、その上にシート状基材を重ねる方法が挙げられる。この場合、より一層強度に定着させるために該積層物をローラーによって加圧することもできる。
【００９２】
本発明の外用組成物及び貼付剤は、就寝時に胸部又は額等の顔・頭部の皮膚に塗布又は貼着して用いられて、スムーズな入眠を促す補助剤または睡眠導入剤として有用である。
【００９３】
【実施例】
以下、本発明の内容を以下の実施例、比較例及び実験例を用いて具体的に説明するが、本発明はこれらに何ら限定されるものではない。
【００９４】
実施例１
下記の処方に従って、本発明の外用組成物を調製した。
【００９５】
２．ポリアクリル酸ナトリウム、水酸化アルミニウムゲル、メチルパラベン、ラベンダーを混合し、１．の撹拌機の中に粉塊をつくらないように添加する
３．添加後、混合物をほんの数分間真空脱泡する。
【００９６】
実施例２
下記の処方に従って、本発明の外用組成物を調製した。
【００９７】
２．約半分量の精製水を１．の中にダマができないように加える
３．他の成分を順次加えていき、最後に残りの精製水を加える。
【００９８】
実施例３
下記の処方に従って、本発明の外用組成物を調製した。
【００９９】
２．ポリアクリル酸ナトリウム、水酸化アルミニウム、ラベンダー抽出物を濃グリセリンに混合する
３．２．の中に１．を徐々に撹拌混練しながら加える
４．添加後、混合物をほんの数分間真空脱泡する。
【０１００】
実施例４
下記の処方に従って、本発明の外用組成物を調製した。
【０１０１】
２．ポリアクリル酸ナトリウム、水酸化アルミニウム、ラベンダー抽出物を混合し、１．の撹拌機に粉塊を作らないように添加する
３．添加後、混合物をほんの数分間真空脱泡する。
【０１０２】
実施例５
下記の処方に従って、本発明の外用組成物を調製した。
【０１０３】
２．ポリアクリル酸ナトリウム、水酸化アルミニウム、ラベンダー、メチルパラベンをグリセリンに混合する
３．２．を１．の撹拌機に粉塊を作らないように添加する
４．添加後、混合物をほんの数分間真空脱泡する。
【０１０４】
実施例６〜９
実施例１〜５（実施例６〜１０にそれぞれ対応する）で調製された各外用組成物を、０．１〜１ｍｍ孔径のメッシュ状のシート基材（ＰＥＴ製）にそれぞれ展延し、適当な大きさ（５×１３ｃｍ）に裁断してアルミニウム製の袋の中に密封してシート状の貼付剤（パップ剤）を調製した。
【０１０５】
【実験例】
実験例１
実施例３で調製した外用組成物を不織布に展延して３ｃｍ×３ｃｍに裁断して貼付剤を調製し、これを３７℃の温熱板に貼付し、該温熱板を一定温度（３７℃）に保つための必要な熱量を経時的に測定した。結果を図１に示す。
【０１０６】
実験例２
実験例１で用いた貼付剤をそれぞれ６人のモニターの額に貼付して、該額部分の降下温度を測定してその平均値を求めた。結果を表１に示す。
【０１０７】
【表１】
これらの結果から、本発明の組成物及び貼付剤が冷却効果、冷却持続性に優れていることが認められた。
【０１０９】
実験例３
寝付きが悪く入眠障害を訴える成人からランダムに３名を選択し、これらを被験者として、実施例６で調製した貼付剤（パップ剤）を就寝時に額に貼付してもらい、睡眠に対する影響を検討した。
【０１１０】
催眠効果は下記の評価項目について、実験実施以前の状態と比較して５段階で評価した。
【０１１１】
・評価項目：安眠感
評価：(1)ある (2)ややある (3)どちらとも言えない (4)あまりない
(5)ない
・評価項目：寝付きのよさ
評価：(1)良かった (2)やや良かった (3)わからない (4)やや悪かった
(5)悪かった
結果を表２に示す。
【０１１２】
【表２】
表からわかるように、被験者のいずれに対しても本発明の貼付剤の使用によって催眠効果が認められた。
【０１１４】
実験例４
下記（１）〜（３）の試験により、ラベンダー香気の吸入及び本発明の貼付剤の使用による、精神安定性（（１）クレペリンテスト、（２）脳波測定）及び末梢皮膚温の上昇を調べた。
【０１１５】
（１）クレペリンテスト
被験者に計算作業を連続的に行ってもらうことにより、作業効率、正解率の変化から、精神安定効果を評価することができる。そこで、２４〜３２才の健常成人１５名から構成されるグループを二群つくり、ラベンダー精油を含浸して調製した臭い紙から常温にてラベンダー香気が揮散している部屋と、香りのない部屋とに分かれてもらって、それぞれの部屋において下記に示す作業を行ってもらった。前者をＡ群、後者をＢ群とする。
【０１１６】
＜作業内容＞
作業は、用紙に印字されている数字を隣同士で加算した後、答えの下１桁の数字を「行間・加算した文字間」に鉛筆で記入していくものである。検査者の号令に従って、１分毎に行を変えながら記入用紙（表／裏両方に数字が印字されてある）の表裏について１５分ずつ行う。１分間を１作業とし、連続して１５回を１セットとした（前半１５分→休憩１０分→後半１５分）。午前と午後の作業効率の違いを見るため、午前と午後の１日２回実施した。結果を図２に示す
香りの無い部屋で作業を行ったＢ群は、前半の作業に比べて後半の作業は正解率が低下する（９９．６％→９９．３８％）に対して、香気が揮散する部屋で作業するＡ群は、後半の作業の正解率が前半に比べて増加する（９９．６３％→９９．８３％）ことが認められた。このことから、ラベンダー精油の香気成分の吸入により、精神安定が得られることが認められた。
【０１１７】
（２）脳波測定
脳波は、脳の神経細胞の活動を電気的にとらえるものであり、その中でもα波は脳波の成分の一つで、一般に、ヒトが自覚的に「気持ちが落ち着く」という印象をもったときの安静状態では、α波の出現量が増加することが知られている（「香料が脳機能に与える影響」フレグランス・ジャーナル、１９８９年第９号、第２０〜２６頁）。従って、脳波のα波出現量を測定することにより安静効果を評価することができる。
【０１１８】
＜実験方法＞
実験は、恒温恒湿室にて、被験者６名を対象として行った。
【０１１９】
まず被験者を２０分間安静にさせた後、各被験者の額に実施例６で調製した貼付剤（パップ剤）を貼って３分間放置し、その後３分間のα波の出現量をBio amp 0523S（エヌ・エフ回路製）を用いて測定した。なお、実施例６で調製した貼付剤（パップ剤）は、貼付後直ちにラベンダーの香りがしだした。
【０１２０】
具体的には被験者の額に２点の電極を装着し、その２点における脳波を測定し高速フーリエ変換後、８〜１３Ｈｚのα波出現量を抽出した。対照実験として、各被験者について貼付剤（パップ剤）を貼付する前に、同様にα波出現量の測定を行った。
【０１２１】
＜結果＞
結果を、対照実験と比較して図３に示す。
【０１２２】
なお、図３中Ａは８〜１３ＨＺの脳波を解析し、さらに８〜１３ＨＺ域内の詳細なα波分布を示したものである。図Ａは覚醒状態において、貼付剤（パップ剤）貼付直後にα波の分布が１０〜１２ＨＺへと移行してきていることを示す。このことから、貼付剤の使用により鎮静効果が得られることがわかる。図３中Ｂは、α波の総出現量を貼付剤（パップ剤）有りと無しとで比較した図である。図中の数値（指数）はα波出現量の増加を確認するための指標であり、これから本発明の貼付剤の貼付によってα波の出現が増加することがわかる。図３中Ｃは、全脳波（８〜１３ＨＺ領域以外の領域の脳波も含む）中に占めるα波の割合を貼付剤（パップ剤）有りと無しとで比較した図である。これからも本発明のパップ剤の貼付によってα波の出現が増加することがわかる。
【０１２３】
以上の結果から明らかなように、本発明の貼付剤を貼付することによってα波の出現量が増加し、本発明の貼付剤の使用によって精神安定化効果が得られることが認められた。
【０１２４】
（３）末梢皮膚表面温度の上昇
＜実験方法＞
被験者６名を対象として、恒温恒湿室にて額に実施例６で調製した貼付剤（パップ剤）を貼り、サーモグラフによって手のひらの温度分布を測定した。
【０１２５】
まずコントロール実験として、各被験者を２０分間リラックスさせて体温が落ち着くのを確認して、開眼状態で３分間（安静前、図Ａ中点線で示す）、更に続けて閉眼状態で３分間（安静後、図Ａ中実線で示す）、手のひらの温度分布を測定した。
【０１２６】
次いで、その３０分間後、再び被験者をリラックスさせて体温が落ち着くのを確認し、それから開眼状態で３分間（安静前、図Ｂ中点線で示す）、その後額に貼付剤を貼って更に閉眼状態で３分間（安静後、図Ｂ中実線で示す）、手のひらの温度分布を測定した。
【０１２７】
それぞれの結果を図４に示す。
【０１２８】
貼付剤を貼らない条件下での安静状態は、安静前に比べて温度分布が隆起しただけであったが、貼付剤を貼った条件下での安静状態では安静前に比べて温度分布が右側（高温部）にシフトし、皮膚表面の温度が上昇しているのが観察された。また、貼付剤を使用した場合の温度分布は（図Ｂ実線）、貼付剤を使用しない場合（図Ａ実線）の温度分布よりも、高温部での隆起が著しかった。このことは、本発明の貼付剤の使用によって、末梢皮膚の血流量が増加して放熱が生じていることを意味する。
【図面の簡単な説明】
【図１】実験例１において、本発明の貼付剤の消費熱量を測定した結果を示す図である。横軸は測定時間（時間）を、縦軸は温熱板を３７℃に一定に保つために必要な熱量（×１０-4）（cal/cm2・sec・℃）を示す。
【図２】実験例４（１）で行ったクレペリンテストをラベンダー香気存在下、非存在下で行った結果を比較した図である。
【図３】実験例４（２）で行った、本発明の貼付剤の使用によるα波出現量を、貼付剤を使用しない場合と比較した図である。図中Ａは８〜１３ＨＺの脳波を解析し、さらに８〜１３ＨＺ域内の詳細なα波分布を示したものである。図中Ｂは、α波の総出現量をパップ剤貼付有りと無しとで比較した図である。図中Ｃは、全脳波（８〜１３ＨＺ領域以外の領域の脳波も含む）中に占めるα波の割合をパップ剤貼付有りと無しとで比較した図である。
【図４】実験例４（３）で行った、本発明の貼付剤の使用による末梢皮膚温上昇を示す図である。図中Ａは貼付剤を貼付しない状態で、安静前（３分間、点線）と安静後（３分間、実線）における末梢皮膚温を測定した結果を示す。また図中Ｂは、安静前（３分間）に貼付剤のない状態で末梢皮膚温を測定した結果（３分間、点線）と、それから貼付剤を貼付した状態で末梢皮膚温を測定した結果（３分間、実線）を示す。[0001]
BACKGROUND OF THE INVENTION
The present invention relates to an external composition containing at least one of linalool or linalyl acetate in an endothermic composition, and a patch containing the same.
[0002]
Moreover, this invention relates to the use as a sleep induction agent of the said external composition and patch.
[0003]
[Prior art]
Conventionally, sleep-inducing drugs such as tranquilizers are used to treat insomnia, but these drugs are deleterious and have many side effects such as tolerance due to continuous use and rebound insomnia. Even benzodiazepine drugs, which are said to have relatively few side effects, have reported side effects such as anterograde amnesia and a tendency to cause a waxy state after taking the drug. Is required.
[0004]
By the way, according to aromatherapy, which has been known for a long time mainly in the European region, pharmacological and psychological therapy with various essential oil scents is widely reported ("Practical aromatherapy" by Sharri Price, Taro Takayama Hayashi). (Translation, 1987) ("Aromatherapy": Robert Tisland, translated by Taro Takayama, 1985), and in various research fields, there have been many reports on the effects of fragrance on physiological and psychological states [Chemistry Technical Journal, August 1990; Fragrance Journal, No. 86, 1987; Fragrance Journal, No. 77, 16, 1986; Japanese Journal of Neuropsychopharmacology, Vol. 15, 39-42, 1995; FOOD & FOOD INGREDIENTS JOURNAL No.156, 1993 etc.). In addition, there are reports of Japanese Patent Application Laid-Open Nos. 4-128234 and 4-149136 regarding the effect of sleeping by the essential oil used in aromatherapy.
[0005]
In such aromatherapy (aroma therapy), lavender essential oil is often used because of its high safety in addition to its sedative, bactericidal, anti-inflammatory, antitussive and relaxing effects. .
[0006]
However, Japanese Patent Laid-Open No. 4-149136 (Patent Publication No. 13,
[0007]
[Problems to be solved by the invention]
The present invention was developed in view of such circumstances, and contains at least one of linalool or linalyl acetate contained in lavender essential oil or the like in the endothermic composition.HaveIt is an object of the present invention to provide an external composition having a cooling action and a sedative action. The composition for external use is useful as a sleep aid or sleep inducer that exerts a hypnotic effect when applied to the human forehead and chest.
[0008]
Another object of the present invention is to provide a patch obtained by laminating the above external composition on a sheet-like substrate.
[0009]
[Means for Solving the Problems]
In order to solve the above-mentioned problems of the prior art, the present inventors have conducted various studies focusing on a savory and highly safe lavender extract. As a result, the lavender extract or its volatile component is endothermic. When applied to the upper body, especially the head, face, or chest, the volatile component of lavender acts effectively from the nasal cavity depending on body temperature, and is combined with the cooling action of the external preparation. He stumbled and found that sleep was guided smoothly. The present invention has been developed based on such knowledge.
[0010]
That is, this invention is an external composition shown to following (1)-(8).
[0011]
(1) An external composition containing at least one of linalool or linalyl acetate in an endothermic composition.
[0012]
(2) The amount of linalool contained in 100 parts by weight of the final composition is 0.0005 to 0.6 parts by weight, and the amount of linalyl acetate is 0.0005 to 0.8 parts by weight (1) The external composition as described.
[0013]
(3) The composition for external use according to (1) or (2), wherein an extract of lavender is contained in the endothermic composition.
[0014]
(4) The external composition according to any one of (1) to (3), wherein the final composition contains water in a proportion of 30 to 95%.
[0015]
(5) The composition for external use according to any one of (1) to (4), wherein the endothermic composition is a composition containing a polysaccharide and water.
[0016]
(6) The composition for external use according to any one of (1) to (4), wherein the endothermic composition is a composition containing polyacrylic acids, polyvalent metals and water.
[0017]
(7) The composition for external use according to (5) or (6), wherein the endothermic composition further comprises a polyhydric alcohol.
[0018]
(8) The endothermic composition is a composition further comprising (i) at least one of tartaric acid, citric acid, phosphoric acid, ethylenediaminetetraacetic acid or a salt thereof, or (ii) a cellulose derivative. (6) or (7) external composition.
[0019]
These external compositions can be used as sleep-inducing agents.
[0020]
Furthermore, this invention is a patch which has the composition for external use in any one of the said.
[0021]
As mentioned above, there has been no report that lavender essential oil and volatile components contained therein have a sleep-inducing action or a hypnotic action.
[0022]
According to further studies by the inventors, the composition for external use of the present invention relaxes the central nervous system by effectively inhaling the volatile components contained in lavender oil from the nasal cavity, and further, the peripheral skin blood flow It has been found that the peripheral skin temperature is increased by increasing the temperature, and heat release from the deep part of the body is promoted.
[0023]
Conventionally, it is known that there is a certain correlation between body temperature and sleep rhythm. That is, the peripheral skin temperature begins to rise prior to falling asleep, and the rectal temperature falls slightly later, and this state continues during sleep (general clinical Vol.34 extra number (1985), 14-16). In addition, it has been pointed out that the mechanism that increases skin blood flow and dissipates heat in the deep part of the body is involved in the onset of body temperature rhythm during sleep (Damm, F., Doring, G., "Body temperature and circadian rhythm" (1973).
[0024]
The composition for external use of the present invention induces a sleep closer to nature by artificially bringing the human biological rhythm to such a natural body temperature rhythm during sleep. Moreover, the composition for external use of the present invention assists the heat dissipation mechanism of the living body by cooling the skin surface, and thereby can bring the sleep smoothly by bringing it closer to the biological rhythm during sleep. Furthermore, according to the composition for external use of the present invention, a sedative action can be given to humans by the action of volatile components of lavender such as linalool that has been volatilized by body temperature, and a peaceful sleep can be brought about from a mental aspect.
[0025]
DETAILED DESCRIPTION OF THE INVENTION
The composition for external use of the present invention contains at least one of linalool or linalyl acetate in an endothermic composition.
[0026]
The linalool used in the present invention may be any linalool that exists widely in nature, and does not ask whether the terpinolene form or limonene form is different from the structural isomer or d form or l form. Preferably, mention may be made of l-linalool which is the same as linalool present in lavender oil. Similarly, linalyl acetate may be any linalyl acetate that exists widely in nature. In addition, these are not limited at all by the origin of acquisition.
[0027]
The proportion of linalool contained in the external composition of the present invention is 0.0005 to 0.6 parts by weight, preferably 0.002 to 0.45 parts by weight, more preferably 0.003 to 100 parts by weight of the final composition. 0.4 parts by weight.
[0028]
The ratio of linalyl acetate contained in the composition for external use of the present invention is 0.0005 to 0.8 parts by weight, preferably 0.002 to 0.7 parts by weight, more preferably 0.003 per 100 parts by weight of the final composition. -0.6 parts by weight.
[0029]
In the composition of the present invention, these components may be blended alone or in combination of two kinds.
[0030]
Among the linalools, d-linalool is generally contained in essential oils such as Mexican linaloe oil, bored rose oil, coriander oil and oyakoju, and l-linalool is generally contained in essential oils such as pepper oil, lavender oil and bergamot oil. Furthermore, linalyl acetate is generally contained in essential oils such as lavender oil, bergamot oil, petitgren oil, jasmine oil, ylang ylang oil, lemon oil and the like. Therefore, in the present invention, these essential oils can be used as the above linalool and / or linalyl acetate as long as the effects of the present invention are not inhibited.
[0031]
A preferred example of such essential oil is lavender oil. In addition to linalyl acetate and l-linalool, lavender oil contains several hundred ingredients such as geraniol, lavandol, nerol, α-pinene, caryophyllene, 1,8-cineole, camphene, l-limonene, dipenene. . Although these lavender oil components may work cooperatively with the effects of the present invention, it is recognized that they do not inhibit the effects of the present invention.
[0032]
Lavender oil can generally be obtained, for example, by steam distillation of lavender spikes or extraction with a solvent such as hexane, petroleum ether or alcohol.
[0033]
Accordingly, the composition for external use of the present invention may be a composition containing the lavender extract extracted as described above alone or in combination of two or more thereof in the endothermic composition.
[0034]
The lavender used in the present invention broadly includes those belonging to the genus Lavender of Lamiaceae and their variants. In general, lavender is classified into (1) Spica-type lavender group, (2) French lavender group, and (3) Fern lavender group (3) Fern-like lavender group, Pterostachys lavender), and (1) is common lavender (Lavandula angustifolia Mill. And its cultivars), lavandin (Lx intermedia Emeric ex Loisel. (Lavandula hybrida Reverchon ex Briq., L. hortensis Hy)) and other strains (for example, spike lavender (L. latifolia Medik. (L. spica auct., Non L.), etc.)). The invention can use any of these lavenders.
[0035]
Moreover, the origin and production area of lavender are not particularly limited, and may be any of France, Italy, United Kingdom, Russia, Australia, North America, Hokkaido, and the like.
[0036]
The lavender extract contains 5 to 60% by weight of linalool, preferably 20 to 45% by weight, or 5 to 80% by weight, preferably 20 to 70% by weight of linalyl acetate. If there are, other components contained therein and the blending ratio thereof are not particularly limited.
[0037]
Although the composition for external use of the present invention is not particularly limited, the lavender extract is 0.01 to 1% by weight, preferably 0.05 to 0.5% by weight, more preferably 0.1 to 0.3%. It is desirable to contain it in the ratio of weight%.
[0038]
In the present invention, the endothermic composition is a composition containing water as an essential component, and broadly means a water-containing composition that exhibits an endothermic action based on the release of latent heat when water evaporates. Based on such a composition, the composition of the present invention is always kept at a temperature lower than room temperature, and has an action of cooling the test object.
[0039]
The water content contained in the endothermic composition is not particularly limited, but the water content contained in 100 parts by weight of the final composition of the present invention is 30 to 95 parts by weight, preferably 40 to 95 parts by weight, more preferably 50-95 weight part, More preferably, 75-95 weight part can be illustrated.
[0040]
The component of the endothermic composition used in the present invention is not particularly limited as long as it has the above-mentioned properties, but the external composition of the present invention is an external preparation such as cream, gel, ointment, plaster, lotion, and emulsion, preferably It is desirable that can be prepared as a cream, gel or ointment. Preferably, it is desirable that the composition for external use of the present invention has a component that can be prepared as a gel-like material having water repellency, moisture release, self-retaining property or adhesiveness.
[0041]
Here, “water-holding” means the property of stably containing water inside, but more preferably means the property of not exuding the contained water even when further compressed.
[0042]
“Self shape retention” means the property of maintaining the shape without causing significant fluidity or disintegration.
[0043]
As a component that can exhibit such properties including water, firstly, polysaccharides generally used as a gelling agent can be exemplified.
[0044]
Specific examples include natural gums such as carrageenan, alginic acid, propylene glycol alginate, tara gum, locust bean gum, glucomannan, xanthan gum, gellan gum, pectin, and pullulan. These can be used alone or in combination of two or more. Preferably, glucomannan and locust bean gum can be exemplified.
[0045]
These polysaccharides are usually 0.1 to 10 parts by weight, preferably 0.2 to 5 parts by weight, more preferably 0.5 to 3 parts by weight, based on 100 parts by weight of the composition for external use of the present invention. It is desirable to mix | blend in the ratio.
[0046]
The endothermic composition may contain a polyhydric alcohol in addition to the polysaccharide.
[0047]
The polyhydric alcohol also serves as a binder for dispersing and emulsifying oily components such as lavender essential oil in water, and further contributes to imparting wettability and improving the feeling of use.
[0048]
The polyhydric alcohol is not particularly limited by linear or branched shapes, molecular weights, and the like, and may be any one that is safe for an adherend (cooling target) or an adherend (cooling target). Any of the commonly used ones can be used. Specific examples include glycerin, ethylene glycol, diethylene glycol, triethylene glycol, polyethylene glycol, propylene glycol, and butylene glycol. Among them, glycerin (including concentrated glycerin), propylene glycol, and butylene glycol are preferable.
[0049]
These polyhydric alcohols are usually blended at a ratio of usually 0.1 to 30 parts by weight, preferably 5 to 20 parts by weight in terms of 100 parts by weight of the composition for external use of the present invention.
[0050]
Furthermore, sugar alcohols such as mannitol and erythrite, or sugars such as trehalose can be blended as necessary.
[0051]
Moreover, you may mix | blend surfactant as needed. Regardless of the type of the surfactant, linalol or linalyl acetate blended in the composition for external use of the present invention, and depending on the type of various perfume ingredients contained in the essential oil, cationic, anionic, The surfactant can be appropriately selected from zwitterionic and nonionic surfactants. In addition, these surfactants may be used individually by 1 type, or may be used in combination of 2 or more type.
[0052]
Secondly, polyacrylic acids and polyvalent metals can be cited as components that can contain water and can exhibit water retention, moisture release and self-retaining properties.
[0053]
Here, the polyacrylic acid is used to include not only polyacrylic acid but also a salt thereof.
[0054]
The polyacrylic acid or polyacrylic acid salt may be linear or branched, and the molecular weight is not particularly limited, but those having a molecular weight of 10,000 to 10,000,000 are usually used. From the viewpoint of increasing the gel strength and stably holding more water, a molecular weight of 1 million to 7 million is particularly desirable.
[0055]
As polyacrylic acid, in addition to a polymer obtained by polymerizing ordinary acrylic acid, a partially crosslinked acrylic acid polymer such as carboxyvinyl polymer (for example, Carbopol (registered trademark)), Polyvinyl alcohol etc. can also be used conveniently.
[0056]
The polyacrylic acid salt is not particularly limited, but is preferably a monovalent metal salt of polyacrylic acid such as sodium polyacrylate or potassium polyacrylate, monoethanolamine polyacrylate, diethanolamine polyacrylate, polyacrylate. Examples include amines of polyacrylic acid such as triethanolamine acrylate, ammonium salts of polyacrylic acid, and the like. These may be used alone or in combination of two or more. More preferably, it is a sodium salt.
[0057]
The polyacrylic acid and the polyacrylic acid salt can be used alone or in combination. Since polyacrylic acid having a molecular weight of 1,000,000 or more is generally difficult to obtain, it is desirable to use polyacrylic acid and a salt of polyacrylic acid (for example, sodium salt) in combination. However, this will not be the case if it becomes easy to obtain polyacrylic acid having a molecular weight of 1 million or more in the future.
[0058]
The blending ratio when polyacrylic acid and a polyacrylic acid salt are used in combination is not particularly limited as long as the average molecular weight is adjusted to 2 million or more, preferably 4 million or more. Is a ratio of 0:10 to 9: 1 (weight ratio), preferably 2: 1 to 1: 2 (weight ratio).
[0059]
The polyacrylic acid and / or the salt of polyacrylic acid is usually added at a ratio of 1 to 20 parts by weight, preferably 3 to 10 parts by weight, per 100 parts by weight of the external composition of the present invention. desirable.
[0060]
In the present invention, the polyvalent metals are used to broadly include polyvalent metals, salts thereof and polyvalent metal compounds.
[0061]
These polyvalent metals are not particularly limited as long as they are divalent or more and can crosslink the polyacrylic acid or the salt of polyacrylic acid, and are used alone or in combination of two or more. You can also
[0062]
Preferred examples include magnesium, calcium, zinc, cadmium, aluminum, titanium, manganese, cobalt, nickel and other polyvalent metals, their salts or their compounds. From the viewpoint, aluminum, magnesium, calcium or a compound thereof is more preferable, and an aluminum compound is particularly desirable.
[0063]
For example, as an aluminum compound, specifically, a hydroxide such as aluminum hydroxide, or a normal salt of an inorganic acid or an organic acid such as aluminum chloride, aluminum sulfate, aluminum acetate or aluminum stearate, or basicity thereof. Examples thereof include salts, double salts such as aluminum alum, aluminates such as sodium aluminate, inorganic aluminum complex salts and organic aluminum chelate compounds. These aluminum compounds may be water-soluble or hardly soluble.
[0064]
These polyvalent metals are usually 0.01 to 10 parts by weight, preferably 0.05 to 1 part by weight, and more preferably 0.1 to 0.00 parts per 100 parts by weight of the composition for external use of the present invention. It is desirable to blend in a proportion of 5 parts by weight.
[0065]
The endothermic composition may contain any of the above components, and (i) at least one of tartaric acid, citric acid, phosphoric acid, ethylenediaminetetraacetic acid or salts thereof, (ii) a polyhydric alcohol, and (iii) At least one selected from the group consisting of cellulose derivatives may be included.
[0066]
As salts of tartaric acid, citric acid, phosphoric acid and ethylenediaminetetraacetic acid, alkali metal salts such as sodium and potassium can be preferably exemplified. Tartaric acid is preferred.
[0067]
These acids or salts thereof are 0.01-2 parts by weight, preferably 0.05-1 part by weight, more preferably 0.1-0. It is appropriately selected from the range of 5 parts by weight.
[0068]
As polyhydric alcohol, what is used in combination with a polysaccharide can be mentioned similarly. Preferable examples include glycerin (including concentrated glycerin), propylene glycol, and butylene glycol. These polyhydric alcohols are useful as a dispersion medium for polyacrylic acid or a salt thereof while contributing to imparting wettability and improving the feeling of use.
[0069]
These polyhydric alcohols are used by appropriately selecting from the range of 0 to 30 parts by weight, preferably 10 to 20 parts by weight in terms of 100 parts by weight of the final composition.
[0070]
The cellulose derivative is useful in terms of improving the processability of the composition of the present invention showing a non-Newtonian fluid, improving the stabilization of the gel, and simplifying the adjustment of the viscosity.
[0071]
Although it does not restrict | limit especially as a cellulose derivative used, Specifically, the alkali metal salt of carboxymethylcellulose, hydroxymethylcellulose, hydroxyethylcellulose, hydroxypropylcellulose, methylcellulose etc. are mentioned, These are combined 1 type (s) or 2 or more types. It can also be used. Preferable examples include carboxymethyl cellulose (hereinafter also referred to as CMC).
[0072]
These cellulose derivatives are appropriately selected from the range of 0.01 to 10 parts by weight, preferably 0.1 to 5 parts by weight per 100 parts by weight of the final composition.
[0073]
Moreover, surfactant can be mix | blended as needed. As described above, the surfactant is a cationic, anionic, zwitterionic, or nonionic, depending on the type of various flavor components blended in the composition for external use of the present invention, regardless of the type. The surfactant can be appropriately selected from surfactants. These surfactants may be used alone or in combination of two or more.
[0074]
In addition to the above-described components, the composition for external use of the present invention may further contain a preservative, a moisturizing agent, a stimulating / relaxing agent, a disinfectant, an antibacterial agent, and the like as necessary.
[0075]
The composition for external use of the present invention prepared by using the aforementioned polysaccharides or polyacrylic acids and polyvalent metals as components of the endothermic composition is, in particular, 75 parts by weight or more, preferably 75 parts by weight per 100 parts by weight of the composition. It can have moisture at a high moisture content of ~ 95 parts by weight. Since the moisture contained in the composition is the main source of cooling action, such a highly hydrous composition of the present invention is excellent in endothermic effect and cooling effect.
[0076]
Further, the composition can stably hold a large amount of water, and therefore, even if it is compressed, it does not exude moisture, and even if it has a high water content of 95 parts by weight, it has consistency. It does not become a fluid state due to a decrease in the thickness, and in this respect, it has the property of being excellent in self-holding property. In addition, it has moderate elasticity even in a high water content state and itself has strong adhesiveness, so it can be easily attached to an adherend without using auxiliary materials such as other adhesive tapes. it can. Further, it is useful in that it can be easily peeled off regardless of the adherend, and the peel-off residue is not left on the adherend, and the safety is high.
[0077]
When the composition for external use of the present invention is applied or applied directly or indirectly to the body, the components contained in the lavender extract such as linalool and linalyl acetate contained in the composition are volatilized depending on the body temperature and effectively act on the nasal cavity. In addition, the nerve can be relaxed and the peripheral skin blood flow rate can be increased to promote heat dissipation from the skin, thereby leading to a biological rhythm during sleep onset in which the body temperature in the deep part of the body falls, thereby prompting sleep onset. In addition, the composition for external use of the present invention has an endothermic action based on the release of latent heat at the time of evaporation because the contained water evaporates from the surface over time. Therefore, if such a composition is applied or affixed to the skin at bedtime, the heat release action in the body can be assisted and promoted by taking heat from the deposited skin in the form of latent heat of vaporization, and smooth sleep can be promoted.
[0078]
The composition for external use of the present invention is particularly suitable for insomnia or sleep disturbance based on mental causes such as anxiety, overwork, depression, arousal, etc., insomnia based on modulation of biological rhythm orEnterUseful for sleep disorders.
[0079]
The application site of the composition for external use of the present invention is not particularly limited, but for the purpose of producing an effect by causing the volatile components of lavender to act on the nasal cavity, it is preferably a region of the upper body close to the nose. More preferably, it is the chest or the face / head, particularly the forehead.
[0080]
Based on such characteristics, the present invention further provides a patch obtained by molding the above external composition into a certain form.
[0081]
Although the form is not particularly limited, a sheet shape is preferable from the viewpoints of ease of handling, portability, storage, and the like. Such a sheet-like patch spreads the above external composition itself into a sheet form, impregnates a liquid composition into a sheet-like base material, or forms an ointment, cream-like or gel-like composition into a sheet. It can be prepared by coating and spreading on a glass-like substrate.
[0082]
Here, as the sheet-like substrate, the composition for external use of the present invention can be supported, and appropriate permeation / permeation is performed so as not to impede permeation of volatile components such as lavender extract and moisture release of the composition for external use. There is no particular limitation as long as it has wettability, and various woven fabrics, nonwoven fabrics, films and the like can be used. As long as it has the above properties, the hole diameter of the sheet-like substrate is not particularly limited, but is usually about 0.001 to 5 mm, preferably about 0.01 to 1 mm.
[0083]
When woven or non-woven fabric is used as the base material, the material is not particularly limited, natural fibers such as cotton, hemp and wool, cellulosic fibers such as rayon and acetate, nylon, vinylon, styrene, polypropylene, polyethylene, polyethylene Examples thereof include synthetic fibers such as terephthalate and acrylic, and natural fibers such as cotton, hemp, and hair.
[0084]
Even when a film is used as the substrate, the material is not particularly limited, and specific examples thereof include styrene, polypropylene, polyethylene terephthalate, and polyethylene. In this case, a mesh-like film can also be used in order to ensure appropriate permeability and moisture permeability. Although the pore diameter in particular of a mesh is not restrict | limited, As mentioned above, 0.001-5 mm normally, Preferably the hole diameter of 0.01-1 mm can be mentioned.
[0085]
The thickness of the sheet-like substrate is not particularly limited as long as it does not interfere with the moisture-releasing property of the external composition, but is usually 1 to 1000 μm, preferably from the viewpoint of ease of use, ease of adaptation to the application site, and the like. 10 to 500 μm.
[0086]
Moreover, it is preferable that the said base material has moderate elasticity so that it may become familiar with the outer shape of an adhesion site | part when a patch is stuck on skin.
[0087]
Although the thickness of the composition for external use which is applied and spread and laminated on such a sheet-like substrate is not particularly limited, it is usually 1 to 7 mm, preferably 4 to 5 mm from the viewpoints of feeling of use, endothermic amount and the like. is there.
[0088]
The patch of the present invention basically comprises an external composition, or an external composition and a sheet-like substrate, but is peeled and removed at the time of use from the viewpoint of handling and hygiene. A release film can also be laminated on the surface of the external composition.
[0089]
As such a release film, polyester, polypropylene, polyethylene, nylon, vinyl chloride, polyethylene terephthalate, or the like can be used.
[0090]
Further, the size of the patch of the present invention is not particularly limited, and can be appropriately selected and prepared according to the place of attachment.
[0091]
The patch of the present invention can be produced according to a conventionally known method using the aforementioned external composition. For example, the composition of the present invention is spread and applied uniformly on a release sheet, and a sheet is formed thereon. A method of stacking substrates is mentioned. In this case, the laminate can be pressed with a roller in order to fix it with higher strength.
[0092]
The composition for external use and the patch of the present invention are used by applying or sticking to the skin of the face or head such as the chest or the forehead at bedtime, and are useful as an auxiliary agent or a sleep induction agent for promoting smooth sleep. .
[0093]
【Example】
Hereinafter, the content of the present invention will be specifically described using the following examples, comparative examples, and experimental examples, but the present invention is not limited thereto.
[0094]
Example 1
An external composition of the present invention was prepared according to the following formulation.
[0095]
2. 1. Mix sodium polyacrylate, aluminum hydroxide gel, methyl paraben, lavender, Add so that no lump is formed in the stirrer
3. After the addition, the mixture is vacuum degassed for only a few minutes.
[0096]
Example 2
An external composition of the present invention was prepared according to the following formulation.
[0097]
2. About half of purified water Add so that no lumps are inside
3. Add the other ingredients in sequence, and finally add the remaining purified water.
[0098]
Example 3
An external composition of the present invention was prepared according to the following formulation.
[0099]
2. Mix sodium polyacrylate, aluminum hydroxide and lavender extract into concentrated glycerin
3.2. 1. Add gradually while stirring and kneading
4). After the addition, the mixture is vacuum degassed for only a few minutes.
[0100]
Example 4
An external composition of the present invention was prepared according to the following formulation.
[0101]
2. 1. Mix sodium polyacrylate, aluminum hydroxide, lavender extract, Add to the agitator so that no lump is formed
3. After the addition, the mixture is vacuum degassed for only a few minutes.
[0102]
Example 5
An external composition of the present invention was prepared according to the following formulation.
[0103]
2. Mix sodium polyacrylate, aluminum hydroxide, lavender, methyl paraben with glycerin.
3.2. 1. Add to the agitator so that no lump is formed
4). After the addition, the mixture is vacuum degassed for only a few minutes.
[0104]
Examples 6-9
Each composition for external use prepared in Examples 1 to 5 (corresponding to Examples 6 to 10 respectively) was spread on a mesh-like sheet substrate (made of PET) having a pore diameter of 0.1 to 1 mm, and appropriate. It was cut into a large size (5 × 13 cm) and sealed in an aluminum bag to prepare a sheet-like patch (a patch).
[0105]
[Experimental example]
Experimental example 1
The composition for external use prepared in Example 3 was spread on a nonwoven fabric and cut into 3 cm × 3 cm to prepare a patch, which was pasted on a 37 ° C. hot plate, and the hot plate was kept at a constant temperature (37 ° C.). The amount of heat necessary to maintain the temperature was measured over time. The results are shown in FIG.
[0106]
Experimental example 2
Each patch used in Experimental Example 1 was affixed to the foreheads of six monitors, and the temperature drop of the forehead part was measured to determine the average value. The results are shown in Table 1.
[0107]
[Table 1]
From these results, it was confirmed that the composition and patch of the present invention were excellent in cooling effect and cooling sustainability.
[0109]
Experimental example 3
Three people were randomly selected from adults who had trouble falling asleep and complained of falling asleep. Using these as subjects, the patch prepared in Example 6 (pap) was applied to the forehead at bedtime, and the effect on sleep was examined. .
[0110]
The hypnotic effect was evaluated on the following evaluation items in five stages as compared with the state before the experiment.
[0111]
・ Evaluation item: A feeling of sleep
Evaluation: (1) Yes (2) Somewhat (3) I can say neither (4) Not much
(5) No
・ Evaluation item: Good sleep
Evaluation: (1) Good (2) Slightly good (3) Don't know (4) Slightly bad
(5) It was bad
The results are shown in Table 2.
[0112]
[Table 2]
As can be seen from the table, a hypnotic effect was observed for any of the subjects by using the patch of the present invention.
[0114]
Experimental Example 4
The following tests (1) to (3) were conducted to examine the increase in mental stability ((1) Kraepelin test, (2) electroencephalogram measurement) and peripheral skin temperature by inhalation of lavender aroma and use of the patch of the present invention. It was.
[0115]
(1) Kraepelin test
By having the subject perform the calculation work continuously, the mental stability effect can be evaluated from the change in work efficiency and accuracy rate. Therefore, two groups consisting of 15 healthy adults aged 24 to 32 years old were made, and a room where lavender aroma was stripped at room temperature from odor paper prepared by impregnating lavender essential oil, and a room without fragrance The following work was done in each room. The former is group A and the latter is group B.
[0116]
<Work contents>
The work is to add the numbers printed on the paper next to each other, and then enter the last one digit of the answer with a pencil in the "line spacing / added character spacing". In accordance with the inspector's decree, change the line every minute and repeat it for 15 minutes on the front and back of the entry form (numbers printed on both front and back). One minute is one work, and 15 times is one set (15 minutes in the first half → 10 minutes in the break → 15 minutes in the second half). In order to see the difference in work efficiency between morning and afternoon, it was held twice a day in the morning and afternoon. The result is shown in FIG.
Group B, who worked in a room with no scent, worked in a room where fragrance was removed, while the accuracy rate in the latter half was lower than that in the first half (99.6% → 99.38%). In group A, the correct answer rate in the latter half of the work was found to increase compared to the first half (99.63% → 99.83%). From this, it was recognized that mental stability can be obtained by inhalation of aroma components of lavender essential oil.
[0117]
(2) EEG measurement
An electroencephalogram electrically captures the activity of nerve cells in the brain. Among them, alpha waves are one of the components of the electroencephalogram. Generally, when humans have the impression that they are "feeling calm". It is known that the appearance amount of α waves increases in a resting state (“Effect of perfume on brain function”, Fragrance Journal, 1989, No. 9, pp. 20-26). Therefore, the resting effect can be evaluated by measuring the α wave appearance amount of the electroencephalogram.
[0118]
<Experiment method>
The experiment was conducted on six subjects in a constant temperature and humidity chamber.
[0119]
First, subjects were allowed to rest for 20 minutes, and then the patch (patch) prepared in Example 6 was applied to each subject's forehead and allowed to stand for 3 minutes. Thereafter, the appearance amount of α waves for 3 minutes was determined as Bio amp 0523S ( NF circuit). Note that the patch (patch) prepared in Example 6 started to smell lavender immediately after being applied.
[0120]
Specifically, two electrodes were attached to the subject's forehead, the brain waves at the two points were measured, and after the fast Fourier transform, the α wave appearance amount of 8 to 13 Hz was extracted. As a control experiment, the α wave appearance amount was similarly measured for each subject before applying the patch (patch).
[0121]
<Result>
The results are shown in FIG. 3 in comparison with the control experiment.
[0122]
In FIG. 3, A represents an electroencephalogram of 8 to 13 HZ, and further shows a detailed α wave distribution in the 8 to 13 HZ region. FIG. A shows that in the awake state, the distribution of α waves has shifted to 10 to 12 HZ immediately after the patch (patch) is applied. This shows that a sedative effect can be obtained by using a patch. B in FIG. 3 is a diagram comparing the total appearance amount of α waves with and without a patch (a patch). The numerical value (index) in the figure is an index for confirming the increase in the amount of α-wave appearance, and it can be seen from this that the appearance of α-wave increases with the application of the patch of the present invention. C in FIG. 3 is a diagram comparing the proportion of α waves in the total electroencephalogram (including electroencephalograms in regions other than the 8-13HZ region) with and without a patch (a patch). From this, it can be seen that the appearance of α waves is increased by applying the cataplasm of the present invention.
[0123]
As is apparent from the above results, it was confirmed that the amount of α-waves increased by applying the patch of the present invention, and that a tranquilizing effect was obtained by using the patch of the present invention.
[0124]
(3) Increase in peripheral skin surface temperature
<Experiment method>
For 6 subjects, the patch (patch) prepared in Example 6 was applied to the forehead in a constant temperature and humidity chamber, and the temperature distribution of the palm was measured by a thermograph.
[0125]
First, as a control experiment, each subject was relaxed for 20 minutes to confirm that the body temperature had settled, and then opened for 3 minutes (before resting, indicated by the dotted line in FIG. A), and then continued for 3 minutes (after resting). The temperature distribution of the palm was measured.
[0126]
Then, after 30 minutes, the subject was relaxed again to confirm that the body temperature had settled, and then opened for 3 minutes (before resting, indicated by the dotted line in FIG. B), and then the patch was applied to the forehead and the eye was closed. For 3 minutes (after rest, indicated by a solid line in FIG. B), the temperature distribution of the palm was measured.
[0127]
Each result is shown in FIG.
[0128]
In the resting state under the condition where the patch was not applied, the temperature distribution only increased compared to before the resting, but in the resting condition under the condition where the patch was applied, the temperature distribution was on the right side compared to before the resting. It was observed that the temperature of the skin surface was increased by shifting to (high temperature part). In addition, the temperature distribution when the patch was used (solid line in FIG. B) was more prominent at the high temperature portion than the temperature distribution when the patch was not used (solid line in FIG. A). This means that the use of the patch of the present invention increases the blood flow in the peripheral skin and generates heat.
[Brief description of the drawings]
FIG. 1 is a diagram showing the results of measurement of heat consumption of a patch of the present invention in Experimental Example 1. FIG. The horizontal axis represents the measurement time (hours), and the vertical axis represents the amount of heat required to keep the hot plate constant at 37 ° C. (× 10-Four) (Cal / cm2・ Sec ・ ℃).
FIG. 2 is a diagram comparing the results of the Kraepelin test performed in Experimental Example 4 (1) in the presence and absence of lavender aroma.
FIG. 3 is a diagram comparing the amount of α-wave appearance by the use of the patch of the present invention performed in Experimental Example 4 (2) with the case where no patch is used. In the figure, A represents an electroencephalogram of 8 to 13HZ, and further shows a detailed α wave distribution in the 8 to 13HZ region. B in the figure is a diagram comparing the total appearance amount of α-wave with and without the patch application. C in the figure is a diagram comparing the proportion of α waves in the whole brain wave (including brain waves in regions other than the 8-13HZ region) with and without the patch applied.
FIG. 4 is a graph showing an increase in peripheral skin temperature due to the use of the patch of the present invention conducted in Experimental Example 4 (3). In the figure, A shows the result of measuring the peripheral skin temperature before resting (3 minutes, dotted line) and after resting (3 minutes, solid line) in a state where no patch is applied. B in the figure shows the result of measuring the peripheral skin temperature (3 minutes, dotted line) before resting (3 minutes) without the patch, and the result of measuring the peripheral skin temperature with the patch applied ( 3 minutes, solid line).
Claims (9)
Priority Applications (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP05028698A JP4284474B2 (en) | 1998-03-03 | 1998-03-03 | Endothermic composition for external use and use as sleep-inducing agent |
| US09/042,891 US6224899B1 (en) | 1997-03-18 | 1998-03-17 | Adhesive cooling composition and process for its preparation |
| US09/348,576 US6228376B1 (en) | 1997-03-18 | 1999-07-07 | Adhesive cooling composition and process for its preparation |
| US09/726,121 US6524612B2 (en) | 1997-03-18 | 2000-11-30 | Adhesive cooling composition and process for its preparation |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP05028698A JP4284474B2 (en) | 1998-03-03 | 1998-03-03 | Endothermic composition for external use and use as sleep-inducing agent |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JPH11246397A JPH11246397A (en) | 1999-09-14 |
| JPH11246397A5 JPH11246397A5 (en) | 2005-09-02 |
| JP4284474B2 true JP4284474B2 (en) | 2009-06-24 |
Family
ID=12854686
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP05028698A Expired - Lifetime JP4284474B2 (en) | 1997-03-18 | 1998-03-03 | Endothermic composition for external use and use as sleep-inducing agent |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JP4284474B2 (en) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2001261505A (en) * | 2000-03-16 | 2001-09-26 | Fuji Flavor Kk | Insect behavior controlling agent |
| JP2006008593A (en) * | 2004-06-25 | 2006-01-12 | Nichiban Co Ltd | Nasal patch |
| JP2006282509A (en) * | 2005-03-31 | 2006-10-19 | Tokyo Medical & Dental Univ | Composition for improving depressed mood |
| JP2011037721A (en) * | 2009-08-06 | 2011-02-24 | Pola Chemical Industries Inc | Skin care preparation for external use exhibiting sleep-improving action |
| TWI568422B (en) | 2010-07-12 | 2017-02-01 | 帝國製藥股份有限公司 | Three-layer structure support and water-based patch using same |
| CN103025322B (en) | 2010-07-12 | 2014-07-23 | 东洋纺株式会社 | Adhesive support for water-based paste formulations |
| JP2017105724A (en) * | 2015-12-09 | 2017-06-15 | 株式会社オーシンエムエルピー | Adhesive cold / heat gel sheet |
| JP2021007523A (en) * | 2019-06-28 | 2021-01-28 | 小林製薬株式会社 | Deep body temperature lowering tool |
| JP2021007524A (en) * | 2019-06-28 | 2021-01-28 | 小林製薬株式会社 | Cognitive function improving tool at high body temperature |
| JP2021007521A (en) * | 2019-06-28 | 2021-01-28 | 小林製薬株式会社 | Deep body temperature lowering tool |
| CN117064626A (en) * | 2023-08-21 | 2023-11-17 | 浙江银达生物技术有限公司 | Medical hydrogel patch |
-
1998
- 1998-03-03 JP JP05028698A patent/JP4284474B2/en not_active Expired - Lifetime
Also Published As
| Publication number | Publication date |
|---|---|
| JPH11246397A (en) | 1999-09-14 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| US6224899B1 (en) | Adhesive cooling composition and process for its preparation | |
| KR101351177B1 (en) | Skin cooling compositions | |
| JP4284474B2 (en) | Endothermic composition for external use and use as sleep-inducing agent | |
| US20030152610A1 (en) | Cosmetic patch | |
| JP4677063B2 (en) | Dutch mustard extract combination external preparation | |
| JP2005002040A (en) | Anti-inflammatory and analgesic plaster | |
| JP2000355545A (en) | Essential oil composition for sleep supplementation and/ or introduction, and agent for sleep supplementation and/or introduction | |
| CN109528486A (en) | A kind of self-heating smoke-less moxibustion plaster | |
| DE19957234A1 (en) | Pharmaceutical plaster containing essential oils | |
| CN105534372B (en) | It is a kind of with antibacterial, disinfection towel and preparation method thereof of going to the lavatory | |
| JP5089933B2 (en) | Water-containing pressure-sensitive adhesive composition and patch using the same | |
| WO2000044336A1 (en) | Sheet-type packs | |
| CN105560498B (en) | It is a kind of with antibacterial, disinfection medical fluid and its application | |
| JPH10330247A (en) | Patches for nails | |
| CN118370711A (en) | Composition with body odor removal effect and application thereof | |
| CN113769024B (en) | Compound essential oil for improving mood and preparation method and application thereof | |
| JP6867210B2 (en) | Patch | |
| JP4836338B2 (en) | Cooling composition | |
| CN105534373B (en) | It is a kind of with antibacterial, disinfection towel and preparation method thereof of going to the lavatory | |
| JP2006008593A (en) | Nasal patch | |
| CN105213677A (en) | A kind of Chinese medicinal film for topical anesthesia and preparation method thereof | |
| CN110545785A (en) | Body cosmetic | |
| JPH0759808A (en) | Blood circulation hydrating body | |
| JPH11209294A (en) | Parasympathomimetic agent containing essential oil as active ingredient | |
| JP2017522269A (en) | Transdermal therapeutic system containing lavender oil |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A521 | Written amendment |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20050303 |
|
| A621 | Written request for application examination |
Free format text: JAPANESE INTERMEDIATE CODE: A621 Effective date: 20050303 |
|
| A131 | Notification of reasons for refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A131 Effective date: 20081022 |
|
| A601 | Written request for extension of time |
Free format text: JAPANESE INTERMEDIATE CODE: A601 Effective date: 20081215 |
|
| A602 | Written permission of extension of time |
Free format text: JAPANESE INTERMEDIATE CODE: A602 Effective date: 20081218 |
|
| A521 | Written amendment |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20090121 |
|
| TRDD | Decision of grant or rejection written | ||
| A01 | Written decision to grant a patent or to grant a registration (utility model) |
Free format text: JAPANESE INTERMEDIATE CODE: A01 Effective date: 20090218 |
|
| A01 | Written decision to grant a patent or to grant a registration (utility model) |
Free format text: JAPANESE INTERMEDIATE CODE: A01 |
|
| A61 | First payment of annual fees (during grant procedure) |
Free format text: JAPANESE INTERMEDIATE CODE: A61 Effective date: 20090310 |
|
| FPAY | Renewal fee payment (event date is renewal date of database) |
Free format text: PAYMENT UNTIL: 20120403 Year of fee payment: 3 |
|
| R150 | Certificate of patent or registration of utility model |
Free format text: JAPANESE INTERMEDIATE CODE: R150 |
|
| FPAY | Renewal fee payment (event date is renewal date of database) |
Free format text: PAYMENT UNTIL: 20120403 Year of fee payment: 3 |
|
| S531 | Written request for registration of change of domicile |
Free format text: JAPANESE INTERMEDIATE CODE: R313531 |
|
| FPAY | Renewal fee payment (event date is renewal date of database) |
Free format text: PAYMENT UNTIL: 20120403 Year of fee payment: 3 |
|
| R350 | Written notification of registration of transfer |
Free format text: JAPANESE INTERMEDIATE CODE: R350 |
|
| FPAY | Renewal fee payment (event date is renewal date of database) |
Free format text: PAYMENT UNTIL: 20130403 Year of fee payment: 4 |
|
| FPAY | Renewal fee payment (event date is renewal date of database) |
Free format text: PAYMENT UNTIL: 20130403 Year of fee payment: 4 |
|
| FPAY | Renewal fee payment (event date is renewal date of database) |
Free format text: PAYMENT UNTIL: 20140403 Year of fee payment: 5 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| EXPY | Cancellation because of completion of term |