JP4803889B2 - Non-aqueous toothpaste - Google Patents
Non-aqueous toothpaste Download PDFInfo
- Publication number
- JP4803889B2 JP4803889B2 JP2001056155A JP2001056155A JP4803889B2 JP 4803889 B2 JP4803889 B2 JP 4803889B2 JP 2001056155 A JP2001056155 A JP 2001056155A JP 2001056155 A JP2001056155 A JP 2001056155A JP 4803889 B2 JP4803889 B2 JP 4803889B2
- Authority
- JP
- Japan
- Prior art keywords
- mass
- oral composition
- present
- composition
- oral
- 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
- 239000000606 toothpaste Substances 0.000 title claims description 20
- 229940034610 toothpaste Drugs 0.000 title claims description 18
- KRHYYFGTRYWZRS-UHFFFAOYSA-M Fluoride anion Chemical compound [F-] KRHYYFGTRYWZRS-UHFFFAOYSA-M 0.000 claims description 26
- FUWUEFKEXZQKKA-UHFFFAOYSA-N beta-thujaplicin Chemical compound CC(C)C=1C=CC=C(O)C(=O)C=1 FUWUEFKEXZQKKA-UHFFFAOYSA-N 0.000 claims description 26
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 24
- SLXKOJJOQWFEFD-UHFFFAOYSA-N 6-aminohexanoic acid Chemical compound NCCCCCC(O)=O SLXKOJJOQWFEFD-UHFFFAOYSA-N 0.000 claims description 18
- 102000004190 Enzymes Human genes 0.000 claims description 18
- 108090000790 Enzymes Proteins 0.000 claims description 18
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 claims description 18
- 229960002684 aminocaproic acid Drugs 0.000 claims description 18
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims description 14
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims description 14
- TUFYVOCKVJOUIR-UHFFFAOYSA-N alpha-Thujaplicin Natural products CC(C)C=1C=CC=CC(=O)C=1O TUFYVOCKVJOUIR-UHFFFAOYSA-N 0.000 claims description 13
- 229930007845 β-thujaplicin Natural products 0.000 claims description 13
- PUPZLCDOIYMWBV-UHFFFAOYSA-N (+/-)-1,3-Butanediol Chemical compound CC(O)CCO PUPZLCDOIYMWBV-UHFFFAOYSA-N 0.000 claims description 12
- 239000001913 cellulose Substances 0.000 claims description 7
- 229920002678 cellulose Polymers 0.000 claims description 7
- 229940105990 diglycerin Drugs 0.000 claims description 7
- GPLRAVKSCUXZTP-UHFFFAOYSA-N diglycerol Chemical compound OCC(O)COCC(O)CO GPLRAVKSCUXZTP-UHFFFAOYSA-N 0.000 claims description 7
- 235000011187 glycerol Nutrition 0.000 claims description 7
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims description 7
- 239000001267 polyvinylpyrrolidone Substances 0.000 claims description 7
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims description 7
- 229940058015 1,3-butylene glycol Drugs 0.000 claims description 6
- 239000002202 Polyethylene glycol Substances 0.000 claims description 6
- 235000019437 butane-1,3-diol Nutrition 0.000 claims description 6
- 229960005150 glycerol Drugs 0.000 claims description 6
- 229920001223 polyethylene glycol Polymers 0.000 claims description 6
- 229960004063 propylene glycol Drugs 0.000 claims description 6
- 239000003795 chemical substances by application Substances 0.000 claims description 3
- 239000000203 mixture Substances 0.000 description 104
- 239000002585 base Substances 0.000 description 27
- 239000000551 dentifrice Substances 0.000 description 24
- -1 hydroxyapatite Chemical class 0.000 description 22
- 229940091249 fluoride supplement Drugs 0.000 description 20
- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical class [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 description 20
- 210000000214 mouth Anatomy 0.000 description 18
- 229940088598 enzyme Drugs 0.000 description 17
- 238000003860 storage Methods 0.000 description 14
- 239000004480 active ingredient Substances 0.000 description 11
- 230000000694 effects Effects 0.000 description 10
- 238000002360 preparation method Methods 0.000 description 10
- 239000002537 cosmetic Substances 0.000 description 9
- 239000003814 drug Substances 0.000 description 9
- 235000013305 food Nutrition 0.000 description 8
- 239000007788 liquid Substances 0.000 description 8
- PUZPDOWCWNUUKD-UHFFFAOYSA-M sodium fluoride Chemical compound [F-].[Na+] PUZPDOWCWNUUKD-UHFFFAOYSA-M 0.000 description 8
- 229910052731 fluorine Inorganic materials 0.000 description 7
- 239000011737 fluorine Substances 0.000 description 7
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 description 6
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- 239000000194 fatty acid Substances 0.000 description 6
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- 235000012239 silicon dioxide Nutrition 0.000 description 6
- 230000001771 impaired effect Effects 0.000 description 5
- 238000004519 manufacturing process Methods 0.000 description 5
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- 238000000926 separation method Methods 0.000 description 5
- 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 4
- RBLGLDWTCZMLRW-UHFFFAOYSA-K dicalcium;phosphate;dihydrate Chemical compound O.O.[Ca+2].[Ca+2].[O-]P([O-])([O-])=O RBLGLDWTCZMLRW-UHFFFAOYSA-K 0.000 description 4
- 230000003631 expected effect Effects 0.000 description 4
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- 230000014759 maintenance of location Effects 0.000 description 4
- 229920003023 plastic Polymers 0.000 description 4
- 239000004033 plastic Substances 0.000 description 4
- NROKBHXJSPEDAR-UHFFFAOYSA-M potassium fluoride Chemical compound [F-].[K+] NROKBHXJSPEDAR-UHFFFAOYSA-M 0.000 description 4
- RMAQACBXLXPBSY-UHFFFAOYSA-N silicic acid Chemical compound O[Si](O)(O)O RMAQACBXLXPBSY-UHFFFAOYSA-N 0.000 description 4
- 239000000377 silicon dioxide Substances 0.000 description 4
- 239000011734 sodium Substances 0.000 description 4
- 229910052708 sodium Inorganic materials 0.000 description 4
- 239000011775 sodium fluoride Substances 0.000 description 4
- 235000013024 sodium fluoride Nutrition 0.000 description 4
- XGRSAFKZAGGXJV-UHFFFAOYSA-N 3-azaniumyl-3-cyclohexylpropanoate Chemical compound OC(=O)CC(N)C1CCCCC1 XGRSAFKZAGGXJV-UHFFFAOYSA-N 0.000 description 3
- 239000004382 Amylase Substances 0.000 description 3
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- 102000016943 Muramidase Human genes 0.000 description 3
- 108010062010 N-Acetylmuramoyl-L-alanine Amidase Proteins 0.000 description 3
- 239000003082 abrasive agent Substances 0.000 description 3
- 235000019418 amylase Nutrition 0.000 description 3
- 230000000844 anti-bacterial effect Effects 0.000 description 3
- 229910000019 calcium carbonate Inorganic materials 0.000 description 3
- 239000001506 calcium phosphate Substances 0.000 description 3
- 238000006243 chemical reaction Methods 0.000 description 3
- 230000000052 comparative effect Effects 0.000 description 3
- 150000001875 compounds Chemical class 0.000 description 3
- 238000007796 conventional method Methods 0.000 description 3
- HNPSIPDUKPIQMN-UHFFFAOYSA-N dioxosilane;oxo(oxoalumanyloxy)alumane Chemical compound O=[Si]=O.O=[Al]O[Al]=O HNPSIPDUKPIQMN-UHFFFAOYSA-N 0.000 description 3
- 238000001035 drying Methods 0.000 description 3
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- 150000002222 fluorine compounds Chemical class 0.000 description 3
- 239000003205 fragrance Substances 0.000 description 3
- 239000004325 lysozyme Substances 0.000 description 3
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- 229960004711 sodium monofluorophosphate Drugs 0.000 description 3
- YUOWTJMRMWQJDA-UHFFFAOYSA-J tin(iv) fluoride Chemical compound [F-].[F-].[F-].[F-].[Sn+4] YUOWTJMRMWQJDA-UHFFFAOYSA-J 0.000 description 3
- MBDOYVRWFFCFHM-SNAWJCMRSA-N (2E)-hexenal Chemical compound CCC\C=C\C=O MBDOYVRWFFCFHM-SNAWJCMRSA-N 0.000 description 2
- IXPNQXFRVYWDDI-UHFFFAOYSA-N 1-methyl-2,4-dioxo-1,3-diazinane-5-carboximidamide Chemical compound CN1CC(C(N)=N)C(=O)NC1=O IXPNQXFRVYWDDI-UHFFFAOYSA-N 0.000 description 2
- MPDGHEJMBKOTSU-YKLVYJNSSA-N 18beta-glycyrrhetic acid Chemical compound C([C@H]1C2=CC(=O)[C@H]34)[C@@](C)(C(O)=O)CC[C@]1(C)CC[C@@]2(C)[C@]4(C)CC[C@@H]1[C@]3(C)CC[C@H](O)C1(C)C MPDGHEJMBKOTSU-YKLVYJNSSA-N 0.000 description 2
- QFOHBWFCKVYLES-UHFFFAOYSA-N Butylparaben Chemical compound CCCCOC(=O)C1=CC=C(O)C=C1 QFOHBWFCKVYLES-UHFFFAOYSA-N 0.000 description 2
- 108010001682 Dextranase Proteins 0.000 description 2
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- 239000004365 Protease Substances 0.000 description 2
- 102100037486 Reverse transcriptase/ribonuclease H Human genes 0.000 description 2
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 2
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- 239000002253 acid Substances 0.000 description 2
- 239000000853 adhesive Substances 0.000 description 2
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- 229940030225 antihemorrhagics Drugs 0.000 description 2
- 239000011230 binding agent Substances 0.000 description 2
- 239000011575 calcium Substances 0.000 description 2
- 229910000389 calcium phosphate Inorganic materials 0.000 description 2
- 235000011010 calcium phosphates Nutrition 0.000 description 2
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- ULDHMXUKGWMISQ-UHFFFAOYSA-N carvone Chemical compound CC(=C)C1CC=C(C)C(=O)C1 ULDHMXUKGWMISQ-UHFFFAOYSA-N 0.000 description 2
- 238000013329 compounding Methods 0.000 description 2
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- KWIUHFFTVRNATP-UHFFFAOYSA-N glycine betaine Chemical compound C[N+](C)(C)CC([O-])=O KWIUHFFTVRNATP-UHFFFAOYSA-N 0.000 description 2
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- XMGQYMWWDOXHJM-UHFFFAOYSA-N limonene Chemical compound CC(=C)C1CCC(C)=CC1 XMGQYMWWDOXHJM-UHFFFAOYSA-N 0.000 description 2
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- OSWPMRLSEDHDFF-UHFFFAOYSA-N methyl salicylate Chemical compound COC(=O)C1=CC=CC=C1O OSWPMRLSEDHDFF-UHFFFAOYSA-N 0.000 description 2
- LXCFILQKKLGQFO-UHFFFAOYSA-N methylparaben Chemical compound COC(=O)C1=CC=C(O)C=C1 LXCFILQKKLGQFO-UHFFFAOYSA-N 0.000 description 2
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- XYJRXVWERLGGKC-UHFFFAOYSA-D pentacalcium;hydroxide;triphosphate Chemical compound [OH-].[Ca+2].[Ca+2].[Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O XYJRXVWERLGGKC-UHFFFAOYSA-D 0.000 description 2
- 238000006116 polymerization reaction Methods 0.000 description 2
- 239000011698 potassium fluoride Substances 0.000 description 2
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- QELSKZZBTMNZEB-UHFFFAOYSA-N propylparaben Chemical compound CCCOC(=O)C1=CC=C(O)C=C1 QELSKZZBTMNZEB-UHFFFAOYSA-N 0.000 description 2
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Landscapes
- Cosmetics (AREA)
Description
【０００１】
【発明の属する技術分野】
本発明は、口腔用組成物用基剤に関し、より詳しくは、水を含まないか又は殆ど水を含まない口腔用組成物を製造するのに適した口腔用組成物用基剤に関する。本発明はさらに、そのような口腔用組成物用基剤を含有する口腔用組成物に関する。
【０００２】
【従来の技術】
歯磨剤等の口腔用組成物には、一般的にカルボキシメチルセルロースナトリウム、カラギーナン或いはキサンタンガムといった粘着剤が配合されており、これらの成分が水に溶けることで粘性を発現し、研磨剤等の粉体成分と液体成分を結合させ、保型性を与えたり、適度の粘性を与えている。従って水を含まない歯磨剤等の口腔用組成物においては、粘度が発現しないため、保型性を保たせることが難しく、口腔用組成物は経時的に粉体成分と液体成分の分離が起きてしまう。
【０００３】
一方歯磨剤等の口腔用組成物には、機能・効能の付与を目的として、製剤に種々の有効成分を配合することがあり、有効成分としては再石灰化促進成分、フッ化物、殺菌剤、抗炎症剤、止血剤、各種酵素等が挙げられる。
再石灰化促進成分として、ハイドロキシアパタイト等のリン酸カルシウム化合物が挙げられるが、その中でもα−第三リン酸カルシウム（α−ＴＣＰと略称する）は口腔内において極めて再石灰化促進効果が高く、虫歯の予防・修復などに有効であることが知られている。
しかしα−ＴＣＰは、水存在下ではアパタイト化合物へ転換する性質があり、その反応はフッ化物又はその他水溶性のリン酸カルシウムの存在で加速され、自己硬化反応を起こすため、通常の水を含有した歯磨剤等の口腔用組成物には安定に配合ができなかった。
【０００４】
またフッ化物としては、フッ化ナトリウム、モノフルオロホスフェート、フッ化カリウム、モノフルオロリン酸ナトリウム、フッ化錫等が挙げられるが、フッ化物の効能はフッ素イオンが歯のハイドロキシアパタイトをフッ素化して歯質を強化することにある。通常の水を含有する歯磨剤等の口腔用組成物にフッ化物を配合すると、口腔用組成物中でフッ素イオンが水に溶けだし、研磨剤等の他の成分へ吸着し、フッ素イオン本来の効果が発揮されないことがある。例えばフッ化ナトリウム或いはフッ化錫等とリン酸カルシウム或いは炭酸カルシウムといった研磨剤が配合された、水を含有する口腔用組成物では、フッ素イオンが研磨剤に吸着しフッ素イオンを不活性化してしまうことが知られている。
【０００５】
酵素としては、溶菌作用やタンパク分解作用を有するリゾチーム、ムタナーゼ、プロテアーゼ、アミラーゼ、デキストラナーゼ等が挙げられるが、これらの酵素の多くは水を含有する組成に配合すると加水分解を起こし、酵素活性が低下するといった問題がある。そこで水を含有する組成に酵素を配合する場合は、加水分解の起こりにくい酵素を選択するか、各酵素個別に安定配合の方法を探索する必要がある。
【０００６】
また、天然系の殺菌剤としてヒノキチオールや、止血剤としてε−アミノカプロン酸を歯磨剤等の口腔用組成物に配合することもあるが、これらの有効成分も水を含有する組成に配合すると、加水分解により定量値が低下する傾向がある。
これら有効成分の安定性に関する問題点は、全て歯磨剤等の口腔用組成物に水が含まれていることに起因している。従って、α−ＴＣＰ、フッ化物、各種酵素、ヒノキチオール及びε−アミノカプロン酸などの安定配合が可能となる、水を殆ど含有しない歯磨剤等の口腔用組成物において、保型性が有り、経時的に粉体成分と液体成分の分離が起こらない組成の口腔用組成物が望まれている。
【０００７】
【発明が解決しようとする課題】
本発明の目的は、口腔用組成物の製造に適した、特に水を含まないか又は水を殆ど含まない口腔用組成物の製造に適した口腔用組成物用基剤を提供することである。本発明の目的はまた、保型性に優れ成分の分離などが起こらない経時的に安定な、特に水を含まないか又は水を殆ど含まない口腔用組成物の製造に適した口腔用組成物用基剤を提供することである。本発明の目的はさらに、通常水の存在下では不安定な有効成分を安定に配合することのできる口腔用組成物用基剤を提供することである。本発明のさらなる目的は、通常水の存在下では不安定な有効成分を安定に配合した口腔用組成物、特に、水を含まないか又は水を殆ど含まない口腔用組成物を提供することである。
【０００８】
【課題を解決するための手段】
本発明者らは上記目的を達成するために鋭意研究を重ねた結果、特定の組成の基剤を使用することによって、安定性が高い口腔用組成物を提供することが可能であることを見出し、本発明を完成させるに至った。
従って本発明は、少なくとも１種の数平均分子量１０，０００〜３６０，０００のポリビニルピロリドン、並びに濃グリセリン、ジグリセリン、プロピレングリコール、１，３−ブチレングリコール及びポリエチレングリコールからなる群から選ばれる少なくとも１種を含有することを特徴とする非水系口腔用組成物用基剤に関する。本発明の好ましい実施態様として、さらに無水ケイ酸及び結晶セルロースからなる群から選ばれる少なくとも１種を含有する上記非水系口腔用組成物用基剤がある。
本発明はさらに、上記口腔用組成物用基剤を含有する口腔用組成物に関する。
本明細書中でいう、非水系口腔用組成物とは、口腔用組成物全体に対する水の含有量が０〜２質量％、好ましくは０〜１質量％、より好ましくは水を全く含有しない口腔用組成物を意味する。さらに、このような非水系口腔用組成物の製造に適した基剤を本明細書中で非水系口腔用組成物用基剤と称する。
【０００９】
本発明はまた、上記口腔用組成物用基剤及びα−第三リン酸カルシウム（α−ＴＣＰ）を含有することを特徴とする口腔用組成物に関する。また、本発明は、上記上記口腔用組成物用基剤、及び少なくとも１種のフッ化物を含有することを特徴とする口腔用組成物に関する。
本発明はさらに、上記口腔用組成物用基剤及び酵素類を含有することを特徴とする口腔用組成物に関する。本発明はさらに、上記口腔用組成物用基剤、並びにヒノキチオール及びε−アミノカプロン酸からなる群から選ばれる少なくとも１種を含有することを特徴とする口腔用組成物に関する。
更に本発明は、上記口腔用組成物用基剤、並びにα−ＴＣＰ、フッ化物、酵素類、ヒノキチオール及びε−アミノカプロン酸から選ばれる少なくとも１種を含有する口腔用組成物も包含する。
本発明の口腔用組成物の好ましい実施態様として、上記口腔用組成物用基剤にα−ＴＣＰとフッ化物とを組み合わせて配合した口腔用組成物がある。
【００１０】
【発明の実施の形態】
本明細書中でいう口腔用組成物とは、練歯磨剤、液状歯磨剤及び潤製歯磨剤などの歯磨剤類、クリーム剤、軟膏剤、添付剤、口中清涼剤、洗口剤、チューインガム又はうがい薬などを包含する。また、本発明の口腔用組成物は望ましくは、非水系口腔用組成物に向けられている。
【００１１】
本発明の口腔用組成物用基剤に用いるポリビニルピロリドンとは、アセチレンの高圧合成法レッペ反応による合成化合物の一種であり、ビニルピロリドンの直鎖重合体である。また、重合反応の触媒量、温度、時間などにより本品の分子量は１０，０００〜７００，０００程度まで存在する。
本発明では、数平均分子量１０，０００〜３６０，０００のポリビニルピロリドンを１種あるいは２種以上使用することができる。すなわち平均分子量が異なるものを２種以上使用してもよい。平均分子量が１０，０００に満たないものは、期待される効果が発揮されず、一方平均分子量が３６０，０００を越えるものは、剤形上配合が困難となる。
このようなポリビニルピロリドンは、医薬品や化粧品を始め、織物・紙業・印刷・インキ工業・保護塗料・飲料清澄剤・接着剤・農芸化学・プラスティック工業などに広く一般的に使用されるものであり、本発明においてはこれらに使用されている市販品を用いることができる。
口腔用組成物における数平均分子量１０，０００〜３６０，０００のポリビニルピロリドンの含有量は、口腔用組成物の全質量に対して０．１〜１５質量％、好ましくは１〜１０質量％である。この量が０．１質量％未満であると、期待される効果が発揮されず、一方１５質量％を越えると、含有量に見合った効果が得られず使用性を損ねる場合がある。
【００１２】
本発明の口腔用組成物用基剤はさらに、濃グリセリン、ジグリセリン、プロピレングリコール、１，３−ブチレングリコール及びポリエチレングリコールからなる群から選ばれる少なくとも１種を含有する。中でも特に好ましく用いられるのは濃グリセリン、ジグリセリンである。
濃グリセリン、ジグリセリン、プロピレングリコール、１，３−ブチレングリコール及びポリエチレングリコールは、医薬品や化粧品をはじめ、食品、雑貨品、石油化学工業、塗料工業など広く一般的に使用されるものである。本発明においては市販品を用いることができる。
口腔用組成物における濃グリセリン、ジグリセリン、プロピレングリコール、１，３−ブチレングリコール及びポリエチレングリコールの少なくとも１種の含有量は、口腔用組成物の全質量に対して１０〜７０質量％が適当であり、好ましくは２０〜６０質量％である。この量が１０質量％未満或いは７０質量％を越えると使用性を損なう場合がある。
【００１３】
本発明の口腔用組成物用基剤にはさらに、無水ケイ酸及び／又は結晶セルロースを含有させることができる。
無水ケイ酸は、二酸化ケイ素のことであり、性状は白色の粉末である。人工的にはケイ酸ナトリウムを酸で処理して二酸化ケイ素を析出させ、ゲル化熟成を行った後、乾燥、粉砕して得られる。また、乾燥減量が１３％以下、強熱減量が１８％以下のものである。ここでいう乾燥減量とは、無水ケイ酸１ｇを１０５℃で２時間熱した際の蒸発成分の重量％のことであり、強熱減量とは、無水ケイ酸１ｇを８５０℃で３０分間熱した際の蒸発成分の重量％のことである。
このような無水ケイ酸は食品や化粧品をはじめ、医薬品、農芸用品、餌類、インキ工業、ゴム工業、プラスチック工業など広く一般に使用されるものである。
口腔用組成物における無水ケイ酸の含有量は、口腔用組成物の全質量に対して０．５〜３０質量％、好ましくは３〜１５質量％である。この量が０．５質量％未満であると、期待される効果が発揮されず、一方３０質量％を越えると、含有量に見合った効果が得られず使用性を損ねる場合がある。
【００１４】
結晶セルロースは、繊維性植物からパルプとして得られたα−セルロースを酸加水分解又はアルカリ加水分解して得られる実質的に一定の重合度を有するセルロース結晶子集合体のことである。
このような結晶セルロースは食品や化粧品をはじめ、医薬品、農芸用品、餌類など広く一般に使用されるものである。
本発明の口腔用組成物における結晶セルロースの含有量は、口腔用組成物の全質量に対して０．５〜３０質量％、好ましくは３〜１０質量％である。この量が０．５質量％未満であると、期待される効果が発揮されず、一方３０質量％を越えると、含有量に見合った効果が得られず使用性を損ねる場合がある。
【００１５】
本発明では、上述の口腔用組成物基剤に、従来、口腔用組成物に使用される添加剤、有効成分など種々の成分を組み合わせて口腔用組成物とすることができる。
本発明の口腔用組成物用基剤は特に、通常水の存在下で不安定な成分と組み合わせるのに有利である。そのような成分として、α−ＴＣＰ、フッ化物、酵素類、ヒノキチオール及びε−アミノカプロン酸などが挙げられる。
本発明の口腔用組成物に用いるα−ＴＣＰとは、α−第三リン酸カルシウム（Ｃａ 3 （ＰＯ 4 ） 2 ）のことであり、医薬品や化粧品をはじめ、食品、雑貨品、石油化学工業など広く一般的に使用されるものである。本発明においては市販品を用いることができる。
本発明の口腔用組成物におけるα−ＴＣＰの含有量は、口腔用組成物の全質量に対して０．１〜５０質量％が適当であり、好ましくは１〜３０質量％である。この量が０．１質量％未満であると、期待される再石化効果が発揮されず、一方５０質量％を越えると使用性を損なう場合がある。
α−ＴＣＰを配合した場合に、更にフッ化物を併用すると、再石灰化作用にフッ素イオンの供給が加味されるため、極めて優れた効果を発揮する。そこでα−ＴＣＰと後述するフッ化物との組み合わせが好ましく用いられる。
【００１６】
本発明の口腔用組成物に用いるフッ化物としては具体的に、フッ化ナトリウム、モノフルオロホスフェート、フッ化カリウム、モノフルオロリン酸ナトリウム、フッ化錫等が挙げられ、これらのうち少なくとも１種を使用することができる。これらのフッ化物は医薬品や化粧品など広く一般的に使用されるものである。本発明においては市販品を用いることができる。
本発明の口腔用組成物におけるフッ化物含有量は、口腔用組成物の全質量に対して０．０１〜３質量％が適当であり、好ましくは歯磨剤等の口腔用組成物中にフッ素として１００〜１０００ｐｐｍの含有量である。
フッ化物として、中でもフッ化ナトリウム及びモノフルオロリン酸ナトリウムが好適である。
【００１７】
本発明の口腔用組成物に用いる酵素類として具体的に、リゾチーム、ムタナーゼ、プロテアーゼ、アミラーゼ、デキストラナーゼ等が挙げられ、これらのうち１種又は２種以上を使用することができる。これらの酵素は、医薬品や化粧品、食品など広く一般的に使用されるものである。本発明においては市販品を用いることができる。
本発明の口腔用組成物における酵素含有量は、口腔用組成物の全質量に対して０．０１〜５質量％が適当であり、好ましくは０．１〜２質量％である。
酵素としては、リゾチーム及びアミラーゼが好適である。
【００１８】
本発明の口腔用組成物に用いるヒノキチオールとは、天然樹木である青森ヒバなどに含まれる特有成分で、結晶性酸性化合物である。ヒノキチオールを含有する他の樹種としては、台湾ヒノキ、北米のウエスタンレッドシダー等が挙げられる。ヒノキチオールは強い抗菌活性と広い抗菌スペクトルを有しており、数少ない天然系殺菌剤のひとつである。
このようなヒノキチオールは食品や化粧品をはじめ、医薬品、農芸用品、建築材料、餌類など広く一般的に使用されるものであり、本発明においてはこれらに使用されている市販品を用いることができる。
本発明の口腔用組成物におけるヒノキチオールの含有量は、口腔用組成物の全質量に対して０．００５〜０．５質量％が適当であり、好ましくは０．０１〜０．２質量％である。
【００１９】
本発明の口腔用組成物に用いるε−アミノカプロン酸とは、抗プラスミン効果、止血効果、抗炎症効果を有する成分であり、化粧品や医薬品をはじめ、食品、農芸用品など広く一般的に使用されるものである。本発明においては市販品を用いることができる。
本発明の口腔用組成物におけるε−アミノカプロン酸の含有量は、口腔用組成物の全質量に対して０．００１〜１質量％が適当であり、好ましくは０．００６〜０．２質量％である。
【００２０】
上述のとおり、本発明の口腔用組成物用基剤に組み合わせるのに適した有効成分として、▲１▼α−ＴＣＰ；▲２▼フッ化物；▲３▼酵素類；▲４▼ヒノキチオール；及び▲５▼ε−アミノカプロン酸がある。これらの▲１▼〜▲５▼群の各群から化合物を１種又は２種以上選んで含ませることができ、また、１群に限らず、２群以上から化合物を選択し併用することができる。中でもα−ＴＣＰとフッ化物の併用が好ましい。
【００２１】
本発明の口腔用組成物にはその種類に応じて、上記成分に加えて、必要により以下の成分を通常の使用量の範囲内で配合することができる。
＜研磨剤＞
シリカゲル、沈降性シリカ、火成性シリカ、含水ケイ酸、ゼオライト、アルミノシリケート、ジルコノシリケート等のシリカ系研磨剤、第二リン酸カルシウム二水和物、第二リン酸カルシウム無水和物、ピロリン酸カルシウム、第三リン酸マグネシウム、第三リン酸カルシウム、水酸化アルミニウム、アルミナ、軽質炭酸カルシウム、重質炭酸カルシウム、炭酸マグネシウム、ケイ酸ジルコニウム、合成樹脂系研磨剤などが挙げられ、これらのうち１種または２種以上を併用して用いることができる。上記研磨剤の配合量は、組成物全体に対して３〜６０質量％が好ましく、より好ましくは１０〜４５質量％である。
【００２２】
＜湿潤剤＞
ソルビット、マルチトール等の多価アルコール等の１種または２種以上を使用することができる。
＜発泡剤＞
ラウリル硫酸ナトリウム、ラウロイルサルコシンナトリウム、アルキルスルホコハク酸ナトリウム、ヤシ油脂肪酸モノグリセリンスルホン酸ナトリウム、α-オレフィンスルホン酸ナトリウム、、N-アシルグルタメート等のN-アシルアミノ酸塩、2-アルキル-N-カルボキシメチル-N-ヒドロキシエチルイミダゾリニウムベタイン、マルチトール脂肪酸エステル、ショ糖脂肪酸エステル、ポリグリセリン脂肪酸エステル、脂肪酸ジエタノールアミド、ポリオキシエチレンソルビタンモノステアレート、ポリオキシエチレン硬化ヒマシ油、ポリオキシエチレン脂肪酸エステル等が挙げられ、これらのうち１種または２種以上を併用して用いることができる。
【００２３】
＜甘味剤＞
サッカリンナトリウム、アスパルテーム、トレハロース、ステビオサイド、ステビアエキス、パラメトキシシンナミックアルデヒド、ネオヘスペリジルジヒドロカルコン、ペリラルチン等。
＜防腐剤＞
メチルパラベン、エチルパラベン、プロピルパラベン、ブチルパラベン等のパラベン類、安息香酸ナトリウム、フェノキシエタノール、塩酸アルキルジアミノエチルグリシン等。
【００２４】
＜香料成分＞
l-メントール、アネトール、メントン、シネオール、リモネン、カルボン、メチルサリシレート、エチルブチレート、オイゲノール、チモール、シンナミックアルデヒド、トランス-２-ヘキセナールなどの中から１種または２種以上を併用して用いることができる。これらの成分は単品で配合してもよいが、これらを含有する精油等を配合してもよい。
また、上記香料成分に加え、脂肪族アルコールやそのエステル、テルペン系炭化水素、フェノールエーテル、アルデヒド、ケトン、ラクトン等の香料成分、精油を本発明の効果を妨げない範囲で配合してもよい。上記香料の配合量は、組成物全体に対して０．０２〜２質量％とすることが好ましい。
【００２５】
＜有効成分＞
ゼオライト、クロルヘキシジン塩類、塩化セチルピリジニウム、塩化ベンザルコニウム、塩化ベンゼトニウム、ビサボロール、トリクロサン、イソプロピルメチルフェノール、酢酸トコフェロール、トラネキサム酸、ジヒドロコレステロール、グリチルレチン酸、グリチルリチン酸塩類、銅クロロフィリン塩、塩化ナトリウム、グァイアズレンスルホン酸塩、塩酸ピリドキシン，などを１種または２種以上を配合することができる。
＜その他＞
青色１号等の色素、酸化チタン等の顔料、ジブチルヒドロキシトルエン等の酸化防止剤、チャ乾留液、グルタミン酸ナトリウム等の矯味剤など。
【００２６】
本発明の口腔用組成物にはその種類に応じて、水を２質量％以下の範囲で配合した場合、上記成分に加えて、必要により以下の粘結剤を配合することもできる。
＜粘結剤＞
カラギーナン（ι、λ、κ）、アルギン酸、アルギン酸ナトリウム、アルギン酸プロピレングリコールエステル、カルシウム含有アルギン酸ナトリウム、アルギン酸カリウム、アルギン酸カルシウム、アルギン酸アンモニウム等のアルギン酸塩及びその誘導体、キサンタンガム、グァーガム、ゼラチン、寒天、カルボキシメチルセルロースナトリウム、ヒドロキシエチルセルロース、ポリアクリル酸ナトリウムなどが挙げられ、これらのうち１種または２種以上を併用して用いることができる。
【００２７】
なお、上記成分を組み合わせた口腔用組成物は、常法に準じて製造できるものであり、その製法は特に限定されるものではない。
また、得られた練歯磨剤等の組成物は、アルミニウムチューブ、ラミネートチューブ、ガラス蒸着チューブ、プラスチックチューブ、プラスチックボトル、エアゾール容器等に充填されて使用することができる。
【００２８】
【発明の効果】
本発明の口腔用組成物用基剤によれば、保型性があって且つ安定性の高い非水系口腔用組成物を得ることができる。また、本発明の口腔用組成物用基剤と、通常水の存在下で不安定な有効成分であるα−ＴＣＰ、フッ化物、各種酵素、ヒノキチオール、ε−アミノカプロン酸などとを組み合わせて、保型性があって且つ有効成分が安定に維持され、粉体成分と液体成分の分離が起こらない経時的に安定な、非水系口腔用組成物を得ることができる。
【００２９】
【実施例】
以下、実験例及び比較例により、本発明を詳細に説明するが、本発明は下記の実施例に制限されるものではない。表１〜３に示す組成（単位：質量％）にて常法により各種練歯磨剤を調製し、以下の試験に供した。
＜歯磨剤保存安定性試験＞
表１に示す練歯磨剤を調製後、下記条件にて過酷保存を行った。過酷保存終了後、下記評価基準に従って各歯磨剤の状態について官能評価を行った。
「過酷保存条件」
１．６０℃の恒温槽中に、１ヶ月間保存
２．５０℃の恒温槽中に、２ヶ月間保存
「評価基準」
○：状態は調製直後と変わらない
×：分離が確認された
【００３０】
＜フッ素イオン測定試験＞
表２に示す歯磨剤を調製後、下記条件にて過酷保存を行った。過酷保存終了後、各歯磨剤の一定量を量り取り、水で分散し直ちに遠心分離し液層と固層とに分離した。これらの液層部分について、フッ素イオンメーターを用いて、フッ素イオン濃度を測定した。ここで検出されたフッ素イオンについては、歯磨剤中で他の成分に吸着していない、活性のあるフッ素イオンと考えられる。なお、活性のあるフッ素イオンの残存率は下記数式（１）より求めた。
「過酷保存条件」
１．６０℃の恒温槽中に、１週間保存
２．６０℃の恒温槽中に、２週間保存
数式（１）：
残存率（％）＝［（上記過酷保存後のフッ素イオンの量）／（歯磨剤調製時のフッ素イオンの量）］×１００
なお、歯磨剤過酷保存品において、フッ素イオン残存率、即ち活性のあるフッ素イオンが８０％以上であった場合、フッ化物は安定であると判断した。
また、実施例３、４、比較例４及び５の歯磨剤の過酷保存における状態安定性は保たれていた。
【００３１】
＜ε−アミノカプロン酸定量試験＞
表３に示す歯磨剤を調製後、下記条件にて過酷保存を行った。過酷保存終了後、各歯磨剤中のε−アミノカプロン酸について液体クロマトグラフ法にて定量試験を行った。なお、ε−アミノカプロン酸の残存率は数式（２）より求めた。
「過酷保存条件」
１．６０℃の恒温槽中に、１ヶ月間保存
２．５０℃の恒温槽中に、２ヶ月間保存
数式（２）：
残存率（％）＝［（上記過酷保存後のε−アミノカプロン酸の量）／ （歯磨剤調製時のε−アミノカプロン酸の量）］×１００
なお、歯磨剤過酷保存品において、ε−アミノカプロン酸残存率が９０%以上であった場合、ε−アミノカプロン酸は安定であると判断した。
また、本発明例５、６、比較例６及び７の歯磨剤の過酷保存における状態安定性は保たれていた。
【００３２】
【表１】
【表２】
【表３】
以上の実験結果から、まず表１から、本発明の口腔用組成物用基剤を用いることで練歯磨剤の状態について分離がなく保存安定性が優れていることがわかる。さらに表２及び３から、本発明の口腔用組成物である練歯磨剤において、フッ化物及びε−アミノカプロン酸の保存安定性が優れていることがわかる。
また下記の実施例７〜１２の常法により調製した練歯磨剤についても上記の実験を行ったところ、上記と同様な結果が得られた。
【００３６】
【実施例７】
練歯磨剤の調製
【実施例８】
練歯磨剤の調製
【実施例９】
練歯磨剤の調製
【実施例１０】
練歯磨剤の調製
【実施例１１】
練歯磨剤の調製
【実施例１２】
練歯磨剤の調製
BACKGROUND OF THE INVENTION
The present invention relates to a base for an oral composition, and more particularly to a base for an oral composition suitable for producing an oral composition containing little or no water. The present invention further relates to an oral composition containing such an oral composition base.
[0002]
[Prior art]
Oral compositions such as dentifrices generally contain an adhesive such as sodium carboxymethylcellulose, carrageenan or xanthan gum, and these ingredients dissolve in water to develop viscosity, and powders such as abrasives Ingredients and liquid components are combined to give shape retention or moderate viscosity. Therefore, in oral compositions such as dentifrices that do not contain water, it is difficult to maintain the shape-retaining property because the viscosity does not develop, and in oral compositions, separation of the powder component and the liquid component occurs over time. End up.
[0003]
On the other hand, oral compositions such as dentifrices may be blended with various active ingredients in preparations for the purpose of imparting functions and efficacy. As active ingredients, remineralization promoting ingredients, fluorides, bactericides, Examples include anti-inflammatory agents, hemostatic agents, various enzymes, and the like.
Examples of the remineralization-promoting component include calcium phosphate compounds such as hydroxyapatite, among which α-tricalcium phosphate (abbreviated as α-TCP) has a very high remineralization promoting effect in the oral cavity. It is known to be effective for restoration and the like.
However, α-TCP has the property of being converted to an apatite compound in the presence of water, and the reaction is accelerated by the presence of fluoride or other water-soluble calcium phosphate, causing a self-curing reaction. The composition for oral cavity such as an agent could not be stably blended.
[0004]
Fluoride includes sodium fluoride, monofluorophosphate, potassium fluoride, sodium monofluorophosphate, tin fluoride, etc. The effect of fluoride is that fluoride ions fluorinate the hydroxyapatite of the teeth and To strengthen quality. When fluoride is added to an oral composition such as a dentifrice containing normal water, fluoride ions start to dissolve in water in the oral composition and are adsorbed to other components such as abrasives. May not be demonstrated. For example, in an oral composition containing water in which an abrasive such as sodium fluoride or tin fluoride and an abrasive such as calcium phosphate or calcium carbonate are blended, fluorine ions may be adsorbed on the abrasive and inactivate the fluorine ions. Are known.
[0005]
Enzymes include lysozyme, mutanase, protease, amylase, dextranase, etc., which have lytic and proteolytic effects, but most of these enzymes are hydrolyzed when mixed in a composition containing water, resulting in enzyme activity. There is a problem that decreases. Therefore, when an enzyme is blended in a composition containing water, it is necessary to select an enzyme that hardly causes hydrolysis or to search for a stable blending method for each enzyme individually.
[0006]
In addition, hinokitiol as a natural disinfectant and ε-aminocaproic acid as a hemostatic agent may be added to oral compositions such as dentifrices, but when these active ingredients are also added to a composition containing water, The quantitative value tends to decrease due to decomposition.
Problems relating to the stability of these active ingredients are all due to the fact that water is contained in oral compositions such as dentifrices. Therefore, the composition for oral cavity such as a dentifrice containing almost no water that can be stably blended with α-TCP, fluoride, various enzymes, hinokitiol, and ε-aminocaproic acid, etc., has a shape retention property, and is stable over time. In addition, an oral composition having a composition that does not cause separation of a powder component and a liquid component is desired.
[0007]
[Problems to be solved by the invention]
An object of the present invention is to provide a base for an oral composition suitable for the production of an oral composition, particularly suitable for the production of an oral composition containing little or no water. . The object of the present invention is also an oral composition suitable for the production of an oral composition that is excellent in shape retention and stable over time, and does not cause separation of components, and particularly contains no or little water. Is to provide a base for use. It is another object of the present invention to provide a base for oral compositions that can stably contain active ingredients that are usually unstable in the presence of water. A further object of the present invention is to provide an oral composition in which an active ingredient that is usually unstable in the presence of water is stably blended, and in particular, an oral composition that contains little or no water. is there.
[0008]
[Means for Solving the Problems]
As a result of intensive studies to achieve the above object, the present inventors have found that it is possible to provide a highly stable oral composition by using a base having a specific composition. The present invention has been completed.
Accordingly, the present invention provides at least one selected from the group consisting of at least one kind of polyvinylpyrrolidone having a number average molecular weight of 10,000 to 360,000, and concentrated glycerin, diglycerin, propylene glycol, 1,3-butylene glycol and polyethylene glycol. The present invention relates to a nonaqueous oral cavity composition base characterized by containing a seed. As a preferred embodiment of the present invention, there is a base for a non-aqueous oral composition containing at least one selected from the group consisting of silicic anhydride and crystalline cellulose.
The present invention further relates to an oral composition containing the above-mentioned base for oral composition.
In the present specification, the non-aqueous oral cavity composition refers to an oral cavity having a water content of 0 to 2% by mass, preferably 0 to 1% by mass, and more preferably no water at all with respect to the entire oral composition. Means a composition. Furthermore, a base suitable for the production of such a non-aqueous oral composition is referred to herein as a non-aqueous oral composition base.
[0009]
The present invention also relates to an oral composition comprising the above-mentioned oral composition base and α-tricalcium phosphate (α-TCP). The present invention also relates to an oral composition comprising the above-mentioned base for oral composition and at least one fluoride.
The present invention further relates to an oral composition comprising the above-mentioned oral composition base and enzymes. The present invention further relates to an oral composition comprising the above-mentioned base for oral composition, and at least one selected from the group consisting of hinokitiol and ε-aminocaproic acid.
Furthermore, the present invention also includes an oral composition containing at least one selected from the above-mentioned bases for oral compositions and α-TCP, fluorides, enzymes, hinokitiol and ε-aminocaproic acid.
As a preferred embodiment of the oral composition of the present invention, there is an oral composition prepared by combining α-TCP and fluoride in the above-mentioned oral composition base.
[0010]
DETAILED DESCRIPTION OF THE INVENTION
The oral composition as used herein refers to dentifrices such as toothpastes, liquid dentifrices and moisturized dentifrices, creams, ointments, attachments, mouth fresheners, mouthwashes, chewing gum or Includes mouthwash. The oral composition of the present invention is desirably directed to a non-aqueous oral composition.
[0011]
The polyvinyl pyrrolidone used for the base for oral compositions of the present invention is a kind of synthetic compound obtained by the high-pressure synthesis method Repe reaction of acetylene, and is a linear polymer of vinyl pyrrolidone. Further, the molecular weight of this product is in the range of about 10,000 to 700,000 depending on the catalyst amount, temperature, time, etc. of the polymerization reaction.
In the present invention, one or more kinds of polyvinylpyrrolidone having a number average molecular weight of 10,000 to 360,000 can be used. That is, two or more types having different average molecular weights may be used. When the average molecular weight is less than 10,000, the expected effect is not exhibited, whereas when the average molecular weight exceeds 360,000, it is difficult to blend in the dosage form.
Such polyvinylpyrrolidone is widely used in pharmaceuticals, cosmetics, textiles, paper industry, printing, ink industry, protective coatings, beverage clarifiers, adhesives, agricultural chemistry, plastic industry, etc. In the present invention, commercially available products used for these can be used.
The content of polyvinylpyrrolidone having a number average molecular weight of 10,000 to 360,000 in the oral composition is 0.1 to 15% by mass, preferably 1 to 10% by mass, based on the total mass of the oral composition. . If this amount is less than 0.1% by mass, the expected effect is not exhibited. On the other hand, if it exceeds 15% by mass, an effect commensurate with the content cannot be obtained and the usability may be impaired.
[0012]
The oral composition base of the present invention further contains at least one selected from the group consisting of concentrated glycerin, diglycerin, propylene glycol, 1,3-butylene glycol and polyethylene glycol. Of these, concentrated glycerin and diglycerin are particularly preferably used.
Concentrated glycerin, diglycerin, propylene glycol, 1,3-butylene glycol and polyethylene glycol are widely used in general, including pharmaceuticals and cosmetics, foods, miscellaneous goods, petrochemical industry, paint industry and the like. In the present invention, commercially available products can be used.
The content of at least one of concentrated glycerin, diglycerin, propylene glycol, 1,3-butylene glycol and polyethylene glycol in the oral composition is suitably 10 to 70% by mass with respect to the total mass of the oral composition. Yes, preferably 20 to 60% by mass. If this amount is less than 10% by mass or exceeds 70% by mass, the usability may be impaired.
[0013]
The base for an oral composition of the present invention can further contain silicic anhydride and / or crystalline cellulose.
Silicic anhydride is silicon dioxide and is a white powder. Artificially, it is obtained by treating sodium silicate with an acid to precipitate silicon dioxide, gelling and aging, and then drying and grinding. Further, the loss on drying is 13% or less, and the loss on ignition is 18% or less. The loss on drying as used herein refers to the weight percentage of the evaporation component when 1 g of anhydrous silicic acid is heated at 105 ° C. for 2 hours, and the loss on ignition is that 1 g of anhydrous silicic acid is heated at 850 ° C. for 30 minutes. It is the weight percent of the evaporation component.
Such silicic acid anhydride is widely used in food, cosmetics, pharmaceuticals, agricultural supplies, baits, ink industry, rubber industry, plastic industry and so on.
The content of silicic anhydride in the oral composition is 0.5 to 30% by mass, preferably 3 to 15% by mass, based on the total mass of the oral composition. If this amount is less than 0.5% by mass, the expected effect is not exhibited. On the other hand, if it exceeds 30% by mass, an effect commensurate with the content cannot be obtained and the usability may be impaired.
[0014]
Crystalline cellulose is an aggregate of cellulose crystallites having a substantially constant degree of polymerization obtained by acid hydrolysis or alkali hydrolysis of α-cellulose obtained as a pulp from a fibrous plant.
Such crystalline cellulose is widely used in foods, cosmetics, pharmaceuticals, agricultural supplies, foods and the like.
Content of the crystalline cellulose in the composition for oral cavity of this invention is 0.5-30 mass% with respect to the total mass of the composition for oral cavity, Preferably it is 3-10 mass%. If this amount is less than 0.5% by mass, the expected effect is not exhibited. On the other hand, if it exceeds 30% by mass, an effect commensurate with the content cannot be obtained and the usability may be impaired.
[0015]
In the present invention, an oral composition can be obtained by combining various components such as additives and active ingredients conventionally used in oral compositions with the aforementioned oral composition base.
The base for oral compositions of the present invention is particularly advantageous in combination with components that are usually unstable in the presence of water. Examples of such components include α-TCP, fluoride, enzymes, hinokitiol, and ε-aminocaproic acid.
Α-TCP used in the composition for oral cavity of the present invention is α-tricalcium phosphate ( Ca 3 (PO 4 ) 2 ), widely used in pharmaceuticals, cosmetics, foods, sundries, petrochemical industries, etc. Generally used. In the present invention, commercially available products can be used.
0.1-50 mass% is suitable with respect to the total mass of the composition for oral cavity, and, as for content of (alpha) -TCP in the composition for oral cavity of this invention, Preferably it is 1-30 mass%. If this amount is less than 0.1% by mass, the expected re-fossilizing effect cannot be exhibited, while if it exceeds 50% by mass, the usability may be impaired.
When α-TCP is blended, if fluoride is used in combination, the supply of fluorine ions is added to the remineralization action, so that an extremely excellent effect is exhibited. Therefore, a combination of α-TCP and a fluoride described later is preferably used.
[0016]
Specific examples of the fluoride used in the oral composition of the present invention include sodium fluoride, monofluorophosphate, potassium fluoride, sodium monofluorophosphate, tin fluoride, and the like. Can be used. These fluorides are widely used in medicines and cosmetics. In the present invention, commercially available products can be used.
The fluoride content in the oral composition of the present invention is suitably 0.01 to 3% by mass with respect to the total mass of the oral composition, preferably as fluorine in the oral composition such as a dentifrice. The content is 100 to 1000 ppm.
Among them, sodium fluoride and sodium monofluorophosphate are preferable as the fluoride.
[0017]
Specific examples of enzymes used in the oral composition of the present invention include lysozyme, mutanase, protease, amylase, dextranase, and the like, and one or more of these can be used. These enzymes are widely used in medicines, cosmetics, foods and the like. In the present invention, commercially available products can be used.
0.01-5 mass% is suitable with respect to the total mass of an oral composition, and, as for enzyme content in the composition for oral cavity of this invention, Preferably it is 0.1-2 mass%.
As the enzyme, lysozyme and amylase are preferable.
[0018]
Hinokitiol used in the composition for oral cavity of the present invention is a unique component contained in natural trees such as Aomori Hiba and is a crystalline acidic compound. Other tree species containing hinokitiol include Taiwan cypress, North American Western red cedar and the like. Hinokitiol has strong antibacterial activity and broad antibacterial spectrum and is one of the few natural fungicides.
Such hinokitiol is widely used in foods, cosmetics, pharmaceuticals, agricultural supplies, building materials, baits, etc., and in the present invention, commercial products used for these can be used. .
The content of hinokitiol in the oral composition of the present invention is suitably 0.005 to 0.5% by mass, preferably 0.01 to 0.2% by mass, based on the total mass of the oral composition. is there.
[0019]
The ε-aminocaproic acid used in the oral composition of the present invention is a component having an antiplasmin effect, a hemostatic effect, and an anti-inflammatory effect, and is widely used in cosmetics, pharmaceuticals, foods, agricultural products, and the like. Is. In the present invention, commercially available products can be used.
The content of ε-aminocaproic acid in the oral composition of the present invention is suitably 0.001 to 1% by mass, preferably 0.006 to 0.2% by mass, based on the total mass of the oral composition. It is.
[0020]
As mentioned above, (1) α-TCP; (2) fluoride; (3) enzymes; (4) hinokitiol; and ▲ as active ingredients suitable for combination with the oral composition base of the present invention There is 5 ▼ ε-aminocaproic acid. One or more compounds can be selected and included from each of the groups (1) to (5), and the compounds can be selected from two or more groups and used in combination. it can. Of these, the combined use of α-TCP and fluoride is preferred.
[0021]
Depending on the type of the composition for oral cavity of the present invention, in addition to the above-mentioned components, the following components can be blended as necessary within the range of normal use amounts.
<Abrasive>
Silica-based abrasives such as silica gel, precipitated silica, pyrogenic silica, hydrous silicic acid, zeolite, aluminosilicate, zirconosilicate, dicalcium phosphate dihydrate, dicalcium phosphate dihydrate, calcium pyrophosphate, third Examples include magnesium phosphate, tricalcium phosphate, aluminum hydroxide, alumina, light calcium carbonate, heavy calcium carbonate, magnesium carbonate, zirconium silicate, and synthetic resin-based abrasive. It can be used in combination. As for the compounding quantity of the said abrasive | polishing agent, 3-60 mass% is preferable with respect to the whole composition, More preferably, it is 10-45 mass%.
[0022]
<Wetting agent>
One kind or two or more kinds of polyhydric alcohols such as sorbitol and maltitol can be used.
<Foaming agent>
Sodium lauryl sulfate, sodium lauroyl sarcosine, sodium alkylsulfosuccinate, sodium palm oil fatty acid monoglycerin sulfonate, sodium α-olefin sulfonate, N-acylamino acid salts such as N-acylglutamate, 2-alkyl-N-carboxymethyl -N-hydroxyethyl imidazolinium betaine, maltitol fatty acid ester, sucrose fatty acid ester, polyglycerin fatty acid ester, fatty acid diethanolamide, polyoxyethylene sorbitan monostearate, polyoxyethylene hydrogenated castor oil, polyoxyethylene fatty acid ester, etc. Of these, one or more of these can be used in combination.
[0023]
<Sweetener>
Sodium saccharin, aspartame, trehalose, stevioside, stevia extract, paramethoxycinnamic aldehyde, neohesperidyl dihydrochalcone, perilartine, etc.
<Preservative>
Parabens such as methylparaben, ethylparaben, propylparaben, butylparaben, sodium benzoate, phenoxyethanol, alkyldiaminoethylglycine hydrochloride and the like.
[0024]
<Perfume ingredients>
Use one or more of l-menthol, anethole, menthone, cineol, limonene, carvone, methyl salicylate, ethyl butyrate, eugenol, thymol, cinnamic aldehyde, trans-2-hexenal, etc. Can do. Although these components may be mix | blended with a single item, you may mix | blend the essential oil etc. which contain these.
In addition to the above fragrance components, fragrance components such as aliphatic alcohols and esters thereof, terpene hydrocarbons, phenol ethers, aldehydes, ketones, and lactones, and essential oils may be blended within a range that does not interfere with the effects of the present invention. It is preferable that the compounding quantity of the said fragrance | flavor shall be 0.02-2 mass% with respect to the whole composition.
[0025]
<Active ingredient>
Zeolite, chlorhexidine salts, cetylpyridinium chloride, benzalkonium chloride, benzethonium chloride, bisabolol, triclosan, isopropylmethylphenol, tocopherol acetate, tranexamic acid, dihydrocholesterol, glycyrrhetinic acid, glycyrrhizinate, copper chlorophyllin salt, sodium chloride, guay One or more of azulene sulfonate, pyridoxine hydrochloride, and the like can be blended.
<Others>
Colors such as Blue No. 1, pigments such as titanium oxide, antioxidants such as dibutylhydroxytoluene, tea dry distillation liquid, and flavoring agents such as sodium glutamate.
[0026]
Depending on the type of the composition for oral cavity of the present invention, when water is blended in the range of 2% by mass or less, the following binder can be blended as necessary in addition to the above components.
<Binder>
Carrageenan (ι, λ, κ), alginic acid, sodium alginate, propylene glycol alginate, calcium-containing sodium alginate, potassium alginate, calcium alginate, ammonium alginate and its derivatives, xanthan gum, guar gum, gelatin, agar, carboxymethylcellulose Examples thereof include sodium, hydroxyethyl cellulose, sodium polyacrylate, and the like, and one or more of these can be used in combination.
[0027]
In addition, the composition for oral cavity which combined the said component can be manufactured according to a conventional method, The manufacturing method is not specifically limited.
The obtained composition such as toothpaste can be used by being filled in an aluminum tube, a laminate tube, a glass vapor deposition tube, a plastic tube, a plastic bottle, an aerosol container or the like.
[0028]
【The invention's effect】
According to the oral composition base of the present invention, a non-aqueous oral composition having shape retention and high stability can be obtained. In addition, the base for oral compositions of the present invention is combined with α-TCP, fluoride, various enzymes, hinokitiol, ε-aminocaproic acid, etc., which are active ingredients that are usually unstable in the presence of water. It is possible to obtain a non-aqueous oral cavity composition that has moldability, maintains an active ingredient stably, and is stable over time without separation of a powder component and a liquid component.
[0029]
【Example】
EXAMPLES Hereinafter, although an Example and a comparative example demonstrate this invention in detail, this invention is not restrict | limited to the following Example. Various toothpastes were prepared by a conventional method with the compositions shown in Tables 1 to 3 (unit: mass%) and subjected to the following tests.
<Dentifrice storage stability test>
After preparing the toothpaste shown in Table 1, severe storage was performed under the following conditions. After severe storage, sensory evaluation was performed on the state of each dentifrice according to the following evaluation criteria.
"Severe storage conditions"
1. Store for 1 month in a 60 ° C constant temperature bath Store for 2 months in a 2.50 ° C constant temperature bath "Evaluation criteria"
○: The state is the same as that immediately after preparation. ×: Separation was confirmed.
<Fluorine ion measurement test>
After preparing the dentifrice shown in Table 2, severe storage was performed under the following conditions. After severe storage, a certain amount of each dentifrice was weighed, dispersed with water, immediately centrifuged, and separated into a liquid layer and a solid layer. About these liquid layer parts, the fluorine ion concentration was measured using the fluorine ion meter. The fluorine ions detected here are considered to be active fluorine ions that are not adsorbed to other components in the dentifrice. The residual ratio of active fluorine ions was determined from the following mathematical formula (1).
"Severe storage conditions"
1. Store for one week in a constant temperature bath at 60 ° C. 2. Store for two weeks in a constant temperature bath at 60 ° C. Formula (1):
Residual rate (%) = [(amount of fluoride ion after severe storage) / (amount of fluoride ion during preparation of dentifrice)] × 100
In the severely preserved dentifrice, the fluoride ion remaining rate, that is, when the active fluorine ion was 80% or more, the fluoride was judged to be stable.
Moreover, the state stability in the severe preservation | save of the dentifrice of Examples 3, 4 and Comparative Examples 4 and 5 was maintained.
[0031]
<Ε-aminocaproic acid quantitative test>
After preparing the dentifrice shown in Table 3, severe storage was performed under the following conditions. After severe storage, a quantitative test was performed on the ε-aminocaproic acid in each dentifrice by a liquid chromatographic method. The residual ratio of ε-aminocaproic acid was determined from Equation (2).
"Severe storage conditions"
1. Store in a constant temperature bath at 60 ° C for 1 month Store in a constant temperature bath at 2.50 ° C for 2 months Formula (2):
Residual rate (%) = [(amount of ε-aminocaproic acid after severe storage) / (amount of ε-aminocaproic acid during preparation of dentifrice)] × 100
In the severely preserved dentifrice, when ε-aminocaproic acid residual rate was 90% or more, ε-aminocaproic acid was judged to be stable.
Moreover, the state stability in the severe preservation | save of the dentifrice of this invention example 5 and 6 and the comparative examples 6 and 7 was maintained.
[0032]
[Table 1]
[Table 2]
[Table 3]
From the above experimental results, it can be seen from Table 1 that, by using the oral composition base of the present invention, the state of the toothpaste is not separated and the storage stability is excellent. Furthermore, it can be seen from Tables 2 and 3 that in the toothpaste that is the oral composition of the present invention, the storage stability of fluoride and ε-aminocaproic acid is excellent.
Moreover, when said experiment was done also about the toothpaste prepared by the conventional method of the following Examples 7-12, the result similar to the above was obtained.
[0036]
[Example 7]
Preparation of toothpaste
[Example 8]
Preparation of toothpaste
[Example 9]
Preparation of toothpaste
[Example 10]
Preparation of toothpaste
Example 11
Preparation of toothpaste
Example 12
Preparation of toothpaste
Claims (3)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2001056155A JP4803889B2 (en) | 2001-03-01 | 2001-03-01 | Non-aqueous toothpaste |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2001056155A JP4803889B2 (en) | 2001-03-01 | 2001-03-01 | Non-aqueous toothpaste |
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| JP2002255772A JP2002255772A (en) | 2002-09-11 |
| JP4803889B2 true JP4803889B2 (en) | 2011-10-26 |
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| JP2001056155A Expired - Lifetime JP4803889B2 (en) | 2001-03-01 | 2001-03-01 | Non-aqueous toothpaste |
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Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP5130601B2 (en) * | 2001-08-07 | 2013-01-30 | 大正製薬株式会社 | Semi-solid oral composition |
| AU2003277607B2 (en) | 2002-11-07 | 2009-01-22 | Taisho Pharmaceutical Co., Ltd. | Base for oral composition and oral composition |
| JP4888636B2 (en) * | 2005-12-21 | 2012-02-29 | ライオン株式会社 | Dentifrice composition |
| MX348278B (en) * | 2009-12-04 | 2017-06-02 | Colgate-Palmolive Company * | NON-WATERPROOF DENTIFRIC DENTIFRIC COMPOSITIONS OF SINGLE PIPE, METHODS OF USE AND MANUFACTURING OF THE SAME. |
| MX2012007164A (en) * | 2009-12-23 | 2012-07-03 | Colgate Palmolive Co | COMPOSITIONS FOR ORAL CARE. |
| WO2022064598A1 (en) * | 2020-09-24 | 2022-03-31 | ライオン株式会社 | Polyhydric alcohol-based dentifrice composition |
| JP7625843B2 (en) * | 2020-12-14 | 2025-02-04 | ライオン株式会社 | Oral Composition |
| JP7844157B2 (en) * | 2021-12-24 | 2026-04-13 | サンスター株式会社 | Hinokitiol-containing composition |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4132771A (en) * | 1977-08-24 | 1979-01-02 | Schreiber Ronald S | Warm two tone flavored dentifrice |
| JPH0259513A (en) * | 1988-08-24 | 1990-02-28 | Kiyuukiyuu Yakuhin Kogyo Kk | Oral cavity mucosa-attaching type halitosis-preventing agent |
| US5032384A (en) * | 1989-01-27 | 1991-07-16 | Block Drug Company, Inc. | Compositions and method for the treatment of disease |
| JPH05331032A (en) * | 1992-05-27 | 1993-12-14 | Tanpei Seiyaku Kk | Composition for oral cavity |
| JP3022039B2 (en) * | 1993-03-05 | 2000-03-15 | サンスター株式会社 | Oral composition for preventing tooth coloring |
| JPH09255542A (en) * | 1996-03-21 | 1997-09-30 | Shiseido Co Ltd | Composition for oral cavity application |
| JPH10139644A (en) * | 1996-11-13 | 1998-05-26 | Sunstar Inc | Oral cavity composition containing bioactive glass |
| CA2373867C (en) * | 1999-07-02 | 2009-10-13 | The Procter & Gamble Company | Compositions comprising organosiloxane resins for delivering oral care substances |
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2001
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