CN116669680A - 口腔用组合物 - Google Patents
口腔用组合物 Download PDFInfo
- Publication number
- CN116669680A CN116669680A CN202180087610.8A CN202180087610A CN116669680A CN 116669680 A CN116669680 A CN 116669680A CN 202180087610 A CN202180087610 A CN 202180087610A CN 116669680 A CN116669680 A CN 116669680A
- Authority
- CN
- China
- Prior art keywords
- oral composition
- sulfate
- mass
- sodium
- component
- 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.)
- Pending
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- 239000000203 mixture Substances 0.000 title claims abstract description 71
- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 claims abstract description 10
- 239000000551 dentifrice Substances 0.000 claims abstract description 10
- BVKZGUZCCUSVTD-UHFFFAOYSA-M Bicarbonate Chemical compound OC([O-])=O BVKZGUZCCUSVTD-UHFFFAOYSA-M 0.000 claims abstract description 9
- BVKZGUZCCUSVTD-UHFFFAOYSA-L Carbonate Chemical compound [O-]C([O-])=O BVKZGUZCCUSVTD-UHFFFAOYSA-L 0.000 claims abstract description 8
- GWRCTWAPTXBPHW-UHFFFAOYSA-N N-[(Ethoxycarbonyl)methyl)-p-menthane-3-carboxamide Chemical compound CCOC(=O)CNC(=O)C1CC(C)CCC1C(C)C GWRCTWAPTXBPHW-UHFFFAOYSA-N 0.000 claims abstract description 8
- ILXQRAXCLBJOAD-UHFFFAOYSA-N N-(2-hydroxy-2-phenylethyl)-5,5-dimethyl-2-propan-2-ylcyclohexane-1-carboxamide Chemical compound CC(C)C1CCC(C)(C)CC1C(=O)NCC(O)c1ccccc1 ILXQRAXCLBJOAD-UHFFFAOYSA-N 0.000 claims abstract description 7
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 claims abstract description 7
- WXABJFUNSDXVNH-UHFFFAOYSA-N 5-methyl-2-propan-2-yl-n-(2-pyridin-2-ylethyl)cyclohexane-1-carboxamide Chemical compound CC(C)C1CCC(C)CC1C(=O)NCCC1=CC=CC=N1 WXABJFUNSDXVNH-UHFFFAOYSA-N 0.000 claims abstract description 5
- -1 polyoxyethylene Polymers 0.000 claims description 56
- 239000000194 fatty acid Substances 0.000 claims description 28
- 235000002639 sodium chloride Nutrition 0.000 claims description 28
- 235000014113 dietary fatty acids Nutrition 0.000 claims description 27
- 229930195729 fatty acid Natural products 0.000 claims description 27
- 229920003171 Poly (ethylene oxide) Polymers 0.000 claims description 13
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 claims description 10
- PMZURENOXWZQFD-UHFFFAOYSA-L Sodium Sulfate Chemical compound [Na+].[Na+].[O-]S([O-])(=O)=O PMZURENOXWZQFD-UHFFFAOYSA-L 0.000 claims description 8
- 239000004359 castor oil Substances 0.000 claims description 7
- 235000019438 castor oil Nutrition 0.000 claims description 7
- 239000003795 chemical substances by application Substances 0.000 claims description 7
- ZEMPKEQAKRGZGQ-XOQCFJPHSA-N glycerol triricinoleate Natural products CCCCCC[C@@H](O)CC=CCCCCCCCC(=O)OC[C@@H](COC(=O)CCCCCCCC=CC[C@@H](O)CCCCCC)OC(=O)CCCCCCCC=CC[C@H](O)CCCCCC ZEMPKEQAKRGZGQ-XOQCFJPHSA-N 0.000 claims description 7
- 229910052938 sodium sulfate Inorganic materials 0.000 claims description 7
- 235000011152 sodium sulphate Nutrition 0.000 claims description 7
- TWRXJAOTZQYOKJ-UHFFFAOYSA-L Magnesium chloride Chemical compound [Mg+2].[Cl-].[Cl-] TWRXJAOTZQYOKJ-UHFFFAOYSA-L 0.000 claims description 6
- CSNNHWWHGAXBCP-UHFFFAOYSA-L Magnesium sulfate Chemical compound [Mg+2].[O-][S+2]([O-])([O-])[O-] CSNNHWWHGAXBCP-UHFFFAOYSA-L 0.000 claims description 6
- WCUXLLCKKVVCTQ-UHFFFAOYSA-M Potassium chloride Chemical compound [Cl-].[K+] WCUXLLCKKVVCTQ-UHFFFAOYSA-M 0.000 claims description 6
- CDBYLPFSWZWCQE-UHFFFAOYSA-L Sodium Carbonate Chemical compound [Na+].[Na+].[O-]C([O-])=O CDBYLPFSWZWCQE-UHFFFAOYSA-L 0.000 claims description 6
- 239000002736 nonionic surfactant Substances 0.000 claims description 6
- BWHMMNNQKKPAPP-UHFFFAOYSA-L potassium carbonate Chemical compound [K+].[K+].[O-]C([O-])=O BWHMMNNQKKPAPP-UHFFFAOYSA-L 0.000 claims description 6
- 150000005215 alkyl ethers Chemical class 0.000 claims description 5
- GRLPQNLYRHEGIJ-UHFFFAOYSA-J potassium aluminium sulfate Chemical compound [Al+3].[K+].[O-]S([O-])(=O)=O.[O-]S([O-])(=O)=O GRLPQNLYRHEGIJ-UHFFFAOYSA-J 0.000 claims description 5
- 239000011780 sodium chloride Substances 0.000 claims description 5
- UIIMBOGNXHQVGW-DEQYMQKBSA-M Sodium bicarbonate-14C Chemical compound [Na+].O[14C]([O-])=O UIIMBOGNXHQVGW-DEQYMQKBSA-M 0.000 claims description 4
- 229940103272 aluminum potassium sulfate Drugs 0.000 claims description 4
- 239000011248 coating agent Substances 0.000 claims description 4
- ZLNQQNXFFQJAID-UHFFFAOYSA-L magnesium carbonate Chemical compound [Mg+2].[O-]C([O-])=O ZLNQQNXFFQJAID-UHFFFAOYSA-L 0.000 claims description 4
- 239000001095 magnesium carbonate Substances 0.000 claims description 4
- 229910000021 magnesium carbonate Inorganic materials 0.000 claims description 4
- OTYBMLCTZGSZBG-UHFFFAOYSA-L potassium sulfate Chemical compound [K+].[K+].[O-]S([O-])(=O)=O OTYBMLCTZGSZBG-UHFFFAOYSA-L 0.000 claims description 4
- 229910052939 potassium sulfate Inorganic materials 0.000 claims description 4
- 235000011151 potassium sulphates Nutrition 0.000 claims description 4
- NKWPZUCBCARRDP-UHFFFAOYSA-L calcium bicarbonate Chemical compound [Ca+2].OC([O-])=O.OC([O-])=O NKWPZUCBCARRDP-UHFFFAOYSA-L 0.000 claims description 3
- 229910000020 calcium bicarbonate Inorganic materials 0.000 claims description 3
- QWDJLDTYWNBUKE-UHFFFAOYSA-L magnesium bicarbonate Chemical compound [Mg+2].OC([O-])=O.OC([O-])=O QWDJLDTYWNBUKE-UHFFFAOYSA-L 0.000 claims description 3
- 229910000022 magnesium bicarbonate Inorganic materials 0.000 claims description 3
- 239000002370 magnesium bicarbonate Substances 0.000 claims description 3
- 235000014824 magnesium bicarbonate Nutrition 0.000 claims description 3
- 229910001629 magnesium chloride Inorganic materials 0.000 claims description 3
- 229910052943 magnesium sulfate Inorganic materials 0.000 claims description 3
- 235000019341 magnesium sulphate Nutrition 0.000 claims description 3
- 239000002324 mouth wash Substances 0.000 claims description 3
- 235000015497 potassium bicarbonate Nutrition 0.000 claims description 3
- 229910000028 potassium bicarbonate Inorganic materials 0.000 claims description 3
- 239000011736 potassium bicarbonate Substances 0.000 claims description 3
- 229910000027 potassium carbonate Inorganic materials 0.000 claims description 3
- 235000011181 potassium carbonates Nutrition 0.000 claims description 3
- 239000001103 potassium chloride Substances 0.000 claims description 3
- 235000011164 potassium chloride Nutrition 0.000 claims description 3
- TYJJADVDDVDEDZ-UHFFFAOYSA-M potassium hydrogencarbonate Chemical compound [K+].OC([O-])=O TYJJADVDDVDEDZ-UHFFFAOYSA-M 0.000 claims description 3
- 229910000029 sodium carbonate Inorganic materials 0.000 claims description 3
- 239000007921 spray Substances 0.000 claims description 3
- HSEYYGFJBLWFGD-UHFFFAOYSA-N 4-methylsulfanyl-2-[(2-methylsulfanylpyridine-3-carbonyl)amino]butanoic acid Chemical compound CSCCC(C(O)=O)NC(=O)C1=CC=CN=C1SC HSEYYGFJBLWFGD-UHFFFAOYSA-N 0.000 claims description 2
- 238000004090 dissolution Methods 0.000 claims description 2
- 229940051866 mouthwash Drugs 0.000 claims description 2
- GJPYYNMJTJNYTO-UHFFFAOYSA-J sodium aluminium sulfate Chemical compound [Na+].[Al+3].[O-]S([O-])(=O)=O.[O-]S([O-])(=O)=O GJPYYNMJTJNYTO-UHFFFAOYSA-J 0.000 claims description 2
- 238000000576 coating method Methods 0.000 claims 1
- 230000000694 effects Effects 0.000 abstract description 24
- 235000019606 astringent taste Nutrition 0.000 abstract description 19
- 150000003839 salts Chemical class 0.000 description 18
- 210000000214 mouth Anatomy 0.000 description 17
- UIIMBOGNXHQVGW-UHFFFAOYSA-M Sodium bicarbonate Chemical compound [Na+].OC([O-])=O UIIMBOGNXHQVGW-UHFFFAOYSA-M 0.000 description 16
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 15
- KWIUHFFTVRNATP-UHFFFAOYSA-N glycine betaine Chemical compound C[N+](C)(C)CC([O-])=O KWIUHFFTVRNATP-UHFFFAOYSA-N 0.000 description 14
- 238000000034 method Methods 0.000 description 14
- 239000003921 oil Substances 0.000 description 12
- 235000019198 oils Nutrition 0.000 description 12
- 239000000049 pigment Substances 0.000 description 12
- 150000004665 fatty acids Chemical class 0.000 description 10
- 239000011230 binding agent Substances 0.000 description 9
- 230000000052 comparative effect Effects 0.000 description 9
- 238000011156 evaluation Methods 0.000 description 9
- 239000000463 material Substances 0.000 description 9
- 229960003237 betaine Drugs 0.000 description 8
- 125000004432 carbon atom Chemical group C* 0.000 description 8
- 235000017557 sodium bicarbonate Nutrition 0.000 description 8
- 229910000030 sodium bicarbonate Inorganic materials 0.000 description 8
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 8
- 239000000377 silicon dioxide Substances 0.000 description 7
- 229940034610 toothpaste Drugs 0.000 description 7
- 239000000606 toothpaste Substances 0.000 description 7
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 6
- 239000002304 perfume Substances 0.000 description 6
- 239000004094 surface-active agent Substances 0.000 description 6
- GWEVSGVZZGPLCZ-UHFFFAOYSA-N Titan oxide Chemical compound O=[Ti]=O GWEVSGVZZGPLCZ-UHFFFAOYSA-N 0.000 description 5
- 125000000217 alkyl group Chemical group 0.000 description 5
- 235000001014 amino acid Nutrition 0.000 description 5
- 229940024606 amino acid Drugs 0.000 description 5
- 235000003599 food sweetener Nutrition 0.000 description 5
- OSWPMRLSEDHDFF-UHFFFAOYSA-N methyl salicylate Chemical compound COC(=O)C1=CC=CC=C1O OSWPMRLSEDHDFF-UHFFFAOYSA-N 0.000 description 5
- 239000003755 preservative agent Substances 0.000 description 5
- 150000005846 sugar alcohols Chemical class 0.000 description 5
- 239000003765 sweetening agent Substances 0.000 description 5
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 description 4
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 description 4
- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 description 4
- FFDGPVCHZBVARC-UHFFFAOYSA-N N,N-dimethylglycine Chemical compound CN(C)CC(O)=O FFDGPVCHZBVARC-UHFFFAOYSA-N 0.000 description 4
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 description 4
- 125000002252 acyl group Chemical group 0.000 description 4
- POJWUDADGALRAB-UHFFFAOYSA-N allantoin Chemical compound NC(=O)NC1NC(=O)NC1=O POJWUDADGALRAB-UHFFFAOYSA-N 0.000 description 4
- 239000002280 amphoteric surfactant Substances 0.000 description 4
- 239000003945 anionic surfactant Substances 0.000 description 4
- FUWUEFKEXZQKKA-UHFFFAOYSA-N beta-thujaplicin Chemical compound CC(C)C=1C=CC=C(O)C(=O)C=1 FUWUEFKEXZQKKA-UHFFFAOYSA-N 0.000 description 4
- POULHZVOKOAJMA-UHFFFAOYSA-N dodecanoic acid Chemical compound CCCCCCCCCCCC(O)=O POULHZVOKOAJMA-UHFFFAOYSA-N 0.000 description 4
- 239000000796 flavoring agent Substances 0.000 description 4
- 235000019634 flavors Nutrition 0.000 description 4
- 238000009472 formulation Methods 0.000 description 4
- 239000003906 humectant Substances 0.000 description 4
- 239000004615 ingredient Substances 0.000 description 4
- 238000002360 preparation method Methods 0.000 description 4
- 230000002335 preservative effect Effects 0.000 description 4
- PUZPDOWCWNUUKD-UHFFFAOYSA-M sodium fluoride Chemical compound [F-].[Na+] PUZPDOWCWNUUKD-UHFFFAOYSA-M 0.000 description 4
- 235000019333 sodium laurylsulphate Nutrition 0.000 description 4
- 159000000000 sodium salts Chemical class 0.000 description 4
- 239000002904 solvent Substances 0.000 description 4
- BDHFUVZGWQCTTF-UHFFFAOYSA-M sulfonate Chemical compound [O-]S(=O)=O BDHFUVZGWQCTTF-UHFFFAOYSA-M 0.000 description 4
- 229940104261 taurate Drugs 0.000 description 4
- MGSRCZKZVOBKFT-UHFFFAOYSA-N thymol Chemical compound CC(C)C1=CC=C(C)C=C1O MGSRCZKZVOBKFT-UHFFFAOYSA-N 0.000 description 4
- 239000004711 α-olefin Substances 0.000 description 4
- 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 3
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 3
- 108010011485 Aspartame Proteins 0.000 description 3
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 3
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 description 3
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 description 3
- IAYPIBMASNFSPL-UHFFFAOYSA-N Ethylene oxide Chemical compound C1CO1 IAYPIBMASNFSPL-UHFFFAOYSA-N 0.000 description 3
- WEEGYLXZBRQIMU-UHFFFAOYSA-N Eucalyptol Chemical compound C1CC2CCC1(C)OC2(C)C WEEGYLXZBRQIMU-UHFFFAOYSA-N 0.000 description 3
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 3
- 229920001214 Polysorbate 60 Polymers 0.000 description 3
- KWYUFKZDYYNOTN-UHFFFAOYSA-M Potassium hydroxide Chemical compound [OH-].[K+] KWYUFKZDYYNOTN-UHFFFAOYSA-M 0.000 description 3
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 3
- 150000008051 alkyl sulfates Chemical class 0.000 description 3
- 150000003863 ammonium salts Chemical class 0.000 description 3
- IAOZJIPTCAWIRG-QWRGUYRKSA-N aspartame Chemical compound OC(=O)C[C@H](N)C(=O)N[C@H](C(=O)OC)CC1=CC=CC=C1 IAOZJIPTCAWIRG-QWRGUYRKSA-N 0.000 description 3
- 230000001680 brushing effect Effects 0.000 description 3
- 239000003093 cationic surfactant Substances 0.000 description 3
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 3
- 239000003086 colorant Substances 0.000 description 3
- 239000002552 dosage form Substances 0.000 description 3
- 229940079593 drug Drugs 0.000 description 3
- 239000003814 drug Substances 0.000 description 3
- 238000005187 foaming Methods 0.000 description 3
- 235000010449 maltitol Nutrition 0.000 description 3
- 239000000845 maltitol Substances 0.000 description 3
- 229940035436 maltitol Drugs 0.000 description 3
- 238000004519 manufacturing process Methods 0.000 description 3
- TWNQGVIAIRXVLR-UHFFFAOYSA-N oxo(oxoalumanyloxy)alumane Chemical compound O=[Al]O[Al]=O TWNQGVIAIRXVLR-UHFFFAOYSA-N 0.000 description 3
- VSIIXMUUUJUKCM-UHFFFAOYSA-D pentacalcium;fluoride;triphosphate Chemical compound [F-].[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 VSIIXMUUUJUKCM-UHFFFAOYSA-D 0.000 description 3
- 238000005498 polishing Methods 0.000 description 3
- 229920001223 polyethylene glycol Polymers 0.000 description 3
- XAEFZNCEHLXOMS-UHFFFAOYSA-M potassium benzoate Chemical compound [K+].[O-]C(=O)C1=CC=CC=C1 XAEFZNCEHLXOMS-UHFFFAOYSA-M 0.000 description 3
- 239000000341 volatile oil Substances 0.000 description 3
- GFQYVLUOOAAOGM-UHFFFAOYSA-N zirconium(iv) silicate Chemical compound [Zr+4].[O-][Si]([O-])([O-])[O-] GFQYVLUOOAAOGM-UHFFFAOYSA-N 0.000 description 3
- XHXUANMFYXWVNG-ADEWGFFLSA-N (-)-Menthyl acetate Chemical compound CC(C)[C@@H]1CC[C@@H](C)C[C@H]1OC(C)=O XHXUANMFYXWVNG-ADEWGFFLSA-N 0.000 description 2
- GVJHHUAWPYXKBD-UHFFFAOYSA-N (±)-α-Tocopherol Chemical compound OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-UHFFFAOYSA-N 0.000 description 2
- LDVVTQMJQSCDMK-UHFFFAOYSA-N 1,3-dihydroxypropan-2-yl formate Chemical compound OCC(CO)OC=O LDVVTQMJQSCDMK-UHFFFAOYSA-N 0.000 description 2
- HFDVRLIODXPAHB-UHFFFAOYSA-N 1-tetradecene Chemical compound CCCCCCCCCCCCC=C HFDVRLIODXPAHB-UHFFFAOYSA-N 0.000 description 2
- WNWHHMBRJJOGFJ-UHFFFAOYSA-N 16-methylheptadecan-1-ol Chemical compound CC(C)CCCCCCCCCCCCCCCO WNWHHMBRJJOGFJ-UHFFFAOYSA-N 0.000 description 2
- XDOFQFKRPWOURC-UHFFFAOYSA-N 16-methylheptadecanoic acid Chemical compound CC(C)CCCCCCCCCCCCCCC(O)=O XDOFQFKRPWOURC-UHFFFAOYSA-N 0.000 description 2
- AXCXHFKZHDEKTP-NSCUHMNNSA-N 4-methoxycinnamaldehyde Chemical compound COC1=CC=C(\C=C\C=O)C=C1 AXCXHFKZHDEKTP-NSCUHMNNSA-N 0.000 description 2
- POJWUDADGALRAB-PVQJCKRUSA-N Allantoin Natural products NC(=O)N[C@@H]1NC(=O)NC1=O POJWUDADGALRAB-PVQJCKRUSA-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
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 description 2
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 description 2
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 description 2
- VUNOFAIHSALQQH-UHFFFAOYSA-N Ethyl menthane carboxamide Chemical compound CCNC(=O)C1CC(C)CCC1C(C)C VUNOFAIHSALQQH-UHFFFAOYSA-N 0.000 description 2
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 description 2
- 240000001238 Gaultheria procumbens Species 0.000 description 2
- 235000007297 Gaultheria procumbens Nutrition 0.000 description 2
- 239000004471 Glycine Substances 0.000 description 2
- 235000005206 Hibiscus Nutrition 0.000 description 2
- 235000007185 Hibiscus lunariifolius Nutrition 0.000 description 2
- 244000284380 Hibiscus rosa sinensis Species 0.000 description 2
- 239000004354 Hydroxyethyl cellulose Substances 0.000 description 2
- 229920000663 Hydroxyethyl cellulose Polymers 0.000 description 2
- QNAYBMKLOCPYGJ-REOHCLBHSA-N L-alanine Chemical compound C[C@H](N)C(O)=O QNAYBMKLOCPYGJ-REOHCLBHSA-N 0.000 description 2
- 239000005639 Lauric acid Substances 0.000 description 2
- 108010014251 Muramidase Proteins 0.000 description 2
- 102000016943 Muramidase Human genes 0.000 description 2
- 108010062010 N-Acetylmuramoyl-L-alanine Amidase Proteins 0.000 description 2
- 235000004347 Perilla Nutrition 0.000 description 2
- 244000124853 Perilla frutescens Species 0.000 description 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 description 2
- 239000002202 Polyethylene glycol Substances 0.000 description 2
- AUNGANRZJHBGPY-SCRDCRAPSA-N Riboflavin Chemical compound OC[C@@H](O)[C@@H](O)[C@@H](O)CN1C=2C=C(C)C(C)=CC=2N=C2C1=NC(=O)NC2=O AUNGANRZJHBGPY-SCRDCRAPSA-N 0.000 description 2
- WINXNKPZLFISPD-UHFFFAOYSA-M Saccharin sodium Chemical compound [Na+].C1=CC=C2C(=O)[N-]S(=O)(=O)C2=C1 WINXNKPZLFISPD-UHFFFAOYSA-M 0.000 description 2
- 239000005844 Thymol Substances 0.000 description 2
- RTAQQCXQSZGOHL-UHFFFAOYSA-N Titanium Chemical compound [Ti] RTAQQCXQSZGOHL-UHFFFAOYSA-N 0.000 description 2
- YKTSYUJCYHOUJP-UHFFFAOYSA-N [O--].[Al+3].[Al+3].[O-][Si]([O-])([O-])[O-] Chemical compound [O--].[Al+3].[Al+3].[O-][Si]([O-])([O-])[O-] YKTSYUJCYHOUJP-UHFFFAOYSA-N 0.000 description 2
- 239000003082 abrasive agent Substances 0.000 description 2
- 125000004442 acylamino group Chemical group 0.000 description 2
- 239000000853 adhesive Substances 0.000 description 2
- 235000004279 alanine Nutrition 0.000 description 2
- 150000001298 alcohols Chemical class 0.000 description 2
- 125000005210 alkyl ammonium group Chemical group 0.000 description 2
- 229960000458 allantoin Drugs 0.000 description 2
- TUFYVOCKVJOUIR-UHFFFAOYSA-N alpha-Thujaplicin Natural products CC(C)C=1C=CC=CC(=O)C=1O TUFYVOCKVJOUIR-UHFFFAOYSA-N 0.000 description 2
- 229940037003 alum Drugs 0.000 description 2
- 229910052782 aluminium Inorganic materials 0.000 description 2
- XAGFODPZIPBFFR-UHFFFAOYSA-N aluminium Chemical compound [Al] XAGFODPZIPBFFR-UHFFFAOYSA-N 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
- 229910052586 apatite Inorganic materials 0.000 description 2
- CUFNKYGDVFVPHO-UHFFFAOYSA-N azulene Chemical class C1=CC=CC2=CC=CC2=C1 CUFNKYGDVFVPHO-UHFFFAOYSA-N 0.000 description 2
- HUMNYLRZRPPJDN-UHFFFAOYSA-N benzaldehyde Chemical compound O=CC1=CC=CC=C1 HUMNYLRZRPPJDN-UHFFFAOYSA-N 0.000 description 2
- 239000001055 blue pigment Substances 0.000 description 2
- 239000011575 calcium Substances 0.000 description 2
- 229960005069 calcium Drugs 0.000 description 2
- 229910052791 calcium Inorganic materials 0.000 description 2
- 229910000019 calcium carbonate Inorganic materials 0.000 description 2
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/02—Inorganic compounds
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Abstract
本发明的目的在于提供一种能够得到清爽感、能够抑制收敛感、并且能够使收敛感的抑制效果持续的洁齿剂等口腔用组合物。本发明提供一种口腔用组合物,其含有(A)选自碳酸盐、碳酸氢盐、硫酸盐和氯化物中的1种以上、以及(B)选自N‑(2‑羟基‑2‑苯基乙基)‑2‑异丙基‑5,5‑二甲基环己烷‑1‑甲酰胺、N‑(乙氧羰基甲基)‑对薄荷烷‑3‑甲酰胺和N‑(2‑(2‑吡啶基)乙基)‑2‑异丙基‑5‑甲基环己烷甲酰胺中的1种以上。
Description
技术领域
本发明涉及一种口腔用组合物。
背景技术
洁齿剂等口腔用组合物通常配合有研磨剂、表面活性剂、湿润剂、粘结剂等,作为表面活性剂的非离子型表面活性剂等用于确保起泡、清扫性等。另外,公知不仅赋予利用研磨剂等的物理性清扫实感,而且通过添加碳酸氢钠、其他盐类来去除口腔内的粘腻感而赋予清爽感的方法。但是,存在以下课题:在碳酸氢钠、其他盐类具有清爽感的同时,还存在具有涩味、特有的异味、刺激等。
专利文献1记载了通过在并用碳酸氢钠和月桂基硫酸钠的口腔用组合物中配合特定的酰胺基甜菜碱型两性活性剂,能够在维持清爽感的同时缓和粘膜刺激。专利文献2记载了通过在含有碳酸氢盐等的口腔用组合物中添加甘氨酸、丙氨酸、亮氨酸、谷氨酸及它们的盐,能够抑制由碳酸氢钠引起的收敛性的显现。专利文献3记载了通过在含有碳酸氢钠等具有收敛性的化合物的口腔用组合物中配合羊毛脂及其衍生物、鲸蜡、巴西棕榈蜡、小烛树蜡、蜂蜡中的1种或2种以上的蜡类,能够改善碳酸氢钠的涩味。
[现有技术文献]
[专利文献]
专利文献1:日本特开平11-49654号公报
专利文献2:专利第3922329号公报
专利文献4:日本特开平11-21219号公报
发明内容
[发明所要解决的课题]
但是,在专利文献1的技术中,涩味(收敛感)的改善不充分。另外,专利文献2和3中的技术也不足以抑制涩味,在涩味的抑制效果的持续性方面也存在改善的余地。涩味(收敛感)有时特别是对年轻人带来不适感,因此期待抑制手段的开发。
本发明的目的在于提供一种口腔用组合物,其能够消除口腔内的粘腻感而带来清爽感(爽快感),能够抑制收敛感,并且能够使收敛感的抑制效果持续。
[用于解决课题的手段]
即,本发明提供以下〔1〕~〔8〕。
〔1〕一种口腔用组合物,其中,含有(A)选自碳酸盐、碳酸氢盐、硫酸盐和氯化物中的1种以上、以及(B)选自N-(2-羟基-2-苯基乙基)-2-异丙基-5,5-二甲基环己烷-1-甲酰胺、N-(乙氧羰基甲基)-对薄荷烷-3-甲酰胺(日文原文:エチル-3-(p-メンタン-3-カルボキサミド)アセテート)和N-(2-(2-吡啶基)乙基)-2-异丙基-5-甲基环己烷甲酰胺中的1种以上(其中,所述口腔用组合物不包括含有(A)硫酸钠和(B)N-(乙氧羰基甲基)-对薄荷烷-3-甲酰胺的洁齿剂组合物)。
〔2〕根据〔1〕记载的口腔用组合物,其中,满足以下至少任意1条:
碳酸盐为选自碳酸钠、碳酸钾和碳酸镁中的1种以上;
碳酸氢盐为选自碳酸氢钠、碳酸氢钾、碳酸氢钙和碳酸氢镁中的1种以上;
硫酸盐为选自硫酸钠、硫酸钾、硫酸镁、硫酸钾、硫酸铝钠和硫酸铝铵中的1种以上;以及
氯化物为选自氯化钠、氯化钾和氯化镁中的1种以上。
〔3〕根据〔1〕或〔2〕记载的口腔用组合物,其中,(A)成分的含量为0.1质量%~10质量%。
〔4〕根据〔1〕~〔3〕中任1项记载的口腔用组合物,其中,(B)成分的含量为0.00001质量%~0.1质量%。
〔5〕根据〔1〕~〔4〕中任一项记载的口腔用组合物,其中,还含有(C)非离子型表面活性剂。
〔6〕根据〔5〕记载的口腔用组合物,其中,(C)成分包含选自聚氧乙烯氢化蓖麻油、聚氧乙烯烷基醚和聚甘油脂肪酸酯中的1种以上。
〔7〕根据〔5〕或〔6〕记载的口腔用组合物,其中,(C)成分的含量为0.1质量%~1质量%。
〔8〕根据〔1〕~〔7〕中任一项记载的口腔用组合物,其中,所述口腔用组合物为洁齿剂、漱口剂、喷雾剂、涂布剂、贴附剂或口腔内溶解剂。
[发明效果]
根据本发明,能够提供一种口腔用组合物,其能够消除口腔内的粘腻感而获得清爽感,能够抑制收敛感,并且能够使收敛感的抑制效果持续。
具体实施方式
以下,对本发明详细进行说明。
本发明的口腔用组合物含有下述(A)和(B)成分,优选进一步含有(C)成分。
[(A)成分]
(A)成分为选自碳酸盐、碳酸氢盐、硫酸盐和氯化物中的1种以上。通过含有(A)成分,能够对口腔用组合物赋予清爽感。在(B)成分为N-(乙氧羰基甲基)-对薄荷烷-3-甲酰胺的情况下,(A)成分为硫酸钠以外,即,选自碳酸盐、碳酸氢盐、硫酸铝盐和氯化物中的1种以上。
作为碳酸盐,例如可举出碳酸钠、碳酸钾和碳酸镁。作为碳酸氢盐,例如可举出碳酸氢钠、碳酸氢钾、碳酸氢钙、碳酸氢镁。作为硫酸盐,例如可举出硫酸钠、硫酸钾、硫酸镁、硫酸铝和明矾。作为明矾,例如可举出硫酸铝钾、硫酸铝钠、硫酸铝铵。作为氯化物,例如可举出氯化钠、氯化钾、氯化镁。其中,优选碳酸氢钠、氯化钠、硫酸铝钾。(A)成分可以为1种,也可以为2种以上的组合。
相对于口腔用组合物整体(100质量%),(A)成分的含量通常为0.05质量%以上,优选为0.1质量%以上,更优选为0.2质量%以上。由此,能够赋予清爽感。上限通常为20质量%以下,优选为10质量%以下,更优选为5质量%以下。由此,能够抑制收敛感的显现。因此,(A)成分的含量通常为0.05质量%~20质量%,优选为0.1质量%~10质量%,更优选为0.2质量%~10质量%,进一步优选为0.2质量%~5质量%。
[(B)成分]
(B)成分为选自N-(2-羟基-2-苯基乙基)-2-异丙基-5,5-二甲基环己烷-1-甲酰胺、N-(乙氧羰基甲基)-对薄荷烷-3-甲酰胺和N-(2-(2-吡啶基)乙基)-2-异丙基-5-甲基环己烷甲酰胺中的1种以上。通过含有(B)成分,能够对口腔用组合物赋予收敛感的抑制及其持续性。在本说明书中,术语“收敛感”是指牙龈紧绷的感觉,区别于刺激(单纯的疼痛)。
(B)成分可以为1种也可以为2种以上的组合,优选至少含有N-(2-羟基-2-苯基乙基)-2-异丙基-5,5-二甲基环己烷-1-甲酰胺和N-(2-(2-吡啶基)乙基)-2-异丙基-5-甲基环己烷甲酰胺。由此,能够赋予更良好的收敛感抑制效果及其持续效果。进而,更优选至少含有N-(2-羟基-2-苯基乙基)-2-异丙基-5,5-二甲基环己烷-1-甲酰胺。由此,能够使收敛感的抑制效果更加持续,另外,能够赋予更良好的清爽感。
相对于口腔用组合物整体(100质量%),(B)成分的含量通常为0.000001质量%以上,优选为0.00001质量%以上,更优选为0.00005质量%以上。由此,能够发挥收敛感的抑制效果以及收敛感的抑制持续效果。上限通常为0.5质量%以下,更优选为0.1质量%以下,进一步优选为0.01质量%以下,更进一步优选为0.005质量%以下。由此,能够抑制对口腔内部的刺激显现、香味显现性的降低。因此,(B)成分的含量通常为0.000001-0.5质量%,优选为0.00001-0.1质量%,更优选为0.00001质量%~0.01质量%,进一步优选为0.00005质量%~0.005质量%。
[(C)成分]
(C)成分为非离子型表面活性剂。通过含有(C)成分,能够对口腔用组合物赋予收敛感的抑制效果。
作为非离子型表面活性剂,例如可举出聚氧乙烯烷基醚、聚氧乙烯氢化蓖麻油、山梨糖醇酐脂肪酸酯、聚氧乙烯山梨糖醇酐脂肪酸酯(例如,聚氧乙烯山梨糖醇酐单硬脂酸酯)、烷醇酰胺、聚氧乙烯脂肪酸酯、聚氧乙烯烯基醚、聚甘油脂肪酸酯、蔗糖脂肪酸酯(例如,麦芽糖脂肪酸酯)、糖醇脂肪酸酯(例如,麦芽糖醇脂肪酸酯、乳糖醇脂肪酸酯)、脂肪酸二乙醇酰胺(例如,月桂酸单或二乙醇酰胺)、聚氧乙烯聚氧丙烯共聚物、聚氧乙烯聚氧丙烯脂肪酸酯。聚氧乙烯烷基醚的烷基链的碳原子数通常为14~18,环氧乙烷平均加成摩尔数通常为15摩尔~30摩尔。聚氧乙烯氢化蓖麻油的环氧乙烷平均加成摩尔数通常为20摩尔~100摩尔,优选为20摩尔~60摩尔。山梨糖醇酐脂肪酸酯的脂肪酸的碳原子数通常为12~18。聚氧乙烯山梨糖醇酐脂肪酸酯的脂肪酸的碳原子数通常为16~18,环氧乙烷平均加成摩尔数通常为10摩尔~40摩尔。烷醇酰胺的烷基链的碳原子数通常为12~14。作为非离子型表面活性剂,优选聚氧乙烯氢化蓖麻油、聚氧乙烯山梨糖醇酐脂肪酸酯、聚氧乙烯烷基醚及聚甘油脂肪酸酯。
相对于口腔用组合物整体(100质量%),(C)成分的含量通常为0.01质量%以上,优选为0.1质量%以上,更优选为0.3质量%以上。由此,能够赋予良好的收敛感的抑制效果。上限通常为5质量%以下,优选为1质量%以下,更优选为0.8质量%以下。由此,能够抑制清爽感的降低和香味显现性的降低。因此,(C)成分的含量通常为0.01质量%~5质量%,优选为0.1质量%~1质量%,更优选为0.3质量%~1质量%,进一步优选为0.3质量%~0.8质量%。
[任意成分]
本实施方式的口腔用组合物在不损害本发明的效果的范围内可以含有已经说明的(A)~(C)成分以外的任意成分。
作为任意成分,例如可举出表面活性剂、甜味剂、香料、药效成分、油性成分、研磨剂、防腐剂、湿润剂、粘结剂、pH调节剂、着色剂(色素)、溶剂。以下,具体进行说明。
-研磨剂-
研磨剂可以是无机研磨剂和有机研磨剂中的任一种。作为无机研磨剂,例如可举出沉淀二氧化硅、硅酸铝、硅酸锆、结晶性硅酸锆、钛结合性二氧化硅等研磨性二氧化硅;磷酸氢钙·2水合盐或非水合物、磷酸二氢钙、磷酸三钙、焦磷酸钙等磷酸钙系化合物;碳酸钙等碳酸钙系研磨剂;氢氧化钙、硫酸钙等碳酸/磷酸以外的钙系研磨剂;氧化铝(aluminiumoxide)、氢氧化铝、氧化铝(alumina)等铝系材料;无水硅酸、沸石、硅酸锆等硅酸系材料;碳酸镁、磷酸三镁等镁系材料;羟基磷灰石、氟磷灰石、钙缺损磷灰石等磷灰石系材料;二氧化钛、云母钛、氧化钛等钛系材料;膨润土等矿物。作为有机研磨剂,例如可举出聚甲基丙烯酸甲酯、合成树脂系研磨剂。其中,优选二氧化硅系研磨剂。
相对于口腔用组合物整体(100质量%),研磨剂的含量通常为70质量%以下,优选为50质量%以下,更优选为8质量%~50质量%。
-表面活性剂-
作为(C)成分以外的表面活性剂,例如,可举出阴离子表面活性剂、两性表面活性剂、阳离子表面活性剂。
作为阴离子表面活性剂,例如可举出烷基硫酸盐、酰基氨基酸盐、酰基牛磺酸盐、α-烯烃磺酸盐、氢化椰油脂肪酸单甘油酯单硫酸盐、月桂基磺基乙酸盐。烷基、酰基可以是直链和支链中的任意一种,可以是饱和和不饱和中的任意一种,其碳原子数通常为10~20,优选为12~18,更优选为12~14。盐能够从药理学上允许的盐中选择。作为药理学上允许的盐,例如可举出碱加成盐和氨基酸盐。作为其具体例,可举出钠盐、钾盐、钙盐、镁盐、铵盐等无机碱盐;三乙基铵盐、三乙醇铵盐、吡啶鎓盐、二异丙基铵盐等有机碱盐;精氨酸盐等碱性氨基酸盐。其中,优选无机碱盐,更优选碱金属盐(例如,钠盐、钾盐)或铵盐,进一步优选钠盐。
作为烷基硫酸盐,例如,可举出月桂基硫酸盐(月桂基硫酸钠)和肉豆蔻酰基硫酸盐。作为酰基氨基酸盐,例如可举出月桂酰基肌氨酸盐、肉豆蔻酰基肌氨酸盐等酰基肌氨酸盐;月桂酰基谷氨酸盐、肉豆蔻酰基谷氨酸盐、棕榈酰基谷氨酸盐等酰基谷氨酸盐;N-月桂酰基-N-甲基甘氨酸盐、椰油酰基甘氨酸盐等酰基甘氨酸盐;N-月桂酰基-β-丙氨酸盐、N-肉豆蔻酰基-β-丙氨酸盐、N-椰油酰基-β-丙氨酸盐、N-月桂酰基-N-甲基-β-丙氨酸盐、N-肉豆蔻酰基-N-甲基-β-丙氨酸盐、N-甲基-N-酰基丙氨酸盐等酰基丙氨酸盐;月桂酰基天冬氨酸盐等酰基天冬氨酸盐。作为酰基牛磺酸盐,例如可举出月桂酰基甲基牛磺酸盐、N-甲基-N-酰基牛磺酸盐、N-椰油酰基甲基牛磺酸盐。作为α-烯烃磺酸盐,可举出十四烯磺酸盐等碳原子数为12~18的α-烯烃磺酸盐。作为阴离子表面活性剂的其它例子,可举出氢化椰油脂肪酸单甘油酯单硫酸钠、月桂醇磺基乙酸酯钠。
从起泡、泡质良好的观点出发,阴离子表面活性剂优选含有磺酸基,更优选烷基硫酸盐、α-烯烃磺酸盐。
作为两性表面活性剂,例如可举出烷基二甲基氨基乙酸甜菜碱(例如,月桂基二甲基氨基乙酸甜菜碱)、脂肪酸酰胺丙基二甲基氨基乙酸甜菜碱(例如,椰油酰胺丙基甜菜碱)等甜菜碱型两性表面活性剂;N-脂肪酸酰基-N-羧甲基-N-羟基乙基乙二胺盐(例如,N-椰油脂肪酸酰基-N-羧甲基-N-羟乙基咪唑啉甜菜碱)、椰油脂肪酸咪唑啉甜菜碱、2-烷基-N-羧甲基-N-羟乙基咪唑啉甜菜碱等咪唑啉型两性表面活性剂;月桂基二甲基氨基乙酸甜菜碱等烷基甜菜碱。作为阳离子表面活性剂,例如可举出烷基铵盐、烷基苄基铵盐。
作为阳离子表面活性剂,例如可举出烷基铵盐、烷基苄基铵盐。
相对于口腔用组合物整体(100质量%),表面活性剂(除(C)成分以外)的含量优选为0.1质量%~3质量%,更优选为0.6质量%~2.5质量%,进一步优选为1质量%~2.5质量%。
-湿润剂-
通过使口腔用组合物含有湿润剂,能够进一步提高使用感。
作为湿润剂,优选糖醇、糖醇以外的多元醇。作为糖醇,例如可举出山梨糖醇、赤藓糖醇、麦芽糖醇、乳糖醇、木糖醇、还原淀粉糖化物等糖醇;甘油;乙二醇、丙二醇、二丙二醇、丁二醇、聚乙二醇等多元醇。作为聚乙二醇,例如可举出平均分子量为150~6000的聚乙二醇,优选平均分子量为190~630的聚乙二醇。具体而言,可举出PEG200、PEG300、PEG400、PEG600。相对于口腔用组合物整体(100质量%),湿润剂的含量通常为40质量%以下,优选为1质量%~30质量%。平均分子量是准医药品原料规格2006记载的平均分子量。
-药效成分-
作为药效成分,例如可举出氯化十六烷基吡啶鎓、苯扎氯铵、苄索氯铵、异丙基甲基苯酚、葡萄糖酸锌、柠檬酸锌、三氯生、百里酚、扁柏酚(Hinokitiol)、氯化溶菌酶等杀菌或抗菌剂;葡聚糖酶、变聚糖酶、淀粉酶、蛋白酶、LeTech酶(日文原文:リテックエンザイム)等酶;氟化钠、单氟磷酸钠、氟化锡等氟化物;ε-氨基己酸、尿囊素、氨甲环酸、甘草酸盐(例如,甘草酸二钾盐)、甘草次酸、甘草次酸盐(例如,甘草次酸硬脂酯)、尿囊素氯羟基铝、薁、二氢胆固醇等抗炎剂;锌、铜盐、锡盐等金属盐;缩聚磷酸盐、乙烷羟基二膦酸酯等牙结石预防剂;维生素E(例如,乙酸生育酚)等血流促进剂;硝酸钾、乳酸铝、氯化锶等知觉过敏抑制剂;羟乙基纤维素二甲基二烯丙基氯化铵等涂布剂;维生素C(例如,抗坏血酸或其盐)、氯化溶菌酶等(A)成分以外的收敛剂;叶绿素铜、葡萄糖酸铜等水溶性铜化合物;牙结石预防剂、丙氨酸、甘氨酸、脯氨酸等氨基酸类;百里香、黄芩、丁香、北美金缕梅等植物提取物;海狗肽(Caropeptide)、聚乙烯吡咯烷酮。药效成分可以单独使用1种,也可以组合使用2种以上。上述药效成分的含量能够根据常规方法适当设定有效量。
-香料-
通过使口腔用组合物含有香料,能够进一步提高使用感。作为香料,例如,可举出薄荷油、留兰香油、日本薄荷油、茴香油、肉桂油、桉树油、冬青(winter green)油、乳香油(mastic oil)、橙花油(neroli oil)(橙花油(orange flower oil))、柠檬草油、茉莉花油、玫瑰油、鸢尾油、丁香油、百里香油、鼠尾草油、小豆蔻油、迷迭香油、月桂油、春黄菊油、葛缕子油、罗勒油、马郁兰油、柠檬油、橙油、酸橙油、柚子油、肉豆蔻油、薰衣草油、金纽扣(paracress)油、香草油、肉桂油、甘椒油、桂叶油、紫苏油、冬青油等天然精油;薄荷醇、香芹酮、肉桂醛、茴香脑、1,8-桉树脑、水杨酸甲酯、丁香酚、百里酚、芳樟醇、柠檬烯、薄荷酮、乙酸薄荷酯、柠檬醛、癸醛、樟脑、冰片(Borneol)、蒎烯、千日菊酰胺、正癸醇、香茅醇、α-松油醇、乙酸香茅酯、桉树脑、乙基芳樟醇、香草醛(vanillin)等上述天然精油中含有的香料成分;乙酸乙酯、丁酸乙酯、乙酸异戊酯、己醛、己烯醛、氨茴酸甲酯(methyl anthranilate)、甲基苯基缩水甘油酸乙酯(ethyl methylphenylglycidate)、苯甲醛、香草醛、乙基香草醛、呋喃酮等香料成分;以及将几个香料成分、天然精油组合而成的薄荷系、水果系、草药系等各种调合香精。作为香料,可以单独使用1种上述例示的香料,也可以组合使用2种以上。
-甜味剂-
通过使口腔用组合物含有甜味剂,能够进一步提高使用感。作为甜味剂,例如可举出糖精、糖精钠、阿斯巴甜、甜菊糖、甜叶菊提取物、对甲氧基肉桂醛、新橙皮苷二氢查耳酮、紫苏葶、甘草酸、甜味蛋白(Thaumatin)、天冬氨酰苯基丙氨酸甲酯(aspartyl-phenylalanine methyl ester)等。作为甜味剂,可以单独使用1种上述例示的甜味剂,也可以组合使用2种以上。
-油性成分-
作为油性成分,例如可举出角鲨烷、液体石蜡、凡士林、微晶蜡等烃类;高级醇(例如,月桂醇、鲸蜡醇、鲸蜡硬脂醇(Cetostearyl alcohol)、油醇、异硬脂醇等碳原子数为8~22的醇);高级脂肪酸(例如,月桂酸、肉豆蔻酸、油酸、异硬脂酸等碳原子数为8~22的脂肪酸)、橄榄油、蓖麻油、椰子油等植物油;肉豆蔻酸异丙酯等脂肪酸酯。
-防腐剂-
通过使口腔用组合物含有防腐剂,能够确保制剂(口腔用组合物)的防腐力。作为防腐剂,例如可举出对羟基苯甲酸酯(例如,对羟基苯甲酸甲酯、对羟基苯甲酸乙酯、对羟基苯甲酸丁酯)、苯甲酸钠等。防腐剂可以单独使用1种,也可以组合使用2种以上。
-粘结剂-
通过口腔用组合物含有任意的粘结剂,能够使粘度最优化,能够进一步提高保形性、使用感。作为粘结剂,可举出以往公知的任意适当的有机粘结剂,例如多糖类、纤维素系粘结剂(例如,羧甲基纤维素(CMC)、羟乙基纤维素、羟丙基纤维素、羟丙基甲基纤维素、甲基纤维素、阳离子化纤维素等)、其他多糖系增粘剂(例如,黄原胶、瓜尔豆胶、结冷胶、黄蓍胶、刺梧桐胶、阿拉伯胶、刺槐豆胶、卡拉胶、海藻酸钠)、合成水溶性高分子(例如,聚丙烯酸钠、羧基乙烯基聚合物、聚乙烯吡咯烷酮、聚乙烯醇、海藻酸丙二醇酯)。进而,也能够配合增稠性二氧化硅、硅酸铝等无机粘结剂。相对于口腔用组合物整体(100质量%),任意的有机粘结剂的含量优选为0质量%~3质量%,更优选为0.1质量%~2质量%。无机粘结剂的含量优选为0质量%~10质量%,更优选为1质量%~8质量%。
-pH调节剂-
通过使口腔用组合物含有pH调节剂,能够确保制剂(口腔用组合物)的pH稳定性。作为pH调节剂,例如可举出邻苯二甲酸、柠檬酸、琥珀酸、乙酸、富马酸、苹果酸及乳酸等有机酸或它们的盐(柠檬酸钠)、磷酸(正磷酸)等无机酸或它们的盐(例如,钾盐、钠盐及铵盐)、氢氧化钠、氢氧化钾等氢氧化物。作为无机酸盐,例如可举出磷酸氢二钠、磷酸二氢钠。
pH调节剂的含量通常设为能够使添加后的口腔用组合物的pH值为5~9,优选为6~8.5的量。
在本说明书中,pH值通常是指从测定开始起在25℃下3分钟后的值。pH值,例如,能够使用东亚电波工业株式会社制造的pH计(型号Hm-30S)进行测定。
-着色剂-
作为着色剂,例如可举出红花红色素、栀子黄色素、栀子蓝色素、紫苏色素、红曲色素、红甘蓝色素、胡萝卜色素、木槿(Hibiscus)色素、可可色素、螺旋藻蓝色素、罗望子色素等天然色素,红色2号、红色3号、红色104号、红色105号、红色106号、红色227号、黄色4号、黄色5号、绿色3号、蓝色1号等法定色素、核黄素、铜叶绿素钠、二氧化钛等。在口腔用组合物包含着色剂的情况下,其含量相对于口腔用组合物整体优选为0.00001质量%~3质量%。
-溶剂-
作为溶剂,例如可举出水(纯化水)、乙醇等,优选水。溶剂可以单独使用1种,也可以组合使用2种以上。
-其他任意成分-
作为上述以外的任意成分的例子,可举出聚异丁烯、聚丁二烯、氨基甲酸酯、硅、天然橡胶。这些其他任意成分的含量能够在不妨碍本发明的效果的范围内适当设定。
[口腔用组合物的剂型和用途]
本发明的口腔用组合物能够制成洁齿剂、漱口剂、喷雾剂、涂布剂、贴附剂、或口腔内溶解剂等口腔用制剂。
口腔用组合物的剂型能够根据利用方式适当选择,没有特别限定。作为剂型,例如,能够以糊状、液状等形式,如果是洁齿剂,则能够制成膏状洁齿剂、液体洁齿剂、液状洁齿剂、湿润洁齿剂。
[口腔用组合物的制造方法]
口腔用组合物的制造方法没有特别限定,能够根据剂型通过各种通常的方法制造得到。例如,作为牙膏使用时,可举出在制备溶解于溶剂中的成分后,混合除此以外的不溶性成分,根据需要进行脱泡(例如,减压等)的方法。得到的牙膏能够容纳于容器中而制成产品。容器的形状、材质没有特别限制,能够使用通常洁齿剂组合物中使用的容器,例如可举出聚乙烯、聚丙烯、聚对苯二甲酸乙二醇酯、尼龙等塑料制层压管等容器等。
实施例
以下,参考实施例和比较例对本发明进行详细阐述。本发明不限于下述实施例。应予说明,下述表中的数值只要没有特别说明则表示质量%。
[实施例及比较例中使用的成分]
-(A)成分-
碳酸氢钠:碳酸氢钠(旭硝子株式会社制造)
硫酸钠:无水硫酸钠(富田制药株式会社制造)
氯化钠:(精选特级盐,日本海水株式会社制造)
硫酸铝钾:(大明化学工业株式会社制造)
-(B)成分-
N-(2-羟基-2-苯基乙基)-2-异丙基-5,5-二甲基环己烷-1-甲酰胺:(Coolact(注册商标)370、高砂香料工业株式会社制造)
N-(乙氧羰基甲基)-对薄荷烷-3-甲酰胺:(WS-5,丰玉香料株式会社制造)
N-(2-(2-吡啶基)乙基)-2-异丙基-5-甲基环己烷甲酰胺:(Evercool(注册商标)190,Givaudan公司制造)
N-乙基-对薄荷烷-3-甲酰胺:(WS-3、德之馨(Symrise)日本公司制造)
-(C)成分-
聚氧乙烯(20)氢化蓖麻油:(日本乳液株式会社制造)
除(A)~(C)成分以外的成分
研磨性二氧化硅:Tixosil(注册商标)73(Solvay公司制造)
氟化钠:(Stella Chemifa株式会社制造)
月桂基硫酸钠:(BASF公司制造)
山梨醇液(70%):(三菱商事生命科学株式会社制造)
丙二醇:(ADEKA公司制造)
增稠性二氧化硅:Carplex(注册商标)#67(DSL日本株式会社制造)
糖精钠:(爱三化学工业株式会社制造)
水(精制水)
关于上述以外的成分,均使用符合准医药品原料规格2006的原料。
实施例1~28和比较例1~8
使用上述成分作为原料,按照后述的制备方法,制备具有下述表1~5所示的配合组成的牙膏。
[牙膏的制备方法]
按照常规方法配合表1~5所示的原料,得到牙膏,将其收纳于层压管中。
[评价方法]
通过4名受试者小组成员,评价牙膏的使用感。将1g牙膏样品置于牙刷(ClinicaAdvantage牙刷,4排紧凑普通型,狮王株式会社制造)上,刷牙3分钟,按照下述所示的评分基准,分别判定清爽感、收敛感的抑制效果、收敛感的抑制效果的持续性。求出4人的分数的平均值,并根据以下评价基准进行评价。
<清爽感>
关于清爽感,基于刷牙后用水冲洗口腔后口腔内有无发粘来评价清爽感。
评分基准
4分:感觉到非常有清爽感
3分:感觉到清爽感
2分:几乎没有感觉到清爽感
1分:没有感觉到清爽感
评价基准
优:平均分为3.5分以上且4.0分以下
良:平均分为3.0分以上且小于3.5分
合格:平均分为2.0分以上且小于3.0分
不合格:平均分小于2.0分
<收敛感的抑制效果>
关于收敛感的抑制效果,对在刷牙后用水冲洗口腔内之后不久的收敛感的强度进行了评价。
评价基准
4分:未感觉到收敛感
3分:几乎感觉不到收敛感
2分:感觉到收敛感
1分:非常强地感觉到收敛感
判定基准
优秀:平均分3.8分以上且4.0分以下
优:平均分3.5分以上且小于3.8分
良:平均分3.0分以上且小于3.5分
合格:平均分2.0分以上且小于3.0分
不合格:平均分小于2.0分
<收敛感的抑制效果的持续性>
关于收敛感的抑制效果的持续性,在刷牙后用水冲洗口腔内之后,对未感到收敛感的时间进行评价。
评价基准
4分:25分钟以上(未感觉到刺激)
3分:15分钟以上且小于25分钟
2分:5分钟以上且小于15分钟
1分:小于5分钟
判定基准
优:平均分3.5分以上且4.0分以下
良:平均分3.0分以上且小于3.5分
合格:平均分2.0分以上且小于3.0分
不合格:平均分小于2.0分
[表1]
[表2]
[表3]
[表4]
[表5]
在仅含有(B)成分的比较例1中,清爽感的评价低,在仅含有(A)成分的比较例2~6中,对口腔粘膜的收敛感的抑制效果低(表5)。与此相对,在作为(A)和(B)成分的组合的实施例1~28中,清爽感、收敛感的抑制效果的评价良好,而且收敛感的抑制效果也是持续的(表1~4)。其中,在进一步使用(C)成分的实施例24~28中,收敛感的抑制效果更加良好(表4)。
在仅含有(B)的对照成分的比较例8中,也与仅含有(B)成分的比较例1相同,清爽感的评价低,但在与其组合了(A)成分的比较例7中,与作为(A)和(B)成分的组合的比较例2~6相同,对口腔粘膜的收敛感的抑制效果低,未发现(B)的对照成分的添加效果(表5)。
这些结果表明,本发明的口腔用组合物能够发挥基于消除口腔中的粘腻感而产生的清爽感,能够抑制收敛感,并且能够使收敛感的抑制效果持续。
Claims (8)
1.一种口腔用组合物,其特征在于,所述口腔用组合物含有:
(A)选自碳酸盐、碳酸氢盐、硫酸盐和氯化物中的1种以上;以及
(B)选自N-(2-羟基-2-苯基乙基)-2-异丙基-5,5-二甲基环己烷-1-甲酰胺、N-(乙氧羰基甲基)-对薄荷烷-3-甲酰胺和N-(2-(2-吡啶基)乙基)-2-异丙基-5-甲基环己烷甲酰胺中的1种以上,
其中,所述口腔用组合物不包括含有(A)硫酸钠和(B)N-(乙氧羰基甲基)-对薄荷烷-3-甲酰胺的洁齿剂组合物。
2.根据权利要求1所述的口腔用组合物,其中,所述口腔用组合物满足以下至少任意1条:
碳酸盐为选自碳酸钠、碳酸钾和碳酸镁中的1种以上;
碳酸氢盐为选自碳酸氢钠、碳酸氢钾、碳酸氢钙和碳酸氢镁中的1种以上;
硫酸盐为选自硫酸钠、硫酸钾、硫酸镁、硫酸铝钾、硫酸铝钠和硫酸铝铵中的1种以上;以及
氯化物为选自氯化钠、氯化钾和氯化镁中的1种以上。
3.根据权利要求1或2所述的口腔用组合物,其中,(A)成分的含量为0.1质量%~10质量%。
4.根据权利要求1~3中任一项所述的口腔用组合物,其中,(B)成分的含量为0.00001质量%~0.1质量%。
5.根据权利要求1~4中任一项所述的口腔用组合物,其中,所述口腔用组合物还含有(C)非离子型表面活性剂。
6.根据权利要求5所述的口腔用组合物,其中,(C)成分包含选自聚氧乙烯氢化蓖麻油、聚氧乙烯烷基醚和聚甘油脂肪酸酯中的1种以上。
7.根据权利要求5或6所述的口腔用组合物,其中,(C)成分的含量为0.1质量%~1质量%。
8.根据权利要求1~7中任一项所述的口腔用组合物,其中,所述口腔用组合物为洁齿剂、漱口剂、喷雾剂、涂布剂、贴附剂或口腔内溶解剂。
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