JP5893249B2 - Oral composition - Google Patents
Oral composition Download PDFInfo
- Publication number
- JP5893249B2 JP5893249B2 JP2011015330A JP2011015330A JP5893249B2 JP 5893249 B2 JP5893249 B2 JP 5893249B2 JP 2011015330 A JP2011015330 A JP 2011015330A JP 2011015330 A JP2011015330 A JP 2011015330A JP 5893249 B2 JP5893249 B2 JP 5893249B2
- Authority
- JP
- Japan
- Prior art keywords
- cetylpyridinium chloride
- hexanol
- oral
- mass
- sodium
- 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.)
- Active
Links
- 239000000203 mixture Substances 0.000 title claims description 46
- YMKDRGPMQRFJGP-UHFFFAOYSA-M cetylpyridinium chloride Chemical compound [Cl-].CCCCCCCCCCCCCCCC[N+]1=CC=CC=C1 YMKDRGPMQRFJGP-UHFFFAOYSA-M 0.000 claims description 40
- 229960001927 cetylpyridinium chloride Drugs 0.000 claims description 40
- ZSIAUFGUXNUGDI-UHFFFAOYSA-N hexan-1-ol Chemical compound CCCCCCO ZSIAUFGUXNUGDI-UHFFFAOYSA-N 0.000 claims description 34
- KBPLFHHGFOOTCA-UHFFFAOYSA-N 1-Octanol Chemical compound CCCCCCCCO KBPLFHHGFOOTCA-UHFFFAOYSA-N 0.000 claims description 32
- 210000000214 mouth Anatomy 0.000 claims description 16
- 239000007788 liquid Substances 0.000 claims description 15
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 14
- NMRPBPVERJPACX-UHFFFAOYSA-N (3S)-octan-3-ol Natural products CCCCCC(O)CC NMRPBPVERJPACX-UHFFFAOYSA-N 0.000 claims description 10
- WOFPPJOZXUTRAU-UHFFFAOYSA-N 2-Ethyl-1-hexanol Natural products CCCCC(O)CCC WOFPPJOZXUTRAU-UHFFFAOYSA-N 0.000 claims description 10
- YIWUKEYIRIRTPP-UHFFFAOYSA-N 2-ethylhexan-1-ol Chemical compound CCCCC(CC)CO YIWUKEYIRIRTPP-UHFFFAOYSA-N 0.000 claims description 10
- 150000001298 alcohols Chemical class 0.000 claims description 3
- 238000002156 mixing Methods 0.000 claims description 3
- -1 polyoxyethylene Polymers 0.000 description 38
- MWKFXSUHUHTGQN-UHFFFAOYSA-N decan-1-ol Chemical compound CCCCCCCCCCO MWKFXSUHUHTGQN-UHFFFAOYSA-N 0.000 description 28
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 18
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 16
- 238000001179 sorption measurement Methods 0.000 description 16
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 14
- 235000014113 dietary fatty acids Nutrition 0.000 description 14
- 239000000194 fatty acid Substances 0.000 description 14
- 229930195729 fatty acid Natural products 0.000 description 14
- 235000002639 sodium chloride Nutrition 0.000 description 14
- 229920003171 Poly (ethylene oxide) Polymers 0.000 description 13
- 230000000694 effects Effects 0.000 description 11
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 11
- 238000009472 formulation Methods 0.000 description 10
- 239000003205 fragrance Substances 0.000 description 10
- PUZPDOWCWNUUKD-UHFFFAOYSA-M sodium fluoride Chemical compound [F-].[Na+] PUZPDOWCWNUUKD-UHFFFAOYSA-M 0.000 description 10
- 239000003002 pH adjusting agent Substances 0.000 description 9
- 239000008213 purified water Substances 0.000 description 9
- 150000003839 salts Chemical class 0.000 description 9
- FTLYMKDSHNWQKD-UHFFFAOYSA-N (2,4,5-trichlorophenyl)boronic acid Chemical compound OB(O)C1=CC(Cl)=C(Cl)C=C1Cl FTLYMKDSHNWQKD-UHFFFAOYSA-N 0.000 description 8
- 235000001014 amino acid Nutrition 0.000 description 8
- 239000004359 castor oil Substances 0.000 description 8
- 235000019438 castor oil Nutrition 0.000 description 8
- 239000000551 dentifrice Substances 0.000 description 8
- 235000011187 glycerol Nutrition 0.000 description 8
- 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 description 8
- 229940085605 saccharin sodium Drugs 0.000 description 8
- 150000001413 amino acids Chemical class 0.000 description 7
- 230000000844 anti-bacterial effect Effects 0.000 description 7
- 239000000377 silicon dioxide Substances 0.000 description 7
- 241000894006 Bacteria Species 0.000 description 6
- 125000002252 acyl group Chemical group 0.000 description 6
- 125000005907 alkyl ester group Chemical group 0.000 description 6
- 239000003899 bactericide agent Substances 0.000 description 6
- 125000002091 cationic group Chemical group 0.000 description 6
- 150000004665 fatty acids Chemical class 0.000 description 6
- 239000005968 1-Decanol Substances 0.000 description 5
- 239000011230 binding agent Substances 0.000 description 5
- 239000002324 mouth wash Substances 0.000 description 5
- 229940051866 mouthwash Drugs 0.000 description 5
- 239000003921 oil Substances 0.000 description 5
- 235000019198 oils Nutrition 0.000 description 5
- 239000011734 sodium Substances 0.000 description 5
- 229910052708 sodium Inorganic materials 0.000 description 5
- 239000011775 sodium fluoride Substances 0.000 description 5
- 235000013024 sodium fluoride Nutrition 0.000 description 5
- PUPZLCDOIYMWBV-UHFFFAOYSA-N (+/-)-1,3-Butanediol Chemical compound CC(O)CCO PUPZLCDOIYMWBV-UHFFFAOYSA-N 0.000 description 4
- ODHCTXKNWHHXJC-VKHMYHEASA-M 5-oxo-L-prolinate Chemical compound [O-]C(=O)[C@@H]1CCC(=O)N1 ODHCTXKNWHHXJC-VKHMYHEASA-M 0.000 description 4
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 description 4
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 description 4
- 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
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 description 4
- 229940071139 pyrrolidone carboxylate Drugs 0.000 description 4
- 239000006228 supernatant 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
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 description 3
- KWIUHFFTVRNATP-UHFFFAOYSA-N Betaine Natural products C[N+](C)(C)CC([O-])=O KWIUHFFTVRNATP-UHFFFAOYSA-N 0.000 description 3
- 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 3
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 description 3
- BIVBRWYINDPWKA-VLQRKCJKSA-L Glycyrrhizinate dipotassium Chemical compound [K+].[K+].O([C@@H]1[C@@H](O)[C@H](O)[C@H](O[C@@H]1O[C@H]1CC[C@]2(C)[C@H]3C(=O)C=C4[C@@H]5C[C@](C)(CC[C@@]5(CC[C@@]4(C)[C@]3(C)CC[C@H]2C1(C)C)C)C(O)=O)C([O-])=O)[C@@H]1O[C@H](C([O-])=O)[C@@H](O)[C@H](O)[C@H]1O BIVBRWYINDPWKA-VLQRKCJKSA-L 0.000 description 3
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 3
- 239000004354 Hydroxyethyl cellulose Substances 0.000 description 3
- 229920000663 Hydroxyethyl cellulose Polymers 0.000 description 3
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 description 3
- KWIUHFFTVRNATP-UHFFFAOYSA-O N,N,N-trimethylglycinium Chemical compound C[N+](C)(C)CC(O)=O KWIUHFFTVRNATP-UHFFFAOYSA-O 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
- 239000012190 activator Substances 0.000 description 3
- 229960003237 betaine Drugs 0.000 description 3
- 125000004432 carbon atom Chemical group C* 0.000 description 3
- 239000001768 carboxy methyl cellulose Substances 0.000 description 3
- 239000003795 chemical substances by application 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
- 229940101029 dipotassium glycyrrhizinate Drugs 0.000 description 3
- 239000000796 flavoring agent Substances 0.000 description 3
- 239000000417 fungicide Substances 0.000 description 3
- 229920000591 gum Polymers 0.000 description 3
- 235000019447 hydroxyethyl cellulose Nutrition 0.000 description 3
- 229910052588 hydroxylapatite Inorganic materials 0.000 description 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 3
- OSWPMRLSEDHDFF-UHFFFAOYSA-N methyl salicylate Chemical compound COC(=O)C1=CC=CC=C1O OSWPMRLSEDHDFF-UHFFFAOYSA-N 0.000 description 3
- 239000002736 nonionic surfactant Substances 0.000 description 3
- 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 3
- 230000007505 plaque formation Effects 0.000 description 3
- 230000001737 promoting effect Effects 0.000 description 3
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 3
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 description 3
- 239000000600 sorbitol Substances 0.000 description 3
- 239000007921 spray Substances 0.000 description 3
- 239000004094 surface-active agent Substances 0.000 description 3
- 230000008719 thickening Effects 0.000 description 3
- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 description 3
- NOOLISFMXDJSKH-KXUCPTDWSA-N (-)-Menthol Chemical compound CC(C)[C@@H]1CC[C@@H](C)C[C@H]1O NOOLISFMXDJSKH-KXUCPTDWSA-N 0.000 description 2
- 229940058015 1,3-butylene glycol Drugs 0.000 description 2
- SVIJYLPSHPPVQF-UHFFFAOYSA-N 2-[2,2-diaminoethyl(dodecyl)amino]acetic acid Chemical compound CCCCCCCCCCCCN(CC(N)N)CC(O)=O SVIJYLPSHPPVQF-UHFFFAOYSA-N 0.000 description 2
- IJALWSVNUBBQRA-UHFFFAOYSA-N 4-Isopropyl-3-methylphenol Chemical compound CC(C)C1=CC=C(O)C=C1C IJALWSVNUBBQRA-UHFFFAOYSA-N 0.000 description 2
- ODHCTXKNWHHXJC-VKHMYHEASA-N 5-oxo-L-proline Chemical compound OC(=O)[C@@H]1CCC(=O)N1 ODHCTXKNWHHXJC-VKHMYHEASA-N 0.000 description 2
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 description 2
- KRKNYBCHXYNGOX-UHFFFAOYSA-K Citrate Chemical compound [O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-K 0.000 description 2
- ZAKOWWREFLAJOT-CEFNRUSXSA-N D-alpha-tocopherylacetate Chemical compound CC(=O)OC1=C(C)C(C)=C2O[C@@](CCC[C@H](C)CCC[C@H](C)CCCC(C)C)(C)CCC2=C1C ZAKOWWREFLAJOT-CEFNRUSXSA-N 0.000 description 2
- RGHNJXZEOKUKBD-SQOUGZDYSA-N D-gluconic acid Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C(O)=O RGHNJXZEOKUKBD-SQOUGZDYSA-N 0.000 description 2
- NOOLISFMXDJSKH-UHFFFAOYSA-N DL-menthol Natural products CC(C)C1CCC(C)CC1O NOOLISFMXDJSKH-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
- PVNIIMVLHYAWGP-UHFFFAOYSA-N Niacin Chemical compound OC(=O)C1=CC=CN=C1 PVNIIMVLHYAWGP-UHFFFAOYSA-N 0.000 description 2
- ZYEMGPIYFIJGTP-UHFFFAOYSA-N O-methyleugenol Chemical compound COC1=CC=C(CC=C)C=C1OC ZYEMGPIYFIJGTP-UHFFFAOYSA-N 0.000 description 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 description 2
- 239000004698 Polyethylene Substances 0.000 description 2
- 239000002202 Polyethylene glycol Substances 0.000 description 2
- 239000004372 Polyvinyl alcohol Substances 0.000 description 2
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 2
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 description 2
- 229930006000 Sucrose Natural products 0.000 description 2
- TVXBFESIOXBWNM-UHFFFAOYSA-N Xylitol Natural products OCCC(O)C(O)C(O)CCO TVXBFESIOXBWNM-UHFFFAOYSA-N 0.000 description 2
- WNLRTRBMVRJNCN-UHFFFAOYSA-N adipic acid Chemical compound OC(=O)CCCCC(O)=O WNLRTRBMVRJNCN-UHFFFAOYSA-N 0.000 description 2
- 125000000217 alkyl group Chemical group 0.000 description 2
- 239000003945 anionic surfactant Substances 0.000 description 2
- 229910052586 apatite Inorganic materials 0.000 description 2
- FUWUEFKEXZQKKA-UHFFFAOYSA-N beta-thujaplicin Chemical compound CC(C)C=1C=CC=C(O)C(=O)C=1 FUWUEFKEXZQKKA-UHFFFAOYSA-N 0.000 description 2
- 235000019437 butane-1,3-diol Nutrition 0.000 description 2
- 229910000019 calcium carbonate Inorganic materials 0.000 description 2
- OSGAYBCDTDRGGQ-UHFFFAOYSA-L calcium sulfate Chemical compound [Ca+2].[O-]S([O-])(=O)=O OSGAYBCDTDRGGQ-UHFFFAOYSA-L 0.000 description 2
- ULDHMXUKGWMISQ-UHFFFAOYSA-N carvone Chemical compound CC(=C)C1CC=C(C)C(=O)C1 ULDHMXUKGWMISQ-UHFFFAOYSA-N 0.000 description 2
- 235000019864 coconut oil Nutrition 0.000 description 2
- 239000003240 coconut oil Substances 0.000 description 2
- 239000012153 distilled water Substances 0.000 description 2
- 238000011156 evaluation Methods 0.000 description 2
- 239000000284 extract Substances 0.000 description 2
- 235000019634 flavors Nutrition 0.000 description 2
- 235000003599 food sweetener Nutrition 0.000 description 2
- 230000000855 fungicidal effect Effects 0.000 description 2
- 229930195712 glutamate Natural products 0.000 description 2
- LPLVUJXQOOQHMX-QWBHMCJMSA-N glycyrrhizinic acid Chemical compound O([C@@H]1[C@@H](O)[C@H](O)[C@H](O[C@@H]1O[C@@H]1C([C@H]2[C@]([C@@H]3[C@@]([C@@]4(CC[C@@]5(C)CC[C@@](C)(C[C@H]5C4=CC3=O)C(O)=O)C)(C)CC2)(C)CC1)(C)C)C(O)=O)[C@@H]1O[C@H](C(O)=O)[C@@H](O)[C@H](O)[C@H]1O LPLVUJXQOOQHMX-QWBHMCJMSA-N 0.000 description 2
- NFIDBGJMFKNGGQ-UHFFFAOYSA-N isopropylmethylphenol Natural products CC(C)CC1=CC=CC=C1O NFIDBGJMFKNGGQ-UHFFFAOYSA-N 0.000 description 2
- XMGQYMWWDOXHJM-UHFFFAOYSA-N limonene Chemical compound CC(=C)C1CCC(C)=CC1 XMGQYMWWDOXHJM-UHFFFAOYSA-N 0.000 description 2
- HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 description 2
- 238000000034 method Methods 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
- 210000002200 mouth mucosa Anatomy 0.000 description 2
- 239000006072 paste Substances 0.000 description 2
- 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 2
- 208000028169 periodontal disease Diseases 0.000 description 2
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- 238000002360 preparation method Methods 0.000 description 2
- 239000003755 preservative agent Substances 0.000 description 2
- QELSKZZBTMNZEB-UHFFFAOYSA-N propylparaben Chemical compound CCCOC(=O)C1=CC=C(O)C=C1 QELSKZZBTMNZEB-UHFFFAOYSA-N 0.000 description 2
- 229940043131 pyroglutamate Drugs 0.000 description 2
- 235000019333 sodium laurylsulphate Nutrition 0.000 description 2
- 239000005720 sucrose Substances 0.000 description 2
- 239000003765 sweetening agent Substances 0.000 description 2
- 229940042585 tocopherol acetate Drugs 0.000 description 2
- RUVINXPYWBROJD-ONEGZZNKSA-N trans-anethole Chemical compound COC1=CC=C(\C=C\C)C=C1 RUVINXPYWBROJD-ONEGZZNKSA-N 0.000 description 2
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- 239000000811 xylitol Substances 0.000 description 2
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- XPALGXXLALUMLE-UHFFFAOYSA-N 2-(dimethylamino)tetradecanoic acid Chemical compound CCCCCCCCCCCCC(N(C)C)C(O)=O XPALGXXLALUMLE-UHFFFAOYSA-N 0.000 description 1
- GTOFKXZQQDSVFH-UHFFFAOYSA-N 2-benzylsuccinic acid Chemical compound OC(=O)CC(C(O)=O)CC1=CC=CC=C1 GTOFKXZQQDSVFH-UHFFFAOYSA-N 0.000 description 1
- UNWFFCPRJXMCNV-UHFFFAOYSA-N 3-[dodecanoyl(methyl)amino]propanoic acid Chemical compound CCCCCCCCCCCC(=O)N(C)CCC(O)=O UNWFFCPRJXMCNV-UHFFFAOYSA-N 0.000 description 1
- PVXPPJIGRGXGCY-DJHAAKORSA-N 6-O-alpha-D-glucopyranosyl-alpha-D-fructofuranose Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@@H]1OC[C@@H]1[C@@H](O)[C@H](O)[C@](O)(CO)O1 PVXPPJIGRGXGCY-DJHAAKORSA-N 0.000 description 1
- SLXKOJJOQWFEFD-UHFFFAOYSA-N 6-aminohexanoic acid Chemical compound NCCCCCC(O)=O SLXKOJJOQWFEFD-UHFFFAOYSA-N 0.000 description 1
- WBZFUFAFFUEMEI-UHFFFAOYSA-M Acesulfame k Chemical compound [K+].CC1=CC(=O)[N-]S(=O)(=O)O1 WBZFUFAFFUEMEI-UHFFFAOYSA-M 0.000 description 1
- 239000004382 Amylase Substances 0.000 description 1
- 102000013142 Amylases Human genes 0.000 description 1
- 108010065511 Amylases Proteins 0.000 description 1
- 239000004475 Arginine Substances 0.000 description 1
- 108010011485 Aspartame Proteins 0.000 description 1
- 206010006326 Breath odour Diseases 0.000 description 1
- 240000004160 Capsicum annuum Species 0.000 description 1
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Description
本発明は、口腔内細菌に対する殺菌活性を有する塩化セチルピリジニウムの歯牙表面への吸着効果を促進した口腔用組成物に関する。より詳細には、塩化セチルピリジニウム及び特定の一価アルコールを０.０２〜０.５質量％含有する口腔用組成物に関する。 The present invention relates to a composition for oral cavity that promotes the adsorption effect of cetylpyridinium chloride having bactericidal activity against oral bacteria on the tooth surface. More specifically, the present invention relates to an oral composition containing 0.02 to 0.5% by mass of cetylpyridinium chloride and a specific monohydric alcohol.
塩化セチルピリジニウムは口腔内細菌に対する殺菌活性が高いだけでなく、口腔粘膜や歯牙表面に吸着し、歯牙や口腔粘膜の表面への口腔内細菌の吸着を阻害し、口腔衛生状態を改善したり、歯垢形成を抑制したりすることが知られている。そのため、塩化セチルピリジニウムは歯周疾患、口臭の予防・改善を目的として多くの口腔用組成物に配合されている。 Cetylpyridinium chloride not only has high bactericidal activity against oral bacteria, but also adsorbs to the oral mucosa and tooth surface, inhibits the adsorption of oral bacteria to the surface of the tooth and oral mucosa, improves oral hygiene, It is known to suppress plaque formation. Therefore, cetylpyridinium chloride is blended in many oral compositions for the purpose of preventing and improving periodontal diseases and bad breath.
この塩化セチルピリジニウムのようなカチオン性殺菌剤の口腔内細菌に対する殺菌活性をさらに高めるために種々の方法が開示されている。特許文献１には、塩化セチルピリジニウムにＮ−長鎖アシル塩基性アミノ酸の低級アルキルエステルまたはその塩を組み合わせると塩化セチルピリジニウムの歯牙への吸着が促進されること、特許文献２には、Ｎ−長鎖アシル塩基性アミノ酸の低級アルキルエステルまたはその塩によるカチオン性殺菌剤の歯牙への吸着促進作用が、ｐＨ５．５〜６．５の領域において最も高まること、特許文献３には、カチオン性殺菌剤と非イオン性界面活性剤とを併用した口腔用組成物に対し、特定の化合物を配合すると、殺菌剤の失活が効果的に防止されること、特許文献４には、塩化セチルピリジニウムに特定のポリオキシエチレン硬化ヒマシ油を組合せると他の界面活性剤と比べて塩化セチルピリジニウムの歯牙への吸着を阻害しないこと、特許文献５には、カチオン性殺菌剤にカチオン性ポリマー及び有機酸やその塩を配合することによりカチオン性殺菌剤の口腔内での滞留性が高まり、歯垢形成を効果的に阻止することができること、特許文献６には、塩化セチルピリジニウムの歯牙への吸着性を高めるために、ポリビニルアルコールが用いることが開示されている。 Various methods have been disclosed for further enhancing the bactericidal activity of the cationic bactericides such as cetylpyridinium chloride against oral bacteria. Patent Document 1 discloses that the combination of cetylpyridinium chloride with a lower alkyl ester of an N-long chain acyl basic amino acid or a salt thereof promotes the adsorption of cetylpyridinium chloride to teeth. The effect of promoting the adsorption of a cationic fungicide to a tooth by a lower alkyl ester of a long-chain acyl basic amino acid or a salt thereof is most enhanced in a pH range of 5.5 to 6.5. Incorporation of a specific compound into a composition for oral cavity in which an agent and a nonionic surfactant are used in combination effectively prevents inactivation of the bactericidal agent, and Patent Document 4 describes cetylpyridinium chloride. The combination of specific polyoxyethylene hydrogenated castor oil does not inhibit the adsorption of cetylpyridinium chloride to teeth compared to other surfactants, patent text 5, the cationic microbicide is mixed with a cationic polymer and an organic acid or a salt thereof to increase the retention of the cationic fungicide in the oral cavity, and can effectively prevent plaque formation; Patent Document 6 discloses that polyvinyl alcohol is used to enhance the adsorptivity of cetylpyridinium chloride to teeth.
本発明は、口腔内細菌に対する殺菌活性を有する塩化セチルピリジニウムの歯牙表面への吸着効果を向上させた口腔用組成物を提供することを課題とする。 This invention makes it a subject to provide the composition for oral cavity which improved the adsorption | suction effect to the tooth surface of the cetyl pyridinium chloride which has bactericidal activity with respect to bacteria in the oral cavity.
本発明者らは、かかる事情に鑑み鋭意検討を重ねた結果、塩化セチルピリジニウムに特定の一価アルコールを０.０２〜０.５質量％配合した場合、塩化セチルピリジニウムの歯牙表面への吸着効果が高まることを見出し、本発明を完成するに至った。 As a result of intensive studies in view of such circumstances, the present inventors have found that when 0.02 to 0.5% by mass of a specific monohydric alcohol is mixed with cetylpyridinium chloride, the adsorption effect of cetylpyridinium chloride on the tooth surface. As a result, the present invention has been completed.
すなわち、本発明は、特に以下の項１〜５の口腔用組成物を提供するものである。
項１．
ヘキサノール、オクタノール、２−エチル−１−ヘキサノール、デカノールからなる群より選ばれる１種以上の一価アルコールを０.０２〜０.５質量％および塩化セチルピリジニウムを０.０１〜０.３質量％含有することを特徴とする口腔用組成物。
項２．
一価アルコールが、１−オクタノール、１−ヘキサノール、１−デカノールであることを特徴とする項１に記載の口腔用組成物。
項３．
一価アルコールの配合量が０．１〜０.５質量％であることを特徴とする項１に記載の口腔用組成物。
項４．
口腔用組成物が液体若しくは液状であることを特徴とする項１〜項３の何れかに記載の口腔用組成物。
項５
ヘキサノール、オクタノール、２−エチル−１−ヘキサノール、デカノールからなる群より選ばれる１種以上の一価アルコールを０.０２〜０.５質量％および塩化セチルピリジニウムを併用することにより、塩化セチルピリジニウムの歯牙への吸着を促進する方法。
That is, this invention provides the composition for oral cavity of the following items 1-5 especially.
Item 1.
One to at least one monohydric alcohol selected from the group consisting of hexanol, octanol, 2-ethyl-1-hexanol, and decanol is 0.02 to 0.5% by mass and cetylpyridinium chloride is 0.01 to 0.3% by mass. An oral composition characterized by containing.
Item 2.
Item 1. The oral composition according to Item 1, wherein the monohydric alcohol is 1-octanol, 1-hexanol, or 1-decanol.
Item 3.
Item 2. The oral composition according to Item 1, wherein the amount of monohydric alcohol is 0.1 to 0.5 mass%.
Item 4.
Item 4. The oral composition according to any one of Items 1 to 3, wherein the oral composition is liquid or liquid.
Item 5
By using 0.02 to 0.5% by mass of one or more monohydric alcohols selected from the group consisting of hexanol, octanol, 2-ethyl-1-hexanol, and decanol and cetylpyridinium chloride, A method of promoting adsorption to teeth.
本発明の口腔用組成物は、塩化セチルピリジニウムの活性をさらに高めて歯牙表面への吸着効果を促進することにより、う蝕や歯周病などを引き起こす口腔内細菌の歯牙表面への吸着を阻害して歯垢の形成を効果的に抑制することが可能となる。 The composition for oral cavity of the present invention inhibits the adsorption of oral bacteria that cause dental caries and periodontal disease on the tooth surface by further increasing the activity of cetylpyridinium chloride and promoting the adsorption effect on the tooth surface. Thus, it is possible to effectively suppress plaque formation.
本発明に係る口腔用組成物は、ヘキサノール、２−エチル−１−ヘキサノール、オクタノール、デカノールからなる群より選ばれる１種以上の一価アルコールを０.１〜０.５質量％および塩化セチルピリジニウム０.０１〜０.３質量％を含有することを特徴とするものである。なお、本願明細書において配合比率は、特に断りのない限り配合質量比率を表す。 The composition for oral cavity according to the present invention comprises 0.1 to 0.5% by mass of one or more monohydric alcohols selected from the group consisting of hexanol, 2-ethyl-1-hexanol, octanol and decanol, and cetylpyridinium chloride. It contains 0.01 to 0.3% by mass. In the present specification, the blending ratio represents the blending mass ratio unless otherwise specified.
本発明に用いる塩化セチルピリジニウムは、第四級アンモニウム化合物に含まれるカチオン性殺菌剤であり、口腔用組成物分野において広く使用されているものである。かかる塩化セチルピリジニウムは、本発明の液体口腔用組成物の全量に対して０．０１〜０.３質量％を配合することができ、好ましくは０．０５質量％を配合することができる。０．０１質量％未満になると、塩化セチルピリジニウムの歯牙表面への吸着効果が低下してしまい、一方０.３質量％を超えると、使用時の苦味等の問題が生じてしまうため好ましくない。 Cetylpyridinium chloride used in the present invention is a cationic bactericidal agent contained in a quaternary ammonium compound and is widely used in the field of oral compositions. Such cetylpyridinium chloride can be blended in an amount of 0.01 to 0.3% by mass, preferably 0.05% by mass, based on the total amount of the liquid oral composition of the present invention. If the amount is less than 0.01% by mass, the effect of adsorbing cetylpyridinium chloride on the tooth surface is reduced.
本発明に用いる一価アルコールとしては、ヘキサノール、オクタノール、２−エチル−１−ヘキサノール、デカノールが挙げられ、このうち、ヘキサノール、オクタノール、２−エチル−１−ヘキサノール、デカノールが好ましく、ヘキサノール、オクタノール、デカノールがより好ましく、１−ヘキサノール、１−オクタノール、１−デカノールがさらに好ましく、１−オクタノール、１−デカノールが最も好ましい。これらは、それぞれ単独であるいは２種以上を組み合わせて用いることができる。配合量としては、０．０２〜０.５質量％であり、０.１〜０.５質量％がさらに好ましい。０.５質量％を超えると口腔用組成物の香味が悪くなったり、所期の効果が期待できなくなる恐れがあるため好ましくなく、０.０２質量％に満たない場合には所期の効果が得られない恐れがあるため好ましくない。 Examples of the monohydric alcohol used in the present invention include hexanol, octanol, 2-ethyl-1-hexanol, and decanol. Among these, hexanol, octanol, 2-ethyl-1-hexanol, and decanol are preferable, and hexanol, octanol, Decanol is more preferable, 1-hexanol, 1-octanol and 1-decanol are more preferable, and 1-octanol and 1-decanol are most preferable. These can be used alone or in combination of two or more. As a compounding quantity, it is 0.02-0.5 mass%, and 0.1-0.5 mass% is still more preferable. If the amount exceeds 0.5% by mass, the flavor of the oral composition may be deteriorated or the desired effect may not be expected. If the amount is less than 0.02% by mass, the desired effect is obtained. This is not preferable because it may not be obtained.
本発明の口腔用組成物は、特に限定するものではないが、練歯磨剤、液体歯磨剤、洗口剤、ジェル剤、パスタ剤、スプレー剤、ガム剤、軟ペースト剤（クリーム状製剤）、軟膏状製剤、等の形態（剤形）として用いることができる。このなかでも、軟ペースト剤（クリーム状製剤）などの液体若しくは液状の形態が好ましく、洗口液剤、液体歯磨剤、スプレー剤などの液体の形態がより好ましく、洗口液剤が最も好ましい。 The composition for oral cavity of the present invention is not particularly limited, but a toothpaste, a liquid dentifrice, a mouthwash, a gel, a pasta, a spray, a gum, a soft paste (cream formulation), It can be used as a form (dosage form) of an ointment-like preparation. Among these, a liquid or liquid form such as a soft paste (cream-form preparation) is preferable, a liquid form such as a mouthwash, a liquid dentifrice, and a spray is more preferable, and a mouthwash is most preferable.
本発明の口腔用組成物は、ヘキサノール、オクタノール、２−エチル−１−ヘキサノール、デカノールおよび塩化セチルピリジニウムの他に、本発明の効果を損なわない範囲であれば、通常口腔用組成物に配合し得る成分をさらに配合してもよい。 In addition to hexanol, octanol, 2-ethyl-1-hexanol, decanol, and cetylpyridinium chloride, the oral composition of the present invention is usually incorporated into the oral composition as long as the effects of the present invention are not impaired. You may mix | blend the component obtained.
界面活性剤としては、ノニオン界面活性剤、アニオン界面活性剤または両性界面活性剤を配合することができる。具体的には、ノニオン界面活性剤としてはショ糖脂肪酸エステル、マルトース脂肪酸エステル、ラクトース脂肪酸エステル等の糖脂肪酸エステル、脂肪酸アルカノールアミド類、ソルビタン脂肪酸エステル、脂肪酸モノグリセライド、ポリオキシエチレン付加係数が４〜１５、アルキル基の炭素数が１０〜１８であるポリオキシエチレンアルキルエーテル系またはポリオキシエチレン付加係数が１０〜１８、アルキル基の炭素数が９であるポリオキシエチレンアルキルフェニルエーテル、セバシン酸ジエチル、ポリオキシエチレン硬化ヒマシ油、ポリオキシエチレンソルビタン脂肪酸エステル、ポリオキシエチレングリセリン脂肪酸エステル、ポリオキシエチレンソルビット脂肪酸エステル、ポリエチレングリコール脂肪酸エステル、ポリエチレンラノリン、ポリエチレンステロール、ポリエチレンラノリンアルコール、アルキルグルコシド、ポリオキシエチレンポリオキシプロピレンブロックコポリマー等が挙げられる。アニオン界面活性剤としては、ラウリル硫酸ナトリウム、ポリオキシエチレンラウリルエーテル硫酸ナトリウム等の硫酸エステル塩、ラウリルスルホコハク酸ナトリウム、ポリオキシエチレンラウリルエーテルスルホコハク酸ナトリウム等のスルホコハク酸塩、ココイルサルコシンナトリウム、ラウロイルメチルアラニンナトリウム等のアシルアミノ酸塩、ココイルメチルタウリンナトリウム等が挙げられる。両性イオン界面活性剤としては、ラウリルジメチルアミノ酢酸ベタイン、ヤシ油脂肪酸アミドプロピルジメチルアミノ酢酸ベタイン等の酢酸ベタイン型活性剤、Ｎ−ココイル−Ｎ−カルボキシメチル−Ｎ−ヒドロキシエチルエチレンジアミンナトリウム等のイミダゾリン型活性剤、Ｎ−ラウリルジアミノエチルグリシン等のアミノ酸型活性剤等が挙げられる。これらの界面活性剤は、単独であるいは２種以上を組み合わせて用いることができる。 As the surfactant, a nonionic surfactant, an anionic surfactant or an amphoteric surfactant can be blended. Specifically, nonionic surfactants include sugar fatty acid esters such as sucrose fatty acid esters, maltose fatty acid esters, and lactose fatty acid esters, fatty acid alkanolamides, sorbitan fatty acid esters, fatty acid monoglycerides, and polyoxyethylene addition coefficients of 4 to 15. A polyoxyethylene alkyl ether type having an alkyl group having 10 to 18 carbon atoms or a polyoxyethylene alkyl phenyl ether having a polyoxyethylene addition coefficient of 10 to 18 and an alkyl group having 9 carbon atoms, diethyl sebacate, poly Oxyethylene hydrogenated castor oil, polyoxyethylene sorbitan fatty acid ester, polyoxyethylene glycerin fatty acid ester, polyoxyethylene sorbit fatty acid ester, polyethylene glycol fatty acid ester, polyester Renranorin, polyethylene sterols, polyethylene lanolin alcohols, alkyl glucosides, polyoxyethylene polyoxypropylene block copolymers, and the like. Anionic surfactants include sulfate esters such as sodium lauryl sulfate and polyoxyethylene lauryl ether sulfate, sodium lauryl sulfosuccinate, sulfosuccinates such as sodium polyoxyethylene lauryl ether sulfosuccinate, cocoyl sarcosine sodium, lauroylmethylalanine Examples include acyl amino acid salts such as sodium, cocoyl methyl taurine sodium and the like. Zwitterionic surfactants include betaine acetate type activators such as lauryl dimethylaminoacetic acid betaine, coconut oil fatty acid amidopropyldimethylaminoacetic acid betaine, and imidazoline type such as N-cocoyl-N-carboxymethyl-N-hydroxyethylethylenediamine sodium. Examples include activators and amino acid type activators such as N-lauryldiaminoethylglycine. These surfactants can be used alone or in combination of two or more.
香味剤としては、例えばメントール、カルボン、サリチル酸メチル、バニリン、ベンジルサクシネート、メチルオイゲノール、アネトール、リモネン、オシメン、ｎ−デシルアルコール、メチルアセタート、シトロネニルアセテート、シネオール、エチルリナロール、ワニリン、タイム、ナツメグ、スペアミント油、ペパーミント油、レモン油、オレンジ油、セージ油、ローズマリー油、珪皮油、シソ油、冬緑油、丁子油、ユーカリ油、ピメント油、ティーツリー油、タバナ油、スターアニス油、フェンネル油、珪藻油、バジル油などが挙げられる。これら香料は、単独であるいは２種以上を組み合わせて用いることができる。 As a flavoring agent, for example, menthol, carvone, methyl salicylate, vanillin, benzyl succinate, methyl eugenol, anethole, limonene, ocimene, n-decyl alcohol, methyl acetate, citronenyl acetate, cineol, ethyl linalool, vanillin, thyme , Nutmeg, spearmint oil, peppermint oil, lemon oil, orange oil, sage oil, rosemary oil, cinnamon oil, perilla oil, winter green oil, clove oil, eucalyptus oil, pimento oil, tea tree oil, tabana oil, star Examples include anise oil, fennel oil, diatom oil, and basil oil. These fragrance | flavors can be used individually or in combination of 2 or more types.
研磨剤としては、例えば研磨性沈降シリカ、研磨性ゲルシリカなどの研磨性シリカ、リン酸水素カルシウム・二水和物および無水物、リン酸カルシウム、第３リン酸カルシウム、第３リン酸マグネシウム、ピロリン酸カルシウム、ハイドロキシアパタイト、不溶性メタリン酸ナトリウム、ケイ酸アルミニウム、ケイ酸ジルコニウム、ケイ酸カルシウム、炭酸カルシウム、炭酸マグネシウム、アルミナ、水酸化アルミニウム、硫酸カルシウム、ポリメタクリル酸メチル、パミス（軽石）、ベントナイト、合成樹脂などが挙げられる。これら粘結剤は、単独であるいは２種以上を組み合わせて使用することができる。 Examples of the abrasive include abrasive silica such as abrasive precipitated silica and abrasive gel silica, calcium hydrogenphosphate dihydrate and anhydride, calcium phosphate, tertiary calcium phosphate, tertiary magnesium phosphate, calcium pyrophosphate, hydroxyapatite Insoluble sodium metaphosphate, aluminum silicate, zirconium silicate, calcium silicate, calcium carbonate, magnesium carbonate, alumina, aluminum hydroxide, calcium sulfate, polymethyl methacrylate, pumice, bentonite, synthetic resin, etc. It is done. These binders can be used alone or in combination of two or more.
粘結剤としては、例えばカルボキシメチルセルロースナトリウム、カルボキシメチルエチルセルロース塩、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、ヒドロキシプロピルメチルセルロースなどのセルロース誘導体、キサンタンガム、ジェランガムなどの微生物産生高分子、トラガントガム、カラヤガム、アラビヤガム、カラギーナン、デキストリンなどの天然高分子または天然ゴム類、ポリビニルアルコール、ポリビニルピロリドンなどの合成高分子、増粘性シリカ、ビーガムなどの無機粘結剤、塩化Ｏ−［２−ヒドロキシ−３−（トリメチルアンモニオ）プロピル］ヒドロキシエチルセルロースなどのカチオン性粘結剤が挙げられる。これら粘結剤は、単独であるいは２種以上を組み合わせて使用することができる。 Examples of the binder include carboxymethyl cellulose sodium, carboxymethyl ethyl cellulose salt, cellulose derivatives such as hydroxyethyl cellulose, hydroxypropyl cellulose, hydroxypropyl methyl cellulose, microbial polymer such as xanthan gum, gellan gum, tragacanth gum, karaya gum, arabiya gum, carrageenan, dextrin. Natural polymers such as natural rubbers, synthetic polymers such as polyvinyl alcohol and polyvinyl pyrrolidone, thickening silica, inorganic binders such as bee gum, O- [2-hydroxy-3- (trimethylammonio) propyl] chloride Cationic binders such as hydroxyethyl cellulose can be mentioned. These binders can be used alone or in combination of two or more.
甘味剤としては、例えばサッカリン、サッカリンナトリウム、アセスルファームカリウム、ステビアエキス、ステビオサイド、ネオヘスペリジルジヒドロカルコン、グリチルリチン、ペリラルチン、ソウマチン、アスパルチルフェニルアラニンメチルエステル、メトキシシンナミックアルデヒド、パラチノース、パラチニット、エリスリトール、マルチトール、キシリトール、ラクチトールなどが挙げられる。これら甘味剤は、単独であるいは２種以上を組み合わせて使用することができる。 Sweetening agents include, for example, saccharin, saccharin sodium, acesulfame potassium, stevia extract, stevioside, neohesperidyl dihydrochalcone, glycyrrhizin, perilartin, saumatine, aspartylphenylalanine methyl ester, methoxycinnamic aldehyde, palatinose, palatinit, erythritol, multi Tall, xylitol, lactitol and the like. These sweeteners can be used alone or in combination of two or more.
湿潤剤としては、例えばグリセリン、エチレングリコール、プロピレングリコール、１,３−ブチレングリコール、ソルビット、ポリエチレングリコール、ポリプロピレングリコールなどを単独であるいは２種以上を組み合わせて使用することができる。 As the wetting agent, for example, glycerin, ethylene glycol, propylene glycol, 1,3-butylene glycol, sorbit, polyethylene glycol, polypropylene glycol and the like can be used alone or in combination of two or more.
保存剤としては、例えばメチルパラベン、プロピルパラベンなどのパラベン類、安息香酸ナトリウムなどの安息香酸塩などが挙げられる。これらの保存剤は、単独であるいは２種以上を組み合わせて使用することができる。 Examples of the preservative include parabens such as methylparaben and propylparaben, and benzoates such as sodium benzoate. These preservatives can be used alone or in combination of two or more.
またｐＨ調整剤としては、クエン酸、リン酸、リンゴ酸、グルコン酸、マレイン酸、アスパラギン酸、コハク酸、グルクロン酸、フマル酸、グルタミン酸、アジピン酸、およびこれらの塩や、塩酸、水酸化ナトリウム、水酸化カリウム、ケイ酸ナトリウムなどが挙げられる。これらの成分は単独あるいは２種以上を組合せて本発明の口腔用組成物に含ませることができる。なお、本発明の口腔用組成物は、口腔内で使用できる範囲であれば、そのｐＨは特に制限されないが、通常ｐＨ３．０〜１０．５、好ましくはｐＨ５．５〜８．０である。 Examples of pH adjusters include citric acid, phosphoric acid, malic acid, gluconic acid, maleic acid, aspartic acid, succinic acid, glucuronic acid, fumaric acid, glutamic acid, adipic acid, and salts thereof, hydrochloric acid, sodium hydroxide , Potassium hydroxide, sodium silicate and the like. These components can be contained in the oral composition of the present invention alone or in combination of two or more. In addition, as long as the composition for oral cavity of this invention is a range which can be used in an oral cavity, the pH will not be restrict | limited, However, Usually, pH is 3.0-10.5, Preferably it is pH 5.5-8.0.
薬効成分としては、殺菌剤として塩化セチルピリジニウム以外にも例えば塩酸クロルヘキシジン、グルコン酸クロルヘキシジン、塩化ベンゼトニウム、塩化ベンザルコニウムなどのカチオン性殺菌剤；ドデシルジアミノエチルグリシンなどの両性殺菌剤；イソプロピルメチルフェノール、トリクロサンなどの非イオン殺菌剤；デキストラナーゼ、アミラーゼ、プロテアーゼ、ムタナーゼ、リゾチーム、溶菌酵素（リテックエンザイム）などの酵素；抗炎症剤としてグリチルレチン酸、グリチルリチン酸ジカリウムなどのグリチルリチン酸塩；血行促進剤としてニコチン酸または酢酸トコフェロールなど；抗プラスミン剤としてトラネキサム酸、イプシロンアミノカプロン酸など；出血改善剤としてアスコルビン酸など；組織修復剤としてアラントインなど；再石灰化剤としてフッ化ナトリウムなどのフッ素化合物；その他、水溶性溶媒で抽出された植物抽出物、クロロフィル、塩化ナトリウム、カロペプタイド、塩化亜鉛、ヒノキチオールなどが挙げられ、これらを単独あるいは２種以上を組み合わせて配合することができる。 As a medicinal component, in addition to cetylpyridinium chloride as a bactericidal agent, for example, cationic bactericides such as chlorhexidine hydrochloride, chlorhexidine gluconate, benzethonium chloride, benzalkonium chloride; amphoteric bactericides such as dodecyldiaminoethylglycine; isopropylmethylphenol, Nonionic fungicides such as triclosan; Enzymes such as dextranase, amylase, protease, mutanase, lysozyme, lytic enzyme (lytechenzyme); Glycyrrhizinate such as glycyrrhetinic acid and dipotassium glycyrrhizinate as anti-inflammatory agents; Nicotinic acid or tocopherol acetate, etc .; Tranexamic acid, epsilon aminocaproic acid, etc. as antiplasmin agent; Ascorbic acid, etc. as bleeding remedy; Fluorine compounds such as sodium fluoride as remineralizing agents; plant extracts extracted with water-soluble solvents, chlorophyll, sodium chloride, caropeptides, zinc chloride, hinokitiol, etc. It can mix | blend combining a seed | species or more.
また、本発明の口腔用組成物には、Ｎ−長鎖アシル塩基性アミノ酸低級アルキルエステルまたはその塩を配合することができる。塩基性アミノ酸部分は、特に、オルニチン、リジン、アルギニンがよく、これらは光学活性体またはラセミ体のいずれであってもよい。アシル基は、炭素数８〜２２の飽和または不飽和の天然または合成脂肪酸残基であり、例えば、ラウロイル基、ミリスチル基、パルミトイル基、ステアロイル基などの単一脂肪酸残基が例示され、ヤシ油脂肪酸残基、牛油脂肪酸残基などの天然系の混合脂肪酸残基であってもよい。低級アルキルエステルとしては、メチルエステル、エチルエステル、プロピルエステルが例示される。これらのＮ−長鎖アシル塩基性アミノ酸低級アルキルエステルの塩としては、塩酸塩、硫酸塩のような無機酸塩；グルタミン酸塩、ピログルタミン酸塩、酢酸塩、酒石酸塩、クエン酸塩、脂肪酸塩、酸性アミノ酸塩などの有機酸塩が挙げられる。特に、グルタミン酸塩、ピログルタミン酸塩、酢酸塩、クエン酸塩が好適である。Ｎ−長鎖アシル塩基性アミノ酸低級アルキルエステルまたはその塩としては、具体的には、Ｎ−ココイル−Ｌ−アルギニンエチルエステル・ピロリドンカルボン酸塩（ＣＡＥ）、Ｎ−ラウリル−Ｌ−アルギニンエチルエステル・ピロリドンカルボン酸塩等が挙げられる。 Moreover, N-long-chain acyl basic amino acid lower alkyl ester or its salt can be mix | blended with the composition for oral cavity of this invention. In particular, the basic amino acid moiety may be ornithine, lysine or arginine, which may be either optically active or racemic. The acyl group is a saturated or unsaturated fatty acid residue having 8 to 22 carbon atoms, and examples thereof include single fatty acid residues such as lauroyl group, myristyl group, palmitoyl group, stearoyl group, and coconut oil. Natural mixed fatty acid residues such as fatty acid residues and beef oil fatty acid residues may also be used. Examples of lower alkyl esters include methyl esters, ethyl esters, and propyl esters. As salts of these N-long chain acyl basic amino acid lower alkyl esters, inorganic acid salts such as hydrochloride and sulfate; glutamate, pyroglutamate, acetate, tartrate, citrate, fatty acid salt, Organic acid salts such as acidic amino acid salts are listed. In particular, glutamate, pyroglutamate, acetate, and citrate are preferable. Specific examples of N-long chain acyl basic amino acid lower alkyl esters or salts thereof include N-cocoyl-L-arginine ethyl ester / pyrrolidone carboxylate (CAE), N-lauryl-L-arginine ethyl ester, Examples include pyrrolidone carboxylate.
以下、本発明を具体的に説明するが、本発明は下記の例に限定されるものではない。なお、以下特に断りのない限り「％」は「質量％」を示す。 Hereinafter, the present invention will be specifically described, but the present invention is not limited to the following examples. In the following, “%” means “mass%” unless otherwise specified.
塩化セチルピリジニウムの歯牙表面への吸着評価方法
歯牙のエナメル質のモデルは、ヒドロキシアパタイト粉末（ＢＩＯ−ＲＡＤ Ｌａｂ． Ｈｙｄｒｏｘｙａｐａｔｉｔｅ Ｂｉｏ−Ｇｅｌ ＨＴＰ Ｇｅｌ）（以下「ＨＡ」と略する。）３００ｍｇを紫外線滅菌したヒト唾液２ｍｌに３７℃にて１５時間浸漬して人工ペリクルをアパタイト表面に形成させ、その後、遠心処理し（３０００ｒｐｍ、１０分間）上清を除去することで作製した。
評価は、上記処理を施したＨＡ粉末３００ｍｇに被検溶液サンプル２ｍｌを加え、３７℃にて１５分間浸漬した。遠心処理（３０００ｒｐｍ、１０分間）後、上清を除去し、蒸留水２ｍｌを添加し攪拌後、更に遠心処理（３０００ｒｐｍ、１０分間）し、上清を除去した。再度、蒸留水２ｍｌを添加し、攪拌後、遠心処理（３０００ｒｐｍ、１０分間）し、上清を除去した。次に抽出液（10mMラウリル硫酸ナトリウム、40mMクエン酸緩衝pH3.0/アセトニトリル＝25/75）を用い、ヒドロキシアパタイトに吸着しているＣＰＣを抽出し、ＨＰＬＣで定量してＨＡ３００ｍｇに吸着したＣＰＣ量を求めた。なお、塩化セチルピリジニウムの吸着量の単位は、（μｇ）／（ＨＡ ５０ｍｇ）である。
判断基準
◎：塩化セチルピリジニウムの吸着量が７９０以上
○：塩化セチルピリジニウムの吸着量が６９０以上７９０未満
×：塩化セチルピリジニウムの吸着量が６９０未満
Evaluation method of adsorption of cetylpyridinium chloride on tooth surface
The tooth enamel model was immersed in hydroxyapatite powder (BIO-RAD Lab. Hydroxyapatite Bio-Gel HTP Gel) (hereinafter abbreviated as “HA”) 300 mg in 2 ml of human saliva UV-sterilized at 37 ° C. for 15 hours. Thus, an artificial pellicle was formed on the apatite surface, and then centrifuged (3000 rpm, 10 minutes) to remove the supernatant.
In the evaluation, 2 ml of the test solution sample was added to 300 mg of the HA powder subjected to the above treatment, and immersed for 15 minutes at 37 ° C. After centrifugation (3000 rpm, 10 minutes), the supernatant was removed, 2 ml of distilled water was added and stirred, and then centrifuged (3000 rpm, 10 minutes) to remove the supernatant. Again, 2 ml of distilled water was added, stirred, and then centrifuged (3000 rpm, 10 minutes) to remove the supernatant. Next, using the extract (10 mM sodium lauryl sulfate, 40 mM citrate buffer pH 3.0 / acetonitrile = 25/75), CPC adsorbed on hydroxyapatite was extracted, quantified by HPLC, and the amount of CPC adsorbed on 300 mg of HA Asked. The unit of the adsorption amount of cetylpyridinium chloride is (μg) / (HA 50 mg).
Judgment criteria ◎: Adsorption amount of cetylpyridinium chloride is 790 or more ○: Adsorption amount of cetylpyridinium chloride is 690 or more and less than 790 ×: Adsorption amount of cetylpyridinium chloride is less than 690
表１及び２に示したとおり、ヘキサノール、オクタノール、２−エチル−１−ヘキサノール、デカノールを０.０２〜０.５質量％と塩化セチルピリジニウムを配合した口腔用組成物は、塩化セチルピリジニウムのヒドロキシアパタイト表面への吸着を促進させることが明らかである。特に塩化セチルピリジニウム０.０５質量％に１−ヘキサノール、１−オクタノール、１−デカノールを０．１〜０.５質量％配合した口腔用組成物はその効果に顕著であることが明らかである。 As shown in Tables 1 and 2, the oral composition containing 0.02-0.5% by mass of hexanol, octanol, 2-ethyl-1-hexanol, and decanol and cetylpyridinium chloride is hydroxy of cetylpyridinium chloride. It is clear that the adsorption to the apatite surface is promoted. In particular, it is clear that an oral composition in which 0.1-0.5% by mass of 1-hexanol, 1-octanol, 1-decanol is mixed with 0.05% by mass of cetylpyridinium chloride is remarkable in its effect.
以下、本発明に係る透明な液体口腔用組成物の実施例の処方を挙げるが、本発明は下記の処方に限定されるものではない。 Hereinafter, although the prescription of the Example of the transparent liquid oral cavity composition which concerns on this invention is given, this invention is not limited to the following prescription.
処方例１ 洗口剤
成分 配 合 量
塩化セチルピリジニウム ０．０５
１−ヘキサノール ０．２
グリセリン １０．０
プロピレングリコール ３．０
ポリオキシエチレン（４０）硬化ヒマシ油 ０．４
香料 ０．１
パラオキシ安息香酸メチル ０．１
Ｎ−ココイル−Ｌ−アルギニンエチルエステル
・ピロリドンカルボン酸塩 ０．０５
サッカリンナトリウム ０．０１
β−グリチルレチン酸 ０．０１
ｐＨ調整剤 適 量
精製水 残 部
合計 １００．０
Formulation Example 1 Mouthwash
Component amount
Cetylpyridinium chloride 0.05
1-Hexanol 0.2
Glycerin 10.0
Propylene glycol 3.0
Polyoxyethylene (40) hydrogenated castor oil 0.4
Fragrance 0.1
Methyl paraoxybenzoate 0.1
N-cocoyl-L-arginine ethyl ester
・ Pyrrolidone carboxylate 0.05
Saccharin sodium 0.01
β-glycyrrhetinic acid 0.01
pH adjusting agent
Purified water balance
Total 100.0
処方例２ 洗口剤
成分 配 合 量
塩化セチルピリジニウム ０．１
１−オクタノール ０．２
グリセリン １０．０
１，３−ブチレングリコール ３．０
モノラウリン酸デカグリセリル ０．３
香料 ０．１
サッカリンナトリウム ０．０１
ｐＨ調整剤 適 量
精製水 残 部
合計 １００．０
Formulation Example 2 Mouthwash
Component amount
Cetylpyridinium chloride 0.1
1-octanol 0.2
Glycerin 10.0
1,3-butylene glycol 3.0
Decaglyceryl monolaurate 0.3
Fragrance 0.1
Saccharin sodium 0.01
pH adjusting agent
Purified water balance
Total 100.0
処方例３ 液体歯磨剤
成分 配 合 量
塩化セチルピリジニウム ０．０５
２−エチル−１−ヘキサノール ０．０２
グリセリン １１．０
プロピレングリコール ３．０
ポリオキシエチレン（６０）硬化ヒマシ油 ０．４
香料 ０．１
酢酸トコフェロール ０．０５
Ｎ−ココイル−Ｌ−アルギニンエチルエステル
・ピロリドンカルボン酸塩 ０．０５
サッカリンナトリウム ０．０１
ｐＨ調整剤 適 量
精製水 残 部
合計 １００．０
Formulation Example 3 Liquid Dentifrice
Component amount
Cetylpyridinium chloride 0.05
2-Ethyl-1-hexanol 0.02
Glycerin 11.0
Propylene glycol 3.0
Polyoxyethylene (60) hydrogenated castor oil 0.4
Fragrance 0.1
Tocopherol acetate 0.05
N-cocoyl-L-arginine ethyl ester
・ Pyrrolidone carboxylate 0.05
Saccharin sodium 0.01
pH adjusting agent
Purified water balance
Total 100.0
処方例４ 液体歯磨剤
成分 配 合 量
塩化セチルピリジニウム ０．０５
１−ヘキサノール ０．１
グリセリン １０．０
エタノール ３．０
モノステアリン酸ポリオキシエチレン
（２０）ソルビタン ０．２
香料 ０．１
グリチルリチン酸ジカリウム ０．０２
サッカリンナトリウム ０．０１
ｐＨ調整剤 適 量
精製水 残 部
合計 １００．０
Formulation Example 4 Liquid Dentifrice
Component amount
Cetylpyridinium chloride 0.05
1-Hexanol 0.1
Glycerin 10.0
Ethanol 3.0
Polyoxyethylene monostearate
(20) Sorbitan 0.2
Fragrance 0.1
Dipotassium glycyrrhizinate 0.02
Saccharin sodium 0.01
pH adjusting agent
Purified water balance
Total 100.0
処方例５ 液状歯磨剤
成分 配 合 量
塩化セチルピリジニウム ０．０５
１−デカノール ０．３
ソルビトール ３０．０
プロピレングリコール ３．０
カルボキシメチルセルロースナトリウム ３．０
香料 １．０
ポリオキシエチレン（６０）硬化ヒマシ油 ０．５
フッ化ナトリウム ０．２
パラオキシ安息香酸メチル ０．１
ｐＨ調整剤 適 量
精製水 残 部
合計 １００．０
Formulation Example 5 Liquid dentifrice
Component amount
Cetylpyridinium chloride 0.05
1-decanol 0.3
Sorbitol 30.0
Propylene glycol 3.0
Sodium carboxymethylcellulose 3.0
Fragrance 1.0
Polyoxyethylene (60) hydrogenated castor oil 0.5
Sodium fluoride 0.2
Methyl paraoxybenzoate 0.1
pH adjusting agent
Purified water balance
Total 100.0
処方例６ 液状歯磨剤
成分 配 合 量
塩化セチルピリジニウム ０．０５
１−オクタノール ０．０５
グリセリン ３０．０
キシリトール ５．０
プロピレングリコール ５．０
ヒドロキシエチルセルロース １．０
香料 １．０
ショ糖脂肪酸エステル ０．５
フッ化ナトリウム ０．２
ｐＨ調整剤 適 量
精製水 残 部
合計 １００．０
Formulation Example 6 Liquid Dentifrice
Component amount
Cetylpyridinium chloride 0.05
1-octanol 0.05
Glycerin 30.0
Xylitol 5.0
Propylene glycol 5.0
Hydroxyethyl cellulose 1.0
Fragrance 1.0
Sucrose fatty acid ester 0.5
Sodium fluoride 0.2
pH adjusting agent
Purified water balance
Total 100.0
処方例７ 歯磨剤
成分 配 合 量
塩化セチルピリジニウム ０．０５
２−エチル−１−ヘキサノール ０．３
炭酸カルシウム ３０．０
ソルビトール ２５．０
グリセリン １０．０
増粘性シリカ ３．０
プロピレングリコール ２．０
カルボキシメチルセルロースナトリウム １．０
香料 １．０
ポリオキシエチレン（６０）硬化ヒマシ油 ０．５
サッカリンナトリウム ０．２
酸化チタン ０．３
フッ化ナトリウム ０．２
グリチルリチン酸ジカリウム ０．１
パラオキシ安息香酸メチル ０．１
ｐＨ調整剤 適 量
精製水 残 部
合計 １００．０
Formulation Example 7 Dentifrice
Component amount
Cetylpyridinium chloride 0.05
2-Ethyl-1-hexanol 0.3
Calcium carbonate 30.0
Sorbitol 25.0
Glycerin 10.0
Thickening silica 3.0
Propylene glycol 2.0
Sodium carboxymethylcellulose 1.0
Fragrance 1.0
Polyoxyethylene (60) hydrogenated castor oil 0.5
Saccharin sodium 0.2
Titanium oxide 0.3
Sodium fluoride 0.2
Dipotassium glycyrrhizinate 0.1
Methyl paraoxybenzoate 0.1
pH adjusting agent
Purified water balance
Total 100.0
処方例８ 歯磨剤
成分 配 合 量
塩化セチルピリジニウム ０．０５
１−ヘキサノール ０．５
ソルビトール ４５．０
研磨性シリカ １８．０
増粘性シリカ ３．０
ポリエチレングリコール４００ ３．０
香料 １．０
ポリオキシエチレン（４０）硬化ヒマシ油 ０．５
カルボキシメチルセルロースナトリウム ０．４
サッカリンナトリウム ０．２
フッ化ナトリウム ０．２
イソプロピルメチルフェノール ０．０５
ｐＨ調整剤 適 量
精製水 残 部
合計 １００．０
Formulation Example 8 Dentifrice
Component amount
Cetylpyridinium chloride 0.05
1-Hexanol 0.5
Sorbitol 45.0
Abrasive silica 18.0
Thickening silica 3.0
Polyethylene glycol 400 3.0
Fragrance 1.0
Polyoxyethylene (40) hydrogenated castor oil 0.5
Sodium carboxymethylcellulose 0.4
Saccharin sodium 0.2
Sodium fluoride 0.2
Isopropyl methylphenol 0.05
pH adjusting agent
Purified water balance
Total 100.0
処方例９ マウススプレイ剤
成分 配 合 量
塩化セチルピリジニウム ０．０５
１−ヘキサノール ０．２
エタノール ３０．０
グリセリン １０．０
ポリオキシエチレン（６０）硬化ヒマシ油 １．０
香料 １．０
ｌ−メントール ０．５
サッカリンナトリウム ０．１
ｐＨ調整剤 適 量
精製水 残 部
合計 １００．０
Formulation Example 9 Mouse Spray
Component amount
Cetylpyridinium chloride 0.05
1-Hexanol 0.2
Ethanol 30.0
Glycerin 10.0
Polyoxyethylene (60) hydrogenated castor oil 1.0
Fragrance 1.0
l-Menthol 0.5
Saccharin sodium 0.1
pH adjusting agent
Purified water balance
Total 100.0
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