TWI652070B - Oral composition - Google Patents
Oral composition Download PDFInfo
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- TWI652070B TWI652070B TW103122575A TW103122575A TWI652070B TW I652070 B TWI652070 B TW I652070B TW 103122575 A TW103122575 A TW 103122575A TW 103122575 A TW103122575 A TW 103122575A TW I652070 B TWI652070 B TW I652070B
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- 239000000203 mixture Substances 0.000 title claims abstract description 106
- -1 alkyl galactosides Chemical class 0.000 claims abstract description 67
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 31
- 230000002401 inhibitory effect Effects 0.000 claims abstract description 28
- 210000000214 mouth Anatomy 0.000 claims abstract description 26
- 125000000217 alkyl group Chemical group 0.000 claims abstract description 20
- 125000004432 carbon atom Chemical group C* 0.000 claims abstract description 20
- 125000002091 cationic group Chemical group 0.000 claims abstract description 17
- 150000001875 compounds Chemical class 0.000 claims abstract description 17
- 239000000417 fungicide Substances 0.000 claims abstract description 15
- 230000000855 fungicidal effect Effects 0.000 claims abstract description 13
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims abstract description 8
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims abstract description 5
- 235000014113 dietary fatty acids Nutrition 0.000 claims description 26
- 239000000194 fatty acid Substances 0.000 claims description 26
- 229930195729 fatty acid Natural products 0.000 claims description 26
- 229920003171 Poly (ethylene oxide) Polymers 0.000 claims description 12
- 239000007788 liquid Substances 0.000 claims description 10
- 208000006558 Dental Calculus Diseases 0.000 claims description 8
- 229930006000 Sucrose Natural products 0.000 claims description 8
- 239000005720 sucrose Substances 0.000 claims description 8
- 206010006326 Breath odour Diseases 0.000 claims description 7
- 229920001214 Polysorbate 60 Polymers 0.000 claims description 7
- 230000015572 biosynthetic process Effects 0.000 claims description 7
- 239000002736 nonionic surfactant Substances 0.000 claims description 7
- 229960001927 cetylpyridinium chloride Drugs 0.000 claims description 6
- YMKDRGPMQRFJGP-UHFFFAOYSA-M cetylpyridinium chloride Chemical compound [Cl-].CCCCCCCCCCCCCCCC[N+]1=CC=CC=C1 YMKDRGPMQRFJGP-UHFFFAOYSA-M 0.000 claims description 6
- RGHNJXZEOKUKBD-SQOUGZDYSA-M D-gluconate Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C([O-])=O RGHNJXZEOKUKBD-SQOUGZDYSA-M 0.000 claims description 5
- 150000005215 alkyl ethers Chemical class 0.000 claims description 5
- UREZNYTWGJKWBI-UHFFFAOYSA-M benzethonium chloride Chemical compound [Cl-].C1=CC(C(C)(C)CC(C)(C)C)=CC=C1OCCOCC[N+](C)(C)CC1=CC=CC=C1 UREZNYTWGJKWBI-UHFFFAOYSA-M 0.000 claims description 5
- 229960001950 benzethonium chloride Drugs 0.000 claims description 5
- 229940050410 gluconate Drugs 0.000 claims description 5
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims description 4
- 229960000686 benzalkonium chloride Drugs 0.000 claims description 2
- CADWTSSKOVRVJC-UHFFFAOYSA-N benzyl(dimethyl)azanium;chloride Chemical compound [Cl-].C[NH+](C)CC1=CC=CC=C1 CADWTSSKOVRVJC-UHFFFAOYSA-N 0.000 claims description 2
- 239000008159 sesame oil Substances 0.000 claims 1
- 235000011803 sesame oil Nutrition 0.000 claims 1
- 238000004220 aggregation Methods 0.000 abstract description 33
- 238000004519 manufacturing process Methods 0.000 description 19
- 208000002925 dental caries Diseases 0.000 description 18
- 230000000694 effects Effects 0.000 description 18
- 241000894006 Bacteria Species 0.000 description 16
- 241000193403 Clostridium Species 0.000 description 13
- 238000009833 condensation Methods 0.000 description 13
- 230000005494 condensation Effects 0.000 description 13
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- 238000001179 sorption measurement Methods 0.000 description 12
- 150000005846 sugar alcohols Chemical class 0.000 description 10
- 239000004094 surface-active agent Substances 0.000 description 10
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- 230000000052 comparative effect Effects 0.000 description 8
- 239000003945 anionic surfactant Substances 0.000 description 7
- WQZGKKKJIJFFOK-SVZMEOIVSA-N (+)-Galactose Chemical compound OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@H]1O WQZGKKKJIJFFOK-SVZMEOIVSA-N 0.000 description 6
- YIWUKEYIRIRTPP-UHFFFAOYSA-N 2-ethylhexan-1-ol Chemical compound CCCCC(CC)CO YIWUKEYIRIRTPP-UHFFFAOYSA-N 0.000 description 6
- KWIUHFFTVRNATP-UHFFFAOYSA-N Betaine Natural products C[N+](C)(C)CC([O-])=O KWIUHFFTVRNATP-UHFFFAOYSA-N 0.000 description 6
- 239000002280 amphoteric surfactant Substances 0.000 description 6
- XKXHCNPAFAXVRZ-UHFFFAOYSA-N benzylazanium;chloride Chemical compound [Cl-].[NH3+]CC1=CC=CC=C1 XKXHCNPAFAXVRZ-UHFFFAOYSA-N 0.000 description 6
- 229960003237 betaine Drugs 0.000 description 6
- RYVMUASDIZQXAA-UHFFFAOYSA-N pyranoside Natural products O1C2(OCC(C)C(OC3C(C(O)C(O)C(CO)O3)O)C2)C(C)C(C2(CCC3C4(C)CC5O)C)C1CC2C3CC=C4CC5OC(C(C1O)O)OC(CO)C1OC(C1OC2C(C(OC3C(C(O)C(O)C(CO)O3)O)C(O)C(CO)O2)O)OC(CO)C(O)C1OC1OCC(O)C(O)C1O RYVMUASDIZQXAA-UHFFFAOYSA-N 0.000 description 6
- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 description 5
- KWIUHFFTVRNATP-UHFFFAOYSA-O N,N,N-trimethylglycinium Chemical compound C[N+](C)(C)CC(O)=O KWIUHFFTVRNATP-UHFFFAOYSA-O 0.000 description 5
- 239000002253 acid Substances 0.000 description 5
- 230000000844 anti-bacterial effect Effects 0.000 description 5
- 239000004359 castor oil Substances 0.000 description 5
- 235000019438 castor oil Nutrition 0.000 description 5
- 239000000551 dentifrice Substances 0.000 description 5
- 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 5
- 238000000034 method Methods 0.000 description 5
- 150000003839 salts Chemical class 0.000 description 5
- 238000012360 testing method Methods 0.000 description 5
- 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 4
- 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 4
- 239000004386 Erythritol Substances 0.000 description 4
- UNXHWFMMPAWVPI-UHFFFAOYSA-N Erythritol Natural products OCC(O)C(O)CO UNXHWFMMPAWVPI-UHFFFAOYSA-N 0.000 description 4
- GOOHAUXETOMSMM-UHFFFAOYSA-N Propylene oxide Chemical group CC1CO1 GOOHAUXETOMSMM-UHFFFAOYSA-N 0.000 description 4
- TVXBFESIOXBWNM-UHFFFAOYSA-N Xylitol Natural products OCCC(O)C(O)C(O)CCO TVXBFESIOXBWNM-UHFFFAOYSA-N 0.000 description 4
- 239000003899 bactericide agent Substances 0.000 description 4
- 125000003438 dodecyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 description 4
- 230000002708 enhancing effect Effects 0.000 description 4
- 235000019414 erythritol Nutrition 0.000 description 4
- UNXHWFMMPAWVPI-ZXZARUISSA-N erythritol Chemical compound OC[C@H](O)[C@H](O)CO UNXHWFMMPAWVPI-ZXZARUISSA-N 0.000 description 4
- 229940009714 erythritol Drugs 0.000 description 4
- 239000003112 inhibitor Substances 0.000 description 4
- VQHSOMBJVWLPSR-WUJBLJFYSA-N maltitol Chemical compound OC[C@H](O)[C@@H](O)[C@@H]([C@H](O)CO)O[C@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O VQHSOMBJVWLPSR-WUJBLJFYSA-N 0.000 description 4
- 239000000845 maltitol Substances 0.000 description 4
- 235000010449 maltitol Nutrition 0.000 description 4
- 229940035436 maltitol Drugs 0.000 description 4
- HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 description 4
- KJIFKLIQANRMOU-UHFFFAOYSA-N oxidanium;4-methylbenzenesulfonate Chemical compound O.CC1=CC=C(S(O)(=O)=O)C=C1 KJIFKLIQANRMOU-UHFFFAOYSA-N 0.000 description 4
- 125000006353 oxyethylene group Chemical group 0.000 description 4
- 244000052769 pathogen Species 0.000 description 4
- 238000006116 polymerization reaction Methods 0.000 description 4
- 150000003856 quaternary ammonium compounds Chemical class 0.000 description 4
- 230000002829 reductive effect Effects 0.000 description 4
- 239000000600 sorbitol Substances 0.000 description 4
- 235000010356 sorbitol Nutrition 0.000 description 4
- 238000003860 storage Methods 0.000 description 4
- 230000001629 suppression Effects 0.000 description 4
- 239000000811 xylitol Substances 0.000 description 4
- 235000010447 xylitol Nutrition 0.000 description 4
- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 description 4
- 229960002675 xylitol Drugs 0.000 description 4
- SERLAGPUMNYUCK-DCUALPFSSA-N 1-O-alpha-D-glucopyranosyl-D-mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO[C@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O SERLAGPUMNYUCK-DCUALPFSSA-N 0.000 description 3
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 description 3
- 229940123208 Biguanide Drugs 0.000 description 3
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 description 3
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 3
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 3
- 241000194017 Streptococcus Species 0.000 description 3
- 238000004458 analytical method Methods 0.000 description 3
- 230000001580 bacterial effect Effects 0.000 description 3
- 244000052616 bacterial pathogen Species 0.000 description 3
- 229910052799 carbon Inorganic materials 0.000 description 3
- 239000003054 catalyst Substances 0.000 description 3
- 239000003795 chemical substances by application Substances 0.000 description 3
- MWKFXSUHUHTGQN-UHFFFAOYSA-N decan-1-ol Chemical class CCCCCCCCCCO MWKFXSUHUHTGQN-UHFFFAOYSA-N 0.000 description 3
- 230000007423 decrease Effects 0.000 description 3
- 238000011156 evaluation Methods 0.000 description 3
- 150000004665 fatty acids Chemical class 0.000 description 3
- 238000009472 formulation Methods 0.000 description 3
- 238000005227 gel permeation chromatography Methods 0.000 description 3
- 230000002779 inactivation Effects 0.000 description 3
- 230000001965 increasing effect Effects 0.000 description 3
- 239000004615 ingredient Substances 0.000 description 3
- 230000005764 inhibitory process Effects 0.000 description 3
- 239000000905 isomalt Substances 0.000 description 3
- 235000010439 isomalt Nutrition 0.000 description 3
- HPIGCVXMBGOWTF-UHFFFAOYSA-N isomaltol Natural products CC(=O)C=1OC=CC=1O HPIGCVXMBGOWTF-UHFFFAOYSA-N 0.000 description 3
- 239000002324 mouth wash Substances 0.000 description 3
- 208000028169 periodontal disease Diseases 0.000 description 3
- 238000000926 separation method Methods 0.000 description 3
- 239000000126 substance Substances 0.000 description 3
- 239000000725 suspension Substances 0.000 description 3
- 241001148471 unidentified anaerobic bacterium Species 0.000 description 3
- KBPLFHHGFOOTCA-UHFFFAOYSA-N 1-Octanol Chemical compound CCCCCCCCO KBPLFHHGFOOTCA-UHFFFAOYSA-N 0.000 description 2
- NLXLAEXVIDQMFP-UHFFFAOYSA-N Ammonia chloride Chemical compound [NH4+].[Cl-] NLXLAEXVIDQMFP-UHFFFAOYSA-N 0.000 description 2
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 description 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 2
- TWRXJAOTZQYOKJ-UHFFFAOYSA-L Magnesium chloride Chemical compound [Mg+2].[Cl-].[Cl-] TWRXJAOTZQYOKJ-UHFFFAOYSA-L 0.000 description 2
- 229930195725 Mannitol Natural products 0.000 description 2
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 2
- VBIIFPGSPJYLRR-UHFFFAOYSA-M Stearyltrimethylammonium chloride Chemical compound [Cl-].CCCCCCCCCCCCCCCCCC[N+](C)(C)C VBIIFPGSPJYLRR-UHFFFAOYSA-M 0.000 description 2
- 241000194019 Streptococcus mutans Species 0.000 description 2
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 description 2
- 230000001070 adhesive effect Effects 0.000 description 2
- 150000008051 alkyl sulfates Chemical class 0.000 description 2
- 239000000872 buffer Substances 0.000 description 2
- WOWHHFRSBJGXCM-UHFFFAOYSA-M cetyltrimethylammonium chloride Chemical compound [Cl-].CCCCCCCCCCCCCCCC[N+](C)(C)C WOWHHFRSBJGXCM-UHFFFAOYSA-M 0.000 description 2
- 238000006243 chemical reaction Methods 0.000 description 2
- 230000015271 coagulation Effects 0.000 description 2
- 210000003298 dental enamel Anatomy 0.000 description 2
- 150000002148 esters Chemical class 0.000 description 2
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- 230000002070 germicidal effect Effects 0.000 description 2
- 238000010438 heat treatment Methods 0.000 description 2
- 230000014759 maintenance of location Effects 0.000 description 2
- 239000000594 mannitol Substances 0.000 description 2
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- 238000005259 measurement Methods 0.000 description 2
- 238000002156 mixing Methods 0.000 description 2
- 229940051866 mouthwash Drugs 0.000 description 2
- 229940041678 oral spray Drugs 0.000 description 2
- 239000000668 oral spray Substances 0.000 description 2
- 230000001717 pathogenic effect Effects 0.000 description 2
- 229920000223 polyglycerol Polymers 0.000 description 2
- 238000002360 preparation method Methods 0.000 description 2
- BAZAXWOYCMUHIX-UHFFFAOYSA-M sodium perchlorate Chemical compound [Na+].[O-]Cl(=O)(=O)=O BAZAXWOYCMUHIX-UHFFFAOYSA-M 0.000 description 2
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- 125000001424 substituent group Chemical group 0.000 description 2
- UBXILKVIJDEQON-UHFFFAOYSA-N 1-chlorododecane;n,n-dimethylmethanamine Chemical compound CN(C)C.CCCCCCCCCCCCCl UBXILKVIJDEQON-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
- PLLBRTOLHQQAQQ-UHFFFAOYSA-N 8-methylnonan-1-ol Chemical compound CC(C)CCCCCCCO PLLBRTOLHQQAQQ-UHFFFAOYSA-N 0.000 description 1
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 description 1
- 241000186045 Actinomyces naeslundii Species 0.000 description 1
- 241000606749 Aggregatibacter actinomycetemcomitans Species 0.000 description 1
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 description 1
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- UXVMQQNJUSDDNG-UHFFFAOYSA-L Calcium chloride Chemical compound [Cl-].[Cl-].[Ca+2] UXVMQQNJUSDDNG-UHFFFAOYSA-L 0.000 description 1
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- 102000004190 Enzymes Human genes 0.000 description 1
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- 208000032139 Halitosis Diseases 0.000 description 1
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 1
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- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 1
- QWZLBLDNRUUYQI-UHFFFAOYSA-M Methylbenzethonium chloride Chemical compound [Cl-].CC1=CC(C(C)(C)CC(C)(C)C)=CC=C1OCCOCC[N+](C)(C)CC1=CC=CC=C1 QWZLBLDNRUUYQI-UHFFFAOYSA-M 0.000 description 1
- CBSOFSBFHDQRLV-UHFFFAOYSA-N N-methylbenzylamine hydrochloride Chemical compound [Cl-].C[NH2+]CC1=CC=CC=C1 CBSOFSBFHDQRLV-UHFFFAOYSA-N 0.000 description 1
- 238000005481 NMR spectroscopy Methods 0.000 description 1
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- NHNBFGGVMKEFGY-UHFFFAOYSA-N Nitrate Chemical compound [O-][N+]([O-])=O NHNBFGGVMKEFGY-UHFFFAOYSA-N 0.000 description 1
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- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 description 1
- 241000194026 Streptococcus gordonii Species 0.000 description 1
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- FGEXJVXTNKHLRJ-UHFFFAOYSA-N [Cl-].[NH4+].C(C1=CC=CC=C1)[Na] Chemical compound [Cl-].[NH4+].C(C1=CC=CC=C1)[Na] FGEXJVXTNKHLRJ-UHFFFAOYSA-N 0.000 description 1
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- 239000007864 aqueous solution Substances 0.000 description 1
- ZPHQBFRCXUIIAZ-UHFFFAOYSA-N benzene;hydrochloride Chemical compound Cl.C1=CC=CC=C1 ZPHQBFRCXUIIAZ-UHFFFAOYSA-N 0.000 description 1
- 230000017531 blood circulation Effects 0.000 description 1
- 210000004556 brain Anatomy 0.000 description 1
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 description 1
- 229910052794 bromium Inorganic materials 0.000 description 1
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- 239000003240 coconut oil Substances 0.000 description 1
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- 239000003086 colorant Substances 0.000 description 1
- 238000007796 conventional method Methods 0.000 description 1
- 210000004268 dentin Anatomy 0.000 description 1
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- 125000000118 dimethyl group Chemical group [H]C([H])([H])* 0.000 description 1
- PFKRTWCFCOUBHS-UHFFFAOYSA-N dimethyl(octadecyl)azanium;chloride Chemical compound [Cl-].CCCCCCCCCCCCCCCCCC[NH+](C)C PFKRTWCFCOUBHS-UHFFFAOYSA-N 0.000 description 1
- LQZZUXJYWNFBMV-UHFFFAOYSA-N dodecan-1-ol Chemical compound CCCCCCCCCCCCO LQZZUXJYWNFBMV-UHFFFAOYSA-N 0.000 description 1
- DDXLVDQZPFLQMZ-UHFFFAOYSA-M dodecyl(trimethyl)azanium;chloride Chemical compound [Cl-].CCCCCCCCCCCC[N+](C)(C)C DDXLVDQZPFLQMZ-UHFFFAOYSA-M 0.000 description 1
- 239000003623 enhancer Substances 0.000 description 1
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- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 description 1
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Abstract
本發明係關於一種口腔用組合物,其良好地保持烷基半乳糖苷之共凝聚抑制效果,且其溶解性得到提高。
本發明係一種口腔用組合物,其含有以下之成分:(A)由下述式(I):
(式中,R表示可經取代之碳數8~18之直鏈或支鏈狀之烷基,G表示半乳糖殘基,E表示氫原子或甲基,m表示0~200之整數,n表示1~30之整數)表示之化合物0.001質量%以上1質量%以下、(B)陽離子性殺菌劑0.001質量%以上0.1質量%以下、及(C)水35質量%以上。
Description
本發明係關於一種口腔用組合物。
齲齒具有作為因病原性細菌向齒面之附著、固著而趨於發病之口腔內感染症之一面。關於口腔細菌向齒面之固著機制,可認為如下:首先,於經唾液之薄膜(pellicle)覆蓋之琺瑯質表面吸附口腔鏈球菌(Streptococcus oralis)、血鏈球菌(Streptococcus sanguis)、格氏鏈球菌(Streptococcus gordonii)、內氏放線菌(Actinomyces naeslundii)等初期固著細菌。然後,該等初期固著細菌隨著增殖相互發生共凝聚(co-aggregation),而開始形成牙垢(牙菌斑)。繼而,隨著牙菌斑之成熟化,微生物菌群自兼性厭氧菌向專性壓氧菌轉變,由具核細梭菌(Fusobacterium nucleatum)代表之專性壓氧菌共凝聚於初期固著細菌。然後,伴放線放線桿菌(Actinobacillus actinomycetemcomitans)、牙齦卟啉單胞菌(Porphyromonas gingivalis)、中間普雷沃菌(Prevotella intermedia)等牙周病相關細菌進而共凝聚於該具核細梭菌並進行固著。進而,竹本等人揭示出,因作為齲齒相關細菌之變種鏈球菌(Streptococcus mutans)、遠緣鏈球菌(Streptococcus sobrinus)等亦與具核細梭菌共凝聚,故具有同樣之固著機理(非專利文獻1)。
如此,細梭菌等齲齒病原菌或牙周病相關細菌之共凝聚極大參與齲齒或牙周病、口臭等之產生或發病、及進展。作為具有有效抑制此種共凝聚之作用之化合物,已知有於半乳糖上醚鍵結有烷基之烷基
半乳糖苷,專利文獻1中,藉由使用該化合物而獲得發揮蛀齒或牙垢形成抑制效果之口腔用組合物。又,專利文獻2中,藉由併用該烷基半乳糖苷與非離子性殺菌劑,獲得具有細梭菌等之共凝聚抑制作用並且將細梭菌屬細菌特異性地殺除之口腔用組合物。
(專利文獻1)日本專利特開2006-124384號公報
(專利文獻2)日本專利特開2007-291083號公報
(非專利文獻1)Journal of Periodontal Research,Vol.30,p252-257
本發明係關於一種口腔用組合物,其含有以下之成分(A)、(B)、及(C):(A)由下述式(I):
(式中,R表示可經取代之碳數8~18之直鏈或支鏈狀之烷基,G表示半乳糖殘基,E表示氫原子或甲基,m表示0~200之整數,n表示1~30之整數)
表示之化合物0.001質量%以上1質量%以下、(B)陽離子性殺菌劑0.001質量%以上0.1質量%以下、及(C)水35質量%以上。
由於烷基半乳糖苷不溶於水,故於使其含於含有大量水之製劑中時,必須增大界面活性劑之含量。關於將此種烷基半乳糖苷與界面活性劑併用之製劑,由本發明者等人明確,若過量地使用界面活性劑
則烷基半乳糖苷之共凝聚抑制效果減退或失活。並且,進而由本發明者等人明確,陽離子性殺菌劑出乎意料地大大有助於提高烷基半乳糖苷之溶解性,並且亦可期待更進一步之附帶效果。
因此,本發明者等人發現,只要為將原本不溶於水之特定之烷基半乳糖苷與特定量之陽離子性殺菌劑併用之口腔用組合物,則可出乎意料地有效提高於水中之溶解性。
根據本發明之口腔用組合物,可不增大界面活性劑之含量而有效地提高烷基半乳糖苷於水中之溶解性,故即便為含有大量水之組合物亦可使烷基半乳糖苷良好地溶解。因此,不僅可良好地保持烷基半乳糖苷對細梭菌等之共凝聚之抑制效果,亦可有效地提高陽離子性殺菌劑向牙齒之吸附性,充分發揮其殺菌效果。因此,若使用本發明之口腔用組合物,則亦可帶來優異之牙垢形成抑制效果或口臭抑制效果。
以下對本發明進行詳細地說明。
本發明之口腔用組合物含有由下述式(I):
(式中,R表示可經取代之碳數8~18之直鏈或支鏈狀之烷基,G表示半乳糖殘基,E表示氫原子或甲基,m表示0~200之整數,n表示
1~30之整數)
表示之化合物0.001質量%以上1質量%以下作為成分(A)。
成分(A)之由式(I)表示之化合物為於碳數8~18之烷基R上直接或者經由1個以上之氧化乙烯基或氧化丙烯基,以α-配置或β-配置醚鍵結有1個以上之半乳糖殘基之化合物。作為式(I)中之R,可為直鏈或支鏈狀之任一者,具體而言可列舉:正辛基、正癸基、正十一烷基、正十二烷基、正十四烷基、正十六烷基、正十八烷基、2-乙基己基、異癸基、月桂基、異硬脂基(異十八烷基)等。就利用下述成分(B)提高成分(A)之溶解性之觀點、及共凝聚抑制效果或於口腔內之滯留性等之觀點、以及提高陽離子性殺菌劑向牙齒之吸附之觀點而言,式(I)中之R較佳為碳數10~18,更佳為碳數10~16,進而較佳為碳數10~14。
又,R之1個以上之氫原子可經取代基取代,作為該取代基,可列舉:碳數1~6之烷氧基、鹵素原子(例如,氟、氯、溴、碘等)、硝基、碳數1~6之鹵代烷基、碳數1~6之鹵代烷氧基。又,本發明中所使用之由式(I)表示之化合物之半乳糖包含吡喃糖型、呋喃糖型或該等之混合物之任一者。式(I)中之m表示氧化乙烯基或氧化丙烯基之聚合度,為0~200之整數,就共凝聚抑制作用之觀點而言,較佳為0~12,更佳為0~3,進而較佳為0。式(I)中之n表示半乳糖之縮合度,為1~30之整數,就起泡性之觀點而言,較佳為1~6,更佳為1~3。
又,作為式(I)中之E,就共凝聚抑制效果之觀點而言,較佳為氫原子。
又,作為成分(A),亦可使用含有兩種由式(I)表示之化合物之混合物。於此情形時,關於式(I)中之R,組合物中之成分(A)之烷基之平均碳數為8~18,就利用下述成分(B)提高成分(A)之溶解性之觀點、及共凝聚抑制效果或於口腔內之滯留性等之觀點、以及提高陽離子性
殺菌劑向牙齒之吸附性之觀點而言,式(I)中之R之平均碳數較佳為碳數10~18,更佳為碳數10~16,進而較佳為碳數10~14。具體而言,較佳為選自月桂基、正辛基、正癸基、異癸基之1種或2種以上。組合物中之成分(A)之氧化乙烯基或氧化丙烯基之聚合度m之平均聚合度x為0~200之數,較佳為0~12之數,更佳為0~3之數,進而較佳為0~1。組合物中之成分(A)之半乳糖之縮合度n之平均縮合度y為1~30之數,就共凝聚抑制作用之觀點而言,較佳為1~6之數,更佳為1~3之數。再者,半乳糖之平均縮合度y可根據由凝膠滲透層析法等分析法獲得之各縮合度之成分之組成算出。例如,於為半乳糖之縮合度1~z之烷基半乳糖苷混合物之情形時,若縮合度z之半乳糖苷之莫耳比為az(a1+a2+a3+...+az=1),則半乳糖之平均縮合度y由y=a1×1+a2×2+...+az×z=Σ(az×z)表示。
又,亦可同樣地算出氧化乙烯基或者氧化丙烯基之平均聚合度x或由R表示之烷基之平均碳數。
上述成分(A)之由式(I)表示之化合物可藉由堀等人之方法(藥學雜誌,Vol.79,No.1,p80-83)或下述製造例1~2而製造。
成分(A)之由式(I)表示之化合物強有力地抑制作為固有菌(indigenous bacterium)之細梭菌屬細菌與齲齒病原菌之共凝聚。此處,作為細梭菌屬細菌,可列舉具核細梭菌、拉氏細梭菌等。又,作為齲齒病原菌,可列舉變種鏈球菌、遠緣鏈球菌等。先前已知之脂肪酸糖酯於口腔內分解產生成為齲齒之原因之酸,但成分(A)之由式(I)表示之化合物於口腔內不分解,不產生成為齲齒之原因之酸。因此,藉由有效地發揮本發明之成分(A)之共凝聚抑制效果,本發明之含有成分(A)之組合物可作為齲齒抑制劑或齲齒預防劑而發揮功能。
就良好地溶解於下述成分(C)之水而充分發揮共凝聚抑制效果之觀點、及提高成分(B)之陽離子性殺菌劑向牙齒之吸附性之觀點而
言,成分(A)之含量於本發明之口腔用組合物中為0.001質量%以上,較佳為0.01質量%以上,更佳為0.02質量%以上。就有效地保持於成分(C)之水中之溶解性之觀點而言,成分(A)之含量於本發明之口腔用組合物中為1質量%以下,較佳為0.9質量%以下,更佳為0.8質量%以下,就保存穩定性之觀點而言,較佳為0.5質量%以下,更佳為0.3質量%以下。又,成分(A)之含量於本發明之口腔用組合物中為0.001質量%以上1質量%以下,較佳為0.01~0.9質量%,更佳為0.02~0.8質量%,進而更佳為0.02~0.5質量%。
本發明之口腔用組合物含有陽離子性殺菌劑0.001質量%以上0.1質量%以下作為成分(B)。藉由含有該成分(B),可使原本不溶於水之成分(A)良好地溶解於下述成分(C)之水中,雖為含有大量水之口腔用組合物,但可抑制界面活性劑之含量之增大,且有效地防止組合物中之成分(A)之分離或不溶物化而提高均一性。因此,可避免成分(A)之共凝聚抑制效果之減退或失活,且容易增大成分(A)之含量直至可充分發揮該效果。又,藉由成分(A)與成分(B)之併用,亦可提高成分(B)向牙齒之吸附性。
作為該成分(B),可列舉選自四級銨化合物、及雙胍化合物之1種或2種以上。作為四級銨化合物,具體而言,例如可列舉:西吡氯銨(cetylpyridinium chloride)、苄索氯銨(benzethonium chloride)、氯化苄烷銨(benzalkonium chloride)、氯化硬脂基二甲基銨、氯化硬脂基三甲基銨、氯化鯨蠟基三甲基銨、甲基苄索氯銨(methylbenzethonium chloride)、氯化月桂基三甲基銨、拉匹氯銨等。
作為雙胍化合物,具體而言,可列舉洛赫西定(chlorhexidine)及其鹽,作為該鹽,可列舉葡萄糖酸洛赫西定、鹽酸洛赫西定。
其中,就提高成分(A)之溶解性之觀點而言,作為成分(B),較佳為選自西吡氯銨、苄索氯銨、氯化苄烷銨、葡萄糖酸洛赫西定、及鹽
酸洛赫西定之1種或2種以上,就殺菌性能之觀點而言,更佳為選自西吡氯銨、苄索氯銨、及氯化苄烷銨之1種或2種以上之四級銨化合物。
就提高成分(A)之溶解性之觀點及殺菌性能之觀點而言,成分(B)之含量於本發明之口腔用組合物中為0.001質量%以上,較佳為0.005質量%以上,更佳為0.008質量%以上。就保持良好之味道或使用感之觀點而言,成分(B)之含量於本發明之口腔用組合物中為0.1質量%以下,較佳為0.08質量%以下,更佳為0.06質量%以下。又,成分(B)之含量於本發明之口腔用組合物中為0.001質量%以上0.1質量%以下,較佳為0.005~0.08質量%,更佳為0.008~0.06質量%。
就良好地保持成分(A)之共凝聚抑制效果之觀點、及提高陽離子性殺菌劑向牙齒之吸附性之觀點而言,成分(A)之含量與成分(B)之含量之質量比((A)/(B))較佳為0.1以上,較佳為1以上,更佳為2以上。就確保成分(A)之溶解性之觀點而言,成分(A)之含量與成分(B)之含量之質量比((A)/(B))較佳為100以下,更佳為90以下,進而較佳為80以下,就保存穩定性之觀點而言,更佳為40以下,進而較佳為30以下。又,成分(A)之含量與成分(B)之含量之質量比((A)/(B))較佳為0.1以上100以下,更佳為1~90,進而較佳為2~80,就保存穩定性之觀點而言,更佳為2~40,進而較佳為2~30。
本發明之口腔用組合物含有水35質量%以上作為成分(C)。本發明中,即便為如此含有大量水之口腔用組合物,亦可藉由將成分(A)與成分(B)以特定之量使用,而提高成分(A)於水中之溶解性,且保持良好之共凝聚抑制效果。就確保作為含有大量水之液狀之口腔用組合物之適度流動性之觀點而言,成分(C)之含量於本發明之口腔用組合物中為35質量%以上,較佳為50質量%以上,更佳為60質量%以上。就使成分(A)良好地溶解且良好地保持共凝聚抑制效果之觀點而言,成分(C)之含量於本發明之口腔用組合物中較佳為99.99質量%以下,
更佳為99.9質量%以下。成分(C)之含量於含有下述成分(D)之非離子性界面活性劑之情形時,較佳為99.8質量%以下,更佳為99.7質量%以下。成分(C)之含量於與成分(D)一併進而含有下述糖醇之情形時,較佳為95質量%以下,更佳為89質量%以下。又,成分(C)之含量於本發明之口腔用組合物中為35質量%以上,較佳為35~99.99質量%,更佳為50~99.9質量%,進而較佳為60~99.9質量%,於含有成分(D)之情形時,較佳為50~99.8質量%,更佳為60~99.7質量%。又,於含有成分(D)及糖醇之情形時,較佳為50~95質量%,更佳為60~89質量%。
再者,成分(C)之含量為本發明之口腔用組合物中之其他成分之剩餘量。
就充分發揮成分(B)向牙齒之吸附性提高效果之觀點、及更良好地保持成分(A)之共凝聚抑制效果之觀點而言,本發明之口腔用組合物較佳為進而含有非離子性界面活性劑作為成分(D)。本發明之口腔用組合物不僅可藉由特定量之成分(B)確保成分(A)之良好之溶解性,而且可藉由成分(D)之非離子性界面活性劑帶來提高成分(B)向牙齒之吸附性之效果,而充分發揮成分(B)之殺菌效果。又,無需增大成分(D)之非離子性界面活性劑之含量,可以不引起成分(A)之共凝聚抑制效果之減退或失活之量有效地含有成分(D),且使組合物之穩定性提高,或使香料等油性成分之溶解性提高。
作為該成分(D),例如可列舉選自聚氧乙烯氫化蓖麻油、聚氧乙烯山梨醇酐脂肪酸酯、聚甘油脂肪酸酯、聚氧乙烯烷基醚、烷基聚葡糖苷、及蔗糖脂肪酸酯之1種或2種以上。就良好地確保成分(A)之共凝聚抑制效果之觀點而言,聚氧乙烯氫化蓖麻油或聚氧乙烯烷基醚中之伸乙氧基之平均加成莫耳數較佳為10~80,更佳為30~60。又,就味道或者於水中之分散性或溶解性之觀點、及良好地確保成分(A)之
共凝聚抑制效果之觀點而言,構成聚氧乙烯山梨醇酐脂肪酸酯或聚甘油脂肪酸酯之脂肪酸之碳數較佳為8~18,更佳為10~16,進而較佳為10~14。就味道或於水中之分散性之觀點、及良好地確保成分(A)之共凝聚抑制效果之觀點而言,聚氧乙烯烷基醚中之烷基之碳數較佳為10~16,更佳為10~14,就同樣之觀點而言,烷基聚葡糖苷中之烷基之碳數較佳為10~16,更佳為10~12。進而,就味道或於水中之分散性之觀點、及提高成分(B)向牙齒之吸附性之觀點而言,構成蔗糖脂肪酸酯之脂肪酸之碳數較佳為10~16,更佳為12~14。
該成分(D)中,就味道之觀點、及確保成分(A)於水中之良好之溶解性與成分(B)向牙齒之良好之吸附性之觀點而言,更佳為選自聚氧乙烯山梨醇酐脂肪酸酯、聚甘油脂肪酸酯、烷基聚葡糖苷、及蔗糖脂肪酸酯之1種或2種以上,進而較佳為至少含有蔗糖脂肪酸酯,就確保成分(A)於水中之良好之溶解性與成分(A)之共凝聚抑制效果之觀點而言,更佳為選自聚氧乙烯氫化蓖麻油、聚氧乙烯山梨醇酐脂肪酸酯、聚甘油脂肪酸酯、及烷基聚葡糖苷之1種或2種以上。
就良好地保持成分(A)於水中之溶解性之觀點、及提高成分(B)向牙齒之吸附性之觀點而言,成分(D)之含量較佳為0.1質量%以上,更佳為0.2質量%以上。就抑制成分(A)之共凝聚抑制效果減退或失活之觀點而言,成分(D)之含量較佳為1.5質量%以下,更佳為1.2質量%以下,進而較佳為1質量%以下。又,成分(D)之含量較佳為0.1質量%以上1.5質量%以下,更佳為0.2~1.2質量%,進而較佳為0.2~1質量%。
就成分(A)之良好之溶解性、及確保成分(B)向牙齒之良好之吸附性之觀點而言,成分(A)及成分(B)之合計含量與成分(D)之含量之質量比({(A)+(B)}/(D))較佳為0.02以上,更佳為0.05以上。就平衡性良好地保持成分(A)之良好之溶解性與共凝聚抑制效果之觀點而言,成分(A)及成分(B)之合計含量與成分(D)之含量之質量比({(A)+
(B)}/(D))較佳為2以下,更佳為1以下,進而較佳為0.8以下,進而更佳為0.6以下。又,成分(A)及成分(B)之合計含量與成分(D)之含量之質量比({(A)+(B)}/(D))較佳為0.02以上2以下,更佳為0.02~1,進而較佳為0.05~0.8,進而更佳為0.05~0.6。
進而,就有效地增強成分(A)之共凝聚抑制效果之觀點而言,本發明之口腔用組合物較佳為含有糖醇。糖醇具有延遲細梭菌屬細菌與齲齒病原菌之結合之作用,且因於口腔內不產生酸而可帶來增強共凝聚抑制效果之作用。作為該糖醇,較佳為碳數4~12者,具體而言,可列舉選自山梨糖醇、甘露醇、木糖醇、赤蘚醇、異麥芽酮糖醇(reduced palatinose)、乳糖醇、麥芽糖醇之1種或2種以上。其中,就增強共凝聚抑制效果之觀點而言,較佳為選自赤蘚醇、木糖醇、麥芽糖醇、及異麥芽酮糖醇之1種或2種以上,就味道與濕潤性、穩定性之觀點而言,較佳為山梨糖醇。
就有效地增強成分(A)之共凝聚抑制效果之觀點、及獲得良好之味道之觀點而言,糖醇之含量於本發明之口腔用組合物中較佳為5質量%以上,更佳為8質量%以上,進而較佳為10質量%以上。就保持成分(A)之良好之溶解性之觀點而言,糖醇之含量較佳為30質量%以下,更佳為25質量%以下,進而較佳為20質量%以下。
本發明之口腔用組合物可於不阻礙本發明之效果之範圍內進而含有除上述成分以外之成分。作為該成分,例如可列舉濕潤劑、黏結劑、牙質強化劑、pH值調整劑、酵素類、抗炎劑、血流促進劑、防腐劑、著色劑、色素類、香料等。再者,陰離子性界面活性劑較佳為於本發明之口腔用組合物中,除不可避免地混入之情形以外不含有,或者含有超過0質量%且為1質量%以下,更佳為含有0.7質量%以下。兩性界面活性劑較佳為於本發明之口腔用組合物中,除不可避免地混入之情形以外不含有,或者含有1質量%以下,較佳為含有0.7質量%
以下。就抑制成分(A)之共凝聚抑制效果減退或失活之觀點而言,除成分(D)、陰離子性界面活性劑、及兩性界面活性劑以外之界面活性劑較佳為於本發明之口腔用組合物中,除不可避免地混入之情形以外不含有,或者含有超過0質量%且為0.5質量%以下,更佳為含有0.1質量%以下。又,除成分(D)、陰離子性界面活性劑、及兩性界面活性劑以外之界面活性劑較佳為於本發明之口腔用組合物中不含有,或者含有超過0質量%且為0.5質量%以下,更佳為含有超過0質量%且為0.1質量%以下。
作為陰離子性界面活性劑,可列舉烷基硫酸鹽、N-醯基麩胺酸鹽、烷基磷酸鹽、N-醯基牛磺酸鹽等,就味道、發泡性、穩定性等之觀點而言,較佳為烷基硫酸鹽,更佳為月桂基硫酸鈉。
作為兩性界面活性劑,可列舉乙酸甜菜鹼、月桂基二甲胺基乙酸甜菜鹼、咪唑啉鎓甜菜鹼、2-烷基-N-羧基甲基-N-羥基乙基咪唑鎓甜菜鹼、月桂基磺基甜菜鹼、椰子油脂肪醯胺丙基甜菜鹼、N-烷基-1-羥基乙基咪唑啉甜菜鹼鈉等。
本發明之口腔用組合物係可藉由常法混合上述各成分而製造,且如上所述含有大量水之組合物,故較佳為液體口腔用組合物。作為該液體口腔用組合物,例如可列舉漱口劑、液狀潔牙劑、水潔牙劑、口腔噴劑、含漱劑等。藉由使用本發明之口腔用組合物,可充分發揮共凝聚抑制效果,故可有效地抑制牙垢形成,藉此亦可有效地抑制齲齒,又,亦可有效地抑制口臭。因此,本發明之口腔用組合物作為牙垢形成抑制用、齲齒抑制用或齲齒預防用,又,作為口臭抑制用均可有效地發揮作用。
關於上述實施態樣,本發明進而揭示以下之口腔用組合物。
[1]一種口腔用組合物,其含有以下之成分(A)、(B)、及(C):(A)由下述式(I):
(式中,R表示可經取代之碳數8~18之直鏈或支鏈狀之烷基,G表示半乳糖殘基,E表示氫原子或甲基,m表示0~200之整數,n表示1~30之整數)
表示之化合物0.001質量%以上1質量%以下、(B)陽離子性殺菌劑0.001質量%以上0.1質量%以下、及(C)水35質量%以上。
[2]如上述[1]之口腔用組合物,其中式(I)中之R較佳為碳數10~18,更佳為碳數10~16,進而較佳為碳數10~14。
[3]如上述[1]或[2]之口腔用組合物,其中式(I)中之m較佳為0~12,更佳為0~3,進而較佳為0。
[4]如上述[1]至[3]之口腔用組合物,其中式(I)中之n較佳為1~6,更佳為1~3。
[5]如上述[1]至[4]之口腔用組合物,其中式(I)中之E較佳為氫原子。
[6]如上述[1]至[5]之口腔用組合物,其中成分(A)之含量較佳為0.01質量%以上,更佳為0.02質量%以上,較佳為0.9質量%以下,更佳為0.8質量%以下,就保存穩定性之觀點而言,較佳為0.5質量%以下,更佳為0.3質量%以下。
[7]如上述[1]至[6]之口腔用組合物,其中成分(B)較佳為選自四級銨化合物、及雙胍化合物之1種或2種以上,更佳為列舉西吡氯銨、苄
索氯銨、氯化苄烷銨、氯化硬脂基二甲基銨、氯化硬脂基三甲基銨、氯化鯨蠟基三甲基銨、甲基苄索氯銨、氯化月桂基三甲基銨、拉匹氯銨、洛赫西定及其鹽,作為該鹽,為選自葡萄糖酸洛赫西定、及鹽酸洛赫西定之1種或2種以上,進而較佳為選自西吡氯銨、苄索氯銨、氯化苄烷銨、葡萄糖酸洛赫西定、及鹽酸洛赫西定之1種或2種以上,又,進而較佳為選自西吡氯銨、苄索氯銨、及氯化苄烷銨之1種或2種以上之四級銨化合物。
[8]如上述[1]至[7]之口腔用組合物,其中成分(B)之含量較佳為0.005質量%以上,更佳為0.008質量%以上,較佳為0.08質量%以下,更佳為0.06質量%以下。
[9]如上述[1]至[8]之口腔用組合物,其中成分(A)之含量與成分(B)之含量之質量比((A)/(B))較佳為0.1以上,更佳為1以上,進而較佳為2以上,較佳為100以下,更佳為90以下,進而較佳為80以下,又,更佳為40以下,進而較佳為30以下。
[10]如上述[1]至[9]之口腔用組合物,其中成分(C)之含量較佳為50質量%以上,更佳為60質量%以上,較佳為99.99質量%以下,更佳為99.9質量%以下,於進而含有成分(D)非離子性界面活性劑之情形時,較佳為99.8質量%以下,更佳為99.7質量%以下。
[11]如上述[1]至[10]之口腔用組合物,其進而含有成分(D)非離子性界面活性劑0.1質量%以上1.5質量%以下,其含量更佳為0.2質量%以上,更佳為1.2質量%以下,進而較佳為1質量%以下。
[12]如上述[11]之口腔用組合物,其中成分(D)較佳為選自聚氧乙烯氫化蓖麻油、聚氧乙烯山梨醇酐脂肪酸酯、聚甘油脂肪酸酯、聚氧乙烯烷基醚、烷基聚葡糖苷、及蔗糖脂肪酸酯之1種或2種以上,更佳為選自聚氧乙烯山梨醇酐脂肪酸酯、聚甘油脂肪酸酯、烷基聚葡糖苷、及蔗糖脂肪酸酯之1種或2種以上,進而較佳為至少含有蔗糖脂肪
酸酯,又,更佳為選自聚氧乙烯氫化蓖麻油、聚氧乙烯山梨醇酐脂肪酸酯、聚甘油脂肪酸酯、及烷基聚葡糖苷之1種或2種以上。
[13]如上述[11]或[12]之口腔用組合物,其中成分(A)及成分(B)之合計含量與成分(D)之含量之質量比({(A)+(B)}/(D))較佳為0.02以上,更佳為0.05以上,較佳為2以下,更佳為1以下,進而較佳為0.8以下,進而更佳為0.6以下。
[14]如上述[1]至[13]之口腔用組合物,其進而含有糖醇,其含量較佳為5質量%以上,更佳為8質量%以上,進而較佳為10質量%以上,較佳為30質量%以下,更佳為25質量%以下,進而較佳為20質量%以下。
[15]如上述[14]之口腔用組合物,其中糖醇較佳為碳數4~12者,為選自山梨糖醇、甘露醇、木糖醇、赤蘚醇、異麥芽酮糖醇、乳糖醇、麥芽糖醇之1種或2種以上,又,較佳為選自赤蘚醇、木糖醇、麥芽糖醇、及異麥芽酮糖醇之1種或2種以上,又,較佳為山梨糖醇。
[16]如上述[1]至[15]之口腔用組合物,其中陰離子性界面活性劑較佳為除不可避免地混入之情形以外不含有,或者較佳為含有超過0質量%且為1質量%以下,更佳為含有0.7質量%以下。
[17]如上述[1]至[16]之口腔用組合物,其中除成分(D)、陰離子性界面活性劑、及兩性界面活性劑以外之界面活性劑較佳為含有0.5質量%以下,更佳為含有0.1質量%以下,較佳為除不可避免地混入之情形以外不含有除成分(D)、陰離子性界面活性劑、及兩性界面活性劑以外之界面活性劑。
[18]如上述[1]至[17]之口腔用組合物,其較佳為液體口腔用組合物,更佳為漱口劑、液狀潔牙劑、水潔牙劑、口腔噴劑、或含漱劑。
[19]如上述[1]至[18]之口腔用組合物,其用於抑制牙垢形成。
[20]如上述[1]至[18]之口腔用組合物,其用於抑制口臭。
[21]如上述[1]至[18]之口腔用組合物,其用於抑制齲齒或預防齲齒。
[22]一種如上述[1]至[18]之口腔用組合物之用途,其用以抑制牙垢形成。
[23]一種如上述[1]至[18]之口腔用組合物之用途,其用以抑制口臭。
[24]一種如上述[1]至[18]之口腔用組合物之用途,其用以抑制或預防齲齒。
以下,根據實施例對本發明進行具體說明。再者,只要表中未特別表示,則各成分之含量表示質量%。
[製造例1]α,β-月桂基半乳糖苷之製造
於觸媒量之對甲苯磺酸一水合物存在下,於加熱、減壓條件下,使D-半乳糖與月桂醇一面脫水一面進行反應。將所得之混合物藉由矽膠管柱進行純化,獲得半乳糖縮合度1~3之月桂基半乳糖苷。藉由凝膠滲透層析法、氣相層析法、1H-NMR(1H-nuclear magnetic resonance,氫核磁共振波譜法)進行分析,結果所得之月桂基半乳糖苷之半乳糖之平均縮合度為1.48,成分中之月桂基單半乳糖苷之組成為吡喃糖苷/呋喃糖苷=83/17,其中吡喃糖苷之α/β比為75/25。將其作為α,β-月桂基半乳糖苷而使用。
[製造例2]α,β-辛基半乳糖苷之製造
以與製造例1同樣之方式,將辛醇作為原料,製造α,β-辛基半乳糖苷。
[製造例3]α,β-2-乙基己基半乳糖苷之製造
於觸媒量之對甲苯磺酸一水合物存在下,於加熱、減壓條件下,使D-半乳糖與2-乙基己醇一面脫水一面進行反應。反應後,加入
氫氧化鈉水溶液中和觸媒,藉由過濾自所得之混合物去除未反應之D-半乳糖。將未反應之醇於減壓下自濾液蒸餾去除,藉此獲得2-乙基己基半乳糖苷。藉由凝膠滲透層析法、氣相層析法、1H-NMR進行分析,結果所得之2-乙基己基半乳糖苷之半乳糖之平均縮合度為1.16,組合物中之單半乳糖苷之組成為吡喃糖苷/呋喃糖苷=40/60,其中吡喃糖苷之α/β比為70/30。將其作為α,β-2-乙基己基半乳糖苷而使用。
[製造例4]α,β-癸基半乳糖苷之製造
除將製造例3之2-乙基己醇變更為癸醇異構物混合物(癸醇,協和醱酵化學(股))以外,根據製造例3而獲得癸基半乳糖苷。所得之癸基半乳糖苷之半乳糖之平均縮合度為1.17,組合物中之單半乳糖苷之組成為吡喃糖苷/呋喃糖苷=46/54,其中吡喃糖苷之α/β比為67/33。將其作為α,β-癸基半乳糖苷而使用。
[製造例5]異癸基半乳糖苷之製造
除將製造例3之2-乙基己醇變更為異癸醇(協和醱酵化學(股))以外,根據製造例3而獲得異癸基半乳糖苷。所得之異癸基半乳糖苷之半乳糖之平均縮合度為1.14。將其作為異癸基半乳糖苷而使用。
[實施例1~11,比較例1~3]
適當使用製造例1~5中所得之化合物作為成分(A),根據表1所示之配方製備口腔用組合物。使用所得之口腔用組合物,根據下述方法對成分(A)之溶解性進行評價。
將結果示於表1。
[試驗例1:溶解性之評價]
藉由目視觀察所得之組合物,根據下述基準進行評價。
A:未觀察到成分(A)之分離或不溶物,具有均勻之透明感。
B:未觀察到成分(A)之分離或不溶物,但輕微白濁。
C:確認有成分(A)之分離或不溶物。
[試驗例2:陽離子性殺菌劑向牙齒之吸附量之評價]
使用作為琺瑯質之主成分之羥磷石灰(Hap)粉末(太平化學產業;以下簡稱Hap)作為牙齒之模型。將10mg之Hap於表1所示之各組合物1mL中浸漬30秒後,利用離子交換水2mL洗淨,於下述高效液相層析法之條件下對藉由以下之流動相萃取吸附於Hap之殺菌劑而得者進行測定,算出吸附量。
(苄索氯銨)
流動相:離子交換水35%、乙腈65%、烷基硫酸鈉0.03mol/L、過氯酸鈉0.1mol/L
管柱:ODS管柱(Octadecylsilyl,十八烷基矽烷):Superspher100(關東化學製)
流速:1mL/min
測定波長:210nm
溫度:40℃
(西吡氯銨)
流動相:離子交換水25%、甲醇75%、過氯酸鈉0.05mol/L
管柱:CAPCELL PAK(SCX)(資生堂製)
流速:1.2mL/min
測定波長:260nm
溫度:40℃
根據表1之結果,併用特定量之成分(A)及陽離子性殺菌劑之實施例1~11提高成分(A)之溶解性並且有效地提高陽離子性殺菌劑向牙齒之吸附性,與此相對,未使用成分(A)之比較例1、未使用陽離子性殺菌劑之比較例2、及併用兩者但成分(A)超過特定量之比較例3無法充分兼備提高成分(A)之溶解性之效果與提高陽離子性殺菌劑向牙齒之吸附性之效果。
[實施例12~26、比較例4~9]
適當使用製造例1~5中所得之化合物作為成分(A),根據表2~3所示之配方製備口腔用組合物。使用所得之口腔用組合物,以與實施例1同樣之方式,對成分(A)之溶解性進行評價。
將結果示於表2~3。
根據表2~3之結果,以特定之量使用陽離子性殺菌劑之實施例12~26之成分(A)之溶解性優異,與此相對,代替陽離子性殺菌劑而使用非離子性殺菌劑之比較例4~9無法溶解成分(A)。
[實施例27~50、比較例10~16]
適當使用製造例1~5中所得之化合物作為成分(A),根據表4~6所示之配方製備口腔用組合物。使用所得之口腔用組合物,以與試驗例1同樣之方式對成分(A)之溶解性進行評價,並且根據下述方法對共凝聚抑制效果進行評價。
將結果示於表4~6。
[試驗例3:共凝聚抑制效果之評價]
(1)使用菌株
作為細梭菌屬細菌而使用具核細梭菌F-1株(以下稱為F-1菌)。作為共凝聚反應之對象細菌,使用作為齲齒病原菌之遠緣鏈球菌B13株(以下稱為Ss菌)。
(2)共凝聚測定法
Ss菌係於腦心浸出物(brain heart infusion)液體培養基中植菌後,於37℃之厭氧條件下培養20小時。F-1菌係於GAM肉汁(bouillon)液體培養基中植菌後,於37℃之厭氧條件下培養20小時。培養結束後,利用離心分離而集菌,以pH值8.0之共凝聚用緩衝液(1mM三(羥基甲基)胺基甲烷、0.1mM氯化鈣、0.1mM氯化鎂、0.15M氯化鈉)洗淨2次。洗淨後,利用共凝聚用緩衝液將F-1菌於600nm之波長下之濁度(OD:UV-1600、UV-Visible spectrophotometer(島津製作所(股)))調整為0.25,將Ss菌於600nm之波長下之濁度調整為0.9,而獲得菌懸濁液。該共凝聚用緩衝液代替表3~5所示之成分(C)之水而使用。於試驗中,使用圓底96孔微盤(TPP公司),將任一之F-1菌懸濁液100μL、Ss菌懸濁液50μL及表3~5所示之口腔用組合物50μL依序混合。於室
溫下靜置一晝夜後,將未確認到凝聚塊之沈澱者評價為有共凝聚抑制效果(+),將確認有凝聚塊之沈澱者評價為無共凝聚抑制效果(-)。
根據表4~6之結果可知,為了使成分(A)溶解而含有過量之成分(D)非離子界面活性劑之比較例10~16之共凝聚抑制效果失活,與此相對,藉由於成分(A)中併用特定量之成分(B)陽離子性殺菌劑而提高成分(A)之溶解性的實施例27~50可減少成分(D)非離子性殺菌劑之含量,結果可發揮良好之共凝聚抑制效果。
[實施例51]
作為液體組合物,獲得以下之漱口液或液體潔牙劑。
Claims (7)
- 一種口腔用組合物,其含有以下之成分(A)、(B)、及(C):(A)由下述式(I):(式中,R表示可經取代之碳數8~18之直鏈或支鏈狀之烷基,G表示半乳糖殘基,E表示氫原子或甲基,m表示0~200之整數,n表示1~30之整數)表示之化合物0.001質量%以上1質量%以下、(B)陽離子性殺菌劑0.001質量%以上0.1質量%以下、及(C)水35質量%以上,成分(B)係選自西吡氯銨、苄索氯銨、氯化苄烷銨、葡萄糖酸洛赫西定、及鹽酸洛赫西定之1種或2種以上,且成分(A)之含量與成分(B)之含量之質量比((A)/(B))為2以上100以下。
- 如請求項1之口腔用組合物,其進而含有成分(D)非離子性界面活性劑0.1質量%以上1.5質量%以下。
- 如請求項2之口腔用組合物,其中成分(A)及成分(B)之合計含量與成分(D)之含量之質量比({(A)+(B)}/(D))為0.02以上2以下。
- 如請求項2之口腔用組合物,其中成分(D)係選自聚氧乙烯氫化菌麻油、聚氧乙烯山梨醇酐脂肪酸酯、聚甘油脂肪酸酯、聚氧乙烯烷基醚、烷基聚葡糖苷及蔗糖脂肪酸酯之1種或2種以上。
- 如請求項1或2之口腔用組合物,其為液體口腔用組合物。
- 如請求項1或2之口腔用組合物,其用於抑制牙垢形成。
- 如請求項1或2之口腔用組合物,其用於抑制口臭。
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AU2018237806B2 (en) | 2017-03-21 | 2022-11-24 | Well Stone Co. | Method for producing oral composition, and oral composition |
JP6955974B2 (ja) * | 2017-11-20 | 2021-10-27 | 花王株式会社 | 泡吐出容器入り液体口腔用組成物 |
JP7023161B2 (ja) * | 2018-04-03 | 2022-02-21 | 花王株式会社 | 液体口腔用組成物 |
WO2022071457A1 (ja) * | 2020-09-30 | 2022-04-07 | サンスター スイス エスエー | プラーク形成抑制用組成物 |
Family Cites Families (15)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4279888A (en) | 1978-12-29 | 1981-07-21 | Lion Corporation | Oral composition |
US5409902A (en) * | 1991-12-31 | 1995-04-25 | Lever Brothers Company | Oral hygiene compositions containing glyceroglycolipids as antiplaque compounds |
US5624906A (en) | 1994-12-08 | 1997-04-29 | Lever Brothers Company, Division Of Conopco, Inc. | Oral hygiene compositions comprising heteroatom containing alkyl aldonamide compounds |
GB9611364D0 (en) | 1996-05-31 | 1996-08-07 | Smithkline Beecham Plc | Composition |
JP3681108B2 (ja) * | 2000-12-08 | 2005-08-10 | サンスター株式会社 | カチオン性殺菌剤を含む口腔用組成物 |
CA2365481C (en) * | 2001-12-18 | 2006-01-03 | Ibm Canada Limited-Ibm Canada Limitee | Encryption method using synchronized continuously calculated pseudo-random key |
WO2006035821A1 (ja) * | 2004-09-29 | 2006-04-06 | Kao Corporation | 口腔用組成物 |
JP4210679B2 (ja) | 2004-09-29 | 2009-01-21 | 花王株式会社 | 口腔用組成物 |
WO2006043621A1 (ja) | 2004-10-20 | 2006-04-27 | Kao Corporation | 液体口腔用組成物 |
JPWO2007066497A1 (ja) | 2005-12-09 | 2009-05-14 | ライオン株式会社 | 歯磨組成物 |
JP4950728B2 (ja) | 2006-03-28 | 2012-06-13 | 花王株式会社 | 口腔用組成物 |
JP4950727B2 (ja) * | 2006-03-28 | 2012-06-13 | 花王株式会社 | 口腔用組成物 |
JP4950726B2 (ja) | 2006-03-28 | 2012-06-13 | 花王株式会社 | 口腔用組成物 |
US8999298B2 (en) | 2008-01-17 | 2015-04-07 | National University Corporation Okayama University | Dental oral composition |
JP5620119B2 (ja) | 2010-02-15 | 2014-11-05 | ライオン株式会社 | 非希釈液体口腔用組成物及びその使用方法 |
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- 2013-12-27 WO PCT/JP2013/085242 patent/WO2015097899A1/ja active Application Filing
- 2013-12-27 JP JP2014517315A patent/JP5593469B1/ja active Active
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EP3090728A4 (en) | 2017-08-09 |
JPWO2015097899A1 (ja) | 2017-03-23 |
EP3090728B1 (en) | 2019-04-17 |
RU2671835C2 (ru) | 2018-11-07 |
CN105792809A (zh) | 2016-07-20 |
TW201529091A (zh) | 2015-08-01 |
JP5593469B1 (ja) | 2014-09-24 |
CN105792809B (zh) | 2020-03-10 |
WO2015097899A1 (ja) | 2015-07-02 |
EP3090728A1 (en) | 2016-11-09 |
US10307358B2 (en) | 2019-06-04 |
US20160324748A1 (en) | 2016-11-10 |
RU2016130613A (ru) | 2018-02-01 |
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