JP2022010431A - Oral composition - Google Patents
Oral composition Download PDFInfo
- Publication number
- JP2022010431A JP2022010431A JP2020111032A JP2020111032A JP2022010431A JP 2022010431 A JP2022010431 A JP 2022010431A JP 2020111032 A JP2020111032 A JP 2020111032A JP 2020111032 A JP2020111032 A JP 2020111032A JP 2022010431 A JP2022010431 A JP 2022010431A
- Authority
- JP
- Japan
- Prior art keywords
- bitterness
- component
- oral composition
- oil
- berberine
- 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.)
- Granted
Links
- 239000000203 mixture Substances 0.000 title claims abstract description 59
- YBHILYKTIRIUTE-UHFFFAOYSA-N berberine Chemical compound C1=C2CC[N+]3=CC4=C(OC)C(OC)=CC=C4C=C3C2=CC2=C1OCO2 YBHILYKTIRIUTE-UHFFFAOYSA-N 0.000 claims abstract description 28
- 229940093265 berberine Drugs 0.000 claims abstract description 28
- QISXPYZVZJBNDM-UHFFFAOYSA-N berberine Natural products COc1ccc2C=C3N(Cc2c1OC)C=Cc4cc5OCOc5cc34 QISXPYZVZJBNDM-UHFFFAOYSA-N 0.000 claims abstract description 28
- ZBJCYZPANVLBRK-UHFFFAOYSA-N Menthone 1,2-glyceryl ketal Chemical compound CC(C)C1CCC(C)CC11OC(CO)CO1 ZBJCYZPANVLBRK-UHFFFAOYSA-N 0.000 claims abstract description 14
- VDDMIRWMCRUXJE-UHFFFAOYSA-N CC(C)C(C(C)CC(C)C1)C1C(NC(C=C1)=CC=C1OC)=O Chemical compound CC(C)C(C(C)CC(C)C1)C1C(NC(C=C1)=CC=C1OC)=O VDDMIRWMCRUXJE-UHFFFAOYSA-N 0.000 claims abstract description 11
- 239000002736 nonionic surfactant Substances 0.000 claims abstract description 11
- 241000972672 Phellodendron Species 0.000 claims description 14
- 239000007788 liquid Substances 0.000 claims description 12
- 239000000419 plant extract Substances 0.000 claims description 12
- 241000037740 Coptis chinensis Species 0.000 claims description 8
- 235000019658 bitter taste Nutrition 0.000 abstract description 59
- 206010013911 Dysgeusia Diseases 0.000 abstract description 17
- 208000028169 periodontal disease Diseases 0.000 abstract description 7
- 208000034619 Gingival inflammation Diseases 0.000 abstract description 6
- 230000001629 suppression Effects 0.000 abstract description 3
- 230000002265 prevention Effects 0.000 abstract description 2
- -1 fatty acid esters Chemical class 0.000 description 29
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 21
- 239000000284 extract Substances 0.000 description 21
- 239000000796 flavoring agent Substances 0.000 description 15
- 235000019634 flavors Nutrition 0.000 description 15
- 230000000694 effects Effects 0.000 description 13
- 239000000194 fatty acid Substances 0.000 description 13
- 239000003205 fragrance Substances 0.000 description 13
- 239000003921 oil Substances 0.000 description 13
- 235000019198 oils Nutrition 0.000 description 13
- 229920003171 Poly (ethylene oxide) Polymers 0.000 description 12
- 235000014113 dietary fatty acids Nutrition 0.000 description 12
- 229930195729 fatty acid Natural products 0.000 description 12
- 238000002156 mixing Methods 0.000 description 12
- 239000002324 mouth wash Substances 0.000 description 10
- 229940051866 mouthwash Drugs 0.000 description 10
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 9
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 9
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 9
- 235000019441 ethanol Nutrition 0.000 description 8
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 7
- 239000004359 castor oil Substances 0.000 description 7
- 235000019438 castor oil Nutrition 0.000 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 description 7
- 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 6
- 239000004480 active ingredient Substances 0.000 description 6
- 239000003795 chemical substances by application Substances 0.000 description 6
- 230000000052 comparative effect Effects 0.000 description 6
- 239000011734 sodium Substances 0.000 description 6
- 229910052708 sodium Inorganic materials 0.000 description 6
- 238000000034 method Methods 0.000 description 5
- 239000000843 powder Substances 0.000 description 5
- 239000002994 raw material Substances 0.000 description 5
- 150000003839 salts Chemical class 0.000 description 5
- NOOLISFMXDJSKH-UTLUCORTSA-N (+)-Neomenthol Chemical compound CC(C)[C@@H]1CC[C@@H](C)C[C@@H]1O NOOLISFMXDJSKH-UTLUCORTSA-N 0.000 description 4
- KWIUHFFTVRNATP-UHFFFAOYSA-N Betaine Natural products C[N+](C)(C)CC([O-])=O KWIUHFFTVRNATP-UHFFFAOYSA-N 0.000 description 4
- NOOLISFMXDJSKH-UHFFFAOYSA-N DL-menthol Natural products CC(C)C1CCC(C)CC1O NOOLISFMXDJSKH-UHFFFAOYSA-N 0.000 description 4
- VUNOFAIHSALQQH-UHFFFAOYSA-N Ethyl menthane carboxamide Chemical compound CCNC(=O)C1CC(C)CCC1C(C)C VUNOFAIHSALQQH-UHFFFAOYSA-N 0.000 description 4
- 230000003110 anti-inflammatory effect Effects 0.000 description 4
- 229960003237 betaine Drugs 0.000 description 4
- 230000035597 cooling sensation Effects 0.000 description 4
- 238000011156 evaluation Methods 0.000 description 4
- 235000011187 glycerol Nutrition 0.000 description 4
- 239000001525 mentha piperita l. herb oil Substances 0.000 description 4
- 229940041616 menthol Drugs 0.000 description 4
- 210000000214 mouth Anatomy 0.000 description 4
- 235000019477 peppermint oil Nutrition 0.000 description 4
- FSYKKLYZXJSNPZ-UHFFFAOYSA-N sarcosine Chemical compound C[NH2+]CC([O-])=O FSYKKLYZXJSNPZ-UHFFFAOYSA-N 0.000 description 4
- 239000007787 solid Substances 0.000 description 4
- 239000002904 solvent Substances 0.000 description 4
- 150000005846 sugar alcohols Polymers 0.000 description 4
- 239000004094 surface-active agent Substances 0.000 description 4
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 3
- QMMFVYPAHWMCMS-UHFFFAOYSA-N Dimethyl sulfide Chemical compound CSC QMMFVYPAHWMCMS-UHFFFAOYSA-N 0.000 description 3
- 241000196324 Embryophyta Species 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
- 235000019596 Masking bitterness Nutrition 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
- 239000002280 amphoteric surfactant Substances 0.000 description 3
- 235000015165 citric acid Nutrition 0.000 description 3
- 150000004665 fatty acids Chemical class 0.000 description 3
- 230000001771 impaired effect Effects 0.000 description 3
- 239000003112 inhibitor Substances 0.000 description 3
- 230000007794 irritation Effects 0.000 description 3
- XMGQYMWWDOXHJM-UHFFFAOYSA-N limonene Chemical compound CC(=C)C1CCC(C)=CC1 XMGQYMWWDOXHJM-UHFFFAOYSA-N 0.000 description 3
- OSWPMRLSEDHDFF-UHFFFAOYSA-N methyl salicylate Chemical compound COC(=O)C1=CC=CC=C1O OSWPMRLSEDHDFF-UHFFFAOYSA-N 0.000 description 3
- 235000019629 palatability Nutrition 0.000 description 3
- 235000013772 propylene glycol Nutrition 0.000 description 3
- 239000008213 purified water Substances 0.000 description 3
- 239000000080 wetting agent Substances 0.000 description 3
- 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 2
- MBDOYVRWFFCFHM-SNAWJCMRSA-N (2E)-hexenal Chemical compound CCC\C=C\C=O MBDOYVRWFFCFHM-SNAWJCMRSA-N 0.000 description 2
- WRMNZCZEMHIOCP-UHFFFAOYSA-N 2-phenylethanol Chemical compound OCCC1=CC=CC=C1 WRMNZCZEMHIOCP-UHFFFAOYSA-N 0.000 description 2
- JHWFWLUAUPZUCP-UHFFFAOYSA-N 3-Ethyl-2-hydroxycyclopent-2-en-1-one Chemical compound CCC1=C(O)C(=O)CC1 JHWFWLUAUPZUCP-UHFFFAOYSA-N 0.000 description 2
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 description 2
- XDEGQMQKHFPBEW-UHFFFAOYSA-N Angelicasaeure-isobutylester Natural products CC=C(C)C(=O)OCC(C)C XDEGQMQKHFPBEW-UHFFFAOYSA-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
- 235000004936 Bromus mango Nutrition 0.000 description 2
- 235000005979 Citrus limon Nutrition 0.000 description 2
- 244000131522 Citrus pyriformis Species 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
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 2
- XDEGQMQKHFPBEW-YVMONPNESA-N Isobutyl angelate Chemical compound C\C=C(\C)C(=O)OCC(C)C XDEGQMQKHFPBEW-YVMONPNESA-N 0.000 description 2
- 102100037644 Kelch-like protein 41 Human genes 0.000 description 2
- 108050003242 Kelch-like protein 41 Proteins 0.000 description 2
- 235000014826 Mangifera indica Nutrition 0.000 description 2
- 240000007228 Mangifera indica Species 0.000 description 2
- 235000006679 Mentha X verticillata Nutrition 0.000 description 2
- 235000002899 Mentha suaveolens Nutrition 0.000 description 2
- 235000001636 Mentha x rotundifolia Nutrition 0.000 description 2
- LRHPLDYGYMQRHN-UHFFFAOYSA-N N-Butanol Chemical compound CCCCO LRHPLDYGYMQRHN-UHFFFAOYSA-N 0.000 description 2
- 241000972673 Phellodendron amurense Species 0.000 description 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 description 2
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 2
- 235000009184 Spondias indica Nutrition 0.000 description 2
- TVXBFESIOXBWNM-UHFFFAOYSA-N Xylitol Natural products OCCC(O)C(O)C(O)CCO TVXBFESIOXBWNM-UHFFFAOYSA-N 0.000 description 2
- 235000006886 Zingiber officinale Nutrition 0.000 description 2
- 244000273928 Zingiber officinale Species 0.000 description 2
- 239000012190 activator Substances 0.000 description 2
- 150000005215 alkyl ethers Chemical class 0.000 description 2
- 239000003945 anionic surfactant Substances 0.000 description 2
- 230000000844 anti-bacterial effect Effects 0.000 description 2
- CUFNKYGDVFVPHO-UHFFFAOYSA-N azulene Chemical compound 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
- 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 description 2
- 229960001950 benzethonium chloride Drugs 0.000 description 2
- 239000003093 cationic surfactant Substances 0.000 description 2
- 229960001927 cetylpyridinium chloride Drugs 0.000 description 2
- YMKDRGPMQRFJGP-UHFFFAOYSA-M cetylpyridinium chloride Chemical compound [Cl-].CCCCCCCCCCCCCCCC[N+]1=CC=CC=C1 YMKDRGPMQRFJGP-UHFFFAOYSA-M 0.000 description 2
- 239000003086 colorant Substances 0.000 description 2
- HCRBXQFHJMCTLF-ZCFIWIBFSA-N ethyl (2r)-2-methylbutanoate Chemical compound CCOC(=O)[C@H](C)CC HCRBXQFHJMCTLF-ZCFIWIBFSA-N 0.000 description 2
- LZCLXQDLBQLTDK-UHFFFAOYSA-N ethyl 2-hydroxypropanoate Chemical compound CCOC(=O)C(C)O LZCLXQDLBQLTDK-UHFFFAOYSA-N 0.000 description 2
- RRAFCDWBNXTKKO-UHFFFAOYSA-N eugenol Chemical compound COC1=CC(CC=C)=CC=C1O RRAFCDWBNXTKKO-UHFFFAOYSA-N 0.000 description 2
- 235000003599 food sweetener Nutrition 0.000 description 2
- 235000008397 ginger Nutrition 0.000 description 2
- JARKCYVAAOWBJS-UHFFFAOYSA-N hexanal Chemical compound CCCCCC=O JARKCYVAAOWBJS-UHFFFAOYSA-N 0.000 description 2
- AOGQPLXWSUTHQB-UHFFFAOYSA-N hexyl acetate Chemical compound CCCCCCOC(C)=O AOGQPLXWSUTHQB-UHFFFAOYSA-N 0.000 description 2
- 239000004615 ingredient Substances 0.000 description 2
- MLFHJEHSLIIPHL-UHFFFAOYSA-N isoamyl acetate Chemical compound CC(C)CCOC(C)=O MLFHJEHSLIIPHL-UHFFFAOYSA-N 0.000 description 2
- PHTQWCKDNZKARW-UHFFFAOYSA-N isoamylol Chemical compound CC(C)CCO PHTQWCKDNZKARW-UHFFFAOYSA-N 0.000 description 2
- ZYTMANIQRDEHIO-KXUCPTDWSA-N isopulegol Chemical compound C[C@@H]1CC[C@@H](C(C)=C)[C@H](O)C1 ZYTMANIQRDEHIO-KXUCPTDWSA-N 0.000 description 2
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 description 2
- UWKAYLJWKGQEPM-LBPRGKRZSA-N linalyl acetate Chemical compound CC(C)=CCC[C@](C)(C=C)OC(C)=O UWKAYLJWKGQEPM-LBPRGKRZSA-N 0.000 description 2
- 230000000873 masking effect Effects 0.000 description 2
- 239000000463 material Substances 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
- VAMXMNNIEUEQDV-UHFFFAOYSA-N methyl anthranilate Chemical compound COC(=O)C1=CC=CC=C1N VAMXMNNIEUEQDV-UHFFFAOYSA-N 0.000 description 2
- 239000003960 organic solvent Substances 0.000 description 2
- NPKKRSHVJIQBKU-UHFFFAOYSA-N ornogenin Natural products CC(OC(=O)C=Cc1ccccc1)C2(O)CCC3(O)C4(O)CC=C5CC(O)CCC5(C)C4CC(OC(=O)C=Cc6ccccc6)C23C NPKKRSHVJIQBKU-UHFFFAOYSA-N 0.000 description 2
- 239000003002 pH adjusting agent Substances 0.000 description 2
- FGIUAXJPYTZDNR-UHFFFAOYSA-N potassium nitrate Chemical compound [K+].[O-][N+]([O-])=O FGIUAXJPYTZDNR-UHFFFAOYSA-N 0.000 description 2
- 229940085605 saccharin sodium Drugs 0.000 description 2
- 239000001509 sodium citrate Substances 0.000 description 2
- NLJMYIDDQXHKNR-UHFFFAOYSA-K sodium citrate Chemical compound O.O.[Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O NLJMYIDDQXHKNR-UHFFFAOYSA-K 0.000 description 2
- PUZPDOWCWNUUKD-UHFFFAOYSA-M sodium fluoride Chemical compound [F-].[Na+] PUZPDOWCWNUUKD-UHFFFAOYSA-M 0.000 description 2
- 239000000243 solution Substances 0.000 description 2
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- URAYPUMNDPQOKB-UHFFFAOYSA-N triacetin Chemical compound CC(=O)OCC(OC(C)=O)COC(C)=O URAYPUMNDPQOKB-UHFFFAOYSA-N 0.000 description 2
- IAEGWXHKWJGQAZ-UHFFFAOYSA-N trimethylpyrazine Chemical compound CC1=CN=C(C)C(C)=N1 IAEGWXHKWJGQAZ-UHFFFAOYSA-N 0.000 description 2
- 239000000811 xylitol Substances 0.000 description 2
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- JIAARYAFYJHUJI-UHFFFAOYSA-L zinc dichloride Chemical compound [Cl-].[Cl-].[Zn+2] JIAARYAFYJHUJI-UHFFFAOYSA-L 0.000 description 2
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- WEEGYLXZBRQIMU-UHFFFAOYSA-N 1,8-cineole Natural products C1CC2CCC1(C)OC2(C)C WEEGYLXZBRQIMU-UHFFFAOYSA-N 0.000 description 1
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- XGRSAFKZAGGXJV-UHFFFAOYSA-N 3-azaniumyl-3-cyclohexylpropanoate Chemical compound OC(=O)CC(N)C1CCCCC1 XGRSAFKZAGGXJV-UHFFFAOYSA-N 0.000 description 1
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- AXCXHFKZHDEKTP-NSCUHMNNSA-N 4-methoxycinnamaldehyde Chemical compound COC1=CC=C(\C=C\C=O)C=C1 AXCXHFKZHDEKTP-NSCUHMNNSA-N 0.000 description 1
- SATQWIIUJKWZNO-UHFFFAOYSA-N 5-(3,3-dimethyloxiran-2-yl)-3-methylpent-1-en-3-ol Chemical compound C=CC(O)(C)CCC1OC1(C)C SATQWIIUJKWZNO-UHFFFAOYSA-N 0.000 description 1
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- TWXUTZNBHUWMKJ-UHFFFAOYSA-N Allyl cyclohexylpropionate Chemical compound C=CCOC(=O)CCC1CCCCC1 TWXUTZNBHUWMKJ-UHFFFAOYSA-N 0.000 description 1
- 244000144730 Amygdalus persica Species 0.000 description 1
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- 239000001738 pogostemon cablin oil Substances 0.000 description 1
- 229920001223 polyethylene glycol Polymers 0.000 description 1
- 229920000642 polymer Polymers 0.000 description 1
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- 239000001267 polyvinylpyrrolidone Substances 0.000 description 1
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- 239000004323 potassium nitrate Substances 0.000 description 1
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- 239000000901 saccharin and its Na,K and Ca salt Substances 0.000 description 1
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- 239000011780 sodium chloride Substances 0.000 description 1
- 235000013758 sodium copper chlorophyllin Nutrition 0.000 description 1
- 229940079841 sodium copper chlorophyllin Drugs 0.000 description 1
- 229940080264 sodium dodecylbenzenesulfonate Drugs 0.000 description 1
- 239000011775 sodium fluoride Substances 0.000 description 1
- 235000013024 sodium fluoride Nutrition 0.000 description 1
- 229940075560 sodium lauryl sulfoacetate Drugs 0.000 description 1
- 235000019333 sodium laurylsulphate Nutrition 0.000 description 1
- 229960004711 sodium monofluorophosphate Drugs 0.000 description 1
- 229950005425 sodium myristyl sulfate Drugs 0.000 description 1
- 235000019830 sodium polyphosphate Nutrition 0.000 description 1
- UAJTZZNRJCKXJN-UHFFFAOYSA-M sodium;2-dodecoxy-2-oxoethanesulfonate Chemical compound [Na+].CCCCCCCCCCCCOC(=O)CS([O-])(=O)=O UAJTZZNRJCKXJN-UHFFFAOYSA-M 0.000 description 1
- UPUIQOIQVMNQAP-UHFFFAOYSA-M sodium;tetradecyl sulfate Chemical compound [Na+].CCCCCCCCCCCCCCOS([O-])(=O)=O UPUIQOIQVMNQAP-UHFFFAOYSA-M 0.000 description 1
- 230000003381 solubilizing effect Effects 0.000 description 1
- 235000019721 spearmint oil Nutrition 0.000 description 1
- 238000010186 staining Methods 0.000 description 1
- ANOBYBYXJXCGBS-UHFFFAOYSA-L stannous fluoride Chemical compound F[Sn]F ANOBYBYXJXCGBS-UHFFFAOYSA-L 0.000 description 1
- 229960002799 stannous fluoride Drugs 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 229910001631 strontium chloride Inorganic materials 0.000 description 1
- AHBGXTDRMVNFER-UHFFFAOYSA-L strontium dichloride Chemical compound [Cl-].[Cl-].[Sr+2] AHBGXTDRMVNFER-UHFFFAOYSA-L 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 description 1
- 235000019408 sucralose Nutrition 0.000 description 1
- BAQAVOSOZGMPRM-QBMZZYIRSA-N sucralose Chemical compound O[C@@H]1[C@@H](O)[C@@H](Cl)[C@@H](CO)O[C@@H]1O[C@@]1(CCl)[C@@H](O)[C@H](O)[C@@H](CCl)O1 BAQAVOSOZGMPRM-QBMZZYIRSA-N 0.000 description 1
- 239000005720 sucrose Substances 0.000 description 1
- BDHFUVZGWQCTTF-UHFFFAOYSA-M sulfonate Chemical compound [O-]S(=O)=O BDHFUVZGWQCTTF-UHFFFAOYSA-M 0.000 description 1
- 150000003871 sulfonates Chemical class 0.000 description 1
- 239000011975 tartaric acid Substances 0.000 description 1
- 235000002906 tartaric acid Nutrition 0.000 description 1
- 235000019640 taste Nutrition 0.000 description 1
- 239000010678 thyme oil Substances 0.000 description 1
- 239000001585 thymus vulgaris Substances 0.000 description 1
- UAXOELSVPTZZQG-UHFFFAOYSA-N tiglic acid Natural products CC(C)=C(C)C(O)=O UAXOELSVPTZZQG-UHFFFAOYSA-N 0.000 description 1
- 229940042585 tocopherol acetate Drugs 0.000 description 1
- GYDJEQRTZSCIOI-LJGSYFOKSA-N tranexamic acid Chemical compound NC[C@H]1CC[C@H](C(O)=O)CC1 GYDJEQRTZSCIOI-LJGSYFOKSA-N 0.000 description 1
- 229960000401 tranexamic acid Drugs 0.000 description 1
- MBDOYVRWFFCFHM-UHFFFAOYSA-N trans-2-hexenal Natural products CCCC=CC=O MBDOYVRWFFCFHM-UHFFFAOYSA-N 0.000 description 1
- 229960002622 triacetin Drugs 0.000 description 1
- 229960003500 triclosan Drugs 0.000 description 1
- VXYADVIJALMOEQ-UHFFFAOYSA-K tris(lactato)aluminium Chemical compound CC(O)C(=O)O[Al](OC(=O)C(C)O)OC(=O)C(C)O VXYADVIJALMOEQ-UHFFFAOYSA-K 0.000 description 1
- CCXAYLQLOLXXKE-DWJAGBRCSA-K trisodium;(2s,3s,4s,5r,6r)-6-[(2s,3r,4s,5s,6s)-2-[[(3s,4ar,6ar,6bs,8as,11s,12ar,14ar,14bs)-11-carboxylato-4,4,6a,6b,8a,11,14b-heptamethyl-14-oxo-2,3,4a,5,6,7,8,9,10,12,12a,14a-dodecahydro-1h-picen-3-yl]oxy]-6-carboxylato-4,5-dihydroxyoxan-3-yl]oxy-3,4,5-t Chemical compound [Na+].[Na+].[Na+].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 CCXAYLQLOLXXKE-DWJAGBRCSA-K 0.000 description 1
- WGIWBXUNRXCYRA-UHFFFAOYSA-H trizinc;2-hydroxypropane-1,2,3-tricarboxylate Chemical compound [Zn+2].[Zn+2].[Zn+2].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O.[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O WGIWBXUNRXCYRA-UHFFFAOYSA-H 0.000 description 1
- MWOOGOJBHIARFG-UHFFFAOYSA-N vanillin Chemical compound COC1=CC(C=O)=CC=C1O MWOOGOJBHIARFG-UHFFFAOYSA-N 0.000 description 1
- FGQOOHJZONJGDT-UHFFFAOYSA-N vanillin Natural products COC1=CC(O)=CC(C=O)=C1 FGQOOHJZONJGDT-UHFFFAOYSA-N 0.000 description 1
- 235000012141 vanillin Nutrition 0.000 description 1
- 229940088594 vitamin Drugs 0.000 description 1
- 239000011782 vitamin Substances 0.000 description 1
- 229930003231 vitamin Natural products 0.000 description 1
- 235000013343 vitamin Nutrition 0.000 description 1
- 229940011671 vitamin b6 Drugs 0.000 description 1
- 239000009637 wintergreen oil Substances 0.000 description 1
- 239000011592 zinc chloride Substances 0.000 description 1
- 235000005074 zinc chloride Nutrition 0.000 description 1
- 239000011746 zinc citrate Substances 0.000 description 1
- 235000006076 zinc citrate Nutrition 0.000 description 1
- 229940068475 zinc citrate Drugs 0.000 description 1
- 239000004711 α-olefin Substances 0.000 description 1
Landscapes
- Cosmetics (AREA)
Abstract
Description
本発明は、ベルベリン由来の苦味が改善し、使用後においても苦味が軽減し、かつスッキリとした使用感を与え、後味が良く、歯肉炎等の歯周病の予防又は抑制用として好適な口腔用組成物に関する。 INDUSTRIAL APPLICABILITY The present invention improves the bitterness derived from berberine, reduces the bitterness even after use, gives a refreshing feeling of use, has a good aftertaste, and is suitable for prevention or suppression of periodontal diseases such as gingival inflammation. Regarding the composition for use.
従来、口腔用組成物には、口腔内の不具合を予防又は治療する目的で種々の有効成分が配合されており、中でもベルベリンを含有するオウバクエキス等の植物エキスは、ベルベリンが抗炎症効果を発揮し、歯肉炎等の歯周病予防に有用な成分である。しかしながら、ベルベリンを含有する植物エキス、特にオウバクエキスは、生薬様の独特なベルベリン由来の苦味があるため、これらを配合した口腔用組成物は嗜好性の点で好ましくなく、苦味が後味に影響し、満足な使用感が得られない傾向にあった。
特許文献1(特開昭62-155209号公報)は、ベルベリン含有の口腔用組成物に脂肪酸アルカノールアミド等のノニオン活性剤を配合することで、ベルベリンの苦味が改善することを提案しているが、後味に着目しておらず後味には未だ改善の余地があった。
特許文献2(特許第6284136号公報)には、イソブチルアンゲレートを有効成分とする苦味抑制剤による、オウバク等の苦味成分を含有する飲食品の苦味マスキング技術が提案されているが、口腔用組成物における苦味マスキング効果は十分でなかった。
また、オウバクエキスについては、歯磨剤組成物等の口腔用組成物に配合されたβ-グリチルレチン酸や、第4級アンモニウム塩殺菌剤の塩化セチルピリジニウム及び塩化ベンゼトニウムの異味マスキングに用いる技術が特許文献3、4(特開2012-148998号公報、特開2015-86164号公報)に提案されているが、効果が限定的であり、オウバクエキス自体の苦味マスキングに関して言及してもいない。
Conventionally, various active ingredients have been blended in oral compositions for the purpose of preventing or treating defects in the oral cavity. Among them, berberine exerts an anti-inflammatory effect in plant extracts such as gingival extract containing berberine. However, it is a useful ingredient for preventing periodontal diseases such as gingival inflammation. However, since plant extracts containing berberine, especially Phellodendron amur extract, have a unique herbal-like bitterness derived from berberine, an oral composition containing them is not preferable in terms of palatability, and the bitterness affects the aftertaste. , There was a tendency that a satisfactory usability could not be obtained.
Patent Document 1 (Japanese Unexamined Patent Publication No. 62-155209) proposes that the bitterness of berberine is improved by adding a nonionic activator such as a fatty acid alkanolamide to an oral composition containing berberine. There was still room for improvement in the aftertaste without paying attention to the aftertaste.
Patent Document 2 (Japanese Patent No. 6284136) proposes a bitterness masking technique for foods and drinks containing a bitterness component such as Phellodendron amur, using a bitterness inhibitor containing isobutyl angelate as an active ingredient. The bitterness masking effect in the composition was not sufficient.
Regarding the Oubaku extract, patented documents include β-glycyrrhetinic acid blended in oral compositions such as dentifrice compositions, and techniques used for masking the taste of cetylpyridinium chloride and benzethonium chloride, which are quaternary ammonium salt bactericides. Although it has been proposed in 3 and 4 (Japanese Patent Laid-Open No. 2012-148998, Japanese Patent Application Laid-Open No. 2015-86164), the effect is limited, and the bitterness masking of the Oubaku extract itself is not mentioned.
ところで、口腔用組成物において、後味としてスッキリとした使用感を付与することは、効果実感にも繋がり商品価値上重要である。消費者調査等から、使用後にもスッキリ感が持続することが歯周病予防の効果実感を醸成することが見出されており、より一層のスッキリ感の持続性が求められている。スッキリ感は、一般的な口腔用香料であるメントールやミント油等を配合することである程度は得られるが、増量すると刺激感等を招くことがあり、また、苦味や刺激の少なさの点から冷感剤(クーリング剤)が配合されることもあるが、冷感剤種によっては、他の配合成分による苦味が増強される場合があった。とりわけ、液体口腔用組成物では、1回の使用量が10~20mLで練歯磨の10~20倍量であり、比較的多いため、より苦味が強く感じられ、嗜好性が損なわれ易い傾向にあり、後味のスッキリとした使用感を確保することは難しかった。 By the way, in the oral composition, it is important to give a refreshing feeling of use as an aftertaste, which leads to a real feeling of effect and is important in terms of commercial value. From consumer surveys and the like, it has been found that maintaining a refreshing feeling even after use fosters a feeling of effectiveness in preventing periodontal disease, and further sustainability of the refreshing feeling is required. A refreshing feeling can be obtained to some extent by adding menthol, mint oil, etc., which are general oral fragrances, but increasing the amount may cause irritation, etc., and also from the viewpoint of bitterness and less irritation. A cooling sensation agent (cooling agent) may be added, but depending on the type of cooling sensation agent, the bitterness due to other ingredients may be enhanced. In particular, in the liquid oral composition, the amount used at one time is 10 to 20 mL, which is 10 to 20 times the amount of toothpaste, and since it is relatively large, the bitterness is felt more strongly and the palatability tends to be impaired. Therefore, it was difficult to secure a refreshing aftertaste.
本発明は、上記事情に鑑みなされたもので、ベルベリン由来の苦味を改善し、使用後においても苦味が軽減し、かつスッキリとした使用感を与える、後味の良い口腔用組成物を提供することを目的とする。 The present invention has been made in view of the above circumstances, and provides an oral composition having a good aftertaste, which improves the bitterness derived from berberine, reduces the bitterness even after use, and gives a refreshing feeling of use. With the goal.
本発明者は、上記目的を達成するため鋭意検討を行った結果、ベルベリン含有の口腔用組成物に特定の冷感剤を配合すると、ベルベリン由来の苦味が改善し、使用直後から経時においても苦味が抑制され、それに伴う違和感も適度に軽減し、かつ顕著にスッキリとした使用感が持続し、後味の良い優れた使用感となることを知見した。即ち、本発明では、(A)ベルベリンと、(B)メントングリセリンアセタール及びN-(4-メトキシフェニル)-5-メチル-p-メンタンカルボキサミドから選ばれる1種以上とを配合することによって、ベルベリン由来の苦味が改善し、使用後においても苦味が抑制されて軽減し、かつスッキリとした使用感を与える、後味の良い口腔用組成物が得られ、歯肉炎等の歯周病の予防又は抑制用として有効であることを知見し、本発明をなすに至った。 As a result of diligent studies to achieve the above object, the present inventor has improved the bitterness derived from berberine when a specific cooling sensation agent is added to the oral composition containing berberine, and the bitterness is improved immediately after use and over time. It was found that the feeling of discomfort associated therewith was moderately reduced, the feeling of use was remarkably refreshed, and the feeling of use was excellent with a good aftertaste. That is, in the present invention, velverin is formed by blending (A) velverin with one or more selected from (B) menthone glycerin acetal and N- (4-methoxyphenyl) -5-methyl-p-menthancarboxamide. An oral composition having a good aftertaste, which improves the derived bitterness, suppresses and reduces the bitterness even after use, and gives a refreshing feeling of use, can prevent or suppress periodontal diseases such as gingival inflammation. It was found that it is effective for use, and the present invention was made.
本発明では、成分(B)によって、成分(A)由来の苦味がマスキングされて適度に抑えられ、成分(A)が、オウバク等の植物エキスとして配合されてもその生薬様の独特な苦味が抑制され、上記優れた作用効果を特異的に与えることができる。また、成分(A)及び(B)を併用して配合することで、1回の使用量が比較的多く、苦味等によって嗜好性が比較的損なわれ易い洗口剤等の液体口腔用組成物であっても、口腔内で使用直後から経時においても苦味が抑制されて適度に軽減し、かつスッキリとした使用感を持続させることができ、後味を一層良いものとできる。
後述の比較例に示すように、成分(B)が配合されていない場合は、同様に冷感剤として公知のN-エチル-p-メンタン-3-カルボキサミド又は3-メントキシプロパン-1,2-ジオールが配合され、更に、香料としてメントールやペパーミント油が添加されていても、成分(A)由来の苦味が軽減せず、使用後の苦味のなさ(使用直後及び10分間経過後)が劣るものであった。これに対して、実施例に示す本発明の成分(A)及び(B)が配合された口腔用組成物(洗口剤)は、使用後の苦味のなさ(使用直後及び10分間経過後)が優れ、使用後のスッキリ感(使用直後及び10分間経過後)も優れ、後味が良かった。
なお、特許文献1、2は、ノニオン活性剤又はイソブチルアンゲレートによる、ベルベリンの苦味改善であり、これに対して、本発明は、口腔用組成物での成分(B)による、成分(A)の苦味改善であり、使用後においてもスッキリとした使用感が持続し、後味の良い優れた使用感を与えることができる。
In the present invention, the bitterness derived from the component (A) is masked and appropriately suppressed by the component (B), and even if the component (A) is blended as a plant extract such as Phellodendron amur, its herbal-like unique bitterness is exhibited. It is suppressed and can specifically give the above-mentioned excellent action and effect. Further, by blending the components (A) and (B) in combination, a liquid oral composition such as a mouthwash, which is used in a relatively large amount at one time and whose palatability is relatively easily impaired by bitterness or the like. Even so, the bitterness is suppressed in the oral cavity immediately after use and even after a lapse of time, the bitterness is moderately reduced, and a refreshing feeling of use can be maintained, and the aftertaste can be further improved.
As shown in the comparative example described later, when the component (B) is not blended, N-ethyl-p-menthane-3-carboxamide or 3-mentoxypropane-1,2, which are also known as cooling sensitizers, are used. -Even if diol is blended and menthol or peppermint oil is added as a fragrance, the bitterness derived from the component (A) is not reduced, and the bitterness after use (immediately after use and after 10 minutes) is inferior. It was a thing. On the other hand, the oral composition (mouthwash) containing the components (A) and (B) of the present invention shown in Examples has no bitterness after use (immediately after use and after 10 minutes have passed). Was excellent, the refreshing feeling after use (immediately after use and after 10 minutes) was also excellent, and the aftertaste was good.
Patent Documents 1 and 2 are for improving the bitterness of berberine by using a nonionic activator or isobutyl angelate, whereas the present invention is based on the component (B) in the oral composition, which is the component (A). ) Is an improvement in bitterness, and a refreshing feeling of use can be maintained even after use, and an excellent feeling of use with a good aftertaste can be given.
従って、本発明は、下記の口腔用組成物を提供する。
〔1〕
(A)ベルベリンと、
(B)メントングリセリンアセタール及びN-(4-メトキシフェニル)-5-メチル-p-メンタンカルボキサミドから選ばれる1種以上と
を含有することを特徴とする口腔用組成物。
〔2〕
(A)ベルベリンが、オウバク及びオウレンから選ばれる植物のエキス由来であり、前記植物エキス(A1)を0.005~0.5質量%含有する〔1〕記載の口腔用組成物。
〔3〕
成分(A1)と成分(B)との量比を示す(B)/(A1)が質量比として0.05~80である〔2〕記載の口腔用組成物。
〔4〕
成分(A)を0.0003~0.03質量%、成分(B)を0.01~0.4質量%含有する〔1〕~〔3〕のいずれかに記載の口腔用組成物。
〔5〕
更に、(C)非イオン性界面活性剤を0.3~1質量%含有する〔1〕~〔4〕のいずれかに記載の口腔用組成物。
〔6〕
成分(C)と成分(B)との量比を示す(C)/(B)が質量比として1~100である〔5〕記載の口腔用組成物。
〔7〕
液体である〔1〕~〔6〕のいずれかに記載の口腔用組成物。
Therefore, the present invention provides the following oral compositions.
[1]
(A) Berberine and
(B) An oral composition comprising one or more selected from menthone glycerin acetal and N- (4-methoxyphenyl) -5-methyl-p-menthancarboxamide.
[2]
(A) The oral composition according to [1], wherein berberine is derived from a plant extract selected from Phellodendron amur and Coptis chinensis and contains 0.005 to 0.5% by mass of the plant extract (A1).
[3]
The oral composition according to [2], wherein (B) / (A1) indicating the quantitative ratio of the component (A1) to the component (B) is 0.05 to 80 as a mass ratio.
[4]
The oral composition according to any one of [1] to [3], which contains 0.0003 to 0.03% by mass of the component (A) and 0.01 to 0.4% by mass of the component (B).
[5]
The oral composition according to any one of [1] to [4], which further contains (C) a nonionic surfactant in an amount of 0.3 to 1% by mass.
[6]
The oral composition according to [5], wherein (C) / (B) indicating the quantitative ratio of the component (C) to the component (B) is 1 to 100 as a mass ratio.
[7]
The oral composition according to any one of [1] to [6], which is a liquid.
本発明によれば、ベルベリン由来の苦味が改善し、使用後においても苦味が軽減し、かつスッキリとした使用感を与える、後味の良い口腔用組成物を提供できる。本発明の口腔用組成物は、ベルベリンによる抗炎症効果を有すると共に、使用後も苦味がほとんどなく、かつ高いスッキリ感が持続して後味に優れ、歯肉炎等の歯周病の予防又は抑制用として好適である。 According to the present invention, it is possible to provide an oral composition having a good aftertaste, which improves the bitterness derived from berberine, reduces the bitterness even after use, and gives a refreshing feeling of use. The oral composition of the present invention has an anti-inflammatory effect due to berberine, has almost no bitterness even after use, maintains a high refreshing feeling and has an excellent aftertaste, and is used for preventing or suppressing periodontal diseases such as gingival inflammation. Is suitable as.
以下、本発明につき更に詳述する。本発明の口腔用組成物は、(A)ベルベリンと、(B)メントングリセリンアセタール及びN-(4-メトキシフェニル)-5-メチル-p-メンタンカルボキサミドから選ばれる1種以上とを含有し、更に好ましくは(C)非イオン性界面活性剤を含有する。 Hereinafter, the present invention will be described in more detail. The oral composition of the present invention contains (A) berberine and (B) one or more selected from (B) menthone glycerin acetal and N- (4-methoxyphenyl) -5-methyl-p-menthan carboxamide. More preferably, it contains (C) a nonionic surfactant.
(A)ベルベリンは、ベルベリンを含有する植物エキスとして配合することができ、オウバク及びオウレンから選ばれる植物のエキス(植物エキス(A1))を配合できる。ベルベリンは、抗炎症効果を有し、歯肉炎等の歯周病を予防又は抑制するための有効成分であり、苦味を有する。
植物エキス(A1)としては、オウバクエキス、オウレンエキスを用いることができ、特にオウバクエキスが好ましい。
オウバクエキス、オウレンエキスは、それぞれの原料植物を親水性有機溶媒(水、エタノール等)によって抽出処理して得られる抽出物を用いることができ、前記抽出物を乾燥させた粉末を用いることもできる。これらは、市販品を使用することもできる。
オウバクエキスは、キハダ(学名:Phellodendoron amurense Ruprecht)又はその他同族植物(ミカン科;Rutaceae)の周皮を除いた樹皮を水、親水性有機溶媒(水、エタノール等)又はこれらの混合液により抽出処理して得られるが、特に水又は含水エタノールによる抽出物が好適であり、その乾燥粉末でもよい。上記オウバクエキスは、市販品を用いることができ、例えば、粉末型の小城製薬(株)製オウバクエキスを使用することができる。
オウレンエキスは、キンポウゲ科オウレン属の植物であるオウレンの根や茎を上記と同様に抽出処理して得られる抽出物やその乾燥粉末を用いることができる。
(A) Berberine can be blended as a plant extract containing berberine, and a plant extract selected from Phellodendron amur and Coptis chinensis (plant extract (A1)) can be blended. Berberine has an anti-inflammatory effect, is an active ingredient for preventing or suppressing periodontal diseases such as gingival inflammation, and has a bitter taste.
As the plant extract (A1), Phellodendron amur extract and Coptis chinensis extract can be used, and Phellodendron amur extract is particularly preferable.
As the Coptis chinensis extract and Coptis chinensis extract, an extract obtained by extracting each raw material plant with a hydrophilic organic solvent (water, ethanol, etc.) can be used, and a powder obtained by drying the extract can also be used. .. Commercially available products can also be used for these.
Oubaku extract is obtained by extracting the bark of Phellodendron amurense (scientific name: Phellodendron amurense Ruprecht) or other related plants (Rutaceae) excluding the peripheral bark with water, a hydrophilic organic solvent (water, ethanol, etc.) or a mixture thereof. However, an extract containing water or hydrous ethanol is particularly suitable, and a dry powder thereof may be used. As the above-mentioned Phellodendron amur extract, a commercially available product can be used, and for example, a powder-type Phellodendron amurus extract manufactured by Koshiro Pharmaceutical Co., Ltd. can be used.
As the Coptis chinensis extract, an extract or a dry powder thereof obtained by extracting the roots and stems of Coptis chinensis, which is a plant belonging to the genus Coptis genus of the family Ranunculales, in the same manner as described above can be used.
成分(A)の配合量は、固形分換算量で組成物全体の0.0003~0.03%(質量%、以下同様)が好ましく、より好ましくは0.0012~0.012%である。配合量が0.0003%以上であると、十分な抗炎症効果が発揮され、0.03%以下であると、十分に苦味が抑制され、かつスッキリ感を付与することができる。
成分(A)として成分(A1)、特にオウバクエキスを配合する場合、その配合量は、特に苦味の抑制及びスッキリ感の付与の点から、組成物全体の0.005~0.5%が好ましく、より好ましくは0.02~0.2%である。
The blending amount of the component (A) is preferably 0.0003 to 0.03% (mass%, the same applies hereinafter) of the entire composition in terms of solid content, and more preferably 0.0012 to 0.012%. When the blending amount is 0.0003% or more, a sufficient anti-inflammatory effect is exhibited, and when it is 0.03% or less, the bitterness is sufficiently suppressed and a refreshing feeling can be imparted.
When the component (A1), particularly Phellodendron amur extract, is blended as the component (A), the blending amount thereof is preferably 0.005 to 0.5% of the total composition from the viewpoint of suppressing bitterness and imparting a refreshing feeling. , More preferably 0.02 to 0.2%.
成分(B)は、メントングリセリンアセタール、N-(4-メトキシフェニル)-5-メチル-p-メンタンカルボキサミドである。これらは、冷感剤として公知であるが、本発明では、成分(A)の苦味抑制剤として作用し、成分(A)由来の苦味を持続的に抑制して軽減すると同時に、スッキリとした使用感を持続的に付与する作用も奏し、後味を改善する。
成分(B)としては、メントングリセリンアセタール及び/又はN-(4-メトキシフェニル)-5-メチル-p-メンタンカルボキサミドを使用でき、中でも、溶解性と共に苦味の抑制及びスッキリ感の付与の点から、メントングリセリンアセタールがより好ましい。
成分(B)は、メントングリセリンアセタール(Frescolat MGA、シムライズ(株)製)やN-(4-メトキシフェニル)-5-メチル-p-メンタンカルボキサミド(WS-12、シムライズ(株)製)等の市販品を使用することができる。
The component (B) is menthone glycerin acetal, N- (4-methoxyphenyl) -5-methyl-p-menthan carboxamide. These are known as cooling sensation agents, but in the present invention, they act as a bitterness inhibitor of the component (A), continuously suppress and reduce the bitterness derived from the component (A), and at the same time, use them neatly. It also has the effect of sustaining a feeling and improves the aftertaste.
As the component (B), menthone glycerin acetal and / or N- (4-methoxyphenyl) -5-methyl-p-menthancarboxamide can be used, and among them, from the viewpoint of solubility, suppression of bitterness and imparting a refreshing feeling. , Menthone glycerin acetal is more preferred.
The component (B) includes menthone glycerin acetal (Frescolat MGA, manufactured by Symrise Co., Ltd.), N- (4-methoxyphenyl) -5-methyl-p-menthancarboxamide (WS-12, manufactured by Symrise Co., Ltd.), and the like. Commercially available products can be used.
成分(B)の配合量は、組成物全体の0.01~0.4%が好ましく、より好ましくは0.05~0.2%である。配合量が0.01%以上であると、十分に苦味を抑制でき、かつスッキリ感を付与できる。0.4%以下であると、成分(B)由来の刺激や嫌味が抑えられ、苦味の抑制効果が十分に維持される。 The blending amount of the component (B) is preferably 0.01 to 0.4%, more preferably 0.05 to 0.2% of the entire composition. When the blending amount is 0.01% or more, the bitterness can be sufficiently suppressed and a refreshing feeling can be imparted. When it is 0.4% or less, irritation and sarcasm derived from the component (B) are suppressed, and the effect of suppressing bitterness is sufficiently maintained.
成分(A)(固形分換算量)と成分(B)との量比を示す成分(B)/成分(A)は、質量比として0.8~1,333が好ましく、より好ましくは4~400、更に好ましくは4~167である。上記範囲内であると、より一層苦味が抑制され、かつスッキリ感が持続的に得られる。
成分(A)として成分(A1)を配合する場合、成分(A1)と成分(B)との量比を示す(B)/(A1)は、質量比として0.05~80が好ましく、より好ましくは0.25~24、更に好ましくは0.25~10である。
The mass ratio of the component (B) / component (A) indicating the amount ratio of the component (A) (solid content equivalent amount) to the component (B) is preferably 0.8 to 1,333, more preferably 4 to 4. 400, more preferably 4 to 167. Within the above range, the bitterness is further suppressed and a refreshing feeling can be continuously obtained.
When the component (A1) is blended as the component (A), the mass ratio of (B) / (A1) indicating the quantitative ratio of the component (A1) to the component (B) is preferably 0.05 to 80, more preferably. It is preferably 0.25 to 24, more preferably 0.25 to 10.
本発明では、更に(C)非イオン性界面活性剤を配合することが好ましい。
(C)非イオン性界面活性剤は、成分(B)を可溶化すると共にその作用効果を一層効果的に発現させる作用を奏する。
非イオン性界面活性剤としては、例えば糖アルコール脂肪酸エステル、糖脂肪酸エステル、ポリグリセリン脂肪酸エステル等の多価アルコール脂肪酸エステル、ポリオキシエチレン脂肪酸エステル、ポリオキシエチレンアルキルエーテル、脂肪酸アルカノールアミド、ポリオキシエチレンポリオキシプロピレンブロックポリマー等が挙げられる。中でも、苦味の抑制及びスッキリ感の付与の点から、ポリオキシエチレン硬化ヒマシ油、ポリオキシエチレンアルキルエーテル、デカグリセリン脂肪酸エステル、ショ糖脂肪酸エステル、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が好ましく、とりわけスッキリ感(後味のスッキリ感)の付与の点から、ポリオキシエチレン硬化ヒマシ油が好ましく、エチレンオキサイドの平均付加モル数5~100のものを使用できる。ポリオキシエチレン硬化ヒマシ油は、比較的苦味のある非イオン性界面活性剤であるが、本発明では、成分(C)として、ポリオキシエチレン硬化ヒマシ油が配合されても、苦味が十分に抑制され、本作用効果に優れる。
In the present invention, it is preferable to further add (C) a nonionic surfactant.
(C) The nonionic surfactant exerts an action of solubilizing the component (B) and more effectively expressing its action and effect.
Examples of the nonionic surfactant include polyalcohol fatty acid esters such as sugar alcohol fatty acid esters, sugar fatty acid esters, and polyglycerin fatty acid esters, polyoxyethylene fatty acid esters, polyoxyethylene alkyl ethers, fatty acid alkanolamides, and polyoxyethylene. Examples thereof include polyoxypropylene block polymers. Among them, polyoxyethylene hydrogenated castor oil, polyoxyethylene alkyl ether, decaglycerin fatty acid ester, sucrose fatty acid ester, and polyoxyethylene polyoxypropylene block copolymer are preferable from the viewpoint of suppressing bitterness and imparting a refreshing feeling, and are particularly refreshing. From the viewpoint of imparting a feeling (refreshing feeling of aftertaste), polyoxyethylene hydrogenated castor oil is preferable, and polyethylene oxide having an average addition molar number of 5 to 100 can be used. Polyoxyethylene hydrogenated castor oil is a nonionic surfactant having a relatively bitter taste, but in the present invention, even if polyoxyethylene hydrogenated castor oil is blended as the component (C), the bitterness is sufficiently suppressed. It is excellent in this effect.
成分(C)の非イオン性界面活性剤の配合量は、成分(B)を可溶化できれば特に限定されないが、組成物全体の0.3~1%が好ましく、より好ましくは0.3~0.8%、更に好ましくは0.5~0.8%である。上記範囲であると、十分に成分(B)が可溶化され、苦味の抑制効果及びスッキリ感の付与効果が高まる。配合量が1%以下であると、成分(C)自身の苦味が抑えられ、苦味の抑制効果が維持される。 The blending amount of the nonionic surfactant of the component (C) is not particularly limited as long as the component (B) can be solubilized, but is preferably 0.3 to 1% of the entire composition, and more preferably 0.3 to 0. It is 8.8%, more preferably 0.5 to 0.8%. Within the above range, the component (B) is sufficiently solubilized, and the effect of suppressing bitterness and the effect of imparting a refreshing feeling are enhanced. When the blending amount is 1% or less, the bitterness of the component (C) itself is suppressed, and the effect of suppressing the bitterness is maintained.
成分(C)と成分(B)との量比を示す(C)/(B)は、質量比として1~100が好ましく、より好ましくは2.5~16である。上記範囲内であると、成分(B)自身の苦味及び成分(C)自身の嫌味が抑えられ、一層苦味が抑制され、かつスッキリ感が持続する。 The mass ratio of (C) / (B) indicating the quantitative ratio of the component (C) to the component (B) is preferably 1 to 100, more preferably 2.5 to 16. Within the above range, the bitterness of the component (B) itself and the sarcasm of the component (C) itself are suppressed, the bitterness is further suppressed, and the refreshing feeling is maintained.
本発明の口腔用組成物は、特に液体の形態に調製し、液体口腔用組成物として好適であり、液体歯磨、洗口剤、口中剤等の剤型にすることができ、特に洗口剤が好ましい。また、通常の方法を採用して調製できる。この場合、組成物の目的、剤型等に応じて、上述した成分以外にも適宜な公知成分を配合できる。液体口腔用組成物には、具体的に湿潤剤、界面活性剤、溶剤、更に必要により甘味剤、着色剤、香料、pH調整剤、有効成分等が配合される。なお、液体口腔用組成物には、研磨剤などの可溶化しない固形成分は通常配合されず、研磨剤は含まないことが好ましい。 The oral composition of the present invention is particularly prepared in the form of a liquid and is suitable as a liquid oral composition, and can be used in the form of liquid toothpaste, mouthwash, mouthwash, etc. Is preferable. In addition, it can be prepared by adopting a usual method. In this case, an appropriate known component may be blended in addition to the above-mentioned components depending on the purpose of the composition, the dosage form, and the like. The liquid oral composition specifically contains a wetting agent, a surfactant, a solvent, and if necessary, a sweetening agent, a coloring agent, a fragrance, a pH adjuster, an active ingredient, and the like. It is preferable that the liquid oral composition does not usually contain a solid component that is not solubilized, such as an abrasive, and does not contain an abrasive.
湿潤剤は、例えばソルビトール、マルチット、ラクチット等の糖アルコール、グリセリン、プロピレングリコール、エチレングリコール、ポリエチレングリコール等の多価アルコールが挙げられる。これら湿潤剤の配合量は、通常、組成物全体の2~20%である。 Examples of the wetting agent include sugar alcohols such as sorbitol, martit and lacchit, and polyhydric alcohols such as glycerin, propylene glycol, ethylene glycol and polyethylene glycol. The blending amount of these wetting agents is usually 2 to 20% of the total composition.
任意の界面活性剤は、公知のアニオン性界面活性剤、カチオン性界面活性剤、両性界面活性剤等を配合できる。
アニオン性界面活性剤は、ラウリル硫酸ナトリウム、ミリスチル硫酸ナトリウム等のアルキル硫酸塩、N-ラウロイルサルコシンナトリウム、N-ミリストイルサルコシンナトリウム等のN-アシルサルコシン塩、ドデシルベンゼンスルホン酸ナトリウム、水素添加ココナッツ脂肪酸モノグリセリドモノ硫酸ナトリウム、ラウリルスルホ酢酸ナトリウム、N-パルミトイルグルタミン酸ナトリウム等のN-アシルグルタミン酸塩、N-メチル-N-アシルタウリンナトリウム、N-メチル-N-アシルアラニンナトリウム、α-オレフィンスルフォン酸ナトリウムが挙げられる。
カチオン性界面活性剤は、アルキルアンモニウム、アルキルベンジルアンモニウム塩が挙げられる。
両性界面活性剤は、アルキルジメチルアミノ酢酸ベタイン、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両性界面活性剤、N-脂肪酸アシル-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塩等のイミダゾリン型両性界面活性剤が挙げられる。
これら任意の界面活性剤の配合量は、組成物全体の0.01~2%が好ましい。
Any surfactant can be blended with known anionic surfactants, cationic surfactants, amphoteric surfactants and the like.
Anionic surfactants include alkyl sulfates such as sodium lauryl sulfate and sodium myristyl sulfate, N-acylsarcosine salts such as N-lauroyl sarcosin sodium and N-myristoyl sarcosin sodium, sodium dodecylbenzene sulfonate, hydrogenated coconut fatty acid monoglyceride. Examples include N-acylglutamate such as sodium monosulfate, sodium lauryl sulfoacetate, and sodium N-palmitoyl glutamate, sodium N-methyl-N-acyltaurine, sodium N-methyl-N-acylalanine, and sodium α-olefin sulfonate. Be done.
Examples of the cationic surfactant include alkylammonium and alkylbenzylammonium salts.
Amphoteric surfactants include betaine acetate-type amphoteric surfactants such as alkyldimethylaminoacetic acid betaine and betaine fatty acid amide propyldimethylaminoacetic acid betaine, and imidazoline-type amphoteric salts such as N-fatty acid acyl-N-carboxymethyl-N-hydroxyethylethylenediamine salt. Examples include surfactants.
The blending amount of these arbitrary surfactants is preferably 0.01 to 2% of the total composition.
甘味剤は、キシリトール、マルチトール、サッカリン、サッカリンナトリウム、ステビオサイド、アスパルテーム等が挙げられる。 Examples of the sweetener include xylitol, maltitol, saccharin, sodium saccharin, stebioside, aspartame and the like.
着色剤は、青色1号、緑色3号、黄色4号、赤色105号等の安全性の高い水溶性色素が挙げられる。 Examples of the colorant include highly safe water-soluble dyes such as Blue No. 1, Green No. 3, Yellow No. 4, and Red No. 105.
香料は、例えば、ユーカリ油、ウィンターグリーン油、カシア油、クローブ油、タイム油、セージ油、バジル油、カルダモン油、コリアンダー油、ペパーミント油、スペアミント油、ハッカ油、オレンジ油、レモン油、マンダリン油、ライム油、グレープフルーツ油、柚子油、スウィーティー油、ラベンダー油、ローズマリー油、ローレル油、カモミル油、キャラウェイ油、マジョラム油、セロリ油、ベイ油、オリガナム油、パインニードル油、ネロリ油、レモングラス油、ローズ油、ジャスミン油、パチュリ油、イリスコンクリート、ローズアブソリュート、オレンジフラワーアブソリュート、バニラアブソリュート、マンゴーアブソリュート、パチュリアブソリュート、ジンジャーオレオレジン、ペッパーオレオレジン、カプシカムオレオレジン、トウガラシ抽出物等の天然香料や、これら天然香料の加工処理(前溜部カット、後溜部カット、分留、液液抽出、エッセンス化、粉末香料化等)した香料、リモネン、ピネン、ブタノール、イソアミルアルコール、n-ヘキセノール、cis-3-ヘキセノール、cis-6-ノネノール、リナロール、α-テルピネオール、メントール、ベンジルアルコール、フェニルエチルアルコール、アネトール、チモール、メチルチャビコール、オイゲノール、カルボン、メントン、プレゴン、1,8-シネオール、ヨノン、キャロン、n-ヘキサナール、trans-2-ヘキセナール、シトラール、シンナムアルデヒド、ベンズアルデヒド、エチルアセテート、エチルブチレート、イソアミルアセテート、ヘキシルアセテート、エチル-2-メチルブチレート、アリルヘキサノエート、アリルシクロヘキサンプロピオネート、リナリルアセテート、メンチルアセテート、カルビールアセテート、フェノキシエチルイソブチレート、メチルジャスモネート、サリチル酸メチル、サリチル酸エチル、メチルシンナメート、メチルアンスラニレート、フェニルエチルグリシデート、エチルラクテート、バニリン、マルトール、炭素数4~12のガンマ又はデルタラクトン、アンブレットリド、ジメチルサルファイド、トリメチルピラジン、エチル-β-メチルチオプロピオネート、フラネオール、エチルシクロペンテノロン、シクロテン、2-メチルブチリックアシッド、プロピオニックアシッド、p-メトキシシンナミックアルデヒド、スピラントール、リナロールオキサイド、バニリルブチルエーテル、イソプレゴール、乳酸メンチル、モノメンチルサクシネート、モノメンチルグルタレート、メンチルエチレングリコールカーボネート、メンチルプロピレングリコールカーボネート、3-メントキシプロパン-1,2-ジオール、N-エチル-p-メンタン-3-カルボキサミド、エチル(3-(p-メンタン-3-カルボキサミド)アセテート、N-(4-シアノメチルフェニル)-p-メンタンカルボキサミド、2-イソプロピル-5-メチル-N-(2-ピリジニルエチル)シクロヘキサンカルボキサミド等の単品香料、ストロベリーフレーバー、アップルフレーバー、メロンフレーバー、バナナフレーバー、ピーチフレーバー、ラズベリーフレーバー、パイナップルフレーバー、グレープフレーバー、トロピカルフルーツフレーバー、マンゴーフレーバー、ウメフレーバー、オレンジフレーバー、レモンフレーバー、グレープフルーツフレーバー、ティーフレーバー、バターフレーバー、ミルクフレーバー等の調合香料が挙げられ、口腔用組成物に用いられる公知の香料素材を組み合わせて使用することができる。更に、エチルアルコール、プロピレングリコール、トリアセチン、グリセリン脂肪酸エステル等の香料溶剤等を添加することもできる。上記香料素材の配合量は、特に限定されず、本発明の効果を妨げない範囲で添加することができるが、通常、組成物全体の0.000001~3%である。 Fragrances include, for example, eucalyptus oil, winter green oil, cassia oil, clove oil, thyme oil, sage oil, basil oil, cardamon oil, coriander oil, peppermint oil, spearmint oil, peppermint oil, orange oil, lemon oil, mandarin oil. , Lime oil, grapefruit oil, yuzu oil, sweetie oil, lavender oil, rosemary oil, laurel oil, camomill oil, caraway oil, majorum oil, celery oil, bay oil, origanum oil, pine needle oil, neroli oil, lemon Glass oil, rose oil, jasmine oil, patchouli oil, iris concrete, rose absolute, orange flower absolute, vanilla absolute, mango absolute, patchuriabsolute, ginger oleoledin, peppermint olegin, capsicum oleoledin, peppermint extract, etc. Natural fragrances, fragrances processed by processing these natural fragrances (front reservoir cut, rear reservoir cut, distilling, liquid extraction, essence, powder fragrance, etc.), limonene, mint, butanol, isoamyl alcohol, n- Hexenol, cis-3-hexenol, cis-6-nonenor, linalol, α-terpineol, menthol, benzyl alcohol, phenylethyl alcohol, anator, timol, methylchabicol, eugenol, carboxylic, menton, pregon, 1,8-cineol , Jonon, Caron, n-hexanal, trans-2-hexenal, citral, cinnamaldehyde, benzaldehyde, ethyl acetate, ethyl butyrate, isoamyl acetate, hexyl acetate, ethyl-2-methylbutyrate, allyl hexanoate, allyl cyclohexane Propionate, Linalyl Acetate, Mentil Acetate, Calvia Acetate, Phenoxyethyl Isobutyrate, Methyl Jasmonate, Methyl Salicylate, Ethyl Salicylate, Methyl Synnate, Methyl Anthranilate, Phenylethyl Glycydate, Ethyl Lactate, Vanillin, Martol, gamma or deltalactone with 4-12 carbon atoms, ambretlide, dimethylsulfide, trimethylpyrazine, ethyl-β-methylthiopropionate, flaneol, ethylcyclopentenolone, cycloten, 2-methylbutyric acid, propio Nickacid, p-methoxycinnamic aldehyde, spirantol, linalol oxide, ba Nirylbutyl ether, isopulegol, menthyl lactate, monomentyl succinate, monomentyl glutarate, menthyl ethylene glycol carbonate, menthyl propylene glycol carbonate, 3-mentoxypropane-1,2-diol, N-ethyl-p-menthane-3 -Carboxamide, ethyl (3- (p-menthan-3-carboxamide) acetate, N- (4-cyanomethylphenyl) -p-menthan carboxamide, 2-isopropyl-5-methyl-N- (2-pyridinylethyl) cyclohexanecarboxamide Single flavor, strawberry flavor, apple flavor, melon flavor, banana flavor, peach flavor, raspberry flavor, pineapple flavor, grape flavor, tropical fruit flavor, mango flavor, ume flavor, orange flavor, lemon flavor, grapefruit flavor, etc. , Butter flavor, milk flavor and the like, and known perfume materials used in oral compositions can be used in combination. Further, a fragrance solvent such as ethyl alcohol, propylene glycol, triacetin, and glycerin fatty acid ester can be added. The blending amount of the fragrance material is not particularly limited and can be added within a range that does not interfere with the effects of the present invention, but is usually 0.000001 to 3% of the total composition.
pH調整剤は、公知のものを必要に応じ配合できる。具体的にはクエン酸、リンゴ酸、乳酸、酒石酸、酢酸、リン酸、ピロリン酸、ポリリン酸、グリセロリン酸やこれらの各種塩、水酸化ナトリウム、水酸化カリウム等が挙げられる。 As the pH adjuster, known ones can be blended as needed. Specific examples thereof include citric acid, malic acid, lactic acid, tartaric acid, acetic acid, phosphoric acid, pyrophosphate, polyphosphoric acid, glycerophosphate and various salts thereof, sodium hydroxide, potassium hydroxide and the like.
有効成分は、塩化セチルピリジニウム、塩化ベンザルコニウム、塩化ベンゼトニウム、イソプロピルメチルフェノール、トリクロサン、ヒノキチオール等の抗菌性物質、グルカナーゼ(デキストラナーゼ、ムタナーゼ等)、プロテアーゼ、塩化リゾチーム等の酵素、フッ化ナトリウム、フッ化第1錫、モノフルオロリン酸ナトリウム等のフッ素含有化合物、アルミニウムクロルヒドロキシアラントイン、アラントイン、グリチルリチン酸、グリチルリチン酸ジカリウム、グリチルリチン酸トリナトリウム、グリチルリチン酸モノアンモニウム、トラネキサム酸、イプシロンアミノカプロン酸、アズレンスルホン酸塩等の抗炎症剤、アスコルビン酸、酢酸トコフェロール、ピリドキシン等のビタミン類、ジヒドロコレステロール、ヒドロコレステロール、クロロフィル、銅クロロフィリンナトリウムや、タイム、オウゴン、カミツレ、チョウジ、ローズマリー、ベニバナ、ハマメリス等の植物抽出物、塩化ナトリウム、硝酸カリウム、乳酸アルミニウム、塩化亜鉛、クエン酸亜鉛、塩化ストロンチウム等の無機塩類、ポリリン酸ナトリウム等の水溶性無機リン酸化合物、グルコン酸銅、カロペプタイド、ポリビニルピロリドン、歯石防止剤、歯垢防止剤が挙げられる。これらの有効成分の添加量は、本発明の効果を妨げない範囲で、有効量とすることができる。 The active ingredients are antibacterial substances such as cetylpyridinium chloride, benzalkonium chloride, benzethonium chloride, isopropylmethylphenol, triclosan, hinokithiol, glucanase (dextranase, mutanase, etc.), protease, enzymes such as lysoteam chloride, sodium fluoride. , Fluorine-containing compounds such as stannous fluoride, sodium monofluorophosphate, aluminum chlorhydroxyalantin, allantin, glycyrrhizinic acid, dipotassium glycyrrhizinate, trisodium glycyrrhizinate, monoammonium glycyrrhizinate, tranexamic acid, epsilon aminocaproic acid, azulene. Anti-inflammatory agents such as sulfonates, vitamins such as ascorbic acid, tocopherol acetate, pyridoxin, dihydrocholesterol, hydrocholesterol, chlorophyll, sodium copper chlorophyllin, thyme, ginger, chamomile, chowji, rosemary, benivana, hamamelis, etc. Plant extracts, sodium chloride, potassium nitrate, aluminum lactate, zinc chloride, zinc citrate, strontium chloride and other inorganic salts, water-soluble inorganic phosphate compounds such as sodium polyphosphate, copper gluconate, caropeptide, polyvinylpyrrolidone, dentin inhibitors , Anti-staining agent. The amount of these active ingredients added can be an effective amount as long as the effects of the present invention are not impaired.
溶剤としては、通常、水が用いられ、水の含有量は組成物全体の60%以上が好ましい。また、エタノール等の低級一価アルコールを、本発明の効果を妨げない範囲で配合することができる。 Water is usually used as the solvent, and the content of water is preferably 60% or more of the whole composition. Further, a lower monohydric alcohol such as ethanol can be blended within a range that does not interfere with the effects of the present invention.
以下、実施例及び比較例、処方例を示し、本発明を具体的に説明するが、本発明は下記の実施例に制限されるものではない。なお、下記の例において%は特に断らない限りいずれも質量%を示す。 Hereinafter, the present invention will be specifically described with reference to Examples, Comparative Examples, and Prescription Examples, but the present invention is not limited to the following Examples. In the following examples,% indicates mass% unless otherwise specified.
[実施例、比較例]
表1に示す基本組成で表2~4に示す成分を配合した液体口腔用組成物(洗口剤)を下記方法で調製し、下記方法で使用感を評価した。結果を表に併記した。
[Examples, comparative examples]
A liquid oral composition (mouthwash) containing the components shown in Tables 2 to 4 with the basic composition shown in Table 1 was prepared by the following method, and the usability was evaluated by the following method. The results are also shown in the table.
調製方法:
液体口腔用組成物(洗口剤)の調製は、表中の組成に応じ、精製水中に水溶性原料(非イオン性界面活性剤、溶剤を除く)を溶解した後、エタノール及び多価アルコールに油溶性原料と非イオン性界面活性剤を溶解した液を、攪拌しながら加え、均一溶解させた。なお、製造にはスリーワンモーター(BL1200、HEIDON社製)を用いた。
Preparation method:
To prepare the liquid oral composition (mouthwash), dissolve the water-soluble raw materials (excluding nonionic surfactants and solvents) in purified water according to the composition in the table, and then add ethanol and polyhydric alcohol. A solution in which an oil-soluble raw material and a nonionic surfactant were dissolved was added with stirring to uniformly dissolve the solution. A three-one motor (BL1200, manufactured by HEIDON) was used for manufacturing.
使用感の評価方法
10名の被験者が、洗口剤10mLを口に含み、30秒間口をすすぎ、吐き出した後、使用後の苦味のなさ(使用直後及び10分間経過後の苦味のなさ)、使用後のスッキリ感(使用直後及び10分間経過後のスッキリ感)について、それぞれ下記の評点基準で評価した。被験者10名の平均値を求め、下記の評価基準に従い、◎、〇、△、×で示した。
Evaluation method of usability 10 subjects contained 10 mL of mouthwash in their mouth, rinsed their mouth for 30 seconds, exhaled, and then had no bitterness after use (no bitterness immediately after use and after 10 minutes). The refreshing feeling after use (the refreshing feeling immediately after use and after 10 minutes) was evaluated according to the following scoring criteria. The average value of 10 subjects was calculated and indicated by ⊚, 〇, Δ, and × according to the following evaluation criteria.
(i)使用後の苦味のなさ(使用直後、10分間経過後)
評点基準
4点:苦味をほとんど感じない
3点:苦味をわずかに感じる
2点:苦味を感じる
1点:苦味を非常に感じる
評価基準
使用後の苦味のなさ平均点
◎:3.5点以上4.0点以下
○:3.0点以上3.5点未満
△:2.0点以上3.0点未満
×:1.0点以上2.0点未満
(I) No bitterness after use (immediately after use, after 10 minutes have passed)
Rating criteria 4 points: Almost no bitterness 3 points: Slight bitterness 2 points: Bitterness 1 point: Very bitterness Evaluation criteria Average score of no bitterness after use ◎: 3.5 points or more 4 .0 points or less ○: 3.0 points or more and less than 3.5 points △: 2.0 points or more and less than 3.0 points ×: 1.0 points or more and less than 2.0 points
(ii)使用後のスッキリ感(使用直後、10分間経過後)
評点基準
4点:スッキリ感を非常に感じる
3点:スッキリ感を感じる
2点:スッキリ感をやや感じる
1点:スッキリ感を全く感じない
評価基準
使用後のスッキリ感平均点
◎:3.5点以上4.0点以下
○:3.0点以上3.5点未満
△:2.0点以上3.0点未満
×:1.0点以上2.0点未満
(Ii) Refreshing feeling after use (immediately after use, after 10 minutes have passed)
Rating criteria 4 points: Very refreshing feeling 3 points: Feeling refreshing feeling 2 points: Feeling refreshing feeling 1 point: Feeling refreshing feeling at all Evaluation criteria Average score after use ◎: 3.5 points 4.0 points or less ○: 3.0 points or more and less than 3.5 points △: 2.0 points or more and less than 3.0 points ×: 1.0 points or more and less than 2.0 points
使用原料の詳細を下記に示す。
(A)オウバクエキス(A1)(小城製薬(株)製、粉末、ベルベリン含有量6%)
(B)メントングリセリンアセタール(Frescolat MGA、シムライズ(株)製)
(B)N-(4-メトキシフェニル)-5-メチル-p-メンタンカルボキサミド(WS-12、シムライズ(株)製)
(C)ポリオキシエチレン(60)硬化ヒマシ油(日光ケミカルズ(株)製)
N-エチル-p-メンタン-3-カルボキサミド(比較品)(WS-3、シムライズ(株)製)
3-メントキシプロパン-1,2-ジオール(比較品)(CA10、高砂香料工業(株)製)
なお、表中のベルベリン量は、ベルベリンの固形分換算量である(以下同様)。
Details of the raw materials used are shown below.
(A) Phellodendron amur extract (A1) (manufactured by Koshiro Pharmaceutical Co., Ltd., powder, berberine content 6%)
(B) Menthone glycerin acetal (Frescolat MGA, manufactured by Symrise Co., Ltd.)
(B) N- (4-Methoxyphenyl) -5-methyl-p-menthancarboxamide (WS-12, manufactured by Symrise Co., Ltd.)
(C) Polyoxyethylene (60) hardened castor oil (manufactured by Nikko Chemicals Co., Ltd.)
N-Ethyl-p-Menthane-3-carboxamide (comparative product) (WS-3, manufactured by Symrise Co., Ltd.)
3-Mentoxypropane-1,2-diol (comparative product) (CA10, manufactured by Takasago International Corporation)
The amount of berberine in the table is the amount converted to solid content of berberine (the same applies hereinafter).
(*)香料組成
アネトール 2
メントール 3
ペパーミント油 20
メンチルラクテート 5
エタノール 70
合計 100%
(*) Fragrance composition Anethole 2
Menthol 3
Peppermint oil 20
Mentil Lactate 5
Ethanol 70
100% in total
表2~4の結果から明らかなように、本発明の成分(A)及び(B)、更には成分(C)が配合された洗口剤(実施例)は、使用後の苦味のなさ(使用直後及び10分間経過後)及び使用後のスッキリ感(使用直後及び10分間経過後)がいずれも優れていた。これらに対して、成分(B)を欠く洗口剤(比較例)は、使用後の苦味のなさ(使用直後及び10分間経過後)が劣り、本発明の目的が達成されなかった。 As is clear from the results in Tables 2 to 4, the mouthwash (Example) containing the components (A) and (B) of the present invention, and further the component (C), has no bitterness after use (examples). Immediately after use and after 10 minutes had passed, and after 10 minutes had passed, the refreshing feeling (immediately after use and after 10 minutes) was excellent. On the other hand, the mouthwash (comparative example) lacking the component (B) was inferior in bitterness after use (immediately after use and after 10 minutes), and the object of the present invention was not achieved.
次に、処方例を示す。処方例の組成を上記と同様の原料を使用して調製し、評価したところ、使用後の苦味のなさ(使用直後及び10分間経過後)及び使用後のスッキリ感(使用直後及び10分間経過後)が、いずれも優れていた。 Next, a prescription example is shown. When the composition of the formulation example was prepared using the same raw materials as above and evaluated, there was no bitterness after use (immediately after use and after 10 minutes) and a refreshing feeling after use (immediately after use and after 10 minutes). ), But both were excellent.
[処方例1]洗口剤
(A)オウバクエキス(A1) 0.05
(ベルベリン量 0.003)
(B)メントングリセリンアセタール 0.12
(C)ポリオキシエチレン(100)硬化ヒマシ油 0.6
キシリトール 4
グリセリン 2
プロピレングリコール 2
エタノール 5
クエン酸 0.01
クエン酸ナトリウム 0.25
サッカリンナトリウム 0.005
スクラロース 0.05
香料 0.1
精製水 残
計 100%
(B)/((A1)) 質量比=2.4
(C)/(B) 質量比=5
[Prescription Example 1] Mouthwash (A) Phellodendron amur extract (A1) 0.05
(Amount of berberine 0.003)
(B) Menthone Glycerin Acetal 0.12
(C) Polyoxyethylene (100) hardened castor oil 0.6
Xylitol 4
Glycerin 2
Propylene glycol 2
Ethanol 5
Citric acid 0.01
Sodium citrate 0.25
Saccharin sodium 0.005
Sucralose 0.05
Fragrance 0.1
Purified water residue
100% in total
(B) / ((A1)) Mass ratio = 2.4
(C) / (B) Mass ratio = 5
[処方例2]口中剤
(A)オウバクエキス(A1) 0.05
(ベルベリン量 0.003)
(B)メントングリセリンアセタール 0.08
(B)N-(4-メトキシフェニル)-5-メチル-p-メンタンカルボキサミド
0.04
(C)ポリオキシエチレン(60)硬化ヒマシ油 0.6
ソルビトール 4
グリセリン 2
プロピレングリコール 5
クエン酸 0.03
クエン酸ナトリウム 0.1
サッカリンナトリウム 0.01
香料 0.1
精製水 残
計 100%
(B)/((A1)) 質量比=2.4
(C)/(B) 質量比=5
[Prescription Example 2] Oral agent (A) Phellodendron amur extract (A1) 0.05
(Amount of berberine 0.003)
(B) Menthone Glycerin Acetal 0.08
(B) N- (4-Methoxyphenyl) -5-methyl-p-menthancarboxamide
0.04
(C) Polyoxyethylene (60) Hardened castor oil 0.6
Sorbitol 4
Glycerin 2
Propylene glycol 5
Citric acid 0.03
Sodium citrate 0.1
Saccharin sodium 0.01
Fragrance 0.1
Purified water residue
100% in total
(B) / ((A1)) Mass ratio = 2.4
(C) / (B) Mass ratio = 5
Claims (7)
(B)メントングリセリンアセタール及びN-(4-メトキシフェニル)-5-メチル-p-メンタンカルボキサミドから選ばれる1種以上と
を含有することを特徴とする口腔用組成物。 (A) Berberine and
(B) An oral composition comprising one or more selected from menthone glycerin acetal and N- (4-methoxyphenyl) -5-methyl-p-menthancarboxamide.
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JP2004059474A (en) | 2002-07-26 | 2004-02-26 | T Hasegawa Co Ltd | p-MENTHANE DERIVATIVE AND COLD SENSING AGENT CONTAINING THE SAME |
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