JP2021169415A - Composition for intraoral application - Google Patents
Composition for intraoral application Download PDFInfo
- Publication number
- JP2021169415A JP2021169415A JP2020072167A JP2020072167A JP2021169415A JP 2021169415 A JP2021169415 A JP 2021169415A JP 2020072167 A JP2020072167 A JP 2020072167A JP 2020072167 A JP2020072167 A JP 2020072167A JP 2021169415 A JP2021169415 A JP 2021169415A
- Authority
- JP
- Japan
- Prior art keywords
- mass
- composition
- less
- oral
- component
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- 239000000203 mixture Substances 0.000 title claims abstract description 95
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 11
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims abstract description 8
- 239000001267 polyvinylpyrrolidone Substances 0.000 claims abstract description 8
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims abstract description 8
- 239000004373 Pullulan Substances 0.000 claims abstract description 7
- 229920001218 Pullulan Polymers 0.000 claims abstract description 7
- 229920006318 anionic polymer Polymers 0.000 claims abstract description 7
- 229920000642 polymer Polymers 0.000 claims abstract description 7
- 235000019423 pullulan Nutrition 0.000 claims abstract description 7
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims abstract description 5
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims abstract description 5
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims abstract description 5
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 claims abstract description 5
- 229920002125 Sokalan® Polymers 0.000 claims abstract description 4
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 claims abstract description 4
- 239000001768 carboxy methyl cellulose Substances 0.000 claims abstract description 4
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 claims abstract description 4
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 claims abstract description 4
- 239000000230 xanthan gum Substances 0.000 claims abstract description 4
- 229920001285 xanthan gum Polymers 0.000 claims abstract description 4
- 235000010493 xanthan gum Nutrition 0.000 claims abstract description 4
- 229940082509 xanthan gum Drugs 0.000 claims abstract description 4
- 210000000214 mouth Anatomy 0.000 claims description 11
- MPDGHEJMBKOTSU-YKLVYJNSSA-N 18beta-glycyrrhetic acid Chemical compound C([C@H]1C2=CC(=O)[C@H]34)[C@@](C)(C(O)=O)CC[C@]1(C)CC[C@@]2(C)[C@]4(C)CC[C@@H]1[C@]3(C)CC[C@H](O)C1(C)C MPDGHEJMBKOTSU-YKLVYJNSSA-N 0.000 claims description 8
- MPDGHEJMBKOTSU-UHFFFAOYSA-N Glycyrrhetinsaeure Natural products C12C(=O)C=C3C4CC(C)(C(O)=O)CCC4(C)CCC3(C)C1(C)CCC1C2(C)CCC(O)C1(C)C MPDGHEJMBKOTSU-UHFFFAOYSA-N 0.000 claims description 4
- FUWUEFKEXZQKKA-UHFFFAOYSA-N beta-thujaplicin Chemical compound CC(C)C=1C=CC=C(O)C(=O)C=1 FUWUEFKEXZQKKA-UHFFFAOYSA-N 0.000 claims description 4
- ZAKOWWREFLAJOT-CEFNRUSXSA-N D-alpha-tocopherylacetate Chemical compound CC(=O)OC1=C(C)C(C)=C2O[C@@](CCC[C@H](C)CCC[C@H](C)CCCC(C)C)(C)CCC2=C1C ZAKOWWREFLAJOT-CEFNRUSXSA-N 0.000 claims description 3
- XSXCZNVKFKNLPR-SDQBBNPISA-N carbazochrome Chemical compound NC(=O)N/N=C/1C(=O)C=C2N(C)CC(O)C2=C\1 XSXCZNVKFKNLPR-SDQBBNPISA-N 0.000 claims description 3
- 229960002631 carbazochrome Drugs 0.000 claims description 3
- 229960003720 enoxolone Drugs 0.000 claims description 3
- 239000004615 ingredient Substances 0.000 claims description 3
- 229940042585 tocopherol acetate Drugs 0.000 claims description 3
- PQUXFUBNSYCQAL-UHFFFAOYSA-N 1-(2,3-difluorophenyl)ethanone Chemical compound CC(=O)C1=CC=CC(F)=C1F PQUXFUBNSYCQAL-UHFFFAOYSA-N 0.000 claims description 2
- IJALWSVNUBBQRA-UHFFFAOYSA-N 4-Isopropyl-3-methylphenol Chemical compound CC(C)C1=CC=C(O)C=C1C IJALWSVNUBBQRA-UHFFFAOYSA-N 0.000 claims description 2
- TUFYVOCKVJOUIR-UHFFFAOYSA-N alpha-Thujaplicin Natural products CC(C)C=1C=CC=CC(=O)C=1O TUFYVOCKVJOUIR-UHFFFAOYSA-N 0.000 claims description 2
- HWDGVJUIHRPKFR-UHFFFAOYSA-I copper;trisodium;18-(2-carboxylatoethyl)-20-(carboxylatomethyl)-12-ethenyl-7-ethyl-3,8,13,17-tetramethyl-17,18-dihydroporphyrin-21,23-diide-2-carboxylate Chemical compound [Na+].[Na+].[Na+].[Cu+2].N1=C(C(CC([O-])=O)=C2C(C(C)C(C=C3C(=C(C=C)C(=C4)[N-]3)C)=N2)CCC([O-])=O)C(=C([O-])[O-])C(C)=C1C=C1C(CC)=C(C)C4=N1 HWDGVJUIHRPKFR-UHFFFAOYSA-I 0.000 claims description 2
- NFIDBGJMFKNGGQ-UHFFFAOYSA-N isopropylmethylphenol Natural products CC(C)CC1=CC=CC=C1O NFIDBGJMFKNGGQ-UHFFFAOYSA-N 0.000 claims description 2
- 229940047670 sodium acrylate Drugs 0.000 claims description 2
- 229940079841 sodium copper chlorophyllin Drugs 0.000 claims description 2
- 235000013758 sodium copper chlorophyllin Nutrition 0.000 claims description 2
- 229930007845 β-thujaplicin Natural products 0.000 claims description 2
- 229920001495 poly(sodium acrylate) polymer Polymers 0.000 abstract description 2
- NNMHYFLPFNGQFZ-UHFFFAOYSA-M sodium polyacrylate Chemical compound [Na+].[O-]C(=O)C=C NNMHYFLPFNGQFZ-UHFFFAOYSA-M 0.000 abstract description 2
- 230000014759 maintenance of location Effects 0.000 description 15
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 8
- 210000002200 mouth mucosa Anatomy 0.000 description 7
- 238000011156 evaluation Methods 0.000 description 6
- JNYAEWCLZODPBN-JGWLITMVSA-N (2r,3r,4s)-2-[(1r)-1,2-dihydroxyethyl]oxolane-3,4-diol Chemical compound OC[C@@H](O)[C@H]1OC[C@H](O)[C@H]1O JNYAEWCLZODPBN-JGWLITMVSA-N 0.000 description 5
- 125000004432 carbon atom Chemical group C* 0.000 description 4
- 230000001747 exhibiting effect Effects 0.000 description 4
- GLDOVTGHNKAZLK-UHFFFAOYSA-N octadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCCCO GLDOVTGHNKAZLK-UHFFFAOYSA-N 0.000 description 4
- 229920001214 Polysorbate 60 Polymers 0.000 description 3
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 3
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 3
- HVUMOYIDDBPOLL-XWVZOOPGSA-N Sorbitan monostearate Chemical compound CCCCCCCCCCCCCCCCCC(=O)OC[C@@H](O)[C@H]1OC[C@H](O)[C@H]1O HVUMOYIDDBPOLL-XWVZOOPGSA-N 0.000 description 3
- 238000011161 development Methods 0.000 description 3
- 230000002708 enhancing effect Effects 0.000 description 3
- -1 fatty acid esters Chemical class 0.000 description 3
- 238000005259 measurement Methods 0.000 description 3
- 210000003296 saliva Anatomy 0.000 description 3
- PUPZLCDOIYMWBV-UHFFFAOYSA-N (+/-)-1,3-Butanediol Chemical compound CC(O)CCO PUPZLCDOIYMWBV-UHFFFAOYSA-N 0.000 description 2
- CUNWUEBNSZSNRX-RKGWDQTMSA-N (2r,3r,4r,5s)-hexane-1,2,3,4,5,6-hexol;(z)-octadec-9-enoic acid Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO.OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO.CCCCCCCC\C=C/CCCCCCCC(O)=O.CCCCCCCC\C=C/CCCCCCCC(O)=O.CCCCCCCC\C=C/CCCCCCCC(O)=O CUNWUEBNSZSNRX-RKGWDQTMSA-N 0.000 description 2
- ZORQXIQZAOLNGE-UHFFFAOYSA-N 1,1-difluorocyclohexane Chemical compound FC1(F)CCCCC1 ZORQXIQZAOLNGE-UHFFFAOYSA-N 0.000 description 2
- 229920000742 Cotton Polymers 0.000 description 2
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 2
- CUFNKYGDVFVPHO-UHFFFAOYSA-N azulene Chemical compound C1=CC=CC2=CC=CC2=C1 CUFNKYGDVFVPHO-UHFFFAOYSA-N 0.000 description 2
- 229960000541 cetyl alcohol Drugs 0.000 description 2
- 235000014113 dietary fatty acids Nutrition 0.000 description 2
- NOPFSRXAKWQILS-UHFFFAOYSA-N docosan-1-ol Chemical compound CCCCCCCCCCCCCCCCCCCCCCO NOPFSRXAKWQILS-UHFFFAOYSA-N 0.000 description 2
- 230000000694 effects Effects 0.000 description 2
- 239000000194 fatty acid Substances 0.000 description 2
- 229930195729 fatty acid Natural products 0.000 description 2
- BXWNKGSJHAJOGX-UHFFFAOYSA-N hexadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCO BXWNKGSJHAJOGX-UHFFFAOYSA-N 0.000 description 2
- IPCSVZSSVZVIGE-UHFFFAOYSA-N hexadecanoic acid Chemical compound CCCCCCCCCCCCCCCC(O)=O IPCSVZSSVZVIGE-UHFFFAOYSA-N 0.000 description 2
- 230000007721 medicinal effect Effects 0.000 description 2
- GOQYKNQRPGWPLP-UHFFFAOYSA-N n-heptadecyl alcohol Natural products CCCCCCCCCCCCCCCCCO GOQYKNQRPGWPLP-UHFFFAOYSA-N 0.000 description 2
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 description 2
- 239000000244 polyoxyethylene sorbitan monooleate Substances 0.000 description 2
- 235000010483 polyoxyethylene sorbitan monopalmitate Nutrition 0.000 description 2
- 239000000249 polyoxyethylene sorbitan monopalmitate Substances 0.000 description 2
- 229920000053 polysorbate 80 Polymers 0.000 description 2
- 239000008213 purified water Substances 0.000 description 2
- 235000011069 sorbitan monooleate Nutrition 0.000 description 2
- 239000001593 sorbitan monooleate Substances 0.000 description 2
- 229940035049 sorbitan monooleate Drugs 0.000 description 2
- 235000011076 sorbitan monostearate Nutrition 0.000 description 2
- 239000001587 sorbitan monostearate Substances 0.000 description 2
- 229940035048 sorbitan monostearate Drugs 0.000 description 2
- 229960005078 sorbitan sesquioleate Drugs 0.000 description 2
- 150000005846 sugar alcohols Polymers 0.000 description 2
- HLZKNKRTKFSKGZ-UHFFFAOYSA-N tetradecan-1-ol Chemical compound CCCCCCCCCCCCCCO HLZKNKRTKFSKGZ-UHFFFAOYSA-N 0.000 description 2
- 229940058015 1,3-butylene glycol Drugs 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
- XZIIFPSPUDAGJM-UHFFFAOYSA-N 6-chloro-2-n,2-n-diethylpyrimidine-2,4-diamine Chemical compound CCN(CC)C1=NC(N)=CC(Cl)=N1 XZIIFPSPUDAGJM-UHFFFAOYSA-N 0.000 description 1
- 239000000120 Artificial Saliva Substances 0.000 description 1
- 239000004215 Carbon black (E152) Substances 0.000 description 1
- 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 1
- 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 1
- 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 1
- 239000004386 Erythritol Substances 0.000 description 1
- UNXHWFMMPAWVPI-UHFFFAOYSA-N Erythritol Natural products OCC(O)C(O)CO UNXHWFMMPAWVPI-UHFFFAOYSA-N 0.000 description 1
- 229930195725 Mannitol Natural products 0.000 description 1
- 235000021314 Palmitic acid Nutrition 0.000 description 1
- 239000002202 Polyethylene glycol Substances 0.000 description 1
- 229920001213 Polysorbate 20 Polymers 0.000 description 1
- IYFATESGLOUGBX-YVNJGZBMSA-N Sorbitan monopalmitate Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@@H](O)[C@H]1OC[C@H](O)[C@H]1O IYFATESGLOUGBX-YVNJGZBMSA-N 0.000 description 1
- 239000004147 Sorbitan trioleate Substances 0.000 description 1
- PRXRUNOAOLTIEF-ADSICKODSA-N Sorbitan trioleate Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)OC[C@@H](OC(=O)CCCCCCC\C=C/CCCCCCCC)[C@H]1OC[C@H](O)[C@H]1OC(=O)CCCCCCC\C=C/CCCCCCCC PRXRUNOAOLTIEF-ADSICKODSA-N 0.000 description 1
- 235000021355 Stearic acid Nutrition 0.000 description 1
- TVXBFESIOXBWNM-UHFFFAOYSA-N Xylitol Natural products OCCC(O)C(O)C(O)CCO TVXBFESIOXBWNM-UHFFFAOYSA-N 0.000 description 1
- IJCWFDPJFXGQBN-RYNSOKOISA-N [(2R)-2-[(2R,3R,4S)-4-hydroxy-3-octadecanoyloxyoxolan-2-yl]-2-octadecanoyloxyethyl] octadecanoate Chemical compound CCCCCCCCCCCCCCCCCC(=O)OC[C@@H](OC(=O)CCCCCCCCCCCCCCCCC)[C@H]1OC[C@H](O)[C@H]1OC(=O)CCCCCCCCCCCCCCCCC IJCWFDPJFXGQBN-RYNSOKOISA-N 0.000 description 1
- 229960004871 acetoxolone Drugs 0.000 description 1
- 150000001298 alcohols Chemical class 0.000 description 1
- 239000003242 anti bacterial agent Substances 0.000 description 1
- 230000000844 anti-bacterial effect Effects 0.000 description 1
- 235000019437 butane-1,3-diol Nutrition 0.000 description 1
- 229910052799 carbon Inorganic materials 0.000 description 1
- 125000002091 cationic group Chemical group 0.000 description 1
- 230000000052 comparative effect Effects 0.000 description 1
- 229960000735 docosanol Drugs 0.000 description 1
- LQZZUXJYWNFBMV-UHFFFAOYSA-N dodecan-1-ol Chemical compound CCCCCCCCCCCCO LQZZUXJYWNFBMV-UHFFFAOYSA-N 0.000 description 1
- UNXHWFMMPAWVPI-ZXZARUISSA-N erythritol Chemical compound OC[C@H](O)[C@H](O)CO UNXHWFMMPAWVPI-ZXZARUISSA-N 0.000 description 1
- 235000019414 erythritol Nutrition 0.000 description 1
- 229940009714 erythritol Drugs 0.000 description 1
- 239000010696 ester oil Substances 0.000 description 1
- 235000003599 food sweetener Nutrition 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 239000003205 fragrance Substances 0.000 description 1
- 235000011187 glycerol Nutrition 0.000 description 1
- 229960005150 glycerol Drugs 0.000 description 1
- 229930195733 hydrocarbon Natural products 0.000 description 1
- 150000002430 hydrocarbons Chemical class 0.000 description 1
- 230000001771 impaired effect Effects 0.000 description 1
- 150000002500 ions Chemical class 0.000 description 1
- 230000007794 irritation Effects 0.000 description 1
- 239000002649 leather substitute Substances 0.000 description 1
- 239000000594 mannitol Substances 0.000 description 1
- 235000010355 mannitol Nutrition 0.000 description 1
- HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 229940043348 myristyl alcohol Drugs 0.000 description 1
- WQEPLUUGTLDZJY-UHFFFAOYSA-N n-Pentadecanoic acid Natural products CCCCCCCCCCCCCCC(O)=O WQEPLUUGTLDZJY-UHFFFAOYSA-N 0.000 description 1
- 239000002736 nonionic surfactant Substances 0.000 description 1
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 1
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 description 1
- 239000003921 oil Substances 0.000 description 1
- 235000019198 oils Nutrition 0.000 description 1
- 229940042125 oral ointment Drugs 0.000 description 1
- 238000001139 pH measurement Methods 0.000 description 1
- 238000012856 packing Methods 0.000 description 1
- 238000010422 painting Methods 0.000 description 1
- 239000000049 pigment Substances 0.000 description 1
- 229920001223 polyethylene glycol Polymers 0.000 description 1
- 235000010486 polyoxyethylene sorbitan monolaurate Nutrition 0.000 description 1
- 239000000256 polyoxyethylene sorbitan monolaurate Substances 0.000 description 1
- 235000010989 polyoxyethylene sorbitan monostearate Nutrition 0.000 description 1
- 239000001818 polyoxyethylene sorbitan monostearate Substances 0.000 description 1
- 229920000136 polysorbate Polymers 0.000 description 1
- 229950008882 polysorbate Drugs 0.000 description 1
- 235000021003 saturated fats Nutrition 0.000 description 1
- 235000003441 saturated fatty acids Nutrition 0.000 description 1
- 150000004671 saturated fatty acids Chemical class 0.000 description 1
- 229920002545 silicone oil Polymers 0.000 description 1
- 239000000243 solution Substances 0.000 description 1
- 229940035044 sorbitan monolaurate Drugs 0.000 description 1
- 235000011071 sorbitan monopalmitate Nutrition 0.000 description 1
- 239000001570 sorbitan monopalmitate Substances 0.000 description 1
- 229940031953 sorbitan monopalmitate Drugs 0.000 description 1
- 229950011392 sorbitan stearate Drugs 0.000 description 1
- 235000019337 sorbitan trioleate Nutrition 0.000 description 1
- 229960000391 sorbitan trioleate Drugs 0.000 description 1
- 235000011078 sorbitan tristearate Nutrition 0.000 description 1
- 239000001589 sorbitan tristearate Substances 0.000 description 1
- 229960004129 sorbitan tristearate Drugs 0.000 description 1
- 239000000600 sorbitol Substances 0.000 description 1
- 229960002920 sorbitol Drugs 0.000 description 1
- 235000010356 sorbitol Nutrition 0.000 description 1
- 239000008117 stearic acid Substances 0.000 description 1
- 239000003765 sweetening agent Substances 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- TUNFSRHWOTWDNC-HKGQFRNVSA-N tetradecanoic acid Chemical compound CCCCCCCCCCCCC[14C](O)=O TUNFSRHWOTWDNC-HKGQFRNVSA-N 0.000 description 1
- 229940034610 toothpaste Drugs 0.000 description 1
- 239000000606 toothpaste Substances 0.000 description 1
- 238000012546 transfer Methods 0.000 description 1
- 235000015112 vegetable and seed oil Nutrition 0.000 description 1
- 239000008158 vegetable oil Substances 0.000 description 1
- 229920002554 vinyl polymer Polymers 0.000 description 1
- 229920003169 water-soluble polymer Polymers 0.000 description 1
- 239000000811 xylitol Substances 0.000 description 1
- 235000010447 xylitol Nutrition 0.000 description 1
- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 description 1
- 229960002675 xylitol Drugs 0.000 description 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicinal Preparation (AREA)
- Cosmetics (AREA)
Abstract
Description
本発明は、口腔内塗布用組成物に関する。 The present invention relates to a composition for oral application.
歯茎や口腔粘膜等の口腔内の患部に対し、直接塗布して用いる組成物は需要性が高く、種々のものが開発されている。 There is a high demand for compositions used by directly applying them to affected areas in the oral cavity such as gums and oral mucosa, and various compositions have been developed.
例えば、特許文献１には、陽イオン性抗菌剤、アズレン、低級１価アルコール及び水溶性ビニル系高分子を含有する口腔用軟膏組成物が開示されており、口腔バイオフィルム殺菌効果を発揮させている。また、特許文献２には、カルバゾクロムやその誘導体と水溶性高分子とを含有する口腔用組成物が開示されており、口腔内粘膜への付着性の向上を試みている。 For example, Patent Document 1 discloses an oral ointment composition containing a cationic antibacterial agent, azulene, a lower monohydric alcohol, and a water-soluble vinyl polymer, and exhibits an oral biofilm bactericidal effect. There is. Further, Patent Document 2 discloses an oral composition containing carbazochrome or a derivative thereof and a water-soluble polymer, and attempts to improve the adhesiveness to the oral mucosa.
しかしながら、口腔内の患部は、唾液によって常時湿潤しているため、上記文献に記載のいずれの組成物であっても、こうした湿潤した患部に対して充分な塗布性や付着性を発現するには至らず、さらなる改善を要する状況にある。 However, since the affected area in the oral cavity is constantly moistened by saliva, any composition described in the above-mentioned documents can be used to exhibit sufficient applicability and adhesiveness to such a moistened affected area. It has not reached the point and is in a situation where further improvement is required.
すなわち、本発明は、口腔内の患部に対して優れた塗布性及び滞留性を発現することのできる口腔内塗布用組成物に関する。 That is, the present invention relates to an intraoral application composition capable of exhibiting excellent applicability and retention on an affected portion in the oral cavity.
そこで本発明者は、種々検討したところ、水を特定量含有させ、かつ粘度を特定の範囲に調整するなか、特定のノニオン性ポリマーを特定量で含有する一方で、特定のアニオン性ポリマーの含有を制限することにより、口腔内における唾液湿潤面に対して優れた塗布性と滞留性を発現することのできる口腔内塗布用組成物が得られることを見出した。 Therefore, as a result of various studies, the present inventor has found that while containing a specific amount of water and adjusting the viscosity to a specific range, a specific nonionic polymer is contained in a specific amount, while a specific anionic polymer is contained. It has been found that by limiting the above, a composition for oral application capable of exhibiting excellent applicability and retention on a saliva-wet surface in the oral cavity can be obtained.
したがって、本発明は、次の成分（Ａ）〜（Ｃ）：
（Ａ）プルラン、ポリビニルピロリドン、及びヒドロキシプロピルメチルセルロースから選ばれる１種又は２種以上のノニオン性ポリマー ０．０１質量％以上１０質量％以下
（Ｂ）カルボキシビニルポリマー、カルボキシメチルセルロースナトリウム、キサンタンガム、及びポリアクリル酸ナトリウムから選ばれる１種又は２種以上のアニオン性ポリマー ０．５質量％未満
（Ｃ）水 ３０質量％以上９５質量％以下
を含有し、かつ
２５℃における粘度が５００ｄＰａ・ｓ以上１００００ｄＰａ・ｓ以下である口腔内塗布用組成物を提供するものである。
Therefore, in the present invention, the following components (A) to (C):
(A) One or more nonionic polymers selected from pullulan, polyvinylpyrrolidone, and hydroxypropylmethyl cellulose 0.01% by mass or more and 10% by mass or less (B) Carboxyvinyl polymer, sodium carboxymethyl cellulose, xanthan gum, and poly One or more anionic polymers selected from sodium acrylate Less than 0.5% by mass (C) Water Contains 30% by mass or more and 95% by mass or less, and has a viscosity at 25 ° C. of 500 dPa · s or more and 10,000 dPa ·. It provides a composition for oral application which is less than or equal to s.
本発明の口腔内塗布用組成物によれば、唾液によって常時湿潤している状態の歯茎や口腔粘膜等の患部に対し、良好な展延性とともに高い付着性を示して、優れた塗布性を発揮するため、使用者に塗り易さを実感させることができる。また、本発明の口腔内塗布用組成物を歯茎や口腔粘膜等の患部に塗布した後においても、高い滞留性を発現することができるため、組成物による作用を長時間にわたり持続させることが可能である。 According to the composition for oral application of the present invention, it exhibits excellent malleability and high adhesiveness to affected areas such as gums and oral mucosa which are constantly moistened by saliva, and exhibits excellent applicability. Therefore, the user can feel the ease of painting. Further, even after the composition for oral application of the present invention is applied to an affected area such as gums and oral mucosa, high retention can be exhibited, so that the action of the composition can be maintained for a long period of time. Is.
なお、「展延性」とは、組成物を患部に塗布した際、組成物の一部が偏在する、いわゆるダマが生じることなく、組成物が塗布方向に沿いながら患部の面上で均一に広がって延びる性質を意味する。また「付着性」とは、組成物を歯茎や口腔粘膜等の湿潤患部に塗布した際、患部に密着して留まる性質を意味する。そして、「塗布性」とは、これら「展延性」と「付着性」を兼ね備えた性質を意味する。
さらに、「滞留性」とは、患部に塗布された組成物が、経時的に安定して患部に留まり残存する性質を意味する。
そして、「口腔内塗布用組成物」とは、歯磨組成物のように歯面を刷掃するための組成物とは異なり、歯茎や口腔粘膜等の湿潤患部に塗り込むように、直接塗布するための組成物であり、また必ずしも適用後のすすぎを要しない組成物である。
“Ductile” means that when the composition is applied to the affected area, a part of the composition is not unevenly distributed, so-called lumps do not occur, and the composition spreads uniformly on the surface of the affected area while following the application direction. Means the property of extending. Further, "adhesiveness" means a property of staying in close contact with the affected area when the composition is applied to a wet affected area such as gums and oral mucosa. The "applicability" means a property having both "ductility" and "adhesiveness".
Further, the “retention” means a property that the composition applied to the affected area remains stable over time and remains in the affected area.
The "composition for oral application" is different from the composition for wiping the tooth surface like a toothpaste composition, and is directly applied so as to be applied to a wet affected area such as gums and oral mucosa. It is a composition for this purpose, and does not necessarily require rinsing after application.
以下、本発明について詳細に説明する。
本発明の口腔内塗布用組成物は、成分（Ａ）として、プルラン、ポリビニルピロリドン、及びヒドロキシプロピルメチルセルロースから選ばれる１種又は２種以上のノニオン性ポリマーを０．０１質量％以上１０質量％以下含有する。このように、特定のノニオン性ポリマーを特定量で含有することにより、所定量の水（Ｃ）が存在するなか、後述するアニオン性ポリマー（Ｂ）の含有が制限されることも相まって適度な粘度を発現しつつ、歯茎や口腔粘膜等の湿潤患部に塗布した際、指又は綿棒や指サック等の塗布用器具の塗布面に組成物のダマが生じたりするのを有効に抑制することができる。
したがって、指や塗布用器具の塗布面に組成物のダマを生じさせることなく、湿潤患部において、均一に広がり延び、良好な塗布性を発揮することができるとともに、塗布後においても患部に長時間安定して残存するという、高い滞留性を発現することができる。
Hereinafter, the present invention will be described in detail.
The composition for oral application of the present invention contains one or more nonionic polymers selected from pullulan, polyvinylpyrrolidone, and hydroxypropylmethylcellulose as the component (A) in an amount of 0.01% by mass or more and 10% by mass or less. contains. As described above, by containing the specific nonionic polymer in a specific amount, the content of the anionic polymer (B), which will be described later, is restricted in the presence of a predetermined amount of water (C), and the viscosity is appropriate. When applied to a wet affected area such as the gums or oral mucosa, it is possible to effectively suppress the occurrence of lumps in the composition on the application surface of a finger or an application device such as a cotton swab or a finger cot. ..
Therefore, the composition can be spread evenly in the wet affected area without causing lumps on the application surface of the finger or the application device, and good applicationability can be exhibited, and the affected area can be applied for a long time even after application. It is possible to exhibit a high retention property that it remains stable.
成分（Ａ）のノニオン性ポリマーは、プルラン、ポリビニルピロリドン、及びヒドロキシプロピルメチルセルロースから選ばれる１種又は２種以上であって、口腔内の患部への塗布性を高める観点からはポリビニルピロリドンが好ましく、口腔内の患部への付着性及び滞留性を高める観点から、プルラン、及びポリビニルピロリドンから選ばれる１種又は２種が好ましく、或いはプルラン及びポリビニルピロリドンの両方を含有してもよい。 The nonionic polymer of the component (A) is one or more selected from pullulan, polyvinylpyrrolidone, and hydroxypropylmethylcellulose, and polyvinylpyrrolidone is preferable from the viewpoint of enhancing the applicability to the affected area in the oral cavity. From the viewpoint of enhancing the adhesion and retention in the affected area in the oral cavity, one or two selected from pullulan and polyvinylpyrrolidone are preferable, or both pullulan and polyvinylpyrrolidone may be contained.
成分（Ａ）の含有量は、口腔内の患部への付着性及び滞留性を高める観点から、本発明の口腔内塗布用組成物中に、０．０１質量％以上であって、好ましくは０．１質量％以上であり、より好ましくは０．５質量％以上であり、さらに好ましくは０．７質量％以上であり、さらに好ましくは１質量％以上であり、さらに好ましくは１．１質量％以上である。また、成分（Ａ）の含有量は、患部に塗布した際におけるダマの発生を良好に抑制して、優れた展延性を発現する観点から、本発明の口腔内塗布用組成物中に、１０質量％以下であって、好ましくは７質量％以下であり、より好ましくは５質量％以下であり、さらに好ましくは２質量％以下である。そして、成分（Ａ）の含有量は、本発明の口腔内塗布用組成物中に、０．０１質量％以上１０質量％以下であって、好ましくは０．１〜７質量％であり、より好ましくは０．５〜５質量％であり、さらに好ましくは０．７〜４質量％であり、さらに好ましくは１〜３．５質量％であり、さらに好ましくは１．１〜２質量である。 The content of the component (A) is 0.01% by mass or more, preferably 0, in the composition for oral application of the present invention from the viewpoint of enhancing the adhesion and retention in the affected area in the oral cavity. .1% by mass or more, more preferably 0.5% by mass or more, still more preferably 0.7% by mass or more, still more preferably 1% by mass or more, still more preferably 1.1% by mass. That is all. Further, the content of the component (A) is 10 in the composition for oral application of the present invention from the viewpoint of satisfactorily suppressing the occurrence of lumps when applied to the affected area and exhibiting excellent ductility. It is 0% by mass or less, preferably 7% by mass or less, more preferably 5% by mass or less, and further preferably 2% by mass or less. The content of the component (A) in the composition for oral application of the present invention is 0.01% by mass or more and 10% by mass or less, preferably 0.1 to 7% by mass, and more. It is preferably 0.5 to 5% by mass, more preferably 0.7 to 4% by mass, still more preferably 1 to 3.5% by mass, still more preferably 1.1 to 2% by mass.
本発明の口腔内塗布用組成物は、成分（Ｂ）として、カルボキシビニルポリマー、カルボキシメチルセルロースナトリウム、キサンタンガム、及びポリアクリル酸ナトリウムから選ばれる１種又は２種以上のアニオン性ポリマーを０．５質量％未満含有する。すなわち、本発明の口腔内塗布用組成物における成分（Ｂ）の含有量は、０質量％超０．５質量％未満であるか、或いは本発明の口腔内塗布用組成物は、成分（Ｂ）を含有しない。このように、特定のアニオン性ポリマーの含有量を制限することにより、上記成分（Ａ）による優れた展延性や付着性の発現を阻害することなく、良好な塗布性と高い滞留性の両立を図ることに大いに寄与することができる。 The composition for oral application of the present invention contains 0.5 mass of one or more anionic polymers selected from carboxyvinyl polymer, sodium carboxymethyl cellulose, xanthan gum, and sodium polyacrylate as the component (B). Contains less than%. That is, the content of the component (B) in the composition for oral application of the present invention is more than 0% by mass and less than 0.5% by mass, or the composition for oral application of the present invention contains the component (B). ) Is not included. By limiting the content of the specific anionic polymer in this way, both good coatability and high retention can be achieved without impeding the development of excellent ductility and adhesiveness by the component (A). It can greatly contribute to the planning.
成分（Ｂ）の含有量は、優れた塗布性と良好な滞留性とを兼ね備える観点から、本発明の口腔内塗布用組成物中に、０．５質量％未満であって、好ましくは０．４質量％以下であり、より好ましくは０．２７質量％以下であり、さらに好ましくは０．２質量％以下であり、よりさらに好ましくは０．０８質量％以下であり、よりさらに好ましくは０．０１質量％以下であり、ことさら好ましいのは、実質０質量％、すなわち、本発明の口腔内塗布用組成物は、成分（Ｂ）を含有しない。 The content of the component (B) is less than 0.5% by mass, preferably 0. In the composition for oral application of the present invention, from the viewpoint of having both excellent coatability and good retention. It is 4% by mass or less, more preferably 0.27% by mass or less, further preferably 0.2% by mass or less, still more preferably 0.08% by mass or less, still more preferably 0. It is 01% by mass or less, and more preferably 0% by mass, that is, the composition for oral application of the present invention does not contain the component (B).
成分（Ｂ）の含有量と成分（Ａ）の含有量との質量比（（Ｂ）／（Ａ））は、優れた塗布性と滞留性とを良好に兼ね備える観点から、好ましくは０．８以下であり、より好ましくは０．４以下であり、さらに好ましくは０．２５以下であり、さらに好ましくは０．２２以下であり、よりさらに好ましくは、本発明の口腔内塗布用組成物が成分（Ｂ）を含有しない場合である、すなわち、成分（Ｂ）の含有量と成分（Ａ）の含有量との質量比（（Ｂ）／（Ａ））が０である。 The mass ratio ((B) / (A)) of the content of the component (B) to the content of the component (A) is preferably 0.8 from the viewpoint of having excellent coatability and retention. The following, more preferably 0.4 or less, still more preferably 0.25 or less, still more preferably 0.22 or less, and even more preferably, the composition for oral application of the present invention is a component. This is the case where (B) is not contained, that is, the mass ratio ((B) / (A)) of the content of the component (B) to the content of the component (A) is 0.
本発明の口腔内塗布用組成物は、成分（Ｃ）として、水を３０質量％以上９５質量％以下含有する。これにより、上記各成分を良好に分散又は溶解させつつ、口腔内への適用後における口腔内塗布用組成物の唾液との相溶性も高め、優れた塗布性と滞留性の発現に寄与することができる。 The composition for oral application of the present invention contains 30% by mass or more and 95% by mass or less of water as the component (C). As a result, while satisfactorily dispersing or dissolving each of the above components, the compatibility of the composition for oral application with saliva after application to the oral cavity is also enhanced, which contributes to the development of excellent coatability and retention. Can be done.
成分（Ｃ）の含有量は、本発明の口腔内塗布用組成物中に、３０質量％以上であって、好ましくは４０質量％以上であり、より好ましくは４５質量％以上であり、さらに好ましくは５０質量％以上であり、９５質量％以下であって、好ましくは９０質量％以下であり、より好ましくは８０質量％以下であり、さらに好ましくは７５質量％以下であり、よりさらに好ましくは６０質量％以下である。
なお、本発明における成分（Ｃ）の水とは、口腔内塗布用組成物に直接配合した精製水等だけでなく、配合した各成分に含まれる水分をも含む、口腔内塗布用組成物中に含まれる全水分を意味する。
The content of the component (C) in the composition for oral application of the present invention is 30% by mass or more, preferably 40% by mass or more, more preferably 45% by mass or more, and further preferably. Is 50% by mass or more, 95% by mass or less, preferably 90% by mass or less, more preferably 80% by mass or less, still more preferably 75% by mass or less, still more preferably 60. It is mass% or less.
The water of the component (C) in the present invention is not only purified water directly blended in the composition for oral application but also water contained in each of the blended components in the composition for oral application. Means the total water content of.
本発明の口腔内塗布用組成物は、さらに薬効成分（Ｄ）を含有することができる。かかる成分（Ｄ）を含有することにより、本発明の口腔内塗布用組成物が発現する優れた塗布性と滞留性により、患部の広きにわたり、所望の薬効を持続的にもたらすことができる。 The composition for oral application of the present invention can further contain the medicinal ingredient (D). By containing such a component (D), the excellent applicability and retention property developed by the composition for oral application of the present invention can sustainably bring about a desired medicinal effect over a wide area of the affected area.
かかる成分（Ｄ）としては、具体的には、グリチルレチン酸、トコフェロール酢酸エステル、ヒノキチオール、イソプロピルメチルフェノール、銅クロロフィリンナトリウム、及びカルバゾクロムから選択される１種又は２種以上が挙げられる。なかでも、グリチルレチン酸及びトコフェロール酢酸エステルから選択される１種又は２種以上が好ましく、少なくとも、グリチルレチン酸を含むことが好ましい、或いは、両方含むのが好ましい。 Specific examples of such component (D) include one or more selected from glycyrrhetinic acid, tocopherol acetate, hinokitiol, isopropylmethylphenol, sodium copper chlorophyllin, and carbazochrome. Among them, one or more selected from glycyrrhetinic acid and tocopherol acetate is preferable, and at least glycyrrhetinic acid is preferably contained, or both are preferably contained.
成分（Ｄ）の含有量は、口腔内の患部における諸症状の緩和効果の観点から、本発明の口腔内塗布用組成物中に、好ましくは０．０１質量％以上であり、より好ましくは０．０２質量％以上であり、さらに好ましくは０．１質量％以上であり、好ましくは３．５質量％以下であり、より好ましくは３質量％以下であり、さらに好ましくは２．５質量％以下である。 The content of the component (D) is preferably 0.01% by mass or more, more preferably 0, in the composition for oral application of the present invention from the viewpoint of alleviating various symptoms in the affected area in the oral cavity. It is 0.02% by mass or more, more preferably 0.1% by mass or more, preferably 3.5% by mass or less, more preferably 3% by mass or less, still more preferably 2.5% by mass or less. Is.
本発明の口腔内塗布用組成物は、さらにノニオン界面活性剤（Ｅ）を含有することができる。かかる成分（Ｅ）を含有することにより、口腔内塗布用組成物の患部への高い付着性を確保することができる。 The composition for oral application of the present invention can further contain a nonionic surfactant (E). By containing such a component (E), high adhesion of the composition for oral application to the affected area can be ensured.
かかる成分（Ｅ）としては、具体的には、モノカプリン酸ソルビタン、モノウンデシル酸ソルビタン、モノラウリン酸ソルビタン、モノトリデシル酸ソルビタン、モノミリスチン酸ソルビタン、モノパルミチン酸ソルビタン、モノオレイン酸ソルビタン、トリオレイン酸ソルビタン、テトラオレイン酸ソルビタン、セスキオレイン酸ソルビタン、モノステアリン酸ソルビタン、及びトリステアリン酸ソルビタン等のソルビタン脂肪酸エステル；モノラウリン酸ポリオキシエチレンソルビタン、モノミリスチン酸ポリオキシエチレンソルビタン、モノパルミチン酸ポリオキシエチレンソルビタン、モノステアリン酸ポリオキシエチレンソルビタン、及びモノオレイン酸ポリオキシエチレンソルビタン等のポリオキシエチレンソルビタン脂肪酸エステルから選ばれる１種又は２種以上が挙げられる。
なかでも、高い付着性を確保する観点から、モノオレイン酸ソルビタン、セスキオレイン酸ソルビタン、モノステアリン酸ソルビタン、モノパルミチン酸ポリオキシエチレンソルビタン、モノステアリン酸ポリオキシエチレンソルビタン及びモノオレイン酸ポリオキシエチレンソルビタンから選ばれる１種又は２種以上が好ましい。
Specific examples of the component (E) include sorbitan monocaprate, sorbitan monoundecylate, sorbitan monolaurate, sorbitan monotridecylate, sorbitan monomyristate, sorbitan monopalmitate, sorbitan monooleate, and sorbitan trioleate. Polysorbate fatty acid esters such as sorbitan tetraoleate, sorbitan sesquioleate, sorbitan monostearate, and sorbitan tristearate; polyoxyethylene sorbitan monolaurate, polyoxyethylene sorbitan monomyristate, polyoxyethylene sorbitan monopalmitate, mono One or more selected from polyoxyethylene sorbitan sorbitan fatty acid esters such as polyoxyethylene sorbitan stearate and polyoxyethylene sorbitan monooleate can be mentioned.
Among them, from the viewpoint of ensuring high adhesion, sorbitan monooleate, sorbitan sesquioleate, sorbitan monostearate, polyoxyethylene sorbitan monopalmitate, polyoxyethylene sorbitan monostearate and polyoxyethylene sorbitan monooleate One or more selected from the above is preferable.
成分（Ｅ）の含有量は、良好な使用感を確保する観点から、本発明の口腔内塗布用組成物中に、好ましくは０．１質量％以上であり、より好ましくは０．５質量％以上であり、さらに好ましくは１質量％以上であり、好ましくは１０質量％以下であり、より好ましくは５質量％以下であり、さらに好ましくは３質量％以下である。 The content of the component (E) is preferably 0.1% by mass or more, more preferably 0.5% by mass, in the composition for oral application of the present invention from the viewpoint of ensuring a good usability. It is more preferably 1% by mass or more, preferably 10% by mass or less, more preferably 5% by mass or less, still more preferably 3% by mass or less.
本発明の口腔内塗布用組成物は、さらに炭素数１２以上２２以下の高級アルコール（Ｆ）を含有することができる。かかる成分（Ｆ）を含有することにより、本発明の口腔内塗布用組成物の展延性を一層高めることができる。 The composition for oral application of the present invention can further contain a higher alcohol (F) having 12 or more and 22 or less carbon atoms. By containing such a component (F), the ductility of the composition for oral application of the present invention can be further enhanced.
かかる成分（Ｆ）としては、セタノール、ステアリルアルコール、ラウリルアルコール、ミリスチルアルコール、及びベヘニルアルコールから選ばれる１種又は２種以上が挙げられる。なかでも、塗布時における組成物の不要なダマの発生を有効に抑制する観点から、炭素数１４以上２０以下の高級アルコールが好ましく、セタノール、及びステアリルアルコールから選ばれる１種又は２種がより好ましい。 Examples of such component (F) include one or more selected from cetanol, stearyl alcohol, lauryl alcohol, myristyl alcohol, and behenyl alcohol. Among them, higher alcohols having 14 to 20 carbon atoms are preferable, and one or two selected from cetanol and stearyl alcohol are more preferable, from the viewpoint of effectively suppressing the generation of unnecessary lumps in the composition at the time of application. ..
成分（Ｆ）の含有量は、適度な粘度の付与に寄与し、塗布時における組成物の不要な転写やダマの発生を有効に抑制する観点から、本発明の口腔用組成物中に、好ましくは０．５質量％以上であり、より好ましくは１質量％以上であって、さらに好ましくは３質量％以上であり、好ましくは２０質量％以下であり、より好ましくは１５質量％以下であり、さらに好ましくは１０質量％以下である。そして、成分（Ｆ）の含有量は、本発明の口腔用組成物中に、好ましくは０．５〜２０質量％であり、より好ましくは１〜１５質量％であり、さらに好ましくは３〜１０質量％である。 The content of the component (F) is preferable in the oral composition of the present invention from the viewpoint of contributing to imparting an appropriate viscosity and effectively suppressing the generation of unnecessary transfer and lumps of the composition at the time of application. Is 0.5% by mass or more, more preferably 1% by mass or more, further preferably 3% by mass or more, preferably 20% by mass or less, and more preferably 15% by mass or less. More preferably, it is 10% by mass or less. The content of the component (F) is preferably 0.5 to 20% by mass, more preferably 1 to 15% by mass, and further preferably 3 to 10% by mass in the oral composition of the present invention. It is mass%.
本発明の口腔内塗布用組成物は、塗布時における組成物の不要なダマの発生を有効に抑制及び不要な刺激性の発現を回避する観点から、エタノールの含有を制限するのが好ましい。具体的には、エタノールの含有量は、本発明の口腔内塗布用組成物中に、好ましくは３質量％未満であり、より好ましくは２質量％以下であり、さらに好ましくは１質量％以下であり、或いは本発明の口腔内塗布用組成物は、エタノールを含有しないのが好ましい。 The composition for oral application of the present invention preferably limits the content of ethanol from the viewpoint of effectively suppressing the generation of unnecessary lumps in the composition at the time of application and avoiding the development of unnecessary irritation. Specifically, the content of ethanol in the composition for oral application of the present invention is preferably less than 3% by mass, more preferably 2% by mass or less, still more preferably 1% by mass or less. Yes, or the composition for oral application of the present invention preferably does not contain ethanol.
本発明の口腔内塗布用組成物は、塗布時における組成物の不要なダマの発生を有効に抑制する観点から、１，３ブチレングリコール、プロピレングリコール、ポリエチレングリコール、グリセリン、ソルビトール、キシリトール、エリスリトール、還元パラチノース、及びマンニトール等の多価アルコールを含有させることができる。
多価アルコールの含有量は、適度な粘度の付与に寄与し、塗布時における組成物の不要なダマの発生を有効に抑制する観点から、本発明の口腔用組成物中に、好ましくは５〜５０質量％であり、より好ましくは１０〜４０質量％であり、さらに好ましくは１５〜３０質量％である。
The composition for oral application of the present invention contains 1,3 butylene glycol, propylene glycol, polyethylene glycol, glycerin, sorbitol, xylitol, and erythritol from the viewpoint of effectively suppressing the generation of unnecessary lumps in the composition during application. Polyhydric alcohols such as reduced palatinose and mannitol can be contained.
The content of the polyhydric alcohol is preferably 5 to 5 in the oral composition of the present invention from the viewpoint of contributing to imparting an appropriate viscosity and effectively suppressing the generation of unnecessary lumps in the composition at the time of application. It is 50% by mass, more preferably 10 to 40% by mass, and even more preferably 15 to 30% by mass.
本発明の口腔内塗布用組成物は、塗布時における組成物の不要なダマの発生を有効に抑制する観点から、ミリスチン酸、パルミチン酸、ステアリン酸等の炭素数１４〜１８の飽和脂肪酸を含有させることができる。
炭素数１４〜１８の飽和脂肪の含有量は、適度な粘度の付与に寄与し、塗布時における組成物の不要なダマの発生を有効に抑制する観点から、本発明の口腔用組成物中に、好ましくは０．２〜５質量％であり、より好ましくは０．４〜３質量％であり、さらに好ましくは０．８〜２質量％である。
The composition for oral application of the present invention contains saturated fatty acids having 14 to 18 carbon atoms such as myristic acid, palmitic acid, and stearic acid from the viewpoint of effectively suppressing the generation of unnecessary lumps in the composition at the time of application. Can be made to.
The content of saturated fat having 14 to 18 carbon atoms contributes to the impartation of appropriate viscosity, and from the viewpoint of effectively suppressing the generation of unnecessary lumps in the composition at the time of application, it is contained in the oral composition of the present invention. , It is preferably 0.2 to 5% by mass, more preferably 0.4 to 3% by mass, and further preferably 0.8 to 2% by mass.
本発明の口腔内塗布用組成物は、本発明の効果を阻害しない範囲で、上記成分以外の成分として、炭化水素油、エステル油、植物油、シリコーン油等の油性成分；水酸化ナトリウム等のｐＨ調整剤；香料；甘味料；色素等を含有することができる。 The composition for oral application of the present invention contains oily components such as hydrocarbon oil, ester oil, vegetable oil, silicone oil and the like; pH such as sodium hydroxide and the like as components other than the above components as long as the effects of the present invention are not impaired. It can contain a regulator; a fragrance; a sweetener; a pigment and the like.
本発明の口腔用組成物の２５℃におけるｐＨは、本発明の口腔内塗布用組成物の長時間にわたる使用を容易にする観点から、好ましくは５以上であり、より好ましくは５．５以上であり、さらに好ましくは６．２以上であり、好ましくは１０．５以下であり、より好ましくは１０以下であり、さらに好ましくは９．５以下である。そして、本発明の口腔用組成物の２５℃におけるｐＨは、好ましくは５〜１０．５であり、より好ましくは５．５〜１０であり、さらに好ましくは６．２〜９．５である。 The pH of the oral composition of the present invention at 25 ° C. is preferably 5 or more, more preferably 5.5 or more, from the viewpoint of facilitating the use of the composition for oral application of the present invention for a long period of time. Yes, more preferably 6.2 or more, preferably 10.5 or less, more preferably 10 or less, still more preferably 9.5 or less. The pH of the oral composition of the present invention at 25 ° C. is preferably 5 to 10.5, more preferably 5.5 to 10, and even more preferably 6.2 to 9.5.
本発明の口腔内塗布用組成物の２５℃における粘度は、良好な展延性と付着性を発現して、優れた塗布性をもたらす観点から、好ましくは５００ｄＰａ・ｓ以上であり、より好ましくは８００ｄＰａ・ｓ以上であり、さらに好ましくは１５００ｄＰａ・ｓ以上であり、さらに好ましくは１７５０ｄＰａ・ｓ以上であり、好ましくは１００００ｄＰａ・ｓ以下であり、より好ましくは７０００ｄＰａ・ｓ以下であり、さらに好ましくは５０００ｄＰａ・ｓ以下であり、さらに好ましくは３０００ｄＰａ・ｓ以下である。
なお、かかる粘度は、粘度測定用の容器に詰め、２５℃の恒温器で２４時間保存した後、ヘリパス型粘度計（ＶＩＳＣＯＭＥＴＥＲ ＴＶＢ−１０ 東機産業株式会社製）を用いて、測定温度を２５℃とし、ロータＴ−Ｃ、回転数２．５ｒ／ｍｉｎ、１分間の測定条件により測定することができる。
The viscosity of the composition for oral application of the present invention at 25 ° C. is preferably 500 dPa · s or more, more preferably 800 dPa, from the viewpoint of exhibiting good spreadability and adhesiveness and providing excellent coatability. · S or more, more preferably 1500 dPa · s or more, further preferably 1750 dPa · s or more, preferably 10000 dPa · s or less, more preferably 7000 dPa · s or less, still more preferably 5000 dPa · s or more. It is s or less, more preferably 3000 dPa · s or less.
The viscosity is measured by packing it in a container for measuring viscosity, storing it in a thermostat at 25 ° C. for 24 hours, and then using a helipas-type viscometer (VISCOMETER TVB-10 manufactured by Toki Sangyo Co., Ltd.) to measure the temperature by 25. The temperature is set to ° C., and the measurement can be performed under the measurement conditions of the rotor TC, the rotation speed of 2.5 r / min, and 1 minute.
本発明の口腔内塗布用組成物を使用する際、指先又は綿棒や指サック等の塗布用器具に直接組成物を載置した後、口腔内の所望の患部に塗布すればよい。本発明の口腔内塗布用組成物がもたらす効果を充分に享受するには、患部に塗布した後、すすぎをしないのがよい。特に、本発明の口腔内塗布用組成物が薬効成分（Ｄ）を含有する場合、充分な薬効をもたらすのに適した使用態様である。 When the composition for oral application of the present invention is used, the composition may be placed directly on a fingertip or an application device such as a cotton swab or a finger cot, and then applied to a desired affected area in the oral cavity. In order to fully enjoy the effects of the composition for oral application of the present invention, it is preferable not to rinse after applying to the affected area. In particular, when the composition for oral application of the present invention contains the medicinal ingredient (D), it is a mode of use suitable for bringing about a sufficient medicinal effect.
以下、本発明について、実施例に基づき具体的に説明する。なお、表中に特に示さない限り、各成分の含有量は質量％を示す。 Hereinafter, the present invention will be specifically described based on examples. Unless otherwise specified in the table, the content of each component indicates mass%.
［実施例１〜１７、比較例１〜６］
表１、２及び３に示す処方にしたがって、各口腔内塗布用組成物を製造した。
得られた口腔内塗布用組成物を用い、下記方法にしたがって測定及び評価を行った。
結果を表１〜３に示す。なお、全ての口腔内塗布用組成物のｐＨは９であった。
[Examples 1 to 17, Comparative Examples 1 to 6]
Each composition for oral application was produced according to the formulations shown in Tables 1, 2 and 3.
Using the obtained composition for oral application, measurement and evaluation were carried out according to the following method.
The results are shown in Tables 1-3. The pH of all the compositions for oral application was 9.
《ｐＨの測定》
各組成物５ｇに、精製水４５ｍＬを加え、よく振り混ぜた液（２５℃）について、ｐＨメーター（ＨＯＲＩＢＡ ＬＡＱＵＡ ｐＨ／ＩＯＮ ＭＥＴＥＲ Ｆ５３；９６１５Ｓ ＪＦ１５（株式会社堀場製作所製））を用いてｐＨを測定した。
<< Measurement of pH >>
45 mL of purified water was added to 5 g of each composition, and the pH of the well-shaken solution (25 ° C.) was measured using a pH meter (HORIBA LAQUA pH / ION METER F53; 9615S JF15 (manufactured by HORIBA, Ltd.)). bottom.
《展延性の評価》
口腔内塗布用組成物０．３ｇを指に取り、人工唾液１００μＬで均一に濡らした人工皮革（モデル歯茎）に約３０ｇ圧で往復１０回塗り込み、組成物の状態を目視により確認し、下記基準にしたがって展延性の評価を行った。
Ａ：ダマがなく均一に広がった
Ｂ：ダマはなくやや均一に広がった
Ｃ：わずかにダマが観察され均一ではない
Ｄ：均一ではなく小さなダマが観察された
Ｅ：均一ではなく大きなダマが観察された
<< Evaluation of malleability >>
Take 0.3 g of the composition for oral application with a finger and apply it to artificial leather (model gum) uniformly moistened with 100 μL of artificial saliva at a pressure of about 30 g 10 times, and visually check the state of the composition. The spreadability was evaluated according to the criteria.
A: No lumps and spread uniformly B: No lumps and spreads slightly uniformly C: Slightly lumps are observed and not uniform D: Non-uniform and small lumps are observed E: Non-uniform and large lumps are observed Was done
《歯茎への付着性の評価》
口腔内塗布用組成物０．３ｇを指に取り、歯茎に塗布した直後、指に付着した組成物を全量回収して組成物重量を測定した。次いで、塗布前との差分を求めて歯茎への付着率（％）を算出し、下記基準にしたがって歯茎への付着性の評価の指標とした。
なお、付着率は、専門パネラー５名の平均値とした。
Ａ：平均８５％以上
Ｂ：平均７５％以上８５％未満
Ｃ：平均６５％以上７５％未満
Ｄ：平均５５％以上６５％未満
Ｅ：平均５５％未満
<< Evaluation of adhesion to gums >>
Immediately after taking 0.3 g of the composition for oral application on a finger and applying it to the gums, the entire amount of the composition adhering to the finger was collected and the weight of the composition was measured. Next, the difference from before application was obtained to calculate the adhesion rate (%) to the gums, which was used as an index for evaluating the adhesion to the gums according to the following criteria.
The adhesion rate was the average value of 5 specialized panelists.
A: Average 85% or more B: Average 75% or more and less than 85% C: Average 65% or more and less than 75% D: Average 55% or more and less than 65% E: Average less than 55%
《滞留性の評価》
口腔内塗布用組成物０．３ｇを指に取り、歯茎に塗布してから１５分経過した後、専門パネラー５名で、歯茎への組成物の滞留性（残留感）を官能評価し、下記の評点に基づき点数化した。次いで、５名の平均点数を求め、下記の評価基準に基づきＡ〜Ｅの５段階で評価した。
＜評点＞
５点：歯茎への組成物の滞留をかなり強く感じる
４点：歯茎への組成物の滞留を強く感じる
３点：歯茎への組成物の滞留を感じる
２点：歯茎への組成物の滞留をやや感じる
１点：歯茎への滞留を感じない
＜評価基準＞
Ａ：平均３．０点以上
Ｂ：平均２．５点以上３．０点未満
Ｃ：平均２．０点以上２．５点未満
Ｄ：平均１．５点以上２．０点未満
Ｅ：平均１．５点未満
<< Evaluation of retention >>
After 15 minutes have passed since 0.3 g of the composition for oral application was taken on a finger and applied to the gums, the retention (residual feeling) of the composition on the gums was sensory-evaluated by five specialized panelists, and the following was performed. Scored based on the score of. Next, the average score of 5 persons was calculated and evaluated on a scale of A to E based on the following evaluation criteria.
<Score>
5 points: Feel the composition staying in the gums quite strongly 4 points: Feel the composition staying in the gums strongly 3 points: Feel the composition staying in the gums 2: Feel the composition staying in the gums Slightly feel 1 point: Do not feel retention in the gums <Evaluation criteria>
A: Average 3.0 points or more B: Average 2.5 points or more and less than 3.0 points C: Average 2.0 points or more and less than 2.5 points D: Average 1.5 points or more and less than 2.0 points E: Average Less than 1.5 points
Claims (5)
（Ａ）プルラン、ポリビニルピロリドン、及びヒドロキシプロピルメチルセルロースから選ばれる１種又は２種以上のノニオン性ポリマー ０．０１質量％以上１０質量％以下
（Ｂ）カルボキシビニルポリマー、カルボキシメチルセルロースナトリウム、キサンタンガム、及びポリアクリル酸ナトリウムから選ばれる１種又は２種以上のアニオン性ポリマー ０．５質量％未満
（Ｃ）水 ３０質量％以上９５質量％以下
を含有し、かつ
２５℃における粘度が５００ｄＰａ・ｓ以上１００００ｄＰａ・ｓ以下である口腔内塗布用組成物。 The following components (A) to (C):
(A) One or more nonionic polymers selected from pullulan, polyvinylpyrrolidone, and hydroxypropylmethyl cellulose 0.01% by mass or more and 10% by mass or less (B) Carboxyvinyl polymer, sodium carboxymethyl cellulose, xanthan gum, and poly One or more anionic polymers selected from sodium acrylate Less than 0.5% by mass (C) Water Contains 30% by mass or more and 95% by mass or less, and has a viscosity at 25 ° C. of 500 dPa · s or more and 10,000 dPa ·. A composition for intraoral application, which is s or less.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2020072167A JP2021169415A (en) | 2020-04-14 | 2020-04-14 | Composition for intraoral application |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2020072167A JP2021169415A (en) | 2020-04-14 | 2020-04-14 | Composition for intraoral application |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| JP2021169415A true JP2021169415A (en) | 2021-10-28 |
Family
ID=78150017
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020072167A Pending JP2021169415A (en) | 2020-04-14 | 2020-04-14 | Composition for intraoral application |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JP2021169415A (en) |
-
2020
- 2020-04-14 JP JP2020072167A patent/JP2021169415A/en active Pending
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP4183830B2 (en) | Alcohol-based antimicrobial composition having a cosmetic appearance | |
| WO2016031461A1 (en) | Oral composition for alleviation of dentin hypersensitivity | |
| JP6751027B2 (en) | Oral care prescription system supplying amorphous calcium phosphate | |
| JP5179626B2 (en) | Dentifrice composition | |
| JP5825053B2 (en) | Liquid-based sweat deodorant composition | |
| JP5276887B2 (en) | Dentifrice composition | |
| JP6851767B2 (en) | Oral composition | |
| WO2008028003A2 (en) | Denture care composition | |
| JP6432307B2 (en) | Aqueous gel composition for tooth surface application | |
| JP2021169415A (en) | Composition for intraoral application | |
| JP6715799B2 (en) | Oral composition | |
| JP2007001954A (en) | Toothpaste composition | |
| JP7138029B2 (en) | Tongue cleaning transparent gel composition and tongue cleaning method using the same | |
| JP7423937B2 (en) | Tongue cleaning composition and tongue cleaning method | |
| JP7404796B2 (en) | Composition for wearing dentures and method for wearing dentures | |
| JP3961479B2 (en) | Liquid oral composition | |
| JP7379013B2 (en) | Oral composition | |
| JP7103355B2 (en) | Toothpaste composition | |
| JP6917192B2 (en) | Oral composition | |
| JP2980771B2 (en) | Transparent liquid oral composition | |
| JP2006241622A (en) | Composition for treating protein fiber | |
| JP2020105164A (en) | Denture mounting composition and denture mounting method | |
| JP2023094685A (en) | Composition for wearing denture | |
| JP2019199467A (en) | Denture base composition and denture base fitting method | |
| JP2014196367A (en) | Composition applied to mucous membrane |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A621 | Written request for application examination |
Free format text: JAPANESE INTERMEDIATE CODE: A621 Effective date: 20230323 |
|
| A131 | Notification of reasons for refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A131 Effective date: 20240305 |
|
| A601 | Written request for extension of time |
Free format text: JAPANESE INTERMEDIATE CODE: A601 Effective date: 20240418 |
|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20240522 |
|
| A131 | Notification of reasons for refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A131 Effective date: 20240806 |
|
| A601 | Written request for extension of time |
Free format text: JAPANESE INTERMEDIATE CODE: A601 Effective date: 20241003 |