JP2022094517A - Emulsified composition for external use - Google Patents
Emulsified composition for external use Download PDFInfo
- Publication number
- JP2022094517A JP2022094517A JP2020207445A JP2020207445A JP2022094517A JP 2022094517 A JP2022094517 A JP 2022094517A JP 2020207445 A JP2020207445 A JP 2020207445A JP 2020207445 A JP2020207445 A JP 2020207445A JP 2022094517 A JP2022094517 A JP 2022094517A
- Authority
- JP
- Japan
- Prior art keywords
- external
- urea
- emulsified composition
- acid
- component
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
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- 239000000203 mixture Substances 0.000 title claims abstract description 107
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 claims abstract description 63
- YGSDEFSMJLZEOE-UHFFFAOYSA-N salicylic acid Chemical compound OC(=O)C1=CC=CC=C1O YGSDEFSMJLZEOE-UHFFFAOYSA-N 0.000 claims abstract description 63
- 239000004202 carbamide Substances 0.000 claims abstract description 62
- -1 sorbitan fatty acid ester Chemical class 0.000 claims abstract description 53
- 235000014113 dietary fatty acids Nutrition 0.000 claims abstract description 43
- 239000000194 fatty acid Substances 0.000 claims abstract description 43
- 229930195729 fatty acid Natural products 0.000 claims abstract description 43
- FJKROLUGYXJWQN-UHFFFAOYSA-N papa-hydroxy-benzoic acid Natural products OC(=O)C1=CC=C(O)C=C1 FJKROLUGYXJWQN-UHFFFAOYSA-N 0.000 claims abstract description 31
- 229960004889 salicylic acid Drugs 0.000 claims abstract description 31
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerol Natural products OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims abstract description 20
- 229940121363 anti-inflammatory agent Drugs 0.000 claims abstract description 19
- 239000002260 anti-inflammatory agent Substances 0.000 claims abstract description 19
- 235000011187 glycerol Nutrition 0.000 claims abstract description 17
- 102000011782 Keratins Human genes 0.000 claims description 32
- 108010076876 Keratins Proteins 0.000 claims description 32
- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 claims description 20
- 150000003839 salts Chemical class 0.000 claims description 19
- 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 16
- 125000004432 carbon atom Chemical group C* 0.000 claims description 16
- LPLVUJXQOOQHMX-QWBHMCJMSA-N glycyrrhizinic acid Chemical compound O([C@@H]1[C@@H](O)[C@H](O)[C@H](O[C@@H]1O[C@@H]1C([C@H]2[C@]([C@@H]3[C@@]([C@@]4(CC[C@@]5(C)CC[C@@](C)(C[C@H]5C4=CC3=O)C(O)=O)C)(C)CC2)(C)CC1)(C)C)C(O)=O)[C@@H]1O[C@H](C(O)=O)[C@@H](O)[C@H](O)[C@H]1O LPLVUJXQOOQHMX-QWBHMCJMSA-N 0.000 claims description 14
- 238000004945 emulsification Methods 0.000 claims description 13
- 229960004949 glycyrrhizic acid Drugs 0.000 claims description 12
- 235000019410 glycyrrhizin Nutrition 0.000 claims description 12
- 239000004471 Glycine Substances 0.000 claims description 10
- VTAJIXDZFCRWBR-UHFFFAOYSA-N Licoricesaponin B2 Natural products C1C(C2C(C3(CCC4(C)CCC(C)(CC4C3=CC2)C(O)=O)C)(C)CC2)(C)C2C(C)(C)CC1OC1OC(C(O)=O)C(O)C(O)C1OC1OC(C(O)=O)C(O)C(O)C1O VTAJIXDZFCRWBR-UHFFFAOYSA-N 0.000 claims description 9
- LPLVUJXQOOQHMX-UHFFFAOYSA-N glycyrrhetinic acid glycoside Natural products C1CC(C2C(C3(CCC4(C)CCC(C)(CC4C3=CC2=O)C(O)=O)C)(C)CC2)(C)C2C(C)(C)C1OC1OC(C(O)=O)C(O)C(O)C1OC1OC(C(O)=O)C(O)C(O)C1O LPLVUJXQOOQHMX-UHFFFAOYSA-N 0.000 claims description 9
- 239000001685 glycyrrhizic acid Substances 0.000 claims description 9
- UYRUBYNTXSDKQT-UHFFFAOYSA-N glycyrrhizic acid Natural products CC1(C)C(CCC2(C)C1CCC3(C)C2C(=O)C=C4C5CC(C)(CCC5(C)CCC34C)C(=O)O)OC6OC(C(O)C(O)C6OC7OC(O)C(O)C(O)C7C(=O)O)C(=O)O UYRUBYNTXSDKQT-UHFFFAOYSA-N 0.000 claims description 9
- 150000004671 saturated fatty acids Chemical class 0.000 claims description 9
- 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 6
- 229960003720 enoxolone Drugs 0.000 claims description 6
- 238000003860 storage Methods 0.000 abstract description 32
- 238000005191 phase separation Methods 0.000 abstract description 26
- 238000000354 decomposition reaction Methods 0.000 abstract description 22
- 230000000694 effects Effects 0.000 description 26
- 229920003171 Poly (ethylene oxide) Polymers 0.000 description 12
- 229920001214 Polysorbate 60 Polymers 0.000 description 9
- 150000004665 fatty acids Chemical class 0.000 description 9
- 238000002360 preparation method Methods 0.000 description 9
- IPCSVZSSVZVIGE-UHFFFAOYSA-N hexadecanoic acid Chemical compound CCCCCCCCCCCCCCCC(O)=O IPCSVZSSVZVIGE-UHFFFAOYSA-N 0.000 description 8
- 239000004094 surface-active agent Substances 0.000 description 8
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 8
- 239000002253 acid Substances 0.000 description 7
- 238000000034 method Methods 0.000 description 7
- 239000003921 oil Substances 0.000 description 7
- VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 description 6
- ASKIVFGGGGIGKH-UHFFFAOYSA-N 2,3-dihydroxypropyl 16-methylheptadecanoate Chemical compound CC(C)CCCCCCCCCCCCCCC(=O)OCC(O)CO ASKIVFGGGGIGKH-UHFFFAOYSA-N 0.000 description 6
- IAYPIBMASNFSPL-UHFFFAOYSA-N Ethylene oxide Chemical compound C1CO1 IAYPIBMASNFSPL-UHFFFAOYSA-N 0.000 description 6
- 150000005215 alkyl ethers Chemical class 0.000 description 6
- UKMSUNONTOPOIO-UHFFFAOYSA-N docosanoic acid Chemical compound CCCCCCCCCCCCCCCCCCCCCC(O)=O UKMSUNONTOPOIO-UHFFFAOYSA-N 0.000 description 6
- VKOBVWXKNCXXDE-UHFFFAOYSA-N icosanoic acid Chemical compound CCCCCCCCCCCCCCCCCCCC(O)=O VKOBVWXKNCXXDE-UHFFFAOYSA-N 0.000 description 6
- OSWPMRLSEDHDFF-UHFFFAOYSA-N methyl salicylate Chemical class COC(=O)C1=CC=CC=C1O OSWPMRLSEDHDFF-UHFFFAOYSA-N 0.000 description 6
- 239000002736 nonionic surfactant Substances 0.000 description 6
- 235000019198 oils Nutrition 0.000 description 6
- 150000005846 sugar alcohols Polymers 0.000 description 6
- 230000000144 pharmacologic effect Effects 0.000 description 5
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 4
- 235000021314 Palmitic acid Nutrition 0.000 description 4
- 235000021355 Stearic acid Nutrition 0.000 description 4
- 239000000654 additive Substances 0.000 description 4
- 230000003110 anti-inflammatory effect Effects 0.000 description 4
- 238000009472 formulation Methods 0.000 description 4
- 239000001788 mono and diglycerides of fatty acids Substances 0.000 description 4
- WQEPLUUGTLDZJY-UHFFFAOYSA-N n-Pentadecanoic acid Natural products CCCCCCCCCCCCCCC(O)=O WQEPLUUGTLDZJY-UHFFFAOYSA-N 0.000 description 4
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 4
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 description 4
- 235000003441 saturated fatty acids Nutrition 0.000 description 4
- 239000008117 stearic acid Substances 0.000 description 4
- TUNFSRHWOTWDNC-HKGQFRNVSA-N tetradecanoic acid Chemical compound CCCCCCCCCCCCC[14C](O)=O TUNFSRHWOTWDNC-HKGQFRNVSA-N 0.000 description 4
- 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 3
- PAFJZWHXMSQJKV-UQZRNVAESA-N (3r,4s)-2-[(1r)-1,2-dihydroxyethyl]oxolane-3,4-diol;octadecanoic acid Chemical compound OC[C@@H](O)C1OC[C@H](O)[C@H]1O.OC[C@@H](O)C1OC[C@H](O)[C@H]1O.OC[C@@H](O)C1OC[C@H](O)[C@H]1O.CCCCCCCCCCCCCCCCCC(O)=O.CCCCCCCCCCCCCCCCCC(O)=O PAFJZWHXMSQJKV-UQZRNVAESA-N 0.000 description 3
- LVYLCBNXHHHPSB-UHFFFAOYSA-N 2-hydroxyethyl salicylate Chemical compound OCCOC(=O)C1=CC=CC=C1O LVYLCBNXHHHPSB-UHFFFAOYSA-N 0.000 description 3
- 235000021357 Behenic acid Nutrition 0.000 description 3
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 description 3
- GYCKQBWUSACYIF-UHFFFAOYSA-N Ethyl salicylate Chemical class CCOC(=O)C1=CC=CC=C1O GYCKQBWUSACYIF-UHFFFAOYSA-N 0.000 description 3
- ILRKKHJEINIICQ-OOFFSTKBSA-N Monoammonium glycyrrhizinate Chemical compound N.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 ILRKKHJEINIICQ-OOFFSTKBSA-N 0.000 description 3
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 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
- 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 3
- 229910052783 alkali metal Inorganic materials 0.000 description 3
- 150000001413 amino acids Chemical class 0.000 description 3
- 239000008346 aqueous phase Substances 0.000 description 3
- 229940116226 behenic acid Drugs 0.000 description 3
- 229910052799 carbon Inorganic materials 0.000 description 3
- 230000000052 comparative effect Effects 0.000 description 3
- 230000001804 emulsifying effect Effects 0.000 description 3
- 150000002148 esters Chemical class 0.000 description 3
- 229940005667 ethyl salicylate Drugs 0.000 description 3
- 229940075507 glyceryl monostearate Drugs 0.000 description 3
- 238000004519 manufacturing process Methods 0.000 description 3
- 229960001047 methyl salicylate Drugs 0.000 description 3
- 238000002156 mixing Methods 0.000 description 3
- GLDOVTGHNKAZLK-UHFFFAOYSA-N octadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCCCO GLDOVTGHNKAZLK-UHFFFAOYSA-N 0.000 description 3
- 239000012071 phase Substances 0.000 description 3
- DCBSHORRWZKAKO-UHFFFAOYSA-N rac-1-monomyristoylglycerol Chemical compound CCCCCCCCCCCCCC(=O)OCC(O)CO DCBSHORRWZKAKO-UHFFFAOYSA-N 0.000 description 3
- 210000003491 skin Anatomy 0.000 description 3
- 239000001587 sorbitan monostearate Substances 0.000 description 3
- 235000011076 sorbitan monostearate Nutrition 0.000 description 3
- 229940035048 sorbitan monostearate Drugs 0.000 description 3
- 239000001589 sorbitan tristearate Substances 0.000 description 3
- 235000011078 sorbitan tristearate Nutrition 0.000 description 3
- 229960004129 sorbitan tristearate Drugs 0.000 description 3
- PUPZLCDOIYMWBV-UHFFFAOYSA-N (+/-)-1,3-Butanediol Chemical compound CC(O)CCO PUPZLCDOIYMWBV-UHFFFAOYSA-N 0.000 description 2
- IZHVBANLECCAGF-UHFFFAOYSA-N 2-hydroxy-3-(octadecanoyloxy)propyl octadecanoate Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)COC(=O)CCCCCCCCCCCCCCCCC IZHVBANLECCAGF-UHFFFAOYSA-N 0.000 description 2
- BSYNRYMUTXBXSQ-UHFFFAOYSA-N Aspirin Chemical compound CC(=O)OC1=CC=CC=C1C(O)=O BSYNRYMUTXBXSQ-UHFFFAOYSA-N 0.000 description 2
- 239000004147 Sorbitan trioleate Substances 0.000 description 2
- 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 2
- 229960001138 acetylsalicylic acid Drugs 0.000 description 2
- 125000000217 alkyl group Chemical group 0.000 description 2
- FPIPGXGPPPQFEQ-OVSJKPMPSA-N all-trans-retinol Chemical compound OC\C=C(/C)\C=C\C=C(/C)\C=C\C1=C(C)CCCC1(C)C FPIPGXGPPPQFEQ-OVSJKPMPSA-N 0.000 description 2
- 239000004359 castor oil Substances 0.000 description 2
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- 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 2
- 229960002389 glycol salicylate Drugs 0.000 description 2
- 239000004615 ingredient Substances 0.000 description 2
- 230000007721 medicinal effect Effects 0.000 description 2
- 230000003020 moisturizing effect Effects 0.000 description 2
- 230000007935 neutral effect Effects 0.000 description 2
- UTOPWMOLSKOLTQ-UHFFFAOYSA-N octacosanoic acid Chemical compound CCCCCCCCCCCCCCCCCCCCCCCCCCCC(O)=O UTOPWMOLSKOLTQ-UHFFFAOYSA-N 0.000 description 2
- ZQBAKBUEJOMQEX-UHFFFAOYSA-N phenyl salicylate Chemical compound OC1=CC=CC=C1C(=O)OC1=CC=CC=C1 ZQBAKBUEJOMQEX-UHFFFAOYSA-N 0.000 description 2
- 239000001818 polyoxyethylene sorbitan monostearate Substances 0.000 description 2
- 235000010989 polyoxyethylene sorbitan monostearate Nutrition 0.000 description 2
- XAEFZNCEHLXOMS-UHFFFAOYSA-M potassium benzoate Chemical compound [K+].[O-]C(=O)C1=CC=CC=C1 XAEFZNCEHLXOMS-UHFFFAOYSA-M 0.000 description 2
- 239000003755 preservative agent Substances 0.000 description 2
- LXNHXLLTXMVWPM-UHFFFAOYSA-N pyridoxine Chemical compound CC1=NC=C(CO)C(CO)=C1O LXNHXLLTXMVWPM-UHFFFAOYSA-N 0.000 description 2
- 229940058287 salicylic acid derivative anticestodals Drugs 0.000 description 2
- 150000003872 salicylic acid derivatives Chemical class 0.000 description 2
- 159000000000 sodium salts Chemical class 0.000 description 2
- 235000019337 sorbitan trioleate Nutrition 0.000 description 2
- 229960000391 sorbitan trioleate Drugs 0.000 description 2
- 230000000087 stabilizing effect Effects 0.000 description 2
- WNIFXKPDILJURQ-UHFFFAOYSA-N stearyl glycyrrhizinate Natural products C1CC(O)C(C)(C)C2CCC3(C)C4(C)CCC5(C)CCC(C(=O)OCCCCCCCCCCCCCCCCCC)(C)CC5C4=CC(=O)C3C21C WNIFXKPDILJURQ-UHFFFAOYSA-N 0.000 description 2
- DRAWQKGUORNASA-UHFFFAOYSA-N (2-hydroxy-3-octadec-9-enoyloxypropyl) octadec-9-enoate Chemical compound CCCCCCCCC=CCCCCCCCC(=O)OCC(O)COC(=O)CCCCCCCC=CCCCCCCCC DRAWQKGUORNASA-UHFFFAOYSA-N 0.000 description 1
- CAKDFKUXFMLCAR-UIOGXPPZSA-N (2S,3S,4S,5R,6R)-6-[(2S,3R,4S,5S,6S)-2-[[(3S,4aR,6aR,6bS,8aS,11S,12aR,14aR,14bS)-11-methoxycarbonyl-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-carboxy-4,5-dihydroxyoxan-3-yl]oxy-3,4,5-trihydroxyoxane-2-carboxylic acid Chemical compound 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@@]([C@@]3(CC[C@H]2C1(C)C)C)(C)CC[C@@]1(C)CC[C@](C[C@H]14)(C)C(=O)OC)C(O)=O)[C@@H]1O[C@H](C(O)=O)[C@@H](O)[C@H](O)[C@H]1O CAKDFKUXFMLCAR-UIOGXPPZSA-N 0.000 description 1
- 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 1
- PDHSAQOQVUXZGQ-JKSUJKDBSA-N (2r,3s)-2-(3,4-dihydroxyphenyl)-3-methoxy-3,4-dihydro-2h-chromene-5,7-diol Chemical compound C1([C@H]2OC3=CC(O)=CC(O)=C3C[C@@H]2OC)=CC=C(O)C(O)=C1 PDHSAQOQVUXZGQ-JKSUJKDBSA-N 0.000 description 1
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- FFJCNSLCJOQHKM-CLFAGFIQSA-N (z)-1-[(z)-octadec-9-enoxy]octadec-9-ene Chemical compound CCCCCCCC\C=C/CCCCCCCCOCCCCCCCC\C=C/CCCCCCCC FFJCNSLCJOQHKM-CLFAGFIQSA-N 0.000 description 1
- ZORQXIQZAOLNGE-UHFFFAOYSA-N 1,1-difluorocyclohexane Chemical compound FC1(F)CCCCC1 ZORQXIQZAOLNGE-UHFFFAOYSA-N 0.000 description 1
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- NWGAAWUUGRXXSC-UHFFFAOYSA-N 1-(2-hydroxypropoxy)propan-2-yl 2-hydroxybenzoate Chemical compound CC(O)COCC(C)OC(=O)C1=CC=CC=C1O NWGAAWUUGRXXSC-UHFFFAOYSA-N 0.000 description 1
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- 239000000263 2,3-dihydroxypropyl (Z)-octadec-9-enoate Substances 0.000 description 1
- WXHLLJAMBQLULT-UHFFFAOYSA-N 2-[[6-[4-(2-hydroxyethyl)piperazin-1-yl]-2-methylpyrimidin-4-yl]amino]-n-(2-methyl-6-sulfanylphenyl)-1,3-thiazole-5-carboxamide;hydrate Chemical compound O.C=1C(N2CCN(CCO)CC2)=NC(C)=NC=1NC(S1)=NC=C1C(=O)NC1=C(C)C=CC=C1S WXHLLJAMBQLULT-UHFFFAOYSA-N 0.000 description 1
- XDZMPRGFOOFSBL-UHFFFAOYSA-N 2-ethoxybenzoic acid Chemical compound CCOC1=CC=CC=C1C(O)=O XDZMPRGFOOFSBL-UHFFFAOYSA-N 0.000 description 1
- LQJBNNIYVWPHFW-UHFFFAOYSA-N 20:1omega9c fatty acid Natural products CCCCCCCCCCC=CCCCCCCCC(O)=O LQJBNNIYVWPHFW-UHFFFAOYSA-N 0.000 description 1
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- HCJMNOSIAGSZBM-UHFFFAOYSA-N 6-methylsalicylic acid Chemical compound CC1=CC=CC(O)=C1C(O)=O HCJMNOSIAGSZBM-UHFFFAOYSA-N 0.000 description 1
- QSBYPNXLFMSGKH-UHFFFAOYSA-N 9-Heptadecensaeure Natural products CCCCCCCC=CCCCCCCCC(O)=O QSBYPNXLFMSGKH-UHFFFAOYSA-N 0.000 description 1
- 239000004215 Carbon black (E152) Substances 0.000 description 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 1
- 229920002683 Glycosaminoglycan Polymers 0.000 description 1
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 1
- OYHQOLUKZRVURQ-HZJYTTRNSA-N Linoleic acid Chemical compound CCCCC\C=C/C\C=C/CCCCCCCC(O)=O OYHQOLUKZRVURQ-HZJYTTRNSA-N 0.000 description 1
- FYYHWMGAXLPEAU-UHFFFAOYSA-N Magnesium Chemical compound [Mg] FYYHWMGAXLPEAU-UHFFFAOYSA-N 0.000 description 1
- 239000004909 Moisturizer Substances 0.000 description 1
- 239000005642 Oleic acid Substances 0.000 description 1
- ZQPPMHVWECSIRJ-UHFFFAOYSA-N Oleic acid Natural products CCCCCCCCC=CCCCCCCCC(O)=O ZQPPMHVWECSIRJ-UHFFFAOYSA-N 0.000 description 1
- ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 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
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- CMPDPBDUZTUXAD-UHFFFAOYSA-N [3-hydroxy-2-(16-methylheptadecanoyloxy)propyl] 16-methylheptadecanoate Chemical compound CC(C)CCCCCCCCCCCCCCC(=O)OCC(CO)OC(=O)CCCCCCCCCCCCCCC(C)C CMPDPBDUZTUXAD-UHFFFAOYSA-N 0.000 description 1
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- ZQPPMHVWECSIRJ-KTKRTIGZSA-N oleic acid Chemical compound CCCCCCCC\C=C/CCCCCCCC(O)=O ZQPPMHVWECSIRJ-KTKRTIGZSA-N 0.000 description 1
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Abstract
Description
本発明は、尿素及びサリチル酸系抗炎症剤を含み、保存による相分離及び尿素の分解を抑制できる外用乳化組成物に関する。 The present invention relates to an external emulsified composition containing urea and a salicylic acid-based anti-inflammatory agent, which can suppress phase separation and urea decomposition by storage.
尿素には、角質中での水分と水素結合を形成することによる水分保持作用や、タンパク質変性による不要な角質を除去したり軟化させたりする作用等があり、外用組成物に使用されている。一方、尿素は、外用組成物中で加水分解され易いため、尿素を含む外用組成物では、尿素の安定化を図ること必要になる。そこで、従来、尿素を安定化させ得る外用組成物の処方について種々検討されている。例えば、特許文献1には、尿素を含む外用組成物において、グリシン等の中性アミノ酸を配合することによって尿素を安定化が図られることが開示されている。また、特許文献2には、外用組成物に尿素10~25重量%、及びレチノール又はその誘導体を含有させることにより、優れた製剤安定性を備えさせ得ることが開示されている。 Urea has a water retention action by forming a hydrogen bond with water in the keratin and an action of removing or softening unnecessary keratin due to protein denaturation, and is used in an external composition. On the other hand, since urea is easily hydrolyzed in the external composition, it is necessary to stabilize the urea in the external composition containing urea. Therefore, various studies have been made on the formulation of an external composition capable of stabilizing urea. For example, Patent Document 1 discloses that urea can be stabilized by blending a neutral amino acid such as glycine in an external composition containing urea. Further, Patent Document 2 discloses that the external composition can be provided with excellent pharmaceutical stability by containing 10 to 25% by weight of urea and retinol or a derivative thereof.
一方、サリチル酸、サリチル酸誘導体、及びこれらの塩等のサリチル酸系抗炎症剤は、消炎鎮痛用途で外用組成物に使用されている。 On the other hand, salicylic acid, salicylic acid derivatives, and salicylic acid-based anti-inflammatory agents such as salts thereof are used in external compositions for anti-inflammatory and analgesic applications.
また、乳化製剤は、水性成分と油性成分を配合でき、様々な製剤処方に対応できると共に、皮膚に適用した際の使用感も優れているため、外用組成物の分野で汎用されている。 Further, the emulsified preparation is widely used in the field of external composition because it can contain an aqueous component and an oily component, can be used for various preparation formulations, and has an excellent usability when applied to the skin.
近年、外用組成物の機能性の向上に対する消費者の要望が高まっており、このような消費者ニーズに追従するために、尿素及びサリチル酸系抗炎症剤を含む外用乳化組成物の開発が望まれている。 In recent years, consumer demand for improving the functionality of external compositions has increased, and in order to meet such consumer needs, it is desired to develop an external emulsified composition containing urea and a salicylic acid-based anti-inflammatory agent. ing.
本発明者は、本発明者は、尿素及びサリチル酸系抗炎症剤を含む外用乳化組成物を開発すべく種々検討を行ったところ、尿素及びサリチル酸系抗炎症剤を含む外用乳化組成物では、保存により相分離及び尿素の分解が生じ、保存安定性の点で問題があることを知得した。 The present inventor has conducted various studies to develop an external emulsified composition containing urea and a salicylic acid-based anti-inflammatory agent, and found that the external emulsified composition containing urea and a salicylic acid-based anti-inflammatory agent is preserved. It was found that there was a problem in terms of storage stability due to phase separation and decomposition of urea.
そこで、本発明は、尿素及びサリチル酸系抗炎症剤を含み、保存による相分離及び尿素の分解を抑制できる外用乳化組成物を提供することを課題とする。 Therefore, it is an object of the present invention to provide an external emulsified composition containing urea and a salicylic acid-based anti-inflammatory agent and capable of suppressing phase separation and decomposition of urea by storage.
本発明者は、前記課題を解決すべく鋭意検討を行ったところ、尿素とサリチル酸系抗炎症剤に加えて、ソルビタン脂肪酸エステル及び/又はグリセリン脂肪酸エステルを含む外用乳化組成物は、保存による相分離及び尿素の分解を抑制でき、優れた保存安定性を備え得ることを見出した。更に、本発明者は、前記外用乳化組成物は、爪周りに塗布した際の伸びが良好で、爪周りの角質の軟化効果が優れることをも見出した。本発明は、かかる知見に基づいて、更に検討を重ねることにより完成したものである。 As a result of diligent studies to solve the above problems, the present inventor has found that an external emulsified composition containing a sorbitan fatty acid ester and / or a glycerin fatty acid ester in addition to urea and a salicylic acid-based anti-inflammatory agent is phase-separated by storage. And it was found that the decomposition of urea can be suppressed and excellent storage stability can be provided. Furthermore, the present inventor has also found that the external emulsified composition has good elongation when applied around the nail and has an excellent softening effect on the keratin around the nail. The present invention has been completed by further studies based on such findings.
即ち、本発明は、下記に掲げる態様の発明を提供する。
項1. (A)尿素、(B)サリチル酸系抗炎症剤、並びに(C)ソルビタン脂肪酸エステル及び/又はグリセリン脂肪酸エステルを含む、外用乳化組成物。
項2. グリシンを含まない、項1に記載の外用乳化組成物。
項3. 更に(D)グリチルリチン酸、グリチルレチン酸、それらの誘導体、及びそれらの塩よりなる群から選択される少なくとも1種のグリチルリチン酸類を含有する、項1又は2に記載の外用乳化組成物。
項4. 更に(E)炭素数14以上の飽和脂肪酸及び/又はその塩を含有する、項1~3のいずれかに記載の外用乳化組成物。
項5. 爪周りの角質の軟化のために使用される、項1~4のいずれかに記載の外用乳化組成物。
That is, the present invention provides the inventions of the following aspects.
Item 1. An external emulsified composition comprising (A) urea, (B) a salicylic acid-based anti-inflammatory agent, and (C) a sorbitan fatty acid ester and / or a glycerin fatty acid ester.
Item 2. Item 2. The external emulsified composition according to Item 1, which does not contain glycine.
Item 3. Item 2. The external emulsification composition according to Item 1 or 2, further comprising (D) at least one glycyrrhizic acid selected from the group consisting of glycyrrhizic acid, glycyrrhetinic acid, derivatives thereof, and salts thereof.
Item 4. Item 2. The external emulsified composition according to any one of Items 1 to 3, further comprising (E) a saturated fatty acid having 14 or more carbon atoms and / or a salt thereof.
Item 5. Item 6. The external emulsified composition according to any one of Items 1 to 4, which is used for softening the keratin around the nail.
本発明の外用乳化組成物によれば、尿素及びサリチル酸系抗炎症剤を含んでいながらも、保存による相分離及び尿素の分解を抑制でき、優れた保存安定性を備えることができる。更に、本発明の外用乳化組成物は、爪周りに塗布した際の伸びが良好で、爪周りの角質の軟化効果が優れおり、爪周りの角質の軟化用途に好適に使用できる。 According to the external emulsification composition of the present invention, although it contains urea and a salicylic acid-based anti-inflammatory agent, phase separation and decomposition of urea due to storage can be suppressed, and excellent storage stability can be provided. Further, the external emulsified composition of the present invention has good elongation when applied around the nail, has an excellent softening effect on the keratin around the nail, and can be suitably used for softening the keratin around the nail.
1.外用乳化組成物1. 1. External emulsification composition
本発明の外用乳化組成物は、(A)尿素、(B)サリチル酸系抗炎症剤、並びに(C)ソルビタン脂肪酸エステル及び/又はグリセリン脂肪酸エステルを含むことを特徴とする。以下、本発明の外用乳化組成物について詳述する。 The external emulsified composition of the present invention is characterized by containing (A) urea, (B) a salicylic acid-based anti-inflammatory agent, and (C) a sorbitan fatty acid ester and / or a glycerin fatty acid ester. Hereinafter, the external emulsified composition of the present invention will be described in detail.
[(A)尿素]
本発明の外用乳化組成物は、尿素((A)成分と表記することもある)を含有する。尿素は、角質での水分保持作用や不要な角質の除去又は軟化作用等を有することが知られている公知の成分である。
[(A) Urea]
The external emulsified composition of the present invention contains urea (sometimes referred to as component (A)). Urea is a known component known to have a water retention action in the keratin, an unnecessary keratin removal or softening action, and the like.
本発明の外用乳化組成物における(A)成分の含有量としては、付与すべき薬効、外用乳化組成物の用途等に応じて適宜設定すればよいが、例えば、1~30重量%、好ましくは5~25重量%、より好ましくは10~20重量%が挙げられる。
[(B)サリチル酸系抗炎症剤]
本発明の外用乳化組成物は、サリチル酸系抗炎症剤((B)成分と表記することもある)を含有する。
The content of the component (A) in the external emulsified composition of the present invention may be appropriately set according to the medicinal effect to be imparted, the intended use of the external emulsified composition, etc., and is, for example, 1 to 30% by weight, preferably 1 to 30% by weight. 5 to 25% by weight, more preferably 10 to 20% by weight.
[(B) Salicylic acid anti-inflammatory agent]
The external emulsified composition of the present invention contains a salicylic acid-based anti-inflammatory agent (sometimes referred to as a component (B)).
サリチル酸系抗炎症剤としては、具体的には、サリチル酸、サリチル酸の誘導体、及びこれらの塩が挙げられる。サリチル酸の誘導体としては、例えば、アセチルサリチル酸(アスピリン)、サリチルアミド(エテンザミド)、スルホサリチル酸、サリチル酸メチル、サリチル酸エチル、サリチル酸グリコール、サリチル酸エチレングリコール、サリチル酸ジプロピレングリコール、サリチル酸チタン、サリチル酸2-エチルヘキシル、サリチル酸ホモメンチル、サリチル酸フェニル等が挙げられる。サリチル酸及びその誘導体の塩としては、例えば、ナトリウム、カリウム等のアルカリ金属塩;マグネシウム等のアルカリ土類金属塩が挙げられる。これらのサリチル酸系抗炎症剤は、1種単独で使用してもよく、2種以上を組み合わせて使用してもよい。 Specific examples of the salicylic acid-based anti-inflammatory agent include salicylic acid, salicylic acid derivatives, and salts thereof. Examples of the derivative of salicylic acid include acetylsalicylic acid (aspirin), salicylic acid (ethenzamid), sulfosalicylic acid, methyl salicylic acid, ethyl salicylic acid, glycol salicylate, ethylene glycol salicylate, dipropylene glycol salicylate, titanium salicylate, 2-ethylhexyl salicylate, and salicylic acid. Examples thereof include homomentyl and phenyl salicylate. Examples of salts of salicylic acid and its derivatives include alkali metal salts such as sodium and potassium; and alkaline earth metal salts such as magnesium. These salicylic acid-based anti-inflammatory agents may be used alone or in combination of two or more.
これらのサリチル酸系抗炎症剤の中でも、好ましくはサリチル酸、サリチル酸の塩、サリチル酸エチル、サリチル酸メチル、より好ましくはサリチル酸が挙げられる。 Among these salicylic acid-based anti-inflammatory agents, salicylic acid, salts of salicylic acid, ethyl salicylate, methyl salicylate, and more preferably salicylic acid can be mentioned.
本発明の外用乳化組成物における(B)成分の含有量としては、付与すべき薬効、外用乳化組成物の用途等に応じて適宜設定すればよいが、例えば、(B)成分の総量で0.01~1重量%、好ましくは0.05~0.5重量%、より好ましくは0.1~0.5重量%が挙げられる。 The content of the component (B) in the external emulsified composition of the present invention may be appropriately set according to the medicinal effect to be imparted, the intended use of the external emulsified composition, etc., but for example, the total amount of the component (B) is 0. 0.01 to 1% by weight, preferably 0.05 to 0.5% by weight, and more preferably 0.1 to 0.5% by weight.
本発明の外用乳化組成物において、(A)成分と(B)成分の比率については、特に制限されないが、例えば、(A)成分の総量100重量部当たり、(B)成分が総量で0.01~300重量部、好ましくは0.05~100重量部、より好ましくは0.1~50重量部が挙げられる。 In the external emulsified composition of the present invention, the ratio of the component (A) to the component (B) is not particularly limited, but for example, the total amount of the component (B) is 0. Examples thereof include 01 to 300 parts by weight, preferably 0.05 to 100 parts by weight, and more preferably 0.1 to 50 parts by weight.
[(C)ソルビタン脂肪酸エステル及び/又はグリセリン脂肪酸エステル]
本発明の外用乳化組成物は、ソルビタン脂肪酸エステル及び/又はグリセリン脂肪酸エステル((C)成分と表記することもある)を含有する。従来技術では、外用乳化組成物において、(A)成分と(B)成分を共存させると、保存による相分離や(A)成分の分解が生じるが、本発明の外用乳化組成物では更にソルビタン脂肪酸エステル及び/又はグリセリン脂肪酸エステルを含むことによって、保存による相分離や(A)成分の分解を抑制することが可能になっている。更に、本発明の外用乳化組成物では、(A)~(C)成分を含むことにより、爪周りに塗布した際の伸びが良好になり、また、優れた爪周りの角質軟化去効果を備えることができる。
[(C) Sorbitan fatty acid ester and / or glycerin fatty acid ester]
The external emulsified composition of the present invention contains a sorbitan fatty acid ester and / or a glycerin fatty acid ester (sometimes referred to as a component (C)). In the prior art, when the component (A) and the component (B) coexist in the external emulsified composition, phase separation and decomposition of the component (A) occur due to storage, but the external emulsified composition of the present invention further causes sorbitan fatty acid. By containing an ester and / or a glycerin fatty acid ester, it is possible to suppress phase separation and decomposition of the component (A) due to storage. Further, in the external emulsification composition of the present invention, by containing the components (A) to (C), the elongation when applied around the nail is improved, and the keratin softening effect around the nail is excellent. be able to.
ソルビタン脂肪酸エステルとは、ソルビタンと脂肪酸のエステルであり、公知のノニオン性界面活性剤である。ソルビタン脂肪酸エステル1分子当たりに結合している脂肪酸の数としては、特に制限されないが、例えば、1~4個、好ましくは1~3個、より好ましくは1又は2個、更に好ましくは1個が挙げられる。ソルビタン脂肪酸エステルを構成する脂肪酸の炭素数としては、特に制限されないが、例えば、10~22個、好ましくは14~22個、より好ましくは16~20個が挙げられる。ソルビタン脂肪酸エステルとして、具体的には、モノオレイン酸ソルビタン、モノステアリン酸ソルビタン、セスキオレイン酸ソルビタン、セスキステアリン酸ソルビタン、ヤシ油脂肪酸ソルビタン、モノパルミチン酸ソルビタン、トリステアリン酸ソルビタン、トリオレイン酸ソルビタン等が挙げられる。これらのソルビタン脂肪酸エステルの中でも、保存による相分離及び尿素の分解をより一層効果的に抑制するという観点から、好ましくはモノステアリン酸ソルビタン、セスキステアリン酸ソルビタン、トリステアリン酸ソルビタン、より好ましくはモノステアリン酸ソルビタンが挙げられる。 The sorbitan fatty acid ester is an ester of sorbitan and a fatty acid, and is a known nonionic surfactant. The number of fatty acids bound per molecule of the sorbitan fatty acid ester is not particularly limited, but is, for example, 1 to 4, preferably 1 to 3, more preferably 1 or 2, and even more preferably 1. Can be mentioned. The carbon number of the fatty acid constituting the sorbitan fatty acid ester is not particularly limited, and examples thereof include 10 to 22, preferably 14 to 22, and more preferably 16 to 20. Specific examples of the sorbitan fatty acid ester include sorbitan monooleate, sorbitan monostearate, sorbitan sesquioleate, sorbitan sesquistearate, sorbitan coconut oil fatty acid, sorbitan monopalmitate, sorbitan tristearate, and sorbitan trioleate. Can be mentioned. Among these sorbitan fatty acid esters, sorbitan monostearate, sorbitan sesquistearate, sorbitan tristearate, and more preferably monostearate are preferable from the viewpoint of more effectively suppressing phase separation and urea decomposition during storage. Sorbitan acid can be mentioned.
グリセリン脂肪酸エステルとは、グリセリンと脂肪酸のエステルであり、公知のノニオン性界面活性剤である。グリセリン脂肪酸エステルを構成する脂肪酸の炭素数としては、例えば、10~22個、好ましくは14~22個、より好ましくは16~20個が挙げられる。前記グリセリン脂肪酸1分子当たりに結合している脂肪酸の数としては、特に制限されないが、例えば、1~3個、好ましくは1又は2個、より好ましくは1個が挙げられる。グリセリン脂肪酸エステルとして、具体的には、モノミリスチン酸グリセリル、モノステアリン酸グリセリル、モノイソステアリン酸グリセリル、モノオレイン酸グリセリル、ジミリスチン酸グリセリル、ジステアリン酸グリセリル、ジイソステアリン酸グリセリル、ジオレイン酸グリセリル等が挙げられる。これらのグリセリン脂肪酸エステルの中でも、保存による相分離及び尿素の分解をより一層効果的に抑制するという観点から、好ましくは、モノステアリン酸グリセリル、モノミリスチン酸グリセリル、モノイソステアリン酸グリセリルが挙げられる。 The glycerin fatty acid ester is an ester of glycerin and a fatty acid, and is a known nonionic surfactant. Examples of the carbon number of the fatty acid constituting the glycerin fatty acid ester include 10 to 22, preferably 14 to 22, and more preferably 16 to 20. The number of fatty acids bound to one molecule of the glycerin fatty acid is not particularly limited, and examples thereof include 1 to 3, preferably 1 or 2, and more preferably 1. Specific examples of the glycerin fatty acid ester include glyceryl monomyristate, glyceryl monostearate, glyceryl monoisostearate, glyceryl monooleate, glyceryl dimyristate, glyceryl distearate, glyceryl diisostearate, and glyceryl dioleate. .. Among these glycerin fatty acid esters, glyceryl monostearate, glyceryl monomyristate, and glyceryl monoisostearate are preferable from the viewpoint of more effectively suppressing phase separation and urea decomposition during storage.
本発明の外用乳化組成物における(C)成分の含有量としては、例えば、(C)成分の総量で0.01~20重量%、好ましくは0.05~10重量%、より好ましくは0.1~5重量%が挙げられる。 The content of the component (C) in the external emulsified composition of the present invention is, for example, 0.01 to 20% by weight, preferably 0.05 to 10% by weight, more preferably 0. 1 to 5% by weight is mentioned.
本発明の外用乳化組成物において、(A)成分と(C)成分の比率については、特に制限されないが、例えば、(A)成分の総量100重量部当たり、(C)成分が総量で0.01~300重量部、好ましくは0.05~100重量部、より好ましくは0.1~50重量部が挙げられる。 In the external emulsified composition of the present invention, the ratio of the component (A) to the component (C) is not particularly limited, but for example, the total amount of the component (C) is 0. Examples thereof include 01 to 300 parts by weight, preferably 0.05 to 100 parts by weight, and more preferably 0.1 to 50 parts by weight.
[グリシン]
本発明の外用乳化組成物は、グリシンを含んでいてもよいが、グリシンを含まないことが好ましい。従来、グリシンは尿素を安定化させる作用があることが知られているが、本発明の外用乳化組成物では、グリシンを含まない場合には、保存による相分離及び尿素の分解をより一層効果的に抑制することが可能になる。
[glycine]
The external emulsified composition of the present invention may contain glycine, but preferably does not contain glycine. Conventionally, it is known that glycine has an action of stabilizing urea, but in the case of the external emulsified composition of the present invention, when glycine is not contained, phase separation by storage and decomposition of urea are more effective. It becomes possible to suppress it.
また、本発明の外用乳化組成物の一態様として、中性アミノ酸(側鎖にアミノ基又はカルボキシル基が含まれていないアミノ酸)を含まないことが挙げられる。 Moreover, one aspect of the external emulsification composition of the present invention is that it does not contain a neutral amino acid (an amino acid whose side chain does not contain an amino group or a carboxyl group).
[(D)グリチルリチン酸類]
本発明の外用乳化組成物は、前述する成分に加えて、グリチルリチン酸、グリチルレチン酸、それらの誘導体、及びそれらの塩よりなる群から選択される少なくとも1種のグリチルリチン酸類((D)成分と表記することもある)を含んでいてもよい。本発明の外用組成物が更に(D)成分を含むことにより、保存による相分離及び尿素の分解の抑制効果を更に向上させつつ、爪周りに塗布した際の伸び及び爪周りの角質軟化効果をより一層向上させることができる。
[(D) Glycyrrhizic acid]
The external emulsified composition of the present invention is designated as at least one glycyrrhizic acid ((D) component) selected from the group consisting of glycyrrhizic acid, glycyrrhetinic acid, derivatives thereof, and salts thereof in addition to the above-mentioned components. May be included). By further containing the component (D) in the external composition of the present invention, the effect of suppressing phase separation and urea decomposition by storage is further improved, and the effect of stretching and softening the keratin around the nail when applied around the nail is obtained. It can be further improved.
グリチルリチン酸、及びグリチルレチン酸は、抗炎症作用や抗アレルギー作用等を有することが知られている公知の薬剤である。 Glycyrrhizic acid and glycyrrhetinic acid are known drugs known to have anti-inflammatory action, antiallergic action and the like.
グリチルリチン酸の誘導体としては、薬学的に許容されることを限度として特に制限されないが、例えば、グリチルリチン酸メチル、グリチルリチン酸ステアリル等が挙げられる。これらのグリチルリチン酸の誘導体は、1種単独で使用してもよく、また2種以上を組み合わせて使用してもよい。 The derivative of glycyrrhizic acid is not particularly limited as long as it is pharmaceutically acceptable, and examples thereof include methyl glycyrrhizinate and stearyl glycyrrhizinate. These derivatives of glycyrrhizic acid may be used alone or in combination of two or more.
グリチルレチン酸の誘導体としては、薬学的に許容されることを限度として特に制限されないが、例えば、グリチルレチン酸ピリドキシン、グリチルレチン酸ステアリル、グリチルレチン酸グリセリル、グリチルレチン酸モノグルクロニド等が挙げられる。これらのグリチルレチン酸の誘導体は、1種単独で使用してもよく、また2種以上を組み合わせて使用してもよい。 The derivative of glycyrrhetinic acid is not particularly limited as long as it is pharmaceutically acceptable, and examples thereof include pyridoxine glycyrrhetinate, stearyl glycyrrhetinate, glyceryl glycyrrhetinate, and monoglucuronide glycyrrhetinate. These derivatives of glycyrrhetinic acid may be used alone or in combination of two or more.
グリチルリチン酸、グリチルレチン酸及び/又はその誘導体の塩としては、薬学的に許容されることを限度として特に制限されないが、例えば、ナトリウム塩、カリウム塩等のアルカリ金属塩;アンモニウム塩等が挙げられる。これらの塩は、1種単独で使用してもよく、また2種以上を組み合わせて使用してもよい。 The salt of glycyrrhizinic acid, glycyrrhetinic acid and / or a derivative thereof is not particularly limited as long as it is pharmaceutically acceptable, and examples thereof include alkali metal salts such as sodium salt and potassium salt; ammonium salts and the like. These salts may be used alone or in combination of two or more.
本発明の外用乳化組成物において、(D)成分として、グリチルリチン酸、グリチルレチン酸、これらの誘導体、及びそれらの塩の中から1種を選択して単独で使用してもよく、また2種以上を組み合わせて使用してもよい。 In the external emulsification composition of the present invention, as the component (D), one of glycyrrhizic acid, glycyrrhetinic acid, derivatives thereof, and salts thereof may be selected and used alone, or two or more thereof. May be used in combination.
(D)成分の中でも、保存による相分離及び尿素の分解の抑制効果、並びに爪周りに塗布した際の伸び及び爪周りの角質軟化効果をより一層向上させるという観点から、好ましくはグリチルリチン酸及びその塩、より好ましくはグリチルリチン酸の塩、更に好ましくはグリチルリチン酸モノアンモニウムが挙げられる。 Among the components (D), glycyrrhizinic acid and its above are preferable from the viewpoint of further improving the phase separation by storage and the effect of suppressing the decomposition of urea, and the effect of stretching around the nail and the effect of softening the keratin around the nail. Examples thereof include a salt, more preferably a salt of glycyrrhizinic acid, and even more preferably monoammonium glycyrrhizinate.
本発明の外用乳化組成物に(D)成分を含有させる場合、その含有量については、特に制限されないが、例えば、(D)成分の総量で0.05~5重量%、好ましくは0.1~1重量%、更に好ましくは0.3~0.5重量%が挙げられる。 When the external emulsified composition of the present invention contains the component (D), the content thereof is not particularly limited, but for example, the total amount of the component (D) is 0.05 to 5% by weight, preferably 0.1. It is about 1% by weight, more preferably 0.3 to 0.5% by weight.
本発明の外用組成物に(D)成分を含有させる場合、(A)成分に対する(D)成分の比率は、特に制限されないが、例えば、(A)成分1重量部当たり、(D)成分が総量で0.01~300重量部、好ましくは0.05~100重量部、より好ましくは0.1~50重量部が挙げられる。 When the component (D) is contained in the external composition of the present invention, the ratio of the component (D) to the component (A) is not particularly limited, but for example, the component (D) is contained in 1 part by weight of the component (A). The total amount is 0.01 to 300 parts by weight, preferably 0.05 to 100 parts by weight, and more preferably 0.1 to 50 parts by weight.
[(E)炭素数14以上の飽和脂肪酸及び/又はその塩]
本発明の外用乳化組成物は、必要に応じて、炭素数14以上の飽和脂肪酸及び/又はその塩((E)成分と表記することもある)を含有してもよい。本発明の外用乳化組成物において、更に(E)成分を含む場合には、保存による相分離を格段顕著に抑制でき、爪周りに塗布した際の伸びもより一層向上させることが可能になる。
[(E) Saturated fatty acids with 14 or more carbon atoms and / or salts thereof]
The external emulsified composition of the present invention may contain a saturated fatty acid having 14 or more carbon atoms and / or a salt thereof (sometimes referred to as a component (E)), if necessary. When the external emulsified composition of the present invention further contains the component (E), the phase separation due to storage can be remarkably suppressed, and the elongation when applied around the nail can be further improved.
飽和脂肪酸及び/又はその塩は、炭素数が14以上であればよいが、保存による相分離をより一層効果的に抑制させ、更に爪周りに塗布した際の伸びもより一層向上させるという観点から、好ましくは炭素数14~30、より好ましくは炭素数14~24、更に好ましくは炭素数14~22、特に好ましくは炭素数18が挙げられる。飽和脂肪酸として、より具体的には、ミリスチリン酸、パルミチン酸、ステアリン酸、アラキジン酸、ベヘン酸、リグノセリン酸、セロチン酸、モンタン酸、メリシン酸;好ましくはミリスチリン酸、パルミチン酸、ステアリン酸、アラキジン酸、ベヘン酸、リグノセリン酸:より好ましくはミリスチリン酸、パルミチン酸、ステアリン酸、アラキジン酸、ベヘン酸;更に好ましくはステアリン酸が挙げられる。 Saturated fatty acids and / or salts thereof may have 14 or more carbon atoms, but from the viewpoint of more effectively suppressing phase separation due to storage and further improving elongation when applied around the nails. , Preferably 14 to 30 carbon atoms, more preferably 14 to 24 carbon atoms, still more preferably 14 to 22 carbon atoms, and particularly preferably 18 carbon atoms. Saturated fatty acids, more specifically, myristic acid, palmitic acid, stearic acid, arachidic acid, behenic acid, lignoseric acid, cellotic acid, montanic acid, melicic acid; preferably myristic acid, palmitic acid, stearic acid, arachidic acid. , Bechenic acid, lignoseric acid: more preferably myristic acid, palmitic acid, stearic acid, arachidic acid, behenic acid; more preferably stealic acid.
炭素数14以上の飽和脂肪酸の塩としては、例えば、ナトリウム塩、カリウム塩等のアルカリ金属塩が挙げられる。 Examples of the salt of saturated fatty acid having 14 or more carbon atoms include alkali metal salts such as sodium salt and potassium salt.
本発明の外用組成物は、(E)成分として、炭素数14以上の飽和脂肪酸及びその塩の中から、1種を選択して使用してもよく、2種以上を組み合わせて使用してもよい。 In the external composition of the present invention, as the component (E), one may be selected and used from among saturated fatty acids having 14 or more carbon atoms and salts thereof, or two or more thereof may be used in combination. good.
本発明の外用乳化組成物に(E)成分を含有させる場合、その含有量としては、特に制限されないが、例えば、(E)成分の総量で0.01~10重量%、好ましくは0.1~6重量%、より好ましくは1~6重量%が挙げられる。 When the component (E) is contained in the external emulsified composition of the present invention, the content thereof is not particularly limited, but for example, the total amount of the component (E) is 0.01 to 10% by weight, preferably 0.1. 6% by weight, more preferably 1 to 6% by weight.
本発明の外用乳化組成物に(E)成分を含有させる場合、(A)成分と(E)成分の比率については、特に制限されないが、例えば、(A)成分の総量100重量部当たり、(E)成分が総量で0.1~1200重量部、好ましくは0.1~100重量部、より好ましくは0.1~50重量部が挙げられる。 When the external emulsifying composition of the present invention contains the component (E), the ratio of the component (A) to the component (E) is not particularly limited, but for example, per 100 parts by weight of the total amount of the component (A), ( E) The total amount of the components is 0.1 to 1200 parts by weight, preferably 0.1 to 100 parts by weight, and more preferably 0.1 to 50 parts by weight.
[多価アルコール]
本発明の外用乳化組成物には、必要に応じて、多価アルコールが含まれていてもよい。
[Multivalent alcohol]
The external emulsified composition of the present invention may contain a polyhydric alcohol, if necessary.
多価アルコールとしては、薬学的に許容されることを限度として、特に制限されないが、例えば、1,3-ブチレングリコール、プロピレングリコール、ジプロピレングリコール、ポリプロピレングリコール、グリセリン等が挙げられる。これらの多価アルコールの中でも、好ましくはグリセリンが挙げられる。これらの多価アルコールは、1種単独で使用してもよく、また2種以上を組み合わせて使用してもよい。 The polyhydric alcohol is not particularly limited as long as it is pharmaceutically acceptable, and examples thereof include 1,3-butylene glycol, propylene glycol, dipropylene glycol, polypropylene glycol, and glycerin. Among these polyhydric alcohols, glycerin is preferable. These polyhydric alcohols may be used alone or in combination of two or more.
本発明の外用乳化組成物に、多価アルコールを含有させる場合、その含有量については、特に制限されないが、例えば、多価アルコールの総量0.1~30重量%、好ましくは0.5~20重量%、より好ましくは1~10重量%が挙げられる。 When the external emulsified composition of the present invention contains a polyhydric alcohol, the content thereof is not particularly limited, but for example, the total amount of the polyhydric alcohol is 0.1 to 30% by weight, preferably 0.5 to 20%. By weight%, more preferably 1 to 10% by weight.
[(C)成分以外の界面活性剤]
本発明の皮膚の外用組成物は、必要に応じて、前記(C)成分以外の界面活性剤を含んでいてもよい。
[Surfactants other than component (C)]
The external composition for skin of the present invention may contain a surfactant other than the above-mentioned component (C), if necessary.
前記(C)成分以外の界面活性剤としては、前記(C)成分以外のノニオン性界面活性剤、アニオン性界面活性剤、カチオン性界面活性剤、両性界面活性剤等が挙げられる。これらの界面活性剤は、1種単独で使用してもよく、2種以上を組み合わせて使用してもよい。これらの界面活性剤の中でも、好ましくはノニオン性界面活性剤が挙げられる。 Examples of the surfactant other than the component (C) include nonionic surfactants, anionic surfactants, cationic surfactants, amphoteric surfactants and the like other than the component (C). These surfactants may be used alone or in combination of two or more. Among these surfactants, a nonionic surfactant is preferable.
本発明で使用されるノニオン性界面活性剤((C)成分以外)としては、薬学的に許容されることを限度として、特に制限されないが、例えば、ポリオキシエチレンソルビタン脂肪酸エステル、ポリオキシエチレンアルキルエーテル、ポリオキシエチレン硬化ヒマシ油等が挙げられる。これらのノニオン性界面活性剤の中でも、好ましくはポリオキシエチレンソルビタン脂肪酸エステル、ポリオキシエチレンアルキルエーテルが挙げられる。 The nonionic surfactant (other than the component (C)) used in the present invention is not particularly limited as long as it is pharmaceutically acceptable, but for example, polyoxyethylene sorbitan fatty acid ester and polyoxyethylene alkyl. Examples thereof include ether and polyoxyethylene cured castor oil. Among these nonionic surfactants, preferably, polyoxyethylene sorbitan fatty acid ester and polyoxyethylene alkyl ether can be mentioned.
ポリオキシエチレンソルビタン脂肪酸エステルを構成する酸化エチレン(EO)の平均付加モル数としては、特に制限されないが、例えば、5~40モル、好ましくは10~30モル、より好ましくは15~25モルが挙げられる。ポリオキシエチレンソルビタン脂肪酸エステルを構成する脂肪酸の炭素数としては、特に制限されないが、例えば、10~22個、好ましくは14~22個、より好ましくは16~20個が挙げられる。ポリオキシエチレンソルビタン脂肪酸エステルとして、具体的には、モノオレイン酸ポリオキシエチレンソルビタン、トリオレイン酸ポリオキシエチレンソルビタン、トリステアリ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等が挙げられる。これらのポリオキシエチレンソルビタン脂肪酸エステルの中でも、酸化エチレン(EO)の平均付加モル数が20であるモノステアリン酸ポリオキシエチレンソルビタン(ポリソルベート60)が挙げられる。 The average number of moles of ethylene oxide (EO) constituting the polyoxyethylene sorbitan fatty acid ester is not particularly limited, and examples thereof include 5 to 40 mol, preferably 10 to 30 mol, and more preferably 15 to 25 mol. Be done. The carbon number of the fatty acid constituting the polyoxyethylene sorbitan fatty acid ester is not particularly limited, and examples thereof include 10 to 22, preferably 14 to 22, and more preferably 16 to 20. Specific examples of the polyoxyethylene sorbitan fatty acid ester include polyoxyethylene sorbitan monooleate, polyoxyethylene sorbitan trioleate, polyoxyethylene sorbitan tristearate, and polyoxyethylene sorbitan monostearate. Among these polyoxyethylene sorbitan fatty acid esters, monostearate polyoxyethylene sorbitan (polysorbate 60) having an average addition mole number of ethylene oxide (EO) of 20 can be mentioned.
ポリオキシエチレンアルキルエーテルを構成する酸化エチレン(EO)の平均付加モル数としては、特に制限されないが、例えば、5~40モル、好ましくは10~30モル、より好ましくは15~25モルが挙げられる。ポリオキシエチレンアルキルエーテルを構成するアルキル基の炭素数としては、特に制限されないが、例えば、10~24個、好ましくは14~24個、より好ましくは16~24個が挙げられる。ポリオキシエチレンアルキルエーテルとして、具体的には、ポリオキシエチレンセチルエーテル、ポリオキシエチレンオレイルエーテル、ポリオキシエチレンステアリルエーテル、ポリオキシエチレンアラキルエーテル等が挙げられる。これらのポリオキシエチレンアルキルエーテルの中でも、好ましくはポリオキシエチレンアラキルエーテルが挙げられる。 The average number of moles of ethylene oxide (EO) constituting the polyoxyethylene alkyl ether is not particularly limited, and examples thereof include 5 to 40 mol, preferably 10 to 30 mol, and more preferably 15 to 25 mol. .. The number of carbon atoms of the alkyl group constituting the polyoxyethylene alkyl ether is not particularly limited, and examples thereof include 10 to 24 carbon atoms, preferably 14 to 24 carbon atoms, and more preferably 16 to 24 carbon atoms. Specific examples of the polyoxyethylene alkyl ether include polyoxyethylene cetyl ether, polyoxyethylene oleyl ether, polyoxyethylene stearyl ether, and polyoxyethylene araquil ether. Among these polyoxyethylene alkyl ethers, polyoxyethylene alkyl ethers are preferable.
本発明の外用乳化組成物に界面活性剤((C)成分以外)を含有させる場合、その含有量については、製剤形態、使用感等に応じて適宜設定すればよいが、例えば、界面活性剤((C)成分以外)の総量で0.5~20重量%、好ましくは1~15重量%、より好ましくは1.5~10重量%が挙げられる。 When the external emulsified composition of the present invention contains a surfactant (other than the component (C)), the content thereof may be appropriately set according to the pharmaceutical form, usability, etc., but for example, the surfactant. The total amount of (other than the component (C)) is 0.5 to 20% by weight, preferably 1 to 15% by weight, and more preferably 1.5 to 10% by weight.
[その他の成分]
本発明の外用乳化組成物は、前述する成分の他に、必要に応じて、通常使用される他の添加剤が含まれていてもよい。このような添加剤としては、例えば(E)成分以外の油性基剤、水、1価低級アルコール、pH調節剤、緩衝剤、可溶化剤、防腐剤、保存剤、酸化防止剤、安定化剤、香料、着色料等が挙げられる。本発明の外用乳化組成物において、これらの添加剤を含有させる場合、その含有量については、使用する添加剤の種類等に応じて適宜設定すればよい。
[Other ingredients]
In addition to the above-mentioned components, the external emulsified composition of the present invention may contain other commonly used additives, if necessary. Examples of such additives include oily bases other than the component (E), water, monohydric lower alcohols, pH regulators, buffers, solubilizers, preservatives, preservatives, antioxidants, and stabilizers. , Fragrances, coloring agents and the like. When these additives are contained in the external emulsification composition of the present invention, the content thereof may be appropriately set according to the type of the additive to be used and the like.
本発明の外用乳化組成物は、前述する成分の他に、薬理成分が含まれていてもよい。このような薬理成分としては、例えば、ステロイド剤、抗ヒスタミン剤、局所麻酔剤、抗炎症剤((B)成分以外)、保湿剤((A)成分以外)、殺菌剤、抗菌剤、鎮痒剤、皮膚保護剤、血行促進成分、ビタミン類、ムコ多糖類等が挙げられる。これらの薬理成分は、1種単独で使用してもよく、また2種以上を組み合わせて使用してもよい。また、本発明の外用組成物において、これらの薬理成分を含有させる場合、その濃度については、使用する薬理成分の種類、期待する効果等に応じて適宜設定すればよい。 The external emulsified composition of the present invention may contain a pharmacological component in addition to the above-mentioned components. Examples of such pharmacological components include steroids, antihistamines, local anesthetics, anti-inflammatory agents (other than component (B)), moisturizers (other than component (A)), bactericides, antibacterial agents, antipruritic agents, and skin. Protective agents, blood circulation promoting ingredients, vitamins, mucopolysaccharides and the like can be mentioned. These pharmacological components may be used alone or in combination of two or more. When these pharmacological components are contained in the external composition of the present invention, the concentration thereof may be appropriately set according to the type of the pharmacological component used, the expected effect, and the like.
[乳化タイプ・製剤形態]
本発明の外用乳化組成物の乳化タイプは、水中油型又は油中水型のいずれであってもよいが、好ましくは水中油型が挙げられる。
[Emulsification type / pharmaceutical form]
The emulsification type of the external emulsification composition of the present invention may be either an oil-in-water type or a water-in-oil type, and an oil-in-water type is preferable.
本発明の外用乳化組成物の製剤形態については、特に制限されないが、例えば、クリーム剤、乳液剤、ローション剤、リニメント剤、エアゾール剤等の外用医薬品が挙げられる。これらの中でも、好ましくはクリーム剤が挙げられる。 The pharmaceutical form of the external emulsified composition of the present invention is not particularly limited, and examples thereof include external pharmaceuticals such as creams, emulsions, lotions, liniments, and aerosols. Among these, a cream agent is preferably mentioned.
[用途]
本発明の外用乳化組成物の用途については、特に制限されないが、本発明の外用乳化組成物は、(A)成分に基づく角質の軟化又は除去作用及び保湿作用、(B)成分に基づく抗炎症作用を発揮できるので、角質の軟化又は除去、保湿、抗炎症等の用途に好適に使用される。特に、本発明の外用乳化組成物は、爪周りに適用した際の伸びが良好で、爪周りの角質を軟化させる効果に優れているので、爪周りの角質の軟化用途に好適に使用される。
[Use]
The use of the external emulsified composition of the present invention is not particularly limited, but the external emulsified composition of the present invention has a keratin softening or removing action and a moisturizing action based on the component (A), and an anti-inflammatory action based on the component (B). Since it can exert its action, it is suitably used for applications such as softening or removing keratin, moisturizing, and anti-inflammatory. In particular, the external emulsifying composition of the present invention has good elongation when applied around the nail and has an excellent effect of softening the keratin around the nail, and is therefore suitably used for softening the keratin around the nail. ..
[製造方法]
本発明の外用乳化組成物は、乳化タイプに応じて、公知の乳化製剤の製剤化手法に従って製造することができる。例えば、本発明の外用乳化組成物の製造方法としては、含有させる成分を水溶性成分と油性成分に分けて、水溶性成分を含む水相と、油性成分を含む油相とを調製し、これらを公知の手法に従って乳化させる方法が挙げられる。
[Production method]
The external emulsified composition of the present invention can be produced according to a known method for formulating an emulsified preparation, depending on the emulsified type. For example, in the method for producing an external emulsified composition of the present invention, the components to be contained are divided into a water-soluble component and an oil-based component, and an aqueous phase containing the water-soluble component and an oil phase containing the oil-based component are prepared. There is a method of emulsifying according to a known method.
以下に実施例を示して本発明をより具体的に説明するが、本発明はこれらに限定されるものではない。 Hereinafter, the present invention will be described in more detail with reference to examples, but the present invention is not limited thereto.
試験例1
表1~3に示す組成の外用乳化組成物(クリーム状の水中油型乳化製剤)を調製した。具体的には、先ず、界面活性剤(モノステアリン酸ソルビタン、セスキステアリン酸ソルビタン、トリステアリン酸ソルビタン、モノイソステアリン酸グリセリル、モノミリスチン酸グリセリル、モノステアリン酸グリセリル、ポリオキシエチレン硬化ヒマシ油10、ポリソルベート60)、脂肪酸(ステアリン酸、ミリスチン酸、パルミチン酸、ベヘン酸、オレイン酸、リノール酸)、炭化水素油(白色ワセリン、流動パラフィン)、セトステアリルアルコール、及びポリオキシエチレン・ステアリルアルコール混合物を所定量混合し、80℃で加熱溶解することにより、油相用組成物を調製した。また、別途、尿素、サリチル酸、グリシン、グリチルリチン酸モノアンモニウム、トリエタノールアミン及び水を所定量混合することにより、水相用組成物を調製した。次いで、80℃に加熱した水相用組成物を、80℃に加熱している油相用組成物に徐々に添加し混合して乳化操作を行い、外用乳化組成物(クリーム状の水中油型乳化製剤)を得た。製造直後の外用乳化組成物は、いずれも相分離を生じていない乳化形態であった。
Test Example 1
An external emulsified composition (creamy oil-in-water emulsified preparation) having the compositions shown in Tables 1 to 3 was prepared. Specifically, first, surfactants (sorbitan monostearate, sorbitan sesquistearate, sorbitan tristearate, glyceryl monoisostearate, glyceryl monomyristate, glyceryl monostearate, polyoxyethylene hydrogenated castor oil 10, polysorbate). 60), fatty acid (stearic acid, myristic acid, palmitic acid, behenic acid, oleic acid, linoleic acid), hydrocarbon oil (white vaseline, liquid paraffin), cetostearyl alcohol, and polyoxyethylene / stearyl alcohol mixture in a predetermined amount. A composition for an oil phase was prepared by mixing and heating and dissolving at 80 ° C. Separately, a composition for an aqueous phase was prepared by mixing a predetermined amount of urea, salicylic acid, glycine, monoammonium glycyrrhizinate, triethanolamine and water. Next, the aqueous phase composition heated to 80 ° C. is gradually added to the oil phase composition heated to 80 ° C., mixed and emulsified, and the external emulsified composition (creamy oil-in-water mold) is performed. Emulsified preparation) was obtained. The external emulsified compositions immediately after production were all in an emulsified form in which phase separation did not occur.
得られた各外用乳化組成物について、乳化状態の安定性、尿素の安定性、及び爪周りに塗布した際の伸びと角質軟化効果について、以下の方法で評価した。 For each of the obtained external emulsified compositions, the stability of the emulsified state, the stability of urea, and the elongation and keratin softening effect when applied around the nail were evaluated by the following methods.
<乳化状態の安定性>
調製直後の各外用乳化組成物16gを20ml容のガラス瓶に充填し、50℃の遮光条件で1カ月間保存した。1カ月間保存後の各外用乳化組成物の外観を目視にて観察し、「相分離が認められず、調製直後と同じ乳化状態を維持している状態」を15点、「相分離が認められ、乳化状態を安定に維持できておらず、振っても均一にならない状態」を1点として、乳化状態の安定性の程度を1~15点の間で評点化した。なお、参考のため、1点及び15点と評価される各外用乳化組成物の外観を図1に示す。
<Stability in emulsified state>
16 g of each external emulsified composition immediately after preparation was filled in a 20 ml glass bottle and stored for 1 month under a light-shielded condition of 50 ° C. The appearance of each external emulsified composition after storage for 1 month was visually observed, and 15 points were "a state in which phase separation was not observed and the same emulsified state as immediately after preparation was maintained", and "phase separation was observed". The degree of stability of the emulsified state was scored between 1 and 15 points, with 1 point being "a state in which the emulsified state could not be stably maintained and was not uniform even when shaken." For reference, FIG. 1 shows the appearance of each external emulsified composition evaluated as 1 point and 15 points.
<尿素の安定性>
調製直後の各外用乳化組成物16gを20ml容のガラス瓶に充填し、50℃の遮光条件で2カ月間保存した。保存前と2カ月保存後の各外用乳化組成物における尿素濃度をHPLCにて定量し、保存前の尿素濃度を100%として2カ月保存後の尿素の残存率(%)の小数点第一位を四捨五入した値を算出した。2カ月保存後の尿素の残存率(%)の値を以下の判定基準に従って分類した。
・判定基準
◎:尿素の残存率が98~100%
○:尿素の残存率が95~97%
△:尿素の残存率が92~94%
×:尿素の残存率が91%以下
<Urea stability>
16 g of each external emulsified composition immediately after preparation was filled in a 20 ml glass bottle and stored for 2 months under a light-shielded condition of 50 ° C. The urea concentration in each external emulsified composition before and after storage for 2 months is quantified by HPLC, and the urea concentration before storage is set to 100%, and the residual rate (%) of urea after storage for 2 months is set to the first decimal place. The rounded value was calculated. The value of the residual rate (%) of urea after storage for 2 months was classified according to the following criteria.
・ Judgment criteria ◎: Urea residual rate is 98-100%
◯: Urea residual rate is 95 to 97%
Δ: Urea residual rate is 92 to 94%
×: Urea residual rate is 91% or less
<爪周りに塗布した際の伸びと角質軟化効果>
爪周りの角層の硬化を自覚している被験者10名に、各外用乳化組成物0.1gを爪周りに1日1回の頻度で1週間塗布させ、1回目の塗布時における爪周りでの伸びと、1週間使用後の爪周りの角質の軟化効果について評価した。爪周りに塗布した際の伸びの評価は、「伸びがよい」、「どちらかといえば伸びがよい」、「どちらでもない」、「どちらかといえば伸びが悪い」、及び「伸びが悪い」の5段階で評価し、「伸びがよい」又は「どちらかといえば伸びがよい」と評価した被験者の合計人数を、爪周りに塗布した際の伸びのスコアとして算出した。また、爪周りの角質の軟化効果については、爪周りの角質の軟化効果の点で、「満足」、「やや満足」、「どちらともいえない」、「やや不満」及び「不満」の5段階で評価し、「満足」又は「やや満足」と評価した被験者の合計人数を、爪周りの角質の軟化効果のスコアとして算出した。
<Elongation and keratin softening effect when applied around nails>
Ten subjects who were aware of the hardening of the stratum corneum around the nails were allowed to apply 0.1 g of each external emulsified composition around the nails once a day for one week, and around the nails at the time of the first application. The elongation and the softening effect of the keratin around the nail after 1 week of use were evaluated. The evaluation of elongation when applied around the nails is "good elongation", "somewhat good elongation", "neither", "somewhat poor elongation", and "poor elongation". The total number of subjects who evaluated "good elongation" or "relatively good elongation" was calculated as a score of elongation when applied around the nail. Regarding the softening effect of the keratin around the nail, there are five stages of "satisfied", "slightly satisfied", "neither", "slightly dissatisfied" and "dissatisfied" in terms of the softening effect of the keratin around the nail. The total number of subjects evaluated as "satisfied" or "slightly satisfied" was calculated as the score of the softening effect of the keratin around the nail.
結果を表1~3に示す。尿素を単独で含む外用乳化組成物では、保存による相分離は生じておらず、尿素の分解も抑制されていたが、爪周りに塗布した際の伸び及び角質の軟化効果が不十分であった(参考例1)。一方、尿素及びサリチル酸を含む外用乳化組成物では、保存による相分離が顕著に生じており、尿素の分解も認められ、更に爪周りに塗布した際の伸び及び角質の軟化効果も不十分であった(比較例1及び2)。 The results are shown in Tables 1 to 3. In the external emulsification composition containing urea alone, phase separation did not occur due to storage and decomposition of urea was suppressed, but the elongation and softening effect of keratin when applied around the nails were insufficient. (Reference example 1). On the other hand, in the external emulsified composition containing urea and salicylic acid, phase separation due to storage occurs remarkably, decomposition of urea is also observed, and the elongation and softening effect of keratin when applied around the nail are insufficient. (Comparative Examples 1 and 2).
これに対して、尿素とサリチル酸と共に、ソルビタン脂肪酸エステル及び/又はグリセリン脂肪酸エステルを含む外用乳化組成物では、保存による相分離と尿素の分解を十分に抑制できており、更に爪周りに塗布した際の伸び及び角質の軟化効果が十分に向上していた(実施例1~15)。更に、グリシンを含まない場合には、保存による尿素の分解を格段顕著に抑制できていた(実施例7~15)。また、グリチルリチン酸モノアンモニウムを含む場合には、保存による相分離と尿素の分解に対する抑制効果、並びに爪周りに塗布した際の伸び及び角質の軟化効果が格段に向上していた(実施例9~15)。また、炭素数14以上の飽和脂肪酸を更に含む場合には、保存による相分離を格段顕著に抑制できており、更に爪周りに塗布した際の伸びについてもより一層向上していた(実施例11~15)。また、比較例1~2の各外用乳化組成物におけるサリチル酸をサリチル酸エチル又はサリチル酸メチルに変更した外用乳化組成物を調製し、試験例1と同じ方法で乳化状態、尿素の安定性、及び爪周りに塗布した際の伸びと角質軟化効果を評価したところ、これに対応する比較例1~2と同程度の相分離、尿素の分解が生じており、爪周りに塗布した際の伸びと角質の軟化効果のスコアも同程度であった。これに対し、実施例1~15の各外用組成物におけるサリチル酸をサリチル酸エチル又はサリチル酸メチルに変更した各外用乳化組成物を調製し、試験例1と同じ方法で乳化状態、尿素の安定性、及び、爪周りに塗布した際の伸びと角質軟化効果を評価したところ、これに対応する実施例1~15と同程度に相分離及び尿素の分解が抑制できており、爪周りに塗布した際の伸びと角質の軟化効果のスコアも同程度であった。 On the other hand, in the external emulsified composition containing sorbitan fatty acid ester and / or glycerin fatty acid ester together with urea and salicylic acid, phase separation and decomposition of urea due to storage can be sufficiently suppressed, and when applied around the nails. The elongation and softening effect of keratin were sufficiently improved (Examples 1 to 15). Furthermore, when glycine was not contained, the decomposition of urea due to storage could be remarkably suppressed (Examples 7 to 15). In addition, when monoammonium glycyrrhizinate was contained, the phase separation by storage and the effect of suppressing the decomposition of urea, and the effect of stretching and softening the keratin when applied around the nail were significantly improved (Examples 9 to 9). 15). Further, when the saturated fatty acid having 14 or more carbon atoms was further contained, the phase separation due to storage could be remarkably suppressed, and the elongation when applied around the nail was further improved (Example 11). ~ 15). Further, an external emulsified composition in which salicylic acid in each of the external emulsified compositions of Comparative Examples 1 and 2 was changed to ethyl salicylate or methyl salicylate was prepared, and the emulsified state, urea stability, and nail circumference were prepared by the same method as in Test Example 1. When the elongation and keratin softening effect when applied to were evaluated, the same degree of phase separation and urea decomposition as in Comparative Examples 1 and 2 corresponding to this occurred, and the elongation and keratin when applied around the nails The softening effect score was similar. On the other hand, each external emulsified composition in which salicylic acid in each external composition of Examples 1 to 15 was changed to ethyl salicylate or methyl salicylate was prepared, and the emulsified state, urea stability, and urea stability were prepared by the same method as in Test Example 1. When the elongation and the keratin softening effect when applied around the nail were evaluated, phase separation and the decomposition of urea could be suppressed to the same extent as in Examples 1 to 15 corresponding to this, and when applied around the nail. The scores of elongation and softening effect of keratin were similar.
処方例
表4に示す組成の外用乳化組成物(クリーム状の水中油型乳化製剤)を調製した。試験例1と同じ方法で、乳化状態、尿素の安定性、爪周りに塗布した際の伸びと角質軟化効果を評価した。処方例1~7の外用乳化組成物はいずれも保存による相分離と尿素の分解を十分に抑制できており、爪周りに塗布した際の伸びと角質軟化効果も優れていた。
Formulation Example An external emulsification composition (creamy oil-in-water emulsified preparation) having the composition shown in Table 4 was prepared. The emulsified state, the stability of urea, the elongation when applied around the nail, and the keratin softening effect were evaluated by the same method as in Test Example 1. The external emulsified compositions of Formulation Examples 1 to 7 were able to sufficiently suppress phase separation and urea decomposition during storage, and were also excellent in elongation and keratin softening effect when applied around the nail.
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