JP2021091609A - Emulsion composition - Google Patents
Emulsion composition Download PDFInfo
- Publication number
- JP2021091609A JP2021091609A JP2019221139A JP2019221139A JP2021091609A JP 2021091609 A JP2021091609 A JP 2021091609A JP 2019221139 A JP2019221139 A JP 2019221139A JP 2019221139 A JP2019221139 A JP 2019221139A JP 2021091609 A JP2021091609 A JP 2021091609A
- Authority
- JP
- Japan
- Prior art keywords
- salt
- weight
- carboxylic acid
- emulsified composition
- pyrrolidone carboxylic
- 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 98
- 239000000839 emulsion Substances 0.000 title abstract description 24
- 150000003839 salts Chemical class 0.000 claims abstract description 52
- ODHCTXKNWHHXJC-VKHMYHEASA-N 5-oxo-L-proline Chemical compound OC(=O)[C@@H]1CCC(=O)N1 ODHCTXKNWHHXJC-VKHMYHEASA-N 0.000 claims abstract description 51
- 229940079889 pyrrolidonecarboxylic acid Drugs 0.000 claims abstract description 49
- JDLSRXWHEBFHNC-UHFFFAOYSA-N Ufenamate Chemical compound CCCCOC(=O)C1=CC=CC=C1NC1=CC=CC(C(F)(F)F)=C1 JDLSRXWHEBFHNC-UHFFFAOYSA-N 0.000 claims abstract description 19
- 229950010121 ufenamate Drugs 0.000 claims abstract description 19
- 238000004945 emulsification Methods 0.000 claims description 34
- 238000000034 method Methods 0.000 claims description 11
- 230000006641 stabilisation Effects 0.000 claims description 8
- 238000011105 stabilization Methods 0.000 claims description 8
- -1 ascorbic acid glucoside Chemical class 0.000 description 55
- 239000003921 oil Substances 0.000 description 31
- 229920003171 Poly (ethylene oxide) Polymers 0.000 description 19
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 14
- 239000007788 liquid Substances 0.000 description 13
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 12
- 239000008346 aqueous phase Substances 0.000 description 12
- 235000014113 dietary fatty acids Nutrition 0.000 description 12
- 239000000194 fatty acid Substances 0.000 description 12
- 229930195729 fatty acid Natural products 0.000 description 12
- 238000003860 storage Methods 0.000 description 12
- 239000004359 castor oil Substances 0.000 description 9
- 230000001804 emulsifying effect Effects 0.000 description 9
- 239000004615 ingredient Substances 0.000 description 9
- 229920002125 Sokalan® Polymers 0.000 description 8
- 238000005191 phase separation Methods 0.000 description 8
- 239000004094 surface-active agent Substances 0.000 description 8
- 235000019438 castor oil Nutrition 0.000 description 7
- 235000011187 glycerol Nutrition 0.000 description 7
- ZEMPKEQAKRGZGQ-XOQCFJPHSA-N glycerol triricinoleate Natural products CCCCCC[C@@H](O)CC=CCCCCCCCC(=O)OC[C@@H](COC(=O)CCCCCCCC=CC[C@@H](O)CCCCCC)OC(=O)CCCCCCCC=CC[C@H](O)CCCCCC ZEMPKEQAKRGZGQ-XOQCFJPHSA-N 0.000 description 7
- 239000002562 thickening agent Substances 0.000 description 7
- 229920001214 Polysorbate 60 Polymers 0.000 description 6
- 239000012071 phase Substances 0.000 description 6
- 150000005846 sugar alcohols Polymers 0.000 description 6
- 239000002253 acid Substances 0.000 description 5
- 150000001298 alcohols Chemical class 0.000 description 5
- 238000009472 formulation Methods 0.000 description 5
- DNIAPMSPPWPWGF-UHFFFAOYSA-N monopropylene glycol Natural products CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 5
- 239000002736 nonionic surfactant Substances 0.000 description 5
- 238000000926 separation method Methods 0.000 description 5
- 229940045920 sodium pyrrolidone carboxylate Drugs 0.000 description 5
- HYRLWUFWDYFEES-UHFFFAOYSA-M sodium;2-oxopyrrolidine-1-carboxylate Chemical compound [Na+].[O-]C(=O)N1CCCC1=O HYRLWUFWDYFEES-UHFFFAOYSA-M 0.000 description 5
- PUPZLCDOIYMWBV-UHFFFAOYSA-N (+/-)-1,3-Butanediol Chemical compound CC(O)CCO PUPZLCDOIYMWBV-UHFFFAOYSA-N 0.000 description 4
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 4
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 description 4
- 239000002537 cosmetic Substances 0.000 description 4
- 239000003814 drug Substances 0.000 description 4
- 230000000694 effects Effects 0.000 description 4
- 239000006210 lotion Substances 0.000 description 4
- PRAKJMSDJKAYCZ-UHFFFAOYSA-N squalane Chemical compound CC(C)CCCC(C)CCCC(C)CCCCC(C)CCCC(C)CCCC(C)C PRAKJMSDJKAYCZ-UHFFFAOYSA-N 0.000 description 4
- KIUKXJAPPMFGSW-DNGZLQJQSA-N (2S,3S,4S,5R,6R)-6-[(2S,3R,4R,5S,6R)-3-Acetamido-2-[(2S,3S,4R,5R,6R)-6-[(2R,3R,4R,5S,6R)-3-acetamido-2,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-2-carboxy-4,5-dihydroxyoxan-3-yl]oxy-5-hydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-3,4,5-trihydroxyoxane-2-carboxylic acid Chemical compound CC(=O)N[C@H]1[C@H](O)O[C@H](CO)[C@@H](O)[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@H](O[C@H]2[C@@H]([C@@H](O[C@H]3[C@@H]([C@@H](O)[C@H](O)[C@H](O3)C(O)=O)O)[C@H](O)[C@@H](CO)O2)NC(C)=O)[C@@H](C(O)=O)O1 KIUKXJAPPMFGSW-DNGZLQJQSA-N 0.000 description 3
- 239000004215 Carbon black (E152) Substances 0.000 description 3
- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 description 3
- 239000004909 Moisturizer Substances 0.000 description 3
- YGSDEFSMJLZEOE-UHFFFAOYSA-N Salicylic acid Natural products OC(=O)C1=CC=CC=C1O YGSDEFSMJLZEOE-UHFFFAOYSA-N 0.000 description 3
- 239000006071 cream Substances 0.000 description 3
- MTHSVFCYNBDYFN-UHFFFAOYSA-N diethylene glycol Chemical compound OCCOCCO MTHSVFCYNBDYFN-UHFFFAOYSA-N 0.000 description 3
- GPLRAVKSCUXZTP-UHFFFAOYSA-N diglycerol Chemical compound OCC(O)COCC(O)CO GPLRAVKSCUXZTP-UHFFFAOYSA-N 0.000 description 3
- 229940079593 drug Drugs 0.000 description 3
- 125000003976 glyceryl group Chemical group [H]C([*])([H])C(O[H])([H])C(O[H])([H])[H] 0.000 description 3
- 229920002674 hyaluronan Polymers 0.000 description 3
- 229960003160 hyaluronic acid Drugs 0.000 description 3
- 229930195733 hydrocarbon Natural products 0.000 description 3
- 150000002430 hydrocarbons Chemical class 0.000 description 3
- 229940057995 liquid paraffin Drugs 0.000 description 3
- 238000002156 mixing Methods 0.000 description 3
- 230000001333 moisturizer Effects 0.000 description 3
- 235000010989 polyoxyethylene sorbitan monostearate Nutrition 0.000 description 3
- 239000001818 polyoxyethylene sorbitan monostearate Substances 0.000 description 3
- 229920002545 silicone oil Polymers 0.000 description 3
- 239000000230 xanthan gum Substances 0.000 description 3
- 235000010493 xanthan gum Nutrition 0.000 description 3
- 229920001285 xanthan gum Polymers 0.000 description 3
- 229940082509 xanthan gum Drugs 0.000 description 3
- 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 2
- 229940058015 1,3-butylene glycol Drugs 0.000 description 2
- VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 description 2
- LVYLCBNXHHHPSB-UHFFFAOYSA-N 2-hydroxyethyl salicylate Chemical compound OCCOC(=O)C1=CC=CC=C1O LVYLCBNXHHHPSB-UHFFFAOYSA-N 0.000 description 2
- BGRXBNZMPMGLQI-UHFFFAOYSA-N 2-octyldodecyl tetradecanoate Chemical compound CCCCCCCCCCCCCC(=O)OCC(CCCCCCCC)CCCCCCCCCC BGRXBNZMPMGLQI-UHFFFAOYSA-N 0.000 description 2
- HIQIXEFWDLTDED-UHFFFAOYSA-N 4-hydroxy-1-piperidin-4-ylpyrrolidin-2-one Chemical compound O=C1CC(O)CN1C1CCNCC1 HIQIXEFWDLTDED-UHFFFAOYSA-N 0.000 description 2
- ISWSIDIOOBJBQZ-UHFFFAOYSA-N Phenol Chemical compound OC1=CC=CC=C1 ISWSIDIOOBJBQZ-UHFFFAOYSA-N 0.000 description 2
- ODHCTXKNWHHXJC-UHFFFAOYSA-N acide pyroglutamique Natural products OC(=O)C1CCC(=O)N1 ODHCTXKNWHHXJC-UHFFFAOYSA-N 0.000 description 2
- 239000000654 additive Substances 0.000 description 2
- 229910052783 alkali metal Inorganic materials 0.000 description 2
- 150000005215 alkyl ethers Chemical class 0.000 description 2
- 239000002585 base Substances 0.000 description 2
- KVYGGMBOZFWZBQ-UHFFFAOYSA-N benzyl nicotinate Chemical compound C=1C=CN=CC=1C(=O)OCC1=CC=CC=C1 KVYGGMBOZFWZBQ-UHFFFAOYSA-N 0.000 description 2
- 235000019437 butane-1,3-diol Nutrition 0.000 description 2
- YKPUWZUDDOIDPM-SOFGYWHQSA-N capsaicin Chemical compound COC1=CC(CNC(=O)CCCC\C=C\C(C)C)=CC=C1O YKPUWZUDDOIDPM-SOFGYWHQSA-N 0.000 description 2
- 239000003795 chemical substances by application Substances 0.000 description 2
- 229960003957 dexamethasone Drugs 0.000 description 2
- UREBDLICKHMUKA-CXSFZGCWSA-N dexamethasone Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@@H](C)[C@@](C(=O)CO)(O)[C@@]1(C)C[C@@H]2O UREBDLICKHMUKA-CXSFZGCWSA-N 0.000 description 2
- 239000004205 dimethyl polysiloxane Substances 0.000 description 2
- 235000013870 dimethyl polysiloxane Nutrition 0.000 description 2
- 239000002612 dispersion medium Substances 0.000 description 2
- 239000003792 electrolyte Substances 0.000 description 2
- 239000010696 ester oil Substances 0.000 description 2
- JYGXADMDTFJGBT-VWUMJDOOSA-N hydrocortisone Chemical compound O=C1CC[C@]2(C)[C@H]3[C@@H](O)C[C@](C)([C@@](CC4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 JYGXADMDTFJGBT-VWUMJDOOSA-N 0.000 description 2
- CGIGDMFJXJATDK-UHFFFAOYSA-N indomethacin Chemical compound CC1=C(CC(O)=O)C2=CC(OC)=CC=C2N1C(=O)C1=CC=C(Cl)C=C1 CGIGDMFJXJATDK-UHFFFAOYSA-N 0.000 description 2
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 description 2
- 238000004519 manufacturing process Methods 0.000 description 2
- OSWPMRLSEDHDFF-UHFFFAOYSA-N methyl salicylate Chemical compound COC(=O)C1=CC=CC=C1O OSWPMRLSEDHDFF-UHFFFAOYSA-N 0.000 description 2
- 230000003020 moisturizing effect Effects 0.000 description 2
- JXTPJDDICSTXJX-UHFFFAOYSA-N n-Triacontane Natural products CCCCCCCCCCCCCCCCCCCCCCCCCCCCCC JXTPJDDICSTXJX-UHFFFAOYSA-N 0.000 description 2
- 229940073665 octyldodecyl myristate Drugs 0.000 description 2
- 239000002674 ointment Substances 0.000 description 2
- ZQPPMHVWECSIRJ-KTKRTIGZSA-N oleic acid Chemical compound CCCCCCCC\C=C/CCCCCCCC(O)=O ZQPPMHVWECSIRJ-KTKRTIGZSA-N 0.000 description 2
- FJKROLUGYXJWQN-UHFFFAOYSA-N papa-hydroxy-benzoic acid Natural products OC(=O)C1=CC=C(O)C=C1 FJKROLUGYXJWQN-UHFFFAOYSA-N 0.000 description 2
- 229920001983 poloxamer Polymers 0.000 description 2
- 229920000435 poly(dimethylsiloxane) Polymers 0.000 description 2
- 229920001451 polypropylene glycol Polymers 0.000 description 2
- 238000002360 preparation method Methods 0.000 description 2
- 239000003755 preservative agent Substances 0.000 description 2
- DQAKJEWZWDQURW-UHFFFAOYSA-N pyrrolidonecarboxylic acid Chemical class OC(=O)N1CCCC1=O DQAKJEWZWDQURW-UHFFFAOYSA-N 0.000 description 2
- 229960004889 salicylic acid Drugs 0.000 description 2
- 159000000000 sodium salts Chemical class 0.000 description 2
- 229940032094 squalane Drugs 0.000 description 2
- 239000003381 stabilizer Substances 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 1
- WCWXSMZXPXIUIR-UHFFFAOYSA-N (3-hydroxy-2,2-dimethylpropyl) 2,2-diethylhexanoate Chemical compound CCCCC(CC)(CC)C(=O)OCC(C)(C)CO WCWXSMZXPXIUIR-UHFFFAOYSA-N 0.000 description 1
- QYIXCDOBOSTCEI-QCYZZNICSA-N (5alpha)-cholestan-3beta-ol Chemical compound C([C@@H]1CC2)[C@@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H]([C@H](C)CCCC(C)C)[C@@]2(C)CC1 QYIXCDOBOSTCEI-QCYZZNICSA-N 0.000 description 1
- OHILSKSRDDTCIR-WKSAPEMMSA-N (8s,9r,10s,11s,13s,14s,16r,17r)-9-fluoro-11,17-dihydroxy-17-(2-hydroxyacetyl)-10,13,16-trimethyl-6,7,8,11,12,14,15,16-octahydrocyclopenta[a]phenanthren-3-one;hydrochloride Chemical compound Cl.C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@@H](C)[C@@](C(=O)CO)(O)[C@@]1(C)C[C@@H]2O OHILSKSRDDTCIR-WKSAPEMMSA-N 0.000 description 1
- WRIDQFICGBMAFQ-UHFFFAOYSA-N (E)-8-Octadecenoic acid Natural products CCCCCCCCCC=CCCCCCCC(O)=O WRIDQFICGBMAFQ-UHFFFAOYSA-N 0.000 description 1
- 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
- LEBVLXFERQHONN-UHFFFAOYSA-N 1-butyl-N-(2,6-dimethylphenyl)piperidine-2-carboxamide Chemical compound CCCCN1CCCCC1C(=O)NC1=C(C)C=CC=C1C LEBVLXFERQHONN-UHFFFAOYSA-N 0.000 description 1
- FDCJDKXCCYFOCV-UHFFFAOYSA-N 1-hexadecoxyhexadecane Chemical compound CCCCCCCCCCCCCCCCOCCCCCCCCCCCCCCCC FDCJDKXCCYFOCV-UHFFFAOYSA-N 0.000 description 1
- IXPNQXFRVYWDDI-UHFFFAOYSA-N 1-methyl-2,4-dioxo-1,3-diazinane-5-carboximidamide Chemical compound CN1CC(C(N)=N)C(=O)NC1=O IXPNQXFRVYWDDI-UHFFFAOYSA-N 0.000 description 1
- JNAYPSWVMNJOPQ-UHFFFAOYSA-N 2,3-bis(16-methylheptadecanoyloxy)propyl 16-methylheptadecanoate Chemical compound CC(C)CCCCCCCCCCCCCCC(=O)OCC(OC(=O)CCCCCCCCCCCCCCC(C)C)COC(=O)CCCCCCCCCCCCCCC(C)C JNAYPSWVMNJOPQ-UHFFFAOYSA-N 0.000 description 1
- JPWUIQIFCDAWQX-UHFFFAOYSA-N 2,3-dihydroxypropyl 2-ethylhexanoate Chemical compound CCCCC(CC)C(=O)OCC(O)CO JPWUIQIFCDAWQX-UHFFFAOYSA-N 0.000 description 1
- CIVCELMLGDGMKZ-UHFFFAOYSA-N 2,4-dichloro-6-methylpyridine-3-carboxylic acid Chemical compound CC1=CC(Cl)=C(C(O)=O)C(Cl)=N1 CIVCELMLGDGMKZ-UHFFFAOYSA-N 0.000 description 1
- ILCOCZBHMDEIAI-UHFFFAOYSA-N 2-(2-octadecoxyethoxy)ethanol Chemical compound CCCCCCCCCCCCCCCCCCOCCOCCO ILCOCZBHMDEIAI-UHFFFAOYSA-N 0.000 description 1
- FKOKUHFZNIUSLW-UHFFFAOYSA-N 2-Hydroxypropyl stearate Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(C)O FKOKUHFZNIUSLW-UHFFFAOYSA-N 0.000 description 1
- MSWZFWKMSRAUBD-IVMDWMLBSA-N 2-amino-2-deoxy-D-glucopyranose Chemical compound N[C@H]1C(O)O[C@H](CO)[C@@H](O)[C@@H]1O MSWZFWKMSRAUBD-IVMDWMLBSA-N 0.000 description 1
- SPCKHVPPRJWQRZ-UHFFFAOYSA-N 2-benzhydryloxy-n,n-dimethylethanamine;2-hydroxypropane-1,2,3-tricarboxylic acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O.C=1C=CC=CC=1C(OCCN(C)C)C1=CC=CC=C1 SPCKHVPPRJWQRZ-UHFFFAOYSA-N 0.000 description 1
- XCPXJFFSGMERLK-UHFFFAOYSA-N 2-butyl-2-ethyloctadecanoic acid Chemical compound CCCCCCCCCCCCCCCCC(CC)(C(O)=O)CCCC XCPXJFFSGMERLK-UHFFFAOYSA-N 0.000 description 1
- TWJNQYPJQDRXPH-UHFFFAOYSA-N 2-cyanobenzohydrazide Chemical compound NNC(=O)C1=CC=CC=C1C#N TWJNQYPJQDRXPH-UHFFFAOYSA-N 0.000 description 1
- GECRRQVLQHRVNH-MRCUWXFGSA-N 2-octyldodecyl (z)-octadec-9-enoate Chemical compound CCCCCCCCCCC(CCCCCCCC)COC(=O)CCCCCCC\C=C/CCCCCCCC GECRRQVLQHRVNH-MRCUWXFGSA-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
- XPFCZYUVICHKDS-UHFFFAOYSA-N 3-methylbutane-1,3-diol Chemical compound CC(C)(O)CCO XPFCZYUVICHKDS-UHFFFAOYSA-N 0.000 description 1
- CYDQOEWLBCCFJZ-UHFFFAOYSA-N 4-(4-fluorophenyl)oxane-4-carboxylic acid Chemical compound C=1C=C(F)C=CC=1C1(C(=O)O)CCOCC1 CYDQOEWLBCCFJZ-UHFFFAOYSA-N 0.000 description 1
- TZZAKSLHHIJRLL-UHFFFAOYSA-N 4-hydroxy-3-methoxybenzamide Chemical compound COC1=CC(C(N)=O)=CC=C1O TZZAKSLHHIJRLL-UHFFFAOYSA-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
- QSBYPNXLFMSGKH-UHFFFAOYSA-N 9-Heptadecensaeure Natural products CCCCCCCC=CCCCCCCCC(O)=O QSBYPNXLFMSGKH-UHFFFAOYSA-N 0.000 description 1
- 229920001817 Agar Polymers 0.000 description 1
- VHUUQVKOLVNVRT-UHFFFAOYSA-N Ammonium hydroxide Chemical compound [NH4+].[OH-] VHUUQVKOLVNVRT-UHFFFAOYSA-N 0.000 description 1
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Natural products OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 description 1
- GHXZTYHSJHQHIJ-UHFFFAOYSA-N Chlorhexidine Chemical compound C=1C=C(Cl)C=CC=1NC(N)=NC(N)=NCCCCCCN=C(N)N=C(N)NC1=CC=C(Cl)C=C1 GHXZTYHSJHQHIJ-UHFFFAOYSA-N 0.000 description 1
- WJLVQTJZDCGNJN-UHFFFAOYSA-N Chlorhexidine hydrochloride Chemical compound Cl.Cl.C=1C=C(Cl)C=CC=1NC(N)=NC(N)=NCCCCCCN=C(N)N=C(N)NC1=CC=C(Cl)C=C1 WJLVQTJZDCGNJN-UHFFFAOYSA-N 0.000 description 1
- KCXVZYZYPLLWCC-UHFFFAOYSA-N EDTA Chemical compound OC(=O)CN(CC(O)=O)CCN(CC(O)=O)CC(O)=O KCXVZYZYPLLWCC-UHFFFAOYSA-N 0.000 description 1
- 239000001856 Ethyl cellulose Substances 0.000 description 1
- ZZSNKZQZMQGXPY-UHFFFAOYSA-N Ethyl cellulose Chemical compound CCOCC1OC(OC)C(OCC)C(OCC)C1OC1C(O)C(O)C(OC)C(CO)O1 ZZSNKZQZMQGXPY-UHFFFAOYSA-N 0.000 description 1
- FPVVYTCTZKCSOJ-UHFFFAOYSA-N Ethylene glycol distearate Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCCOC(=O)CCCCCCCCCCCCCCCCC FPVVYTCTZKCSOJ-UHFFFAOYSA-N 0.000 description 1
- 229930091371 Fructose Natural products 0.000 description 1
- RFSUNEUAIZKAJO-ARQDHWQXSA-N Fructose Chemical compound OC[C@H]1O[C@](O)(CO)[C@@H](O)[C@@H]1O RFSUNEUAIZKAJO-ARQDHWQXSA-N 0.000 description 1
- 239000005715 Fructose Substances 0.000 description 1
- 229920002683 Glycosaminoglycan Polymers 0.000 description 1
- HSRJKNPTNIJEKV-UHFFFAOYSA-N Guaifenesin Chemical compound COC1=CC=CC=C1OCC(O)CO HSRJKNPTNIJEKV-UHFFFAOYSA-N 0.000 description 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 1
- 239000004166 Lanolin Substances 0.000 description 1
- 235000021360 Myristic acid Nutrition 0.000 description 1
- TUNFSRHWOTWDNC-UHFFFAOYSA-N Myristic acid Natural products CCCCCCCCCCCCCC(O)=O TUNFSRHWOTWDNC-UHFFFAOYSA-N 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
- OQILCOQZDHPEAZ-UHFFFAOYSA-N Palmitinsaeure-octylester Natural products CCCCCCCCCCCCCCCC(=O)OCCCCCCCC OQILCOQZDHPEAZ-UHFFFAOYSA-N 0.000 description 1
- LRJOMUJRLNCICJ-JZYPGELDSA-N Prednisolone acetate Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@@](C(=O)COC(=O)C)(O)[C@@]1(C)C[C@@H]2O LRJOMUJRLNCICJ-JZYPGELDSA-N 0.000 description 1
- KCLANYCVBBTKTO-UHFFFAOYSA-N Proparacaine Chemical compound CCCOC1=CC=C(C(=O)OCCN(CC)CC)C=C1N KCLANYCVBBTKTO-UHFFFAOYSA-N 0.000 description 1
- ODHCTXKNWHHXJC-GSVOUGTGSA-N Pyroglutamic acid Natural products OC(=O)[C@H]1CCC(=O)N1 ODHCTXKNWHHXJC-GSVOUGTGSA-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
- 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 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
- NCHJGQKLPRTMAO-XWVZOOPGSA-N [(2R)-2-[(2R,3R,4S)-3,4-dihydroxyoxolan-2-yl]-2-hydroxyethyl] 16-methylheptadecanoate Chemical compound CC(C)CCCCCCCCCCCCCCC(=O)OC[C@@H](O)[C@H]1OC[C@H](O)[C@H]1O NCHJGQKLPRTMAO-XWVZOOPGSA-N 0.000 description 1
- FPVRUILUEYSIMD-RPRRAYFGSA-N [(8s,9r,10s,11s,13s,14s,16r,17r)-9-fluoro-11-hydroxy-17-(2-hydroxyacetyl)-10,13,16-trimethyl-3-oxo-6,7,8,11,12,14,15,16-octahydrocyclopenta[a]phenanthren-17-yl] acetate Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@@H](C)[C@@](C(=O)CO)(OC(C)=O)[C@@]1(C)C[C@@H]2O FPVRUILUEYSIMD-RPRRAYFGSA-N 0.000 description 1
- MZVQCMJNVPIDEA-UHFFFAOYSA-N [CH2]CN(CC)CC Chemical group [CH2]CN(CC)CC MZVQCMJNVPIDEA-UHFFFAOYSA-N 0.000 description 1
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 description 1
- 239000000443 aerosol Substances 0.000 description 1
- 238000004220 aggregation Methods 0.000 description 1
- 230000002776 aggregation Effects 0.000 description 1
- 239000003513 alkali Substances 0.000 description 1
- QYIXCDOBOSTCEI-UHFFFAOYSA-N alpha-cholestanol Natural products C1CC2CC(O)CCC2(C)C2C1C1CCC(C(C)CCCC(C)C)C1(C)CC2 QYIXCDOBOSTCEI-UHFFFAOYSA-N 0.000 description 1
- QGZKDVFQNNGYKY-UHFFFAOYSA-N ammonia Natural products N QGZKDVFQNNGYKY-UHFFFAOYSA-N 0.000 description 1
- 150000003863 ammonium salts Chemical class 0.000 description 1
- 239000002280 amphoteric surfactant Substances 0.000 description 1
- 239000003945 anionic surfactant Substances 0.000 description 1
- 230000000844 anti-bacterial effect Effects 0.000 description 1
- 229940121363 anti-inflammatory agent Drugs 0.000 description 1
- 239000002260 anti-inflammatory agent Substances 0.000 description 1
- 229940125715 antihistaminic agent Drugs 0.000 description 1
- 239000000739 antihistaminic agent Substances 0.000 description 1
- 239000003963 antioxidant agent Substances 0.000 description 1
- 235000006708 antioxidants Nutrition 0.000 description 1
- 239000003908 antipruritic agent Substances 0.000 description 1
- 239000007864 aqueous solution Substances 0.000 description 1
- 235000010323 ascorbic acid Nutrition 0.000 description 1
- 229960005070 ascorbic acid Drugs 0.000 description 1
- 239000011668 ascorbic acid Substances 0.000 description 1
- 239000003899 bactericide agent Substances 0.000 description 1
- UREZNYTWGJKWBI-UHFFFAOYSA-M benzethonium chloride Chemical compound [Cl-].C1=CC(C(C)(C)CC(C)(C)C)=CC=C1OCCOCC[N+](C)(C)CC1=CC=CC=C1 UREZNYTWGJKWBI-UHFFFAOYSA-M 0.000 description 1
- 229960001950 benzethonium chloride Drugs 0.000 description 1
- 229960005274 benzocaine Drugs 0.000 description 1
- BLFLLBZGZJTVJG-UHFFFAOYSA-N benzocaine Chemical compound CCOC(=O)C1=CC=C(N)C=C1 BLFLLBZGZJTVJG-UHFFFAOYSA-N 0.000 description 1
- 229950004580 benzyl nicotinate Drugs 0.000 description 1
- MSWZFWKMSRAUBD-UHFFFAOYSA-N beta-D-galactosamine Natural products NC1C(O)OC(CO)C(O)C1O MSWZFWKMSRAUBD-UHFFFAOYSA-N 0.000 description 1
- 230000017531 blood circulation Effects 0.000 description 1
- 239000000872 buffer Substances 0.000 description 1
- 229960003150 bupivacaine Drugs 0.000 description 1
- 159000000007 calcium salts Chemical class 0.000 description 1
- 229960002504 capsaicin Drugs 0.000 description 1
- 235000017663 capsaicin Nutrition 0.000 description 1
- 229940007061 capsicum extract Drugs 0.000 description 1
- 239000001943 capsicum frutescens fruit extract Substances 0.000 description 1
- 239000001768 carboxy methyl cellulose Substances 0.000 description 1
- 235000010418 carrageenan Nutrition 0.000 description 1
- 239000000679 carrageenan Substances 0.000 description 1
- 229920001525 carrageenan Polymers 0.000 description 1
- 229940113118 carrageenan Drugs 0.000 description 1
- 239000003093 cationic surfactant Substances 0.000 description 1
- 238000005119 centrifugation Methods 0.000 description 1
- 229960001927 cetylpyridinium chloride Drugs 0.000 description 1
- YMKDRGPMQRFJGP-UHFFFAOYSA-M cetylpyridinium chloride Chemical compound [Cl-].CCCCCCCCCCCCCCCC[N+]1=CC=CC=C1 YMKDRGPMQRFJGP-UHFFFAOYSA-M 0.000 description 1
- 239000002738 chelating agent Substances 0.000 description 1
- 229960003260 chlorhexidine Drugs 0.000 description 1
- 229960003333 chlorhexidine gluconate Drugs 0.000 description 1
- YZIYKJHYYHPJIB-UUPCJSQJSA-N chlorhexidine gluconate Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C(O)=O.OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C(O)=O.C1=CC(Cl)=CC=C1NC(=N)NC(=N)NCCCCCCNC(=N)NC(=N)NC1=CC=C(Cl)C=C1 YZIYKJHYYHPJIB-UUPCJSQJSA-N 0.000 description 1
- 229960004504 chlorhexidine hydrochloride Drugs 0.000 description 1
- 229960002023 chloroprocaine Drugs 0.000 description 1
- VDANGULDQQJODZ-UHFFFAOYSA-N chloroprocaine Chemical compound CCN(CC)CCOC(=O)C1=CC=C(N)C=C1Cl VDANGULDQQJODZ-UHFFFAOYSA-N 0.000 description 1
- KXKPYJOVDUMHGS-OSRGNVMNSA-N chondroitin sulfate Chemical compound CC(=O)N[C@H]1[C@H](O)O[C@H](OS(O)(=O)=O)[C@H](O)[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](C(O)=O)O1 KXKPYJOVDUMHGS-OSRGNVMNSA-N 0.000 description 1
- 229960001747 cinchocaine Drugs 0.000 description 1
- PUFQVTATUTYEAL-UHFFFAOYSA-N cinchocaine Chemical compound C1=CC=CC2=NC(OCCCC)=CC(C(=O)NCCN(CC)CC)=C21 PUFQVTATUTYEAL-UHFFFAOYSA-N 0.000 description 1
- 239000003086 colorant Substances 0.000 description 1
- DNTGGZPQPQTDQF-XBXARRHUSA-N crotamiton Chemical compound C/C=C/C(=O)N(CC)C1=CC=CC=C1C DNTGGZPQPQTDQF-XBXARRHUSA-N 0.000 description 1
- 229960003338 crotamiton Drugs 0.000 description 1
- 229960003657 dexamethasone acetate Drugs 0.000 description 1
- 229960001193 diclofenac sodium Drugs 0.000 description 1
- 229940105990 diglycerin Drugs 0.000 description 1
- 229960000520 diphenhydramine Drugs 0.000 description 1
- 229960000525 diphenhydramine hydrochloride Drugs 0.000 description 1
- SZXQTJUDPRGNJN-UHFFFAOYSA-N dipropylene glycol Chemical compound OCCCOCCCO SZXQTJUDPRGNJN-UHFFFAOYSA-N 0.000 description 1
- 235000019325 ethyl cellulose Nutrition 0.000 description 1
- 229920001249 ethyl cellulose Polymers 0.000 description 1
- GJQLBGWSDGMZKM-UHFFFAOYSA-N ethylhexyl palmitate Chemical compound CCCCCCCCCCCCCCCC(=O)OC(CC)CCCCC GJQLBGWSDGMZKM-UHFFFAOYSA-N 0.000 description 1
- 230000003631 expected effect Effects 0.000 description 1
- 150000004665 fatty acids Chemical class 0.000 description 1
- 229960004369 flufenamic acid Drugs 0.000 description 1
- 239000003205 fragrance Substances 0.000 description 1
- 239000000499 gel Substances 0.000 description 1
- 239000000451 gelidium spp. gum Substances 0.000 description 1
- 229960002442 glucosamine Drugs 0.000 description 1
- 229930182478 glucoside Natural products 0.000 description 1
- 229940075507 glyceryl monostearate Drugs 0.000 description 1
- KWIUHFFTVRNATP-UHFFFAOYSA-N glycine betaine Chemical compound C[N+](C)(C)CC([O-])=O KWIUHFFTVRNATP-UHFFFAOYSA-N 0.000 description 1
- 229960002389 glycol salicylate Drugs 0.000 description 1
- 230000005484 gravity Effects 0.000 description 1
- 229960000890 hydrocortisone Drugs 0.000 description 1
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 description 1
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 description 1
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 description 1
- 229960003943 hypromellose Drugs 0.000 description 1
- 229960000905 indomethacin Drugs 0.000 description 1
- QXJSBBXBKPUZAA-UHFFFAOYSA-N isooleic acid Natural products CCCCCCCC=CCCCCCCCCC(O)=O QXJSBBXBKPUZAA-UHFFFAOYSA-N 0.000 description 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 1
- 239000004310 lactic acid Substances 0.000 description 1
- 235000014655 lactic acid Nutrition 0.000 description 1
- 229940039717 lanolin Drugs 0.000 description 1
- 235000019388 lanolin Nutrition 0.000 description 1
- 239000000865 liniment Substances 0.000 description 1
- 229910003002 lithium salt Inorganic materials 0.000 description 1
- 159000000002 lithium salts Chemical class 0.000 description 1
- 238000002690 local anesthesia Methods 0.000 description 1
- 229960002373 loxoprofen Drugs 0.000 description 1
- WORCCYVLMMTGFR-UHFFFAOYSA-M loxoprofen sodium Chemical compound [Na+].C1=CC(C(C([O-])=O)C)=CC=C1CC1C(=O)CCC1 WORCCYVLMMTGFR-UHFFFAOYSA-M 0.000 description 1
- 229960003511 macrogol Drugs 0.000 description 1
- 159000000003 magnesium salts Chemical class 0.000 description 1
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 description 1
- 229960002409 mepivacaine Drugs 0.000 description 1
- INWLQCZOYSRPNW-UHFFFAOYSA-N mepivacaine Chemical compound CN1CCCCC1C(=O)NC1=C(C)C=CC=C1C INWLQCZOYSRPNW-UHFFFAOYSA-N 0.000 description 1
- 229910052751 metal Inorganic materials 0.000 description 1
- 239000002184 metal Substances 0.000 description 1
- 229960001047 methyl salicylate Drugs 0.000 description 1
- 239000001788 mono and diglycerides of fatty acids Substances 0.000 description 1
- TZBAVQKIEKDGFH-UHFFFAOYSA-N n-[2-(diethylamino)ethyl]-1-benzothiophene-2-carboxamide;hydrochloride Chemical compound [Cl-].C1=CC=C2SC(C(=O)NCC[NH+](CC)CC)=CC2=C1 TZBAVQKIEKDGFH-UHFFFAOYSA-N 0.000 description 1
- 239000000041 non-steroidal anti-inflammatory agent Substances 0.000 description 1
- 229940021182 non-steroidal anti-inflammatory drug Drugs 0.000 description 1
- 125000001400 nonyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- CKQVRZJOMJRTOY-UHFFFAOYSA-N octadecanoic acid;propane-1,2,3-triol Chemical compound OCC(O)CO.CCCCCCCCCCCCCCCCCC(O)=O CKQVRZJOMJRTOY-UHFFFAOYSA-N 0.000 description 1
- HMMGMWAXVFQUOA-UHFFFAOYSA-N octamethylcyclotetrasiloxane Chemical compound C[Si]1(C)O[Si](C)(C)O[Si](C)(C)O[Si](C)(C)O1 HMMGMWAXVFQUOA-UHFFFAOYSA-N 0.000 description 1
- 229940049964 oleate Drugs 0.000 description 1
- 239000002245 particle Substances 0.000 description 1
- 239000008194 pharmaceutical composition Substances 0.000 description 1
- 230000035790 physiological processes and functions Effects 0.000 description 1
- 229920003023 plastic Polymers 0.000 description 1
- 229920001223 polyethylene glycol Polymers 0.000 description 1
- 229920000259 polyoxyethylene lauryl ether Polymers 0.000 description 1
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 description 1
- 239000000244 polyoxyethylene sorbitan monooleate Substances 0.000 description 1
- 229920000053 polysorbate 80 Polymers 0.000 description 1
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
- XAEFZNCEHLXOMS-UHFFFAOYSA-M potassium benzoate Chemical compound [K+].[O-]C(=O)C1=CC=CC=C1 XAEFZNCEHLXOMS-UHFFFAOYSA-M 0.000 description 1
- 229960005205 prednisolone Drugs 0.000 description 1
- OIGNJSKKLXVSLS-VWUMJDOOSA-N prednisolone Chemical compound O=C1C=C[C@]2(C)[C@H]3[C@@H](O)C[C@](C)([C@@](CC4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 OIGNJSKKLXVSLS-VWUMJDOOSA-N 0.000 description 1
- 229960002800 prednisolone acetate Drugs 0.000 description 1
- 229960004919 procaine Drugs 0.000 description 1
- MFDFERRIHVXMIY-UHFFFAOYSA-N procaine Chemical compound CCN(CC)CCOC(=O)C1=CC=C(N)C=C1 MFDFERRIHVXMIY-UHFFFAOYSA-N 0.000 description 1
- 229960003981 proparacaine Drugs 0.000 description 1
- 229940093625 propylene glycol monostearate Drugs 0.000 description 1
- 229940043131 pyroglutamate Drugs 0.000 description 1
- 235000010413 sodium alginate Nutrition 0.000 description 1
- 239000000661 sodium alginate Substances 0.000 description 1
- 229940005550 sodium alginate Drugs 0.000 description 1
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 1
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 description 1
- 239000001540 sodium lactate Substances 0.000 description 1
- 229940005581 sodium lactate Drugs 0.000 description 1
- 235000011088 sodium lactate Nutrition 0.000 description 1
- JGMJQSFLQWGYMQ-UHFFFAOYSA-M sodium;2,6-dichloro-n-phenylaniline;acetate Chemical compound [Na+].CC([O-])=O.ClC1=CC=CC(Cl)=C1NC1=CC=CC=C1 JGMJQSFLQWGYMQ-UHFFFAOYSA-M 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 229940035044 sorbitan monolaurate Drugs 0.000 description 1
- 235000011069 sorbitan monooleate Nutrition 0.000 description 1
- 239000001593 sorbitan monooleate Substances 0.000 description 1
- 229940035049 sorbitan monooleate 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
- 235000011076 sorbitan monostearate Nutrition 0.000 description 1
- 239000001587 sorbitan monostearate Substances 0.000 description 1
- 229940035048 sorbitan monostearate Drugs 0.000 description 1
- 229960005078 sorbitan sesquioleate Drugs 0.000 description 1
- 235000019337 sorbitan trioleate Nutrition 0.000 description 1
- 229960000391 sorbitan trioleate Drugs 0.000 description 1
- 230000000087 stabilizing effect Effects 0.000 description 1
- 229940098760 steareth-2 Drugs 0.000 description 1
- 150000003431 steroids Chemical class 0.000 description 1
- 229960002372 tetracaine Drugs 0.000 description 1
- GKCBAIGFKIBETG-UHFFFAOYSA-N tetracaine Chemical compound CCCCNC1=CC=C(C(=O)OCCN(C)C)C=C1 GKCBAIGFKIBETG-UHFFFAOYSA-N 0.000 description 1
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 1
- LENZDBCJOHFCAS-UHFFFAOYSA-N tris Chemical compound OCC(N)(CO)CO LENZDBCJOHFCAS-UHFFFAOYSA-N 0.000 description 1
- 239000011782 vitamin Substances 0.000 description 1
- 229940088594 vitamin Drugs 0.000 description 1
- 235000013343 vitamin Nutrition 0.000 description 1
- 229930003231 vitamin Natural products 0.000 description 1
- 235000019155 vitamin A Nutrition 0.000 description 1
- 239000011719 vitamin A Substances 0.000 description 1
- 229920003169 water-soluble polymer Polymers 0.000 description 1
- 239000001993 wax Substances 0.000 description 1
- UHVMMEOXYDMDKI-JKYCWFKZSA-L zinc;1-(5-cyanopyridin-2-yl)-3-[(1s,2s)-2-(6-fluoro-2-hydroxy-3-propanoylphenyl)cyclopropyl]urea;diacetate Chemical compound [Zn+2].CC([O-])=O.CC([O-])=O.CCC(=O)C1=CC=C(F)C([C@H]2[C@H](C2)NC(=O)NC=2N=CC(=CC=2)C#N)=C1O UHVMMEOXYDMDKI-JKYCWFKZSA-L 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Cosmetics (AREA)
Abstract
Description
本発明は、ピロリドンカルボン酸及び/又はその塩を含有する乳化組成物でありながら、性状の安定性に優れた乳化組成物に関する。 The present invention relates to an emulsified composition containing pyrrolidone carboxylic acid and / or a salt thereof, which is excellent in property stability.
乳化組成物は、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。このため、乳化組成物は、外用医薬品や化粧料の分野において汎用されている。 The emulsified composition can contain an aqueous component and an oily component, can be used for various pharmaceutical formulations, and has an excellent usability when applied to the skin. Therefore, the emulsified composition is widely used in the fields of external medicines and cosmetics.
ピロリドンカルボン酸ナトリウムは、外用組成物において保湿剤として配合される成分であり、乳化組成物にも配合される。 Sodium pyrrolidone carboxylate is a component to be blended as a moisturizer in an external composition, and is also blended in an emulsified composition.
例えば、特許文献1には、α−モノアルキルグリセリルエーテルと、ワックス類と、所定のシリコーン油とを含有する乳化組成物において、グリセリン、果糖、トリメチルグリシン、乳酸ナトリウム、ピロリドンカルボン酸ソーダからなる群より選択される保湿剤が配合されてよいことが記載されている。特許文献2には、所定の寒天とキサンタンガムとを所定の質量比で混合した水溶性高分子0.1〜10質量%と、水30質量%以上とを含有する乳化組成物において、ヒアルロン酸又はその塩、ピロリドンカルボン酸又はその塩、グリセリン、ジグリセリン、及びポリグリセリンから選ばれる1種以上の保湿剤が配合されてよいことが記載されている。特許文献3には、アスコルビン酸グルコシド、2−アミノ−2−ヒドロキシメチル−1,3−プロパンジオール、及びエチレンジアミン四酢酸又はその塩を含む所定pHの皮膚外用組成物が、乳化組成物として調製されることができ、ピロリドンカルボン酸又はその塩が配合されてよいことが記載されている。 For example, Patent Document 1 describes a group consisting of glycerin, fructose, trimethylglycine, sodium lactate, and sodium pyrrolidone carboxylate in an emulsified composition containing α-monoalkylglyceryl ether, waxes, and a predetermined silicone oil. It is stated that a more selected moisturizer may be incorporated. Patent Document 2 describes hyaluronic acid or hyaluronic acid in an emulsified composition containing 0.1 to 10% by mass of a water-soluble polymer obtained by mixing a predetermined agar and xanthan gum in a predetermined mass ratio and 30% by mass or more of water. It is described that one or more moisturizing agents selected from the salt, pyrrolidone carboxylic acid or a salt thereof, glycerin, diglycerin, and polyglycerin may be blended. In Patent Document 3, a composition for external use on the skin at a predetermined pH containing ascorbic acid glucoside, 2-amino-2-hydroxymethyl-1,3-propanediol, and ethylenediaminetetraacetic acid or a salt thereof is prepared as an emulsifying composition. It is described that pyrrolidonecarboxylic acid or a salt thereof may be blended.
特許文献1〜3に記載の乳化組成物にはピロリドンカルボン酸又はその塩が配合されてよいことが記載されているものの、実際に、ピロリドンカルボン酸又はその塩が配合された場合の乳化組成物の性状安定性については検討されていない。本発明者は、ピロリドンカルボン酸又はその塩を配合した乳化組成物を調製したところ、保存後において分離が生じ、性状が不安定となる課題に直面した。 Although it is described that the emulsified composition described in Patent Documents 1 to 3 may contain pyrrolidone carboxylic acid or a salt thereof, the emulsified composition when pyrrolidone carboxylic acid or a salt thereof is actually blended. The property stability of the product has not been investigated. The present inventor has faced a problem that when an emulsified composition containing pyrrolidone carboxylic acid or a salt thereof is prepared, separation occurs after storage and the properties become unstable.
そこで、本発明は、ピロリドンカルボン酸又はその塩を含む乳化組成物であって、優れた乳化安定性を備える乳化組成物を提供することを目的とする。 Therefore, an object of the present invention is to provide an emulsified composition containing pyrrolidone carboxylic acid or a salt thereof, which has excellent emulsification stability.
本発明者は、ピロリドンカルボン酸又はその塩を含む乳化組成物について鋭意検討を行ったところ、これまで乳化安定化効果が知られていなかったウフェナマートを配合することで、優れた乳化安定性が備わることを予期せずして見出した。本発明は、この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。 The present inventor has diligently studied an emulsified composition containing pyrrolidone carboxylic acid or a salt thereof, and found that by blending ufenamate, which has not been known to have an emulsifying stabilizing effect, excellent emulsifying stability is provided. I found that unexpectedly. The present invention has been completed by further studies based on this finding.
即ち、本発明は、下記に掲げる態様の発明を提供する。
項1. ピロリドンカルボン酸及び/又はその塩、並びにウフェナマートを含有する乳化組成物。
項2. 前記ピロリドンカルボン酸及び/又はその塩を総量で0.001〜10重量%含む、項1に記載の乳化組成物。
項3. 前記ピロリドンカルボン酸及び/又はその塩の総量1重量部当たり、前記ウフェナマートが1.5重量部以上で含まれる、項1又は2に記載の乳化組成物。
項4. ピロリドンカルボン酸及び/又はその塩を含む乳化組成物中に、前記ピロリドンカルボン酸及び/又はその塩と共に、ウフェナマートを配合する、乳化安定化方法。
That is, the present invention provides the inventions of the following aspects.
Item 1. An emulsified composition containing pyrrolidone carboxylic acid and / or a salt thereof, and ufenamate.
Item 2. Item 2. The emulsified composition according to Item 1, which contains 0.001 to 10% by weight of the pyrrolidone carboxylic acid and / or a salt thereof in total.
Item 3. Item 2. The emulsified composition according to Item 1 or 2, wherein the ufenamate is contained in an amount of 1.5 parts by weight or more per 1 part by weight of the total amount of the pyrrolidone carboxylic acid and / or a salt thereof.
Item 4. An emulsification stabilization method in which ufenamate is blended together with the pyrrolidone carboxylic acid and / or a salt thereof in an emulsification composition containing a pyrrolidone carboxylic acid and / or a salt thereof.
本発明によると、ピロリドンカルボン酸又はその塩を含む乳化組成物に、優れた乳化安定性を備えさせることができる。 According to the present invention, an emulsified composition containing pyrrolidone carboxylic acid or a salt thereof can be provided with excellent emulsification stability.
1.乳化組成物
本発明の乳化組成物は、ピロリドンカルボン酸及び/又はその塩、並びにウフェナマートを含有することを特徴とする。以下、本発明の乳化組成物について詳述する。
1. 1. Emulsifying Composition The emulsifying composition of the present invention is characterized by containing pyrrolidone carboxylic acid and / or a salt thereof, and ufenamate. Hereinafter, the emulsified composition of the present invention will be described in detail.
ピロリドンカルボン酸及び/又はその塩
本発明の乳化組成物に含まれるピロリドンカルボン酸及び/又はその塩は、保湿剤として公知の成分である。ピロリドンカルボン酸及び/又はその塩は、乳化組成物中で保存後における性状を不安定化させるが、本発明の乳化組成物は、優れた乳化安定性を奏する。
Pyrrolidone carboxylic acid and / or a salt thereof The pyrrolidone carboxylic acid and / or a salt thereof contained in the emulsifying composition of the present invention is a known component as a moisturizer. Pyrrolidone carboxylic acid and / or a salt thereof destabilizes the properties of the emulsified composition after storage, but the emulsified composition of the present invention exhibits excellent emulsification stability.
ピロリドンカルボン酸は、ピログルタミン酸又はピドル酸とも称される成分である。ピロリドンカルボン酸の立体構造については特に限定されず、D−ピロリドンカルボン酸、L−ピロリドンカルボン酸、及びDL−ピロリドンカルボン酸のいずれであってもよい。 Pyrrolidone carboxylic acid is a component also called pyroglutamic acid or pyrramic acid. The three-dimensional structure of the pyrrolidone carboxylic acid is not particularly limited, and may be any of D-pyrrolidone carboxylic acid, L-pyrrolidone carboxylic acid, and DL-pyrrolidone carboxylic acid.
ピロリドンカルボン酸の塩としては、薬学的又は香粧学的に許容されるものである限り特に制限されないが、ナトリウム塩、カリウム塩、リチウム塩等のアルカリ金属塩;カルシウム塩、マグネシウム塩等のアルカリ土類金属塩;アンモニウム塩、アルカノールアミン塩等が挙げられる。これらのピロリドンカルボン酸の塩は、1種を単独で用いてもよいし、複数種を組み合わせて用いてもよい。これらのピロリドンカルボン酸の中でも、好ましくはアルカリ金属塩が挙げられ、より好ましくはナトリウム塩が挙げられる。 The salt of pyrrolidone carboxylic acid is not particularly limited as long as it is pharmaceutically or cosmetically acceptable, but it is an alkali metal salt such as a sodium salt, a potassium salt or a lithium salt; an alkali such as a calcium salt or a magnesium salt. Earth metal salts; ammonium salts, alkanolamine salts and the like can be mentioned. As the salts of these pyrrolidone carboxylic acids, one type may be used alone, or a plurality of types may be used in combination. Among these pyrrolidone carboxylic acids, an alkali metal salt is preferable, and a sodium salt is more preferable.
本発明の乳化組成物は保存後における乳化安定性に優れるため、乳化粒子の凝集を引き起こしやすい電解質がより多く共存していても効果的に乳化安定性を得ることができる。このような観点から、本発明の乳化組成物は、ピロリドンカルボン酸及びピロリドンカルボン酸の塩の中でも、完全電離によってより多くの電解質を生じるピロリドンカルボン酸の塩を含んでいることがより一層好ましい。 Since the emulsified composition of the present invention is excellent in emulsification stability after storage, it is possible to effectively obtain emulsification stability even if more electrolytes that easily cause aggregation of emulsified particles coexist. From this point of view, it is even more preferable that the emulsified composition of the present invention contains a salt of pyrrolidone carboxylic acid and a salt of pyrrolidone carboxylic acid which produces more electrolyte by complete ionization among the salts of pyrrolidone carboxylic acid.
本発明の乳化組成物におけるピロリドンカルボン酸及び/又はその塩の含有量としては特に限定されず、付与すべき保湿性等に応じて適宜決定することができるが、ピロリドンカルボン酸及びその塩の総量で、例えば0.001〜10重量%が挙げられる。より一層好ましい乳化安定性を得る観点から、ピロリドンカルボン酸及び/又はその塩の含有量の好ましい例として、0.001〜5重量%が挙げられる。また、本発明の乳化組成物は保存後における乳化安定性に優れるため、ピロリドンカルボン酸及び/又はその塩が比較的多く含まれていても、効果的に乳化安定性を得ることができる。このような観点から、本発明の乳化組成物におけるピロリドンカルボン酸及び/又はその塩の含有量の好適な例として、0.1〜10重量%、好ましくは1〜10重量%、より好ましくは2〜10重量%が挙げられる。 The content of pyrrolidone carboxylic acid and / or a salt thereof in the emulsified composition of the present invention is not particularly limited and can be appropriately determined depending on the moisturizing property to be imparted and the like, but the total amount of pyrrolidone carboxylic acid and its salt thereof. For example, 0.001 to 10% by weight can be mentioned. From the viewpoint of obtaining even more preferable emulsion stability, a preferred example of the content of pyrrolidone carboxylic acid and / or a salt thereof is 0.001 to 5% by weight. Further, since the emulsified composition of the present invention is excellent in emulsification stability after storage, it is possible to effectively obtain emulsification stability even if a relatively large amount of pyrrolidone carboxylic acid and / or a salt thereof is contained. From this point of view, as a preferable example of the content of pyrrolidone carboxylic acid and / or a salt thereof in the emulsified composition of the present invention, 0.1 to 10% by weight, preferably 1 to 10% by weight, more preferably 2. 10% by weight is mentioned.
ウフェナマート
本発明の乳化組成物に含まれるウフェナマートは、フルフェナム酸ブチルとも称され、水難溶性の非ステロイド性抗炎症薬として公知の成分である。ピロリドンカルボン酸及び/又はその塩を含む乳化組成物は保存後における性状が不安定であるが、本発明の乳化組成物は、ウフェナマートを配合することで、優れた乳化安定性を奏する。
Ufenamate Ufenamate contained in the emulsified composition of the present invention, also referred to as butyl flufenamic acid, is a component known as a poorly water-soluble non-steroidal anti-inflammatory drug. The emulsified composition containing pyrrolidone carboxylic acid and / or a salt thereof has unstable properties after storage, but the emulsified composition of the present invention exhibits excellent emulsification stability by blending ufenamate.
本発明の乳化組成物におけるウフェナマートの含有量については特に限定されず、付与すべき乳化安定性に応じて適宜設定されるが、例えば1〜20重量%、好ましくは2〜10重量%、更に好ましくは3〜7重量%が挙げられる。 The content of ufenamate in the emulsified composition of the present invention is not particularly limited and is appropriately set according to the emulsification stability to be imparted, but is, for example, 1 to 20% by weight, preferably 2 to 10% by weight, more preferably. Is 3 to 7% by weight.
本発明の乳化組成物において、ピロリドンカルボン酸及び/又はその塩に対するウフェナマートの比率については、上記の各成分の各含有量に応じて定まるが、より一層優れた乳化安定性を得る観点から、例えば、ピロリドンカルボン酸及び/又はその塩の総量1重量部当たりのウフェナマートの含有量として、例えば1.5重量部以上、好ましくは1.8重量部以上、より好ましくは2重量部以上が挙げられる。ピロリドンカルボン酸及び/又はその塩の総量1重量部当たりのウフェナマートの含有量の範囲の上限としては特に限定されないが、例えば40重量部以下、好ましくは20重量部以下、より好ましくは10重量部以下、更に好ましくは5重量部以下が挙げられる。 In the emulsified composition of the present invention, the ratio of ufenamate to pyrrolidone carboxylic acid and / or a salt thereof is determined according to each content of each of the above components, but from the viewpoint of obtaining even better emulsification stability, for example. The content of ufenamate per 1 part by weight of the total amount of pyrrolidone carboxylic acid and / or a salt thereof includes, for example, 1.5 parts by weight or more, preferably 1.8 parts by weight or more, and more preferably 2 parts by weight or more. The upper limit of the range of the content of ufenamate per 1 part by weight of the total amount of pyrrolidone carboxylic acid and / or a salt thereof is not particularly limited, but for example, 40 parts by weight or less, preferably 20 parts by weight or less, more preferably 10 parts by weight or less. , More preferably 5 parts by weight or less.
油分
本発明の乳化組成物は、油相の基剤成分として油分を含む。油分としては薬学的又は香粧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、液状油、固形油、高級アルコール等が挙げられる。これらの油分は、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。
Oil content The emulsified composition of the present invention contains an oil content as a base component of the oil phase. The oil content is not particularly limited as long as it is pharmaceutically or cosmetically acceptable, and examples thereof include liquid oils, solid oils, and higher alcohols. These oils may be used alone or in combination of two or more.
本発明の乳化組成物における油分の含有量については、乳化組成物の乳化タイプ、形態、用途等に応じて適宜設定すればよいが、例えば、2〜60重量%、好ましくは4〜30重量%、より好ましくは4〜15重量%、さらに好ましくは6〜8重量%が挙げられる。 The oil content in the emulsified composition of the present invention may be appropriately set according to the emulsified type, form, use, etc. of the emulsified composition, and is, for example, 2 to 60% by weight, preferably 4 to 30% by weight. , More preferably 4 to 15% by weight, still more preferably 6 to 8% by weight.
本発明の乳化組成物においては、上記の油分の中でも、液状油を含有することが好ましい。液状油とは、25℃において液状の形態を保つ油である。液状油としては、化粧料や外用医薬品等に通常用いられるものであればよく、例えば、;オレイン酸、インステアリン酸等の脂肪酸;エチルヘキサン酸セチル、パルミチン酸エチルヘキシル、ミリスチン酸オクチルドデシル、ミリスチン酸イソプロピル、ジエチルヘキサン酸ネオペンチルグリコール、トリ2−エチルへキサン酸グリセリル、オレイン酸オクチルドデシル、ミリスチン酸イソプロピル、トリイソステアリン酸グリセリル、ジバラメトキシケイヒ酸?モノエチルへキサン酸グリセリル等のエステル油;ジメチルポリシロキサン、メチルハイドロジエンポリシロキサン、メチルフェニルポリシロキサン、オクタメチルシクロテトラシロキサン等のシリコーン油;流動パラフィン、スクワレン、スクワラン等の液状炭化水素油等が挙げられる。 The emulsified composition of the present invention preferably contains a liquid oil among the above oils. The liquid oil is an oil that maintains a liquid form at 25 ° C. The liquid oil may be any liquid oil usually used for cosmetics, external medicines, etc. For example; fatty acids such as oleic acid and instearic acid; cetyl ethylcaproic acid, ethylhexyl palmitate, octyldodecyl myristate, myristic acid. Isopropyl, neopentyl glycol diethylcaproate, glyceryl tri2-ethylhexanoate, octyldodecyl oleate, isopropyl myristate, glyceryl triisostearate, dibaramethoxysilicic acid? Ester oils such as glyceryl monoethylhexanoate; silicone oils such as dimethylpolysiloxane, methylhydrodienepolysiloxane, methylphenylpolysiloxane, octamethylcyclotetrasiloxane; liquid hydrocarbon oils such as liquid paraffin, squalane, squalane, etc. Be done.
これらの液状油は、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。 These liquid oils may be used alone or in combination of two or more.
これらの液状油の中でも、好ましくは、エステル油、シリコーン油、液状炭化水素油が挙げられ、より好ましくはミリスチン酸オクチルドデシル、ミリスチン酸イソプロピル、ジメチルポリシロキサン、流動パラフィンが挙げられる。また、これらの液状油の中でも、より一層好ましい乳化安定性を得る観点から、好ましくは液状炭化水素油が挙げられ、より好ましくは流動パラフィンが挙げられる。 Among these liquid oils, ester oils, silicone oils and liquid hydrocarbon oils are preferable, and octyldodecyl myristate, isopropyl myristate, dimethylpolysiloxane and liquid paraffin are more preferable. Further, among these liquid oils, liquid hydrocarbon oil is preferably mentioned, and liquid paraffin is more preferable, from the viewpoint of obtaining even more preferable emulsion stability.
本発明の乳化安定化剤に液状油を含有させる場合、その含有量については、特に制限されず、乳化組成物の乳化タイプ、形態、用途等に応じて適宜設定すればよいが、例えば、0.5〜30重量%、好ましくは1〜20重量%、より好ましくは3〜10重量%、さらに好ましくは5〜8重量%が挙げられる。 When the emulsification stabilizer of the present invention contains a liquid oil, the content thereof is not particularly limited and may be appropriately set according to the emulsification type, form, application, etc. of the emulsification composition. .5 to 30% by weight, preferably 1 to 20% by weight, more preferably 3 to 10% by weight, still more preferably 5 to 8% by weight.
水
本発明の乳化組成物は、水相の基剤成分として水を含む。本発明の乳化組成物における水の含有量について、乳化組成物の乳化タイプ、形態、用途等に応じて適宜設定すればよいが、例えば、30〜95重量%、好ましくは30〜90重量%、より好ましくは30〜80重量%、更に好ましくは30〜75重量%が挙げられる。
Emulsion composition of the water present invention comprises water as a base component of the aqueous phase. The water content in the emulsified composition of the present invention may be appropriately set according to the emulsified type, form, application, etc. of the emulsified composition, and is, for example, 30 to 95% by weight, preferably 30 to 90% by weight. More preferably, it is 30 to 80% by weight, and further preferably 30 to 75% by weight.
また、本発明の乳化組成物は保存後の水相分離を抑制する優れた乳化安定性を備えているため、本来的に水相分離がより一層生じやすい、水を多く含む場合であっても、優れた乳化安定性を得ることが可能になる。このような本発明の効果を鑑みれば、本発明の乳化組成物の好適な態様として、水の含有量が比較的多い乳化組成物が挙げられる。より具体的には、本発明の乳化組成物における水の含有量の好適な例として、例えば、40〜95重量%、好ましくは45〜95重量%、より好ましくは50〜95重量%、さらに好ましくは55〜95重量%、一層好ましくは60〜95重量%が挙げられる。 Further, since the emulsified composition of the present invention has excellent emulsification stability that suppresses aqueous phase separation after storage, even when a large amount of water is contained, which is inherently more likely to cause aqueous phase separation. , It becomes possible to obtain excellent emulsification stability. In view of such effects of the present invention, a preferred embodiment of the emulsified composition of the present invention is an emulsified composition having a relatively high water content. More specifically, as a preferable example of the water content in the emulsified composition of the present invention, for example, 40 to 95% by weight, preferably 45 to 95% by weight, more preferably 50 to 95% by weight, still more preferable. Is 55 to 95% by weight, more preferably 60 to 95% by weight.
界面活性剤
本発明の乳化組成物は、油相及び水相を乳化させる成分として界面活性剤を含む。界面活性剤としては、薬学的又は香粧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、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。
Surfactant The emulsifying composition of the present invention contains a surfactant as a component for emulsifying the oil phase and the aqueous phase. The surfactant is not particularly limited as long as it is pharmaceutically or cosmetically acceptable, and for example, a nonionic surfactant, an anionic surfactant, a cationic surfactant, and an amphoteric surfactant. And so on.
界面活性剤のHLB値としては、より一層優れた乳化安定性を得る観点から、例えば10〜19、好ましくは13〜17.5、より好ましくは13.5〜15.5が挙げられる。HLB値は、川上法(HLB値=7+11.7log(親水部の式量の総和/親油部の式量の総和))に従って算出される値である。 Examples of the HLB value of the surfactant include 10 to 19, preferably 13 to 17.5, and more preferably 13.5 to 15.5 from the viewpoint of obtaining even more excellent emulsion stability. The HLB value is a value calculated according to the Kawakami method (HLB value = 7 + 11.7 log (sum of formulas of hydrophilic part / sum of formulas of lipophilic part)).
これらの界面活性剤の中でも、より優れた乳化安定性を得る観点から、好ましくはノニオン性界面活性剤が挙げられる。 Among these surfactants, a nonionic surfactant is preferable from the viewpoint of obtaining more excellent emulsion stability.
ノニオン性界面活性剤としては、具体的には、ポリオキシエチレン硬化ヒマシ油類(例えば、PEG−40水添ヒマシ油、PEG−50水添ヒマシ油、PEG−60水添ヒマシ油、PEG−80水添ヒマシ油、PEG−100水添ヒマシ油、);ソルビタン脂肪酸エステル類(例えば、ソルビタンモノオレエート、ソルビタンモノイソステアレート、ソルビタンモノラウレート、ソルビタンモノパルミテート、ソルビタンモノステアレート、ソルビタンセスキオレエート、ソルビタントリオレエート、ペンタ−2−エチルヘキシル酸ジグリセロールソルビタン、テトラ−2−エチルヘキシル酸ジグリセロールソルビタン等);グリセリン脂肪酸エステル類(例えば、モノ綿実油脂肪酸グリセリル、モノエルカ酸グリセリル、セスキオレイン酸グリセリル、モノステアリン酸グリセリル(ステアリン酸グリセリン)、α,α’−オレイン酸ピログルタミン酸グリセリル、モノステアリン酸グリセリンリンゴ酸等);プロピレングリコール脂肪酸エステル類(例えば、モノステアリン酸プロピレングリコール等);グリセリンアルキルエーテル;ステアレス−2;ポリオキシエチレンソルビタン脂肪酸エステル類(例えば、ポリオキシエチレンソルビタンモノオレエート、ポリオキシエチレンソルビタンモノステアレート、ポリオキシエチレンソルビタンテトラオレエート等);ポリオキシエチレンソルビット脂肪酸エステル類(例えば、ポリオキシエチレンソルビットモノラウレート、ポリオキシエチレンソルビットモノオレエート、ポリオキシエチレンソルビットペンタオレエート、ポリオキシエチレンソルビットモノステアレート等);ポリオキシエチレングリセリン脂肪酸エステル類(例えば、ポリオキシエチレングリセリンモノステアレート、ポリオキシエチレングリセリンモノイソステアレート、ポリオキシエチレングリセリントリイソステアレート等);ポリオキシエチレン脂肪酸エステル類(例えば、ポリオキシエチレンモノオレエート、ポリオキシエチレンモノステアレート、ポリオキシエチレンジステアレート、ポリオキシエチレンモノジオレエート、ジステアリン酸エチレングリコール等);ポリオキシエチレンアルキルエーテル類(例えば、ポリオキシエチレンラウリルエーテル、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ベヘニルエーテル、ポリオキシエチレン2−オクチルドデシルエーテル、ポリオキシエチレンコレスタノールエーテル等);プルロニック型類(例えば、プルロニック等);ポリオキシエチレン・ポリオキシプロピレンアルキルエーテル類(例えば、ポリオキシエチレン・ポリオキシプロピレン−セチルエーテル、ポリオキシエチレン・ポリオキシプロピレン−2−デシルテトラデシルエーテル、ポリオキシエチレン・ポリオキシプロピレンモノブチルエーテル、ポリオキシエチレン・ポリオキシプロピレン水添ラノリン、ポリオキシエチレン・ポリオキシプロピレングリセリンエーテル等);ステアレス−21等が挙げられる。 Specific examples of the nonionic surfactant include polyoxyethylene hydrogenated castor oils (for example, PEG-40 hydrogenated castor oil, PEG-50 hydrogenated castor oil, PEG-60 hydrogenated castor oil, and PEG-80. Hydrogenated castor oil, PEG-100 hydrogenated castor oil,); sorbitan fatty acid esters (eg, sorbitan monooleate, sorbitan monoisostearate, sorbitan monolaurate, sorbitan monopalmitate, sorbitan monostearate, sorbitan sesqui Oleate, sorbitan trioleate, penta-2-ethylhexylate diglycerol sorbitan, tetra-2-ethylhexylate diglycerol sorbitan, etc.); glycerin fatty acid esters (eg, monocotton oil fatty acid glyceryl, monoerucate glyceryl, sesquioleate glyceryl, Glyceryl monostearate (glycerin stearate), α, α'-glyceryl pyroglutamate oleate, glycerin maloic acid, etc.); propylene glycol fatty acid esters (eg, propylene glycol monostearate, etc.); glycerin alkyl ether; Steareth-2; Polyoxyethylene sorbitan fatty acid esters (eg, polyoxyethylene sorbitan monooleate, polyoxyethylene sorbitan monostearate, polyoxyethylene sorbitan tetraoleate, etc.); Polyoxyethylene sorbitan fatty acid esters (eg, polyoxyethylene sorbitan tetraoleate, etc.) Polyoxyethylene sorbit monolaurate, polyoxyethylene sorbit monooleate, polyoxyethylene sorbit pentaoleate, polyoxyethylene sorbit monostearate, etc.); Polyoxyethylene glycerin fatty acid esters (eg, polyoxyethylene glycerin monosteare) Rate, polyoxyethylene glycerin monoisostearate, polyoxyethylene glycerin triisostearate, etc.); Polyoxyethylene fatty acid esters (eg, polyoxyethylene monooleate, polyoxyethylene monostearate, polyoxyethylene distea) Rate, polyoxyethylene monodiolate, ethylene glycol distearate, etc.); Polyoxyethylene alkyl ethers (eg, polyoxyethylene lauryl ether, polyoxyethylene oleyl ether, polyoxyethylene stearyl ether, polyoxyethylene behenyl ether) , Polyoxyethylene 2-octyldodecyl ether, polyoxyethylene cholestanol ether, etc.); Pluronic types (eg, Pluronic, etc.); Polyoxyethylene / polyoxypropylene alkyl ethers (eg, polyoxyethylene / polyoxypropylene-) Cetyl ether, polyoxyethylene / polyoxypropylene-2-decyltetradecyl ether, polyoxyethylene / polyoxypropylene monobutyl ether, polyoxyethylene / polyoxypropylene hydrogenated lanolin, polyoxyethylene / polyoxypropylene glycerin ether, etc.) ; Stairless-21 and the like can be mentioned.
これらの界面活性剤は、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。 These surfactants may be used alone or in combination of two or more.
これらのノニオン性界面活性剤の中でも、より優れた乳化安定性を得る観点から、好ましくはポリオキシエチレン硬化ヒマシ油類、ポリオキシエチレンソルビタン脂肪酸エステル類、ポリオキシエチレン脂肪酸エステル類が挙げられ、より好ましくは、PEG−60水添ヒマシ油、ポリオキシエチレンソルビタンモノステアレート、ポリオキシエチレンモノステアレートが挙げられる。また、これらのノニオン性界面活性剤の中でも、より一層優れた乳化安定性を得る観点から、ポリオキシエチレンソルビタン脂肪酸エステル類が挙げられ、より好ましくは、ポリオキシエチレンソルビタンモノステアレートが挙げられる。 Among these nonionic surfactants, polyoxyethylene hydrogenated castor oils, polyoxyethylene sorbitan fatty acid esters, and polyoxyethylene fatty acid esters are preferable from the viewpoint of obtaining more excellent emulsion stability. Preferred include PEG-60 hydrogenated castor oil, polyoxyethylene sorbitan monostearate, and polyoxyethylene monostearate. Further, among these nonionic surfactants, polyoxyethylene sorbitan fatty acid esters are mentioned, and more preferably, polyoxyethylene sorbitan monostearate is mentioned from the viewpoint of obtaining even more excellent emulsion stability.
本発明の乳化組成物において、界面活性剤の含有量については、使用する界面活性剤の種類等に応じて適宜設定すればよいが、例えば0.5〜7重量%、好ましくは1〜5重量%、より好ましくは2〜5重量%、更に好ましくは3〜5重量%が挙げられる。 In the emulsified composition of the present invention, the content of the surfactant may be appropriately set according to the type of the surfactant to be used and the like, and is, for example, 0.5 to 7% by weight, preferably 1 to 5% by weight. %, More preferably 2 to 5% by weight, still more preferably 3 to 5% by weight.
その他の成分
本発明の乳化組成物は、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、多価アルコール、増粘剤、pH調節剤、緩衝剤、可溶化剤、キレート剤、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。
Other Ingredients In addition to the above-mentioned ingredients, the emulsified composition of the present invention may contain other commonly used additives, if necessary. Such additives include, for example, polyhydric alcohols, thickeners, pH regulators, buffers, solubilizers, chelating agents, preservatives, preservatives, antioxidants, stabilizers, fragrances, colorants. And so on.
多価アルコールとしては、薬学的又は香粧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、プロピレングリコール、1,3−ブチレングリコール、エチレングリコール、イソプレングリコール、ジエチレングリコール、ジプロピレングリコール等の2価アルコール;グリセリン等の3価アルコール、マクロゴール4000、マクロゴール6000等のポリエチレングリコール等が挙げられる。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。これらの多価アルコールの中でも、より優れた乳化安定性を得る観点から、好ましくは2価アルコール、3価アルコールが挙げられ、より好ましくは1,3−ブチレングリコール、グリセリンが挙げられる。 The polyhydric alcohol is not particularly limited as long as it is pharmaceutically or cosmetically acceptable, and for example, propylene glycol, 1,3-butylene glycol, ethylene glycol, isoprene glycol, diethylene glycol, dipropylene glycol and the like. Divalent alcohols; trihydric alcohols such as glycerin, polyethylene glycols such as macrogol 4000 and macrogol 6000, and the like. These polyhydric alcohols may be used alone or in combination of two or more. Among these polyhydric alcohols, from the viewpoint of obtaining more excellent emulsion stability, dihydric alcohols and trihydric alcohols are preferable, and 1,3-butylene glycol and glycerin are more preferable.
本発明の乳化組成物において、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、使用する多価アルコールの種類等に応じて適宜設定すればよいが、例えば1〜20重量%、好ましくは5〜18重量%、より好ましくは10〜16重量%が挙げられる。 When the emulsified composition of the present invention contains a polyhydric alcohol, the content thereof may be appropriately set according to the type of the polyhydric alcohol used, for example, 1 to 20% by weight, preferably 5. ~ 18% by weight, more preferably 10 to 16% by weight.
増粘剤としては、薬学的又は香粧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、カルボキシビニルポリマー、ヒプロメロース、ポリビニルピロリドン、アルギン酸ナトリウム、エチルセルロース、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、カラギーナン等が挙げられる。これらの増粘剤の中でも、より優れた乳化安定性を得る観点から、好ましくはキサンタンガムが挙げられる。また、これらの増粘剤のうち、カルボキシビニルポリマーは、ピロリドンカルボン酸及び/又はその塩との共存下で極端な粘度低下を受けるため、ピロリドンカルボン酸及び/又はその塩を含む通常の乳化組成物に配合すると保存安定性の顕著な低下を招来するが、本発明の乳化組成物は保存後における乳化安定性に優れるため、カルボキシビニルポリマーが含まれていても効果的に乳化安定性を得ることができる。このような本発明の効果に鑑みれば、本発明の乳化組成物には増粘剤として少なくともカルボキシビニルポリマーを含んでいることが好ましい。 The thickener is not particularly limited as long as it is pharmaceutically or cosmetically acceptable, and for example, carboxyvinyl polymer, hypromellose, polyvinylpyrrolidone, sodium alginate, ethyl cellulose, sodium carboxymethyl cellulose, xanthan gum, carrageenan, etc. Can be mentioned. Among these thickeners, xanthan gum is preferably mentioned from the viewpoint of obtaining more excellent emulsion stability. Further, among these thickeners, the carboxyvinyl polymer undergoes an extreme decrease in viscosity in the coexistence with pyrrolidone carboxylic acid and / or a salt thereof, and therefore has a normal emulsification composition containing pyrrolidone carboxylic acid and / or a salt thereof. When blended in a product, the storage stability is significantly reduced. However, since the emulsified composition of the present invention has excellent emulsification stability after storage, the emulsification stability can be effectively obtained even if a carboxyvinyl polymer is contained. be able to. In view of such effects of the present invention, it is preferable that the emulsified composition of the present invention contains at least a carboxyvinyl polymer as a thickener.
本発明の乳化組成物において増粘剤を含有させる場合、その含有量については、使用する増粘剤の種類等に応じて適宜設定すればよいが、より優れた乳化安定性を得る観点から、例えば0.1〜2重量%、好ましくは0.1〜1.8重量%、より好ましくは0.2〜1.5重量%、更に好ましくは0.3〜1重量%、一層好ましくは0.3〜0.6重量%が挙げられる。また、本発明の乳化組成物にカルボキシビニルポリマーを含む場合、カルボキシビニルポリマーの含有量としては、例えば0.1〜1重量%、好ましくは0.3〜0.5重量%、より好ましくは0.35〜0.45重量%が挙げられる。また、ピロリドンカルボン酸及び/又はその塩に対するカルボキシビニルポリマーの比率については、上記の各成分の各含有量に応じて定まるが、例えば、ピロリドンカルボン酸及び/又はその塩の総量1重量部当たりのカルボキシビニルポリマーの含有量として、例えば0.01〜0.5重量部、好ましくは0.03〜0.3重量部、より好ましくは0.06〜0.2重量部が挙げられる。 When a thickener is contained in the emulsified composition of the present invention, the content thereof may be appropriately set according to the type of thickener used and the like, but from the viewpoint of obtaining better emulsification stability, the content thereof may be appropriately set. For example, 0.1 to 2% by weight, preferably 0.1 to 1.8% by weight, more preferably 0.2 to 1.5% by weight, still more preferably 0.3 to 1% by weight, still more preferably 0. 3 to 0.6% by weight is mentioned. When the emulsified composition of the present invention contains a carboxyvinyl polymer, the content of the carboxyvinyl polymer is, for example, 0.1 to 1% by weight, preferably 0.3 to 0.5% by weight, more preferably 0. .35 to 0.45% by weight. The ratio of the carboxyvinyl polymer to the pyrrolidone carboxylic acid and / or its salt is determined according to the content of each of the above components. For example, per 1 part by weight of the total amount of the pyrrolidone carboxylic acid and / or its salt. Examples of the content of the carboxyvinyl polymer include 0.01 to 0.5 parts by weight, preferably 0.03 to 0.3 parts by weight, and more preferably 0.06 to 0.2 parts by weight.
更に、本発明の乳化組成物は、前述する成分の他に、薬学的又は香粧学的な生理機能を発揮できる薬効成分が、必要に応じて含まれていてもよい。このような薬効成分としては、例えば、ステロイド剤(デキサメタゾン、塩酸デキサメタゾン、酢酸デキサメタゾン、塩酸ヒドロコルチゾン、吉草酸プレドニゾロン、酢酸プレドニゾロン等)、抗ヒスタミン剤(ジフェンヒドラミン、塩酸ジフェンヒドラミン、マレイン酸クロルフェニラミン等)、局所麻酔剤(リドカイン、ジブカイン、プロカイン、テトラカイン、ブピバカイン、メピバカイン、クロロプロカイン、プロパラカイン、メプリルカイン又はこれらの塩)、安息香酸アルキルエステル(例えばアミノ安息香酸エチル、塩酸パラブチルアミノ安息香酸ジエチルアミノエチル)、オルソカイン、オキセサゼイン、オキシポリエントキシデカン、ロートエキス、ペルカミンパーゼ、テシットデシチン等)、抗炎症剤(アラントイン、サリチル酸、サリチル酸グリコール、サリチル酸メチル、インドメタシン、フェルビナク、ジクロフェナクナトリウム、ロキソプロフェンナトリウム等)、殺菌剤(塩化ベンザルコニウム、塩化デカリニウム、塩化ベンゼトニウム、塩化セチルピリジニウム、塩酸クロルヘキシジン、グルコン酸クロルヘキシジン、アンモニア水、スルファジアジン、乳酸、フェノール等)、鎮痒剤(クロタミトン、チアントール等)、皮膚保護剤(コロジオン、ヒマシ油等)、血行促進成分(ノニル酸ワニリルアミド、ニコチン酸ベンジルエステル、カプサイシン、トウガラシエキス等)、ビタミン類(ビタミンA,B,C,D,E等)、ムコ多糖類(コンドロイチン硫酸ナトリウム、グルコサミン、ヒアルロン酸等)等が挙げられる。これらの薬効成分は、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、本発明の乳化組成物において、これらの薬効成分を含有させる場合、その含有量については、使用する薬効成分の種類、期待する効果等に応じて適宜設定すればよい。 Further, the emulsified composition of the present invention may contain, if necessary, a medicinal ingredient capable of exerting a pharmaceutical or cosmetic physiological function in addition to the above-mentioned ingredients. Examples of such medicinal ingredients include steroids (dexamethasone, dexamethasone hydrochloride, dexamethasone acetate, hydrocortisone hydrochloride, prednisolone salicate, prednisolone acetate, etc.), antihistamines (diphenhydramine, diphenhydramine hydrochloride, chlorhexidine maleate, etc.), and local anesthesia. Agents (lydocaine, dibucaine, procaine, tetracaine, bupivacaine, mepivacaine, chloroprocaine, proparacaine, meprilcaine or salts thereof), salicylic acid alkyl esters (eg ethyl aminobenzoate, diethylaminoethyl parabutylaminobenzoate), orthokine, Oxesazein, oxypolyentoxydecane, funnel extract, percaminepase, tesitdecitin, etc.), anti-inflammatory agents (alantine, salicylic acid, glycol salicylate, methyl salicylate, indomethacin, fervinac, diclofenac sodium, sodium loxoprofen, etc.), bactericides (benzalconium chloride, benzalconium chloride, etc.) Dexamethasone chloride, benzethonium chloride, cetylpyridinium chloride, chlorhexidine hydrochloride, chlorhexidine gluconate, aqueous ammonia, sulfaziazine, lactic acid, phenol, etc.), antipruritic agents (crotamiton, thiantolu, etc.), skin protectants (colodione, castor oil, etc.), blood circulation promotion Ingredients (nonyl acid vanillylamide, nicotinic acid benzyl ester, capsaicin, capsicum extract, etc.), vitamins (vitamins A, B, C, D, E, etc.), mucopolysaccharides (sodium chondroitin sulfate, glucosamine, hyaluronic acid, etc.), etc. Can be mentioned. These medicinal ingredients may be used alone or in combination of two or more. In addition, when these medicinal ingredients are contained in the emulsified composition of the present invention, the content thereof may be appropriately set according to the type of the medicinal ingredient to be used, the expected effect, and the like.
製剤形態・用途
本発明の乳化組成物の乳化タイプは、油中水型又は水中油型のいずれであってもよい。本発明の乳化組成物は、保存後の分離を抑制する優れた乳化安定性を奏するため、本来的に水相分離がより一層生じやすい、水中油型のような水を多く含むものであっても、優れた乳化安定性を備えさせることが可能になる。このような本発明の効果に鑑みれば、本発明の乳化組成物の好ましい乳化タイプは、水の含有量が比較的多い水中油型である。
Formulation Form / Use The emulsified type of the emulsified composition of the present invention may be either a water-in-oil type or an oil-in-water type. Since the emulsified composition of the present invention exhibits excellent emulsification stability that suppresses separation after storage, it originally contains a large amount of water such as an oil-in-water type, which is more likely to cause aqueous phase separation. However, it becomes possible to provide excellent emulsification stability. In view of such effects of the present invention, the preferred emulsified type of the emulsified composition of the present invention is the oil-in-water type having a relatively high water content.
本発明の乳化組成物は、化粧料、外用医薬部外品、外用医薬品等の外用剤として使用することができる。本発明の乳化組成物の製品形態については、特に制限されないが、例えば、クリーム剤、軟膏剤、乳液剤、ゲル剤、油剤、ローション剤、リニメント剤、エアゾール剤等が挙げられる。これらの中でも、好ましくは、クリーム剤、軟膏剤、乳液剤、ローション剤が挙げられ、より好ましくは、クリーム剤、乳液剤、ローション剤が挙げられる。 The emulsified composition of the present invention can be used as an external preparation for cosmetics, quasi-drugs for external use, pharmaceuticals for external use, and the like. The product form of the emulsified composition of the present invention is not particularly limited, and examples thereof include creams, ointments, emulsions, gels, oils, lotions, liniments, and aerosols. Among these, creams, ointments, emulsions and lotions are preferable, and creams, emulsions and lotions are more preferable.
製造方法
本発明の乳化組成物は、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 emulsified composition of the present invention can be produced according to a known formulation method of an emulsified preparation according to the emulsified type. For example, in the method for producing an emulsified composition of the present invention, the components to be contained are divided into a water-soluble component and an oil-based component, an aqueous phase containing the water-soluble component and an oil phase containing the oil-based component are prepared, and these are prepared. Examples thereof include a method of emulsifying according to a known method.
2.乳化安定化方法
上述するように、ウフェナマートは、ピロリドンカルボン酸及び/又はその塩を含む乳化組成物において優れた乳化安定性を発現させる。従って、本発明は、更に、ピロリドンカルボン酸及び/又はその塩を含む乳化組成物中に、ピロリドンカルボン酸及び/又はその塩と共に、ウフェナマートを配合する、乳化安定化方法を提供する。
2. Emulsification Stabilization Method As described above, ufenamate exhibits excellent emulsion stability in an emulsification composition containing a pyrrolidone carboxylic acid and / or a salt thereof. Therefore, the present invention further provides an emulsification stabilization method in which ufenamate is blended together with pyrrolidone carboxylic acid and / or a salt thereof in an emulsification composition containing pyrrolidone carboxylic acid and / or a salt thereof.
本発明の乳化安定化方法において、乳化安定化とは、保存後において乳化組成物の分離を抑制することをいう。分離とは、乳化組成物から、水相及び/又は油相が分離することをいう。乳化安定化のより好ましい態様としては、保存後において乳化組成物からの水相の分離を抑制することが挙げられ、より好ましい態様としては、保存後において乳化組成物の乳化状態が均一であること、つまりエマルジョン中の液滴が分散媒中に均一に分散した状態が保たれることが挙げられる。 In the emulsification stabilization method of the present invention, emulsification stabilization means suppressing the separation of the emulsified composition after storage. Separation means that the aqueous phase and / or the oil phase are separated from the emulsified composition. A more preferable embodiment of the emulsion stabilization is to suppress the separation of the aqueous phase from the emulsified composition after storage, and a more preferable embodiment is that the emulsified state of the emulsified composition is uniform after storage. That is, the droplets in the emulsion are kept uniformly dispersed in the dispersion medium.
本発明の乳化安定化方法において、使用する各成分の種類や含有量、乳化組成物に配合される成分の種類や含有量、及び製剤形態等については、前記「1.乳化組成物」の場合と同様である。 In the case of the above-mentioned "1. Emulsification composition", the type and content of each component used in the emulsion stabilization method of the present invention, the type and content of the component to be blended in the emulsification composition, the formulation form, etc. Is similar to.
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
表1及び2に示すに示す乳化組成物を調製した。具体的には、(B)成分を(I)の各成分の混合物に加え、70〜80℃で溶解させ、油相を調製した。一方、(II)の各成分の混合物を75〜85℃で溶解させ、更に(A)成分の50重量%水溶液を加え、水相を調製した。70〜80℃に加温した油相に、70〜80℃に加温した水相を加え、ホモミキサーを用いて撹拌して乳化し、35℃まで冷却した。これによって、乳化組成物(乳液剤;水中油型)を製造した。
Test Examples The emulsified compositions shown in Tables 1 and 2 were prepared. Specifically, the component (B) was added to the mixture of the components (I) and dissolved at 70 to 80 ° C. to prepare an oil phase. On the other hand, a mixture of each component of (II) was dissolved at 75 to 85 ° C., and a 50% by weight aqueous solution of component (A) was further added to prepare an aqueous phase. An aqueous phase heated to 70 to 80 ° C. was added to the oil phase heated to 70 to 80 ° C., and the mixture was stirred and emulsified using a homomixer and cooled to 35 ° C. As a result, an emulsified composition (milky lotion; oil-in-water type) was produced.
得られた各乳化組成物10gを、15mLの透明プラスチックチューブに充填し、密封して、遠心分離機により3,000rpmで10分遠心した。遠心後の各乳化組成物を目視にて観察し、以下の基準に基づいて乳化安定性を評価した。結果を表1及び2に示す。
−−:相分離が明確に認められ、水相の濁りの程度が少ない。
−:相分離が明確に認められ、水相の濁りの程度が大きい。
+:相分離が認められず、クリーミング傾向のみ認められる。
++:相分離が認められず、チューブの底先端部にのみ僅かなクリーミング傾向が認められる。
+++:相分離が認められず、乳化状態も均一である。
なお、クリーミング傾向とは、乳化状態の不均一状態をいい、具体的には、生成したエマルジョン中の液滴が、分散媒との比重差によって浮上又は沈降する過程にある状態をいう。
10 g of each of the obtained emulsified compositions was filled in a 15 mL transparent plastic tube, sealed, and centrifuged at 3,000 rpm for 10 minutes by a centrifuge. Each emulsified composition after centrifugation was visually observed, and the emulsified stability was evaluated based on the following criteria. The results are shown in Tables 1 and 2.
−−: Phase separation is clearly observed, and the degree of turbidity of the aqueous phase is small.
-: Phase separation is clearly observed, and the degree of turbidity of the aqueous phase is large.
+: No phase separation is observed, only creaming tendency is observed.
++: No phase separation is observed, and a slight creaming tendency is observed only at the bottom tip of the tube.
+++: No phase separation is observed and the emulsified state is uniform.
The creaming tendency refers to a non-uniform state in an emulsified state, and specifically, a state in which droplets in the produced emulsion are in the process of floating or settling due to the difference in specific gravity with the dispersion medium.
表2から明らかなように、ピロリドンカルボン酸ナトリウムを含まない乳化組成物では乳化状態は安定である(参考例)が、ピロリドンカルボン酸ナトリウムを含む乳化組成物では乳化状態が不安定になる(比較例1、2)ことが認められた。これに対し、表1から明らかなように、ピロリドンカルボン酸ナトリウムを含む乳化組成物に更にウフェナマートを配合することで、乳化状態が安定化した(実施例1〜7)。この乳化安定性の向上効果は、特に、実施例1、4〜7において顕著であった。 As is clear from Table 2, the emulsified state is stable in the emulsified composition containing no sodium pyrrolidone carboxylate (reference example), but the emulsified state becomes unstable in the emulsified composition containing sodium pyrrolidone carboxylate (comparison). Examples 1 and 2) were found. On the other hand, as is clear from Table 1, the emulsified state was stabilized by further adding ufenamate to the emulsified composition containing sodium pyrrolidone carboxylate (Examples 1 to 7). This effect of improving the emulsion stability was particularly remarkable in Examples 1, 4 to 7.
処方例
表3及び4に示す処方の乳化組成物(水中油型)を調製した。いずれの乳化組成物も、優れた乳化安定性を有していた。
Formulation Examples The emulsified compositions (oil-in-water type) of the formulations shown in Tables 3 and 4 were prepared. Both emulsified compositions had excellent emulsification stability.
Claims (4)
Priority Applications (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP2019221139A JP2021091609A (en) | 2019-12-06 | 2019-12-06 | Emulsion composition |
JP2024106482A JP2024114984A (en) | 2019-12-06 | 2024-07-01 | Emulsion composition |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP2019221139A JP2021091609A (en) | 2019-12-06 | 2019-12-06 | Emulsion composition |
Related Child Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2024106482A Division JP2024114984A (en) | 2019-12-06 | 2024-07-01 | Emulsion composition |
Publications (1)
Publication Number | Publication Date |
---|---|
JP2021091609A true JP2021091609A (en) | 2021-06-17 |
Family
ID=76311953
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2019221139A Pending JP2021091609A (en) | 2019-12-06 | 2019-12-06 | Emulsion composition |
JP2024106482A Pending JP2024114984A (en) | 2019-12-06 | 2024-07-01 | Emulsion composition |
Family Applications After (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2024106482A Pending JP2024114984A (en) | 2019-12-06 | 2024-07-01 | Emulsion composition |
Country Status (1)
Country | Link |
---|---|
JP (2) | JP2021091609A (en) |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2021091610A (en) * | 2019-12-06 | 2021-06-17 | 小林製薬株式会社 | Emulsion stabilizing method |
Citations (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2010270029A (en) * | 2009-05-20 | 2010-12-02 | Shiseido Co Ltd | Oil-in-water type emulsified skin care preparation for external use |
JP2019156772A (en) * | 2018-03-14 | 2019-09-19 | ロート製薬株式会社 | External composition |
-
2019
- 2019-12-06 JP JP2019221139A patent/JP2021091609A/en active Pending
-
2024
- 2024-07-01 JP JP2024106482A patent/JP2024114984A/en active Pending
Patent Citations (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2010270029A (en) * | 2009-05-20 | 2010-12-02 | Shiseido Co Ltd | Oil-in-water type emulsified skin care preparation for external use |
JP2019156772A (en) * | 2018-03-14 | 2019-09-19 | ロート製薬株式会社 | External composition |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2021091610A (en) * | 2019-12-06 | 2021-06-17 | 小林製薬株式会社 | Emulsion stabilizing method |
Also Published As
Publication number | Publication date |
---|---|
JP2024114984A (en) | 2024-08-23 |
Similar Documents
Publication | Publication Date | Title |
---|---|---|
JP5432470B2 (en) | Ceramide solution and external preparation for skin | |
JP6903410B2 (en) | Oil-in-water emulsified composition | |
JP2024114984A (en) | Emulsion composition | |
JP6753312B2 (en) | Topical skin preparation for medical use | |
JP6967369B2 (en) | Emulsifying composition | |
JP6817733B2 (en) | Preparation for internal bleeding treatment | |
JP7464358B2 (en) | Emulsion composition | |
JP7570174B2 (en) | Emulsion stabilization method | |
JP7092494B2 (en) | Water-in-oil emulsification composition | |
JP7312527B2 (en) | emulsion composition | |
JP7465066B2 (en) | Emulsion stabilizer | |
JP7565143B2 (en) | External pharmaceutical composition | |
JP7584886B2 (en) | Emulsion composition | |
JP2007063136A (en) | External preparation comprising urea formulated therein | |
JP7398274B2 (en) | External composition | |
JP7270374B2 (en) | external composition | |
JP7499024B2 (en) | External Composition | |
JP2020100583A (en) | Emulsified composition | |
JP7499023B2 (en) | External Composition | |
JP6906899B2 (en) | Emulsified composition | |
JP7535851B2 (en) | Oily topical composition | |
WO2022131081A1 (en) | Emulsified composition for external application | |
JP2003212751A (en) | Gel composition and oil-in-water (o/w) composition | |
JP2023090338A (en) | emulsion composition | |
JP2024029227A (en) | External composition |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
A621 | Written request for application examination |
Free format text: JAPANESE INTERMEDIATE CODE: A621 Effective date: 20221128 |
|
A977 | Report on retrieval |
Free format text: JAPANESE INTERMEDIATE CODE: A971007 Effective date: 20230921 |
|
A131 | Notification of reasons for refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A131 Effective date: 20230926 |
|
A601 | Written request for extension of time |
Free format text: JAPANESE INTERMEDIATE CODE: A601 Effective date: 20231124 |
|
A02 | Decision of refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A02 Effective date: 20240402 |