CN1161100C - 具有改进的皮肤感受的局部用组合物 - Google Patents
具有改进的皮肤感受的局部用组合物 Download PDFInfo
- Publication number
- CN1161100C CN1161100C CNB961968753A CN96196875A CN1161100C CN 1161100 C CN1161100 C CN 1161100C CN B961968753 A CNB961968753 A CN B961968753A CN 96196875 A CN96196875 A CN 96196875A CN 1161100 C CN1161100 C CN 1161100C
- Authority
- CN
- China
- Prior art keywords
- compositions
- skin
- acid
- alkyl
- carbon atoms
- 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.)
- Expired - Lifetime
Links
- 239000000203 mixture Substances 0.000 title claims abstract description 170
- 230000000699 topical effect Effects 0.000 title claims abstract description 8
- 125000000217 alkyl group Chemical group 0.000 claims abstract description 46
- 125000004432 carbon atom Chemical group C* 0.000 claims abstract description 41
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 30
- 239000002280 amphoteric surfactant Substances 0.000 claims abstract description 28
- 239000003945 anionic surfactant Substances 0.000 claims abstract description 24
- 239000003093 cationic surfactant Substances 0.000 claims abstract description 18
- 229920006395 saturated elastomer Polymers 0.000 claims abstract description 14
- 150000003839 salts Chemical class 0.000 claims abstract description 12
- -1 phosphate radical Chemical class 0.000 claims description 93
- KWIUHFFTVRNATP-UHFFFAOYSA-N glycine betaine Chemical compound C[N+](C)(C)CC([O-])=O KWIUHFFTVRNATP-UHFFFAOYSA-N 0.000 claims description 48
- 229960003237 betaine Drugs 0.000 claims description 30
- 238000000034 method Methods 0.000 claims description 29
- YGSDEFSMJLZEOE-UHFFFAOYSA-N salicylic acid Chemical compound OC(=O)C1=CC=CC=C1O YGSDEFSMJLZEOE-UHFFFAOYSA-N 0.000 claims description 27
- PEDCQBHIVMGVHV-UHFFFAOYSA-N glycerol group Chemical group OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims description 25
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 claims description 17
- 235000019333 sodium laurylsulphate Nutrition 0.000 claims description 17
- 125000000118 dimethyl group Chemical group [H]C([H])([H])* 0.000 claims description 16
- FJKROLUGYXJWQN-UHFFFAOYSA-N papa-hydroxy-benzoic acid Natural products OC(=O)C1=CC=C(O)C=C1 FJKROLUGYXJWQN-UHFFFAOYSA-N 0.000 claims description 15
- 125000000913 palmityl 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])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 14
- GHMLBKRAJCXXBS-UHFFFAOYSA-N resorcinol Chemical compound OC1=CC=CC(O)=C1 GHMLBKRAJCXXBS-UHFFFAOYSA-N 0.000 claims description 13
- 229960004889 salicylic acid Drugs 0.000 claims description 13
- FPIPGXGPPPQFEQ-OVSJKPMPSA-N all-trans-retinol Chemical group OC\C=C(/C)\C=C\C=C(/C)\C=C\C1=C(C)CCCC1(C)C FPIPGXGPPPQFEQ-OVSJKPMPSA-N 0.000 claims description 11
- 239000002253 acid Substances 0.000 claims description 10
- RXKJFZQQPQGTFL-UHFFFAOYSA-N dihydroxyacetone Chemical compound OCC(=O)CO RXKJFZQQPQGTFL-UHFFFAOYSA-N 0.000 claims description 10
- 150000002148 esters Chemical class 0.000 claims description 10
- 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 claims description 10
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 claims description 10
- BDJRBEYXGGNYIS-UHFFFAOYSA-N nonanedioic acid Chemical compound OC(=O)CCCCCCCC(O)=O BDJRBEYXGGNYIS-UHFFFAOYSA-N 0.000 claims description 10
- 239000004342 Benzoyl peroxide Substances 0.000 claims description 9
- OMPJBNCRMGITSC-UHFFFAOYSA-N Benzoylperoxide Chemical compound C=1C=CC=CC=1C(=O)OOC(=O)C1=CC=CC=C1 OMPJBNCRMGITSC-UHFFFAOYSA-N 0.000 claims description 9
- 239000007864 aqueous solution Substances 0.000 claims description 9
- 235000019400 benzoyl peroxide Nutrition 0.000 claims description 9
- 238000004140 cleaning Methods 0.000 claims description 9
- REZZEXDLIUJMMS-UHFFFAOYSA-M dimethyldioctadecylammonium chloride Chemical compound [Cl-].CCCCCCCCCCCCCCCCCC[N+](C)(C)CCCCCCCCCCCCCCCCCC REZZEXDLIUJMMS-UHFFFAOYSA-M 0.000 claims description 9
- 229960001727 tretinoin Drugs 0.000 claims description 9
- 229910019142 PO4 Inorganic materials 0.000 claims description 8
- 239000006185 dispersion Substances 0.000 claims description 7
- FPIPGXGPPPQFEQ-UHFFFAOYSA-N 13-cis retinol Natural products OCC=C(C)C=CC=C(C)C=CC1=C(C)CCCC1(C)C FPIPGXGPPPQFEQ-UHFFFAOYSA-N 0.000 claims description 6
- HVYJSOSGTDINLW-UHFFFAOYSA-N 2-[dimethyl(octadecyl)azaniumyl]acetate Chemical compound CCCCCCCCCCCCCCCCCC[N+](C)(C)CC([O-])=O HVYJSOSGTDINLW-UHFFFAOYSA-N 0.000 claims description 6
- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 claims description 6
- AGBQKNBQESQNJD-UHFFFAOYSA-N alpha-Lipoic acid Natural products OC(=O)CCCCC1CCSS1 AGBQKNBQESQNJD-UHFFFAOYSA-N 0.000 claims description 6
- SUMDYPCJJOFFON-UHFFFAOYSA-N beta-hydroxyethanesulfonic acid Natural products OCCS(O)(=O)=O SUMDYPCJJOFFON-UHFFFAOYSA-N 0.000 claims description 6
- 235000019136 lipoic acid Nutrition 0.000 claims description 6
- 229960002663 thioctic acid Drugs 0.000 claims description 6
- OAAZUWWNSYWWHG-UHFFFAOYSA-N 1-phenoxypropan-1-ol Chemical compound CCC(O)OC1=CC=CC=C1 OAAZUWWNSYWWHG-UHFFFAOYSA-N 0.000 claims description 5
- HEFNNWSXXWATRW-UHFFFAOYSA-N Ibuprofen Chemical compound CC(C)CC1=CC=C(C(C)C(O)=O)C=C1 HEFNNWSXXWATRW-UHFFFAOYSA-N 0.000 claims description 5
- IMQLKJBTEOYOSI-GPIVLXJGSA-N Inositol-hexakisphosphate Chemical group OP(O)(=O)O[C@H]1[C@H](OP(O)(O)=O)[C@@H](OP(O)(O)=O)[C@H](OP(O)(O)=O)[C@H](OP(O)(O)=O)[C@@H]1OP(O)(O)=O IMQLKJBTEOYOSI-GPIVLXJGSA-N 0.000 claims description 5
- CMWTZPSULFXXJA-UHFFFAOYSA-N Naproxen Natural products C1=C(C(C)C(O)=O)C=CC2=CC(OC)=CC=C21 CMWTZPSULFXXJA-UHFFFAOYSA-N 0.000 claims description 5
- IMQLKJBTEOYOSI-UHFFFAOYSA-N Phytic acid Chemical group OP(O)(=O)OC1C(OP(O)(O)=O)C(OP(O)(O)=O)C(OP(O)(O)=O)C(OP(O)(O)=O)C1OP(O)(O)=O IMQLKJBTEOYOSI-UHFFFAOYSA-N 0.000 claims description 5
- 229910052799 carbon Inorganic materials 0.000 claims description 5
- 150000001768 cations Chemical class 0.000 claims description 5
- 229940120503 dihydroxyacetone Drugs 0.000 claims description 5
- IQDGSYLLQPDQDV-UHFFFAOYSA-N dimethylazanium;chloride Chemical compound Cl.CNC IQDGSYLLQPDQDV-UHFFFAOYSA-N 0.000 claims description 5
- UVCJGUGAGLDPAA-UHFFFAOYSA-N ensulizole Chemical compound N1C2=CC(S(=O)(=O)O)=CC=C2N=C1C1=CC=CC=C1 UVCJGUGAGLDPAA-UHFFFAOYSA-N 0.000 claims description 5
- 229960000890 hydrocortisone Drugs 0.000 claims description 5
- 229960001680 ibuprofen Drugs 0.000 claims description 5
- 239000004310 lactic acid Substances 0.000 claims description 5
- 235000014655 lactic acid Nutrition 0.000 claims description 5
- 229960002009 naproxen Drugs 0.000 claims description 5
- CMWTZPSULFXXJA-VIFPVBQESA-N naproxen Chemical compound C1=C([C@H](C)C(O)=O)C=CC2=CC(OC)=CC=C21 CMWTZPSULFXXJA-VIFPVBQESA-N 0.000 claims description 5
- 239000000467 phytic acid Chemical group 0.000 claims description 5
- 229940068041 phytic acid Drugs 0.000 claims description 5
- 235000002949 phytic acid Nutrition 0.000 claims description 5
- 229960003471 retinol Drugs 0.000 claims description 5
- 235000020944 retinol Nutrition 0.000 claims description 5
- 239000011607 retinol Substances 0.000 claims description 5
- 239000010452 phosphate Substances 0.000 claims description 4
- 239000003755 preservative agent Substances 0.000 claims description 4
- 108700004121 sarkosyl Proteins 0.000 claims description 4
- KSAVQLQVUXSOCR-UHFFFAOYSA-M sodium lauroyl sarcosinate Chemical compound [Na+].CCCCCCCCCCCC(=O)N(C)CC([O-])=O KSAVQLQVUXSOCR-UHFFFAOYSA-M 0.000 claims description 4
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 3
- JVTAAEKCZFNVCJ-UHFFFAOYSA-M Lactate Chemical compound CC(O)C([O-])=O JVTAAEKCZFNVCJ-UHFFFAOYSA-M 0.000 claims description 3
- 125000003047 N-acetyl group Chemical group 0.000 claims description 3
- DXGLGDHPHMLXJC-UHFFFAOYSA-N oxybenzone Chemical compound OC1=CC(OC)=CC=C1C(=O)C1=CC=CC=C1 DXGLGDHPHMLXJC-UHFFFAOYSA-N 0.000 claims description 3
- 229960001173 oxybenzone Drugs 0.000 claims description 3
- AFDXODALSZRGIH-QPJJXVBHSA-N (E)-3-(4-methoxyphenyl)prop-2-enoic acid Chemical compound COC1=CC=C(\C=C\C(O)=O)C=C1 AFDXODALSZRGIH-QPJJXVBHSA-N 0.000 claims description 2
- GWEHVDNNLFDJLR-UHFFFAOYSA-N 1,3-diphenylurea Chemical compound C=1C=CC=CC=1NC(=O)NC1=CC=CC=C1 GWEHVDNNLFDJLR-UHFFFAOYSA-N 0.000 claims description 2
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 claims description 2
- KRKNYBCHXYNGOX-UHFFFAOYSA-K Citrate Chemical compound [O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-K 0.000 claims description 2
- NHNBFGGVMKEFGY-UHFFFAOYSA-N Nitrate Chemical compound [O-][N+]([O-])=O NHNBFGGVMKEFGY-UHFFFAOYSA-N 0.000 claims description 2
- JZMJDSHXVKJFKW-UHFFFAOYSA-M methyl sulfate(1-) Chemical compound COS([O-])(=O)=O JZMJDSHXVKJFKW-UHFFFAOYSA-M 0.000 claims description 2
- AFDXODALSZRGIH-UHFFFAOYSA-N p-coumaric acid methyl ether Natural products COC1=CC=C(C=CC(O)=O)C=C1 AFDXODALSZRGIH-UHFFFAOYSA-N 0.000 claims description 2
- GGHPAKFFUZUEKL-UHFFFAOYSA-M sodium;hexadecyl sulfate Chemical compound [Na+].CCCCCCCCCCCCCCCCOS([O-])(=O)=O GGHPAKFFUZUEKL-UHFFFAOYSA-M 0.000 claims description 2
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims 3
- 230000002500 effect on skin Effects 0.000 claims 3
- USIUVYZYUHIAEV-UHFFFAOYSA-N diphenyl ether Chemical compound C=1C=CC=CC=1OC1=CC=CC=C1 USIUVYZYUHIAEV-UHFFFAOYSA-N 0.000 claims 2
- AGBQKNBQESQNJD-SSDOTTSWSA-N (R)-lipoic acid Chemical compound OC(=O)CCCC[C@@H]1CCSS1 AGBQKNBQESQNJD-SSDOTTSWSA-N 0.000 claims 1
- MKDRQQLTZMMMHY-UHFFFAOYSA-N 2-hydroxyethylsulfonyl dodecanoate Chemical compound CCCCCCCCCCCC(=O)OS(=O)(=O)CCO MKDRQQLTZMMMHY-UHFFFAOYSA-N 0.000 claims 1
- CPELXLSAUQHCOX-UHFFFAOYSA-M Bromide Chemical compound [Br-] CPELXLSAUQHCOX-UHFFFAOYSA-M 0.000 claims 1
- 239000004201 L-cysteine Substances 0.000 claims 1
- 235000009470 Theobroma cacao Nutrition 0.000 claims 1
- 229940022663 acetate Drugs 0.000 claims 1
- 150000001450 anions Chemical group 0.000 claims 1
- LLEMOWNGBBNAJR-UHFFFAOYSA-N biphenyl-2-ol Chemical compound OC1=CC=CC=C1C1=CC=CC=C1 LLEMOWNGBBNAJR-UHFFFAOYSA-N 0.000 claims 1
- 229940006460 bromide ion Drugs 0.000 claims 1
- 244000240602 cacao Species 0.000 claims 1
- KIWBPDUYBMNFTB-UHFFFAOYSA-M ethyl sulfate Chemical compound CCOS([O-])(=O)=O KIWBPDUYBMNFTB-UHFFFAOYSA-M 0.000 claims 1
- XMBWDFGMSWQBCA-UHFFFAOYSA-M iodide Chemical compound [I-] XMBWDFGMSWQBCA-UHFFFAOYSA-M 0.000 claims 1
- 229940006461 iodide ion Drugs 0.000 claims 1
- 229940045996 isethionic acid Drugs 0.000 claims 1
- 125000001421 myristyl 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])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 claims 1
- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 claims 1
- 239000000080 wetting agent Substances 0.000 claims 1
- 150000001875 compounds Chemical class 0.000 abstract description 8
- 206010013786 Dry skin Diseases 0.000 abstract description 6
- 230000003750 conditioning effect Effects 0.000 abstract description 6
- 230000037336 dry skin Effects 0.000 abstract description 6
- 125000004417 unsaturated alkyl group Chemical group 0.000 abstract 1
- 210000003491 skin Anatomy 0.000 description 89
- 239000012071 phase Substances 0.000 description 62
- 239000002245 particle Substances 0.000 description 47
- 239000004615 ingredient Substances 0.000 description 45
- 238000003756 stirring Methods 0.000 description 36
- 239000000194 fatty acid Substances 0.000 description 22
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 21
- 235000014113 dietary fatty acids Nutrition 0.000 description 21
- 229930195729 fatty acid Natural products 0.000 description 21
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 description 20
- 239000000463 material Substances 0.000 description 20
- 150000004665 fatty acids Chemical class 0.000 description 19
- 239000003995 emulsifying agent Substances 0.000 description 18
- 239000000126 substance Substances 0.000 description 18
- BXWNKGSJHAJOGX-UHFFFAOYSA-N hexadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCO BXWNKGSJHAJOGX-UHFFFAOYSA-N 0.000 description 16
- 239000004698 Polyethylene Substances 0.000 description 14
- GLDOVTGHNKAZLK-UHFFFAOYSA-N octadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCCCO GLDOVTGHNKAZLK-UHFFFAOYSA-N 0.000 description 14
- 229920000573 polyethylene Polymers 0.000 description 14
- 230000000475 sunscreen effect Effects 0.000 description 14
- 239000000516 sunscreening agent Substances 0.000 description 14
- 150000001732 carboxylic acid derivatives Chemical class 0.000 description 13
- 239000004094 surface-active agent Substances 0.000 description 13
- 239000000306 component Substances 0.000 description 12
- 235000011187 glycerol Nutrition 0.000 description 12
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 description 11
- 229930006000 Sucrose Natural products 0.000 description 11
- 239000012530 fluid Substances 0.000 description 11
- 239000003921 oil Substances 0.000 description 11
- 235000019198 oils Nutrition 0.000 description 11
- 239000005720 sucrose Substances 0.000 description 11
- ULGZDMOVFRHVEP-RWJQBGPGSA-N Erythromycin Chemical compound O([C@@H]1[C@@H](C)C(=O)O[C@@H]([C@@]([C@H](O)[C@@H](C)C(=O)[C@H](C)C[C@@](C)(O)[C@H](O[C@H]2[C@@H]([C@H](C[C@@H](C)O2)N(C)C)O)[C@H]1C)(C)O)CC)[C@H]1C[C@@](C)(OC)[C@@H](O)[C@H](C)O1 ULGZDMOVFRHVEP-RWJQBGPGSA-N 0.000 description 10
- 239000003795 chemical substances by application Substances 0.000 description 10
- 230000008569 process Effects 0.000 description 10
- 235000000346 sugar Nutrition 0.000 description 10
- 239000003760 tallow Substances 0.000 description 10
- NOOLISFMXDJSKH-UTLUCORTSA-N (+)-Neomenthol Chemical compound CC(C)[C@@H]1CC[C@@H](C)C[C@@H]1O NOOLISFMXDJSKH-UTLUCORTSA-N 0.000 description 9
- NLXLAEXVIDQMFP-UHFFFAOYSA-N Ammonia chloride Chemical compound [NH4+].[Cl-] NLXLAEXVIDQMFP-UHFFFAOYSA-N 0.000 description 9
- NOOLISFMXDJSKH-UHFFFAOYSA-N DL-menthol Natural products CC(C)C1CCC(C)CC1O NOOLISFMXDJSKH-UHFFFAOYSA-N 0.000 description 9
- AEMRFAOFKBGASW-UHFFFAOYSA-N Glycolic acid Chemical compound OCC(O)=O AEMRFAOFKBGASW-UHFFFAOYSA-N 0.000 description 9
- 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 9
- 125000000129 anionic group Chemical group 0.000 description 9
- 238000009835 boiling Methods 0.000 description 9
- 235000013312 flour Nutrition 0.000 description 9
- 229940041616 menthol Drugs 0.000 description 9
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 9
- 239000002736 nonionic surfactant Substances 0.000 description 9
- 239000011734 sodium Substances 0.000 description 9
- 229910052708 sodium Inorganic materials 0.000 description 9
- 229940083542 sodium Drugs 0.000 description 9
- ICIDSZQHPUZUHC-UHFFFAOYSA-N 2-octadecoxyethanol Chemical compound CCCCCCCCCCCCCCCCCCOCCO ICIDSZQHPUZUHC-UHFFFAOYSA-N 0.000 description 8
- 125000003342 alkenyl group Chemical group 0.000 description 8
- 125000002947 alkylene group Chemical group 0.000 description 8
- 229960000541 cetyl alcohol Drugs 0.000 description 8
- NOPFSRXAKWQILS-UHFFFAOYSA-N docosan-1-ol Chemical compound CCCCCCCCCCCCCCCCCCCCCCO NOPFSRXAKWQILS-UHFFFAOYSA-N 0.000 description 8
- 229920000435 poly(dimethylsiloxane) Polymers 0.000 description 8
- 229920000642 polymer Polymers 0.000 description 8
- 229920001451 polypropylene glycol Polymers 0.000 description 8
- 239000000047 product Substances 0.000 description 8
- 235000013599 spices Nutrition 0.000 description 8
- ILCOCZBHMDEIAI-UHFFFAOYSA-N 2-(2-octadecoxyethoxy)ethanol Chemical compound CCCCCCCCCCCCCCCCCCOCCOCCO ILCOCZBHMDEIAI-UHFFFAOYSA-N 0.000 description 7
- 244000060011 Cocos nucifera Species 0.000 description 7
- 235000013162 Cocos nucifera Nutrition 0.000 description 7
- 150000001298 alcohols Chemical class 0.000 description 7
- SHGAZHPCJJPHSC-YCNIQYBTSA-N all-trans-retinoic acid Chemical compound OC(=O)\C=C(/C)\C=C\C=C(/C)\C=C\C1=C(C)CCCC1(C)C SHGAZHPCJJPHSC-YCNIQYBTSA-N 0.000 description 7
- 235000013870 dimethyl polysiloxane Nutrition 0.000 description 7
- 239000004664 distearyldimethylammonium chloride (DHTDMAC) Substances 0.000 description 7
- 229930195733 hydrocarbon Natural products 0.000 description 7
- 150000002430 hydrocarbons Chemical class 0.000 description 7
- 238000002156 mixing Methods 0.000 description 7
- GOQYKNQRPGWPLP-UHFFFAOYSA-N n-heptadecyl alcohol Natural products CCCCCCCCCCCCCCCCCO GOQYKNQRPGWPLP-UHFFFAOYSA-N 0.000 description 7
- 235000021317 phosphate Nutrition 0.000 description 7
- 229930002330 retinoic acid Natural products 0.000 description 7
- 229940098760 steareth-2 Drugs 0.000 description 7
- 229940100458 steareth-21 Drugs 0.000 description 7
- ZQCIPRGNRQXXSK-UHFFFAOYSA-N 1-octadecoxypropan-2-ol Chemical compound CCCCCCCCCCCCCCCCCCOCC(C)O ZQCIPRGNRQXXSK-UHFFFAOYSA-N 0.000 description 6
- 239000003109 Disodium ethylene diamine tetraacetate Substances 0.000 description 6
- ZGTMUACCHSMWAC-UHFFFAOYSA-L EDTA disodium salt (anhydrous) Chemical compound [Na+].[Na+].OC(=O)CN(CC([O-])=O)CCN(CC(O)=O)CC([O-])=O ZGTMUACCHSMWAC-UHFFFAOYSA-L 0.000 description 6
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 6
- 239000004743 Polypropylene Substances 0.000 description 6
- 239000004480 active ingredient Substances 0.000 description 6
- MRUAUOIMASANKQ-UHFFFAOYSA-N cocamidopropyl betaine Chemical compound CCCCCCCCCCCC(=O)NCCC[N+](C)(C)CC([O-])=O MRUAUOIMASANKQ-UHFFFAOYSA-N 0.000 description 6
- 235000019301 disodium ethylene diamine tetraacetate Nutrition 0.000 description 6
- 125000003438 dodecyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 description 6
- LXCFILQKKLGQFO-UHFFFAOYSA-N methylparaben Chemical compound COC(=O)C1=CC=C(O)C=C1 LXCFILQKKLGQFO-UHFFFAOYSA-N 0.000 description 6
- 235000019271 petrolatum Nutrition 0.000 description 6
- 229920001155 polypropylene Polymers 0.000 description 6
- 229940078491 ppg-15 stearyl ether Drugs 0.000 description 6
- IBLKWZIFZMJLFL-UHFFFAOYSA-N 1-phenoxypropan-2-ol Chemical compound CC(O)COC1=CC=CC=C1 IBLKWZIFZMJLFL-UHFFFAOYSA-N 0.000 description 5
- QCDWFXQBSFUVSP-UHFFFAOYSA-N 2-phenoxyethanol Chemical compound OCCOC1=CC=CC=C1 QCDWFXQBSFUVSP-UHFFFAOYSA-N 0.000 description 5
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 5
- PWKSKIMOESPYIA-BYPYZUCNSA-N L-N-acetyl-Cysteine Chemical compound CC(=O)N[C@@H](CS)C(O)=O PWKSKIMOESPYIA-BYPYZUCNSA-N 0.000 description 5
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 5
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Abstract
本发明组合物用于局部施用于皮肤,这些组合物产生改进的皮肤感受。这些组合物可以留存型产品形式或在使用后从皮肤上漂洗去或擦去。这些组合物也用于调理和清洁皮肤,使皮肤脱屑及缓解干燥皮肤。一种个人护理用组合物,包含:(a)约0.1%至约20%重的下式两性表面活性剂:其中R1为未取代的、饱和或未饱和的、直链或支化的约C9至约C22的烷基;m为1至约3的整数;n为0或1;R2和R3分别选自C1至约C3烷基和C1至约C3的单羟基烷基;R4选自饱和或未饱和的C1至约C5的烷基和饱和或未饱和的C1至约C5的单羟基烷基;X选自CO2、SO3和SO4;及上述化合物的药物上可接受的盐;(b)约0.1%至约20%重的阴离子表面活性剂,(c)约0.1%至约15%重的阳离子表面活性剂,和(d)约0.1%至约99.7%重的水。
Description
技术领域
本发明组合物用于人体皮肤的局部施用。这些组合物提供改进的皮肤感受。这些组合物可以是留存(leave-on)型产品或是使用后从皮肤上清洗或擦去的产品。这些组合物也可用于调理皮肤、用于使皮肤脱屑、用于清洁和洁净皮肤、用于收缩皮肤毛孔和用于缓解干燥皮肤。
发明背景
许多年来,人们采用各种介质处理人体皮肤,以使皮肤保持清洁和处于光滑和柔软的状态。皮肤在暴露于低湿度或刺激性洗涤液下一定时间后会有发干的趋势。从生理学的观点,干燥性是皮肤水含量的量度。在正常条件下,皮肤的水含量和蒸汽压高于环境空气的,从而从皮肤表面向外蒸发水分。由于从皮肤表面过度失去水分,皮肤会变得干燥,从而从角质层中损失水分。低湿度则加速该过程,加剧了皮肤的干燥。同样,连续和长期的接触或浸泡于肥皂或洗涤液中也会引起角质层干燥。这一现象的原因是这些溶液促进了皮肤表面和脂质的溶解,和促进了皮肤吸湿性水溶性组分的溶解。
另外,在正常皮肤中,角质层以细胞或细胞簇的形式脱落。皮肤问题,如干燥、干癣、鳞癣、痤疮、胼胝、光损伤、老化和晒斑都被描述为角朊化紊乱,其中皮肤表面角质层细胞的脱落相对于正常的年轻健康皮肤有所改变。这种改变产生了大的细胞簇脱落,产生可见的皮肤鳞屑,角朊质在皮肤的表面或小囊或管道内积累以及皮肤表面粗糙。这些状态可以通过除去最外层角朊质而改善。即通过脱屑作用。
另外,需要向皮肤有效输送大量活性物质,可以通过直接施用这类组合物或用清洁用组合物通过清洁过程而输送。
因此,需要一种局部用护肤组合物,它给皮肤光滑和舒适的感受,它用于处理干燥皮肤并用于提供脱屑作用。也需要提供具有这些优点的清洁用产品。也需要一种组合物,它也用于向皮肤输送大量活性物,直接地或通过清洁过程输送。
本发明已发现,含有两性的、阴离子的和阳离子的表面活性剂的组合的扩肤组合物可用于提供这些护肤效果。
因此本发明的一个目的是提供皮肤局部用的护肤组合物。
本发明的另一个目的是提供具有改进的皮肤调理性能的护肤组合物,它性质温和对皮肤无刺激。
本发明的另一个目的是提供改善皮肤干燥的护肤组合物,它使皮肤光滑、柔软、细腻。
本发明的另一个目的是提供用于向皮肤输送多种活性物的护肤组合物。
本发明的另一个目的是提供一种护肤组合物,当它以清洁用组合物的形式时,可通过清洁过程向皮肤输送各种活性物。
本发明的另一个目的是提供护理皮肤的方法。
本发明的另一个目的是提供清洁皮肤、洁净皮肤、使皮肤脱屑、缓解干燥、收缩毛孔和向皮肤输送活性物的方法。
本发明的另一个目的是使皮肤感觉光滑柔软。
这些和其它目的从以下详细描述中更清楚看到。
发明概述
本发明涉及局部用个人护理组合物,它包括:
(a)约0.1%至约20%重的下式两性表面活性剂:
其中R1为未取代的、饱和或未饱和的、直链或支化的约C9至约C22的烷基;m为1至约3的整数;n为0或1;R2和R3分别选自C1至约C3烷基和约C1至约C3的单羟基烷基;R4选自饱和或未饱和的C1至约C5的烷基和饱和或未饱和的C1至约C5的单羟基烷基;X选自CO2、SO3和SO4;及上述化合物的药物上可接受的盐;
(b)约0.1%至约20%重的阴离子表面活性剂,
(c)约0.1%至约15%重的阳离子表面活性剂,和
(d)约45%至约99.7%重的水。
本发明还涉及采用这些组合物处理皮肤的方法,尤其是调理、清洁、洁净和脱屑皮肤的方法,收缩毛孔方法和缓解皮肤干燥的方法。
本发明还涉及制备以下组合物的方法,该组合物包括:
(a)约0.1%至约20%重的下式两性表面活性剂:
其中R1为未取代的、饱和或未饱和的、直链或支化的约C9至约C22的烷基;m为1至约3的整数;n为0或1;R2和R3分别选自C1至约C3烷基和约C1至约C3的单羟基烷基;R4选自饱和或未饱和的C1至约C5的烷基和饱和或未饱和的C1至约C5的单羟基烷基;X选自CO2、SO3和SO4;及上述化合物的药物上可接受的盐;
(b)约0.1%至约20%重的阴离子表面活性剂,
(c)约0.1%至约15%重的阳离子表面活性剂,和
(d)约45%至约99.7%重的水。
该方法包括:
(i)将所述两性表面活性剂水溶液和所述阴离子表面活性剂水溶液结合形成所述两性的和阴离子的表面活性剂复合物的水分散体;和
(ii)将所述复合物的水分散体与所述阳离子表面活性剂的水溶液结合。
本文采用的所有百分数和比率都是以总组合物的重量计,所有测定都在25℃进行,除非另有说明。所有重量百分数除了另有说明,都以活性物重量为基础计。本发明可以包括基本成分以及非必需成分和这里所述的辅助成分,或由或基本上由这些组分构成。
发明详细描述
本发明组合物用于施用于人体皮肤。这些组合物用于调理皮肤、使皮肤脱屑、处理干燥皮肤、向皮肤输送活性物、用于清洁用实施方案中、用于清洁皮肤而不会使皮肤过分干燥或对皮肤产生刺激。
不受理论束缚,认为这些组合物的两性表面活性剂能与阴离子和阳离子表面活性剂组分复合。另外,阴离子表面活性剂也能与阳离子表面活性剂复合。这种多重复合物趋于粘稠和润滑,产生柔软光滑、轻松皮肤的感觉。这些复合物也被认为相对于单个表面活性剂组分更稳定。这些复合物用于辅助向皮肤输送组合物中存在着的任何种活性成分。对于清洁用组合物,这些复合物易于从组合物中沉降出来,从而帮助向皮肤表面输送任一活性物,使皮肤柔软光滑。因为设想的复合物可含有两性、阴离子和阳离子表面活性剂的各种组合,因此这些复合物能有效的清洁皮肤,和促进脱屑过程。由于各表面活性剂的电荷被复合了,使表面活性剂相对于游离的表面活性剂更温和,不刺激皮肤。
本发明组合物可配制成各种产品形式,包括但不限于乳膏、洗液、摩丝、喷剂、“漂洗”清洁剂、“无水”清洁剂、条块、凝胶等形式。术语“漂洗”在这里是指组合物采取的形式是,它用于清洁过程时,最终用水将它从皮肤上冲洗或漂去以完成清洗过程。术语“无水”在这里是指组合物采取的形式是,它用于清洁过程时,无需用水,而是用擦拭工具将其擦去,擦拭工具如棉球、棉片、纸巾、毛巾等。
术语“药物上可接受的”在这里是指所述组合物及其组分足够纯,适于与人体皮肤和组织接触,不产生不当毒性、刺激、不相容、不稳定、过敏反应等。
术语“药物上可接受的盐”在这里是指任一种通常采用的盐适于与人体皮肤和组织接触,不产生不当毒性、刺激、不相容、不稳定、过敏反应等。
两性表面活性剂
本发明的组合物含约0.1%至约20%,更优选约0.2%至约10%,最优选约0.5%至约5%的两性表面活性剂。
术语“两性表面活性剂”在这里也包括两性离子表面活性剂,它是本领域配剂师熟知的两性表面活性剂的一个子部分。
多种两性表面活性剂可适用于本发明组合物。尤其有用的是那些广义地描述为脂族仲胺和叔胺的衍生物,优选其中氮为阳离子状态,其中脂族基团可以是直链或支链型,其中一个基团含有可离子化的水溶性基团,如羧基、磺酸根、硫酸根、磷酸根或膦酸根。
用于本发明组合物中的两性表面活性剂的非限制性实例公开于McCutcheon的
洗涤剂与乳化剂,北美版(1986),Allured PublishingCorporation出版;和McCutcheon的
功能物质,北美版(1992);两文献都全部引入作为参考。
优选的两性或两性离子表面活性剂是甜菜碱、磺内酰胺(sultaine)和羟基磺内酰胺。甜菜碱的例子包括高级烷基甜菜碱,如可可基二甲基羧甲基甜菜碱、月桂基二甲基羧甲基甜菜碱、月桂基二甲基α-羧乙基甜碱、鲸蜡基二甲基羧甲基甜菜碱、鲸蜡基二甲基甜菜碱(购自Lonza公司的Lonzaine 16SP)、月桂基双(2-羟乙基)羧甲基甜菜碱、硬脂基双(2-羟丙基)羧甲基甜菜碱、油基二甲基γ-羧丙基甜菜碱、月桂基双(2-羟丙基)α-羧乙基甜菜碱、可可基二甲基磺丙基甜菜碱、硬脂基二甲基磺丙基甜菜碱、硬脂基甜菜碱、月桂基二甲基磺乙基甜菜碱、月桂基双(2-羟乙基)磺丙基甜菜碱、和酰氨基甜菜碱和酰氨基磺基甜菜碱(其中RCONH(CH2)3基团连至甜菜碱的氮原子上)、油基甜菜碱(购自Henkel的两性VelvetexOLB-50)和可可酰胺丙基甜菜碱(购自Henkel的Velvetex BK-50和BA-35)。
磺内酰胺和羟基磺内酰胺的实例包括例如可可酰胺丙基羟基磺内酰胺(购自Rhone-Poulene的Mirataine CBS)。
这里优选的两性表面活性剂具有以下结构:
其中R1为具有约9至约22个碳原子的未取代的、饱和或未饱和的、直链或支化的链烷基。R1优选约11至约18个碳原子,更优选约12至约18个碳原子,进一步优选约14至约18个碳原子;m为1至约3的整数;更优选约2至约3,进一步优选约3的整数;n为0或1,优选1;R2和R3各自选自1至约3个碳原子的烷基、它可为未取代的或被羟基单取代的,优选R2和R3为CH3;X选自CO2、SO3和SO4;R4选自具有1至约5个碳原子的、饱和或未饱和的、直链或支化的烷基,它可未取代或被羟基单取代。当X为CO2,R4优选具有1或3个碳原子、更优选1个碳原子。当X为SO3或SO4时,R4优选具有约2至约4个碳原子,更优选3个碳原子。
本发明的两性表面活性剂的实例包括以下化合物:
鲸蜡基二甲基甜菜碱(该物质也具有CTFA命名鲸蜡基甜菜碱)
可可酰胺丙基甜菜碱
其中R具有约9至约13个碳原子,
可可酰胺丙基羟基磺内酰胺
其中R具有约9至约13个碳原子,
硬脂基二甲基甜菜碱
和二十二烷基甜菜碱
本发明优选的两性表面活性剂包括鲸蜡基二甲基甜菜碱、可可酰氨丙基甜菜碱、硬脂基二甲基甜菜碱和可可酰氨丙基羟基磺内酰胺。更优选鲸蜡基二甲基甜菜碱、硬脂基二甲基甜菜碱和可可酰氨丙基甜菜碱。最优选鲸蜡基二甲基甜菜碱。
其它适用的两性表面活性剂的实例有烷基亚氢基乙酸盐、亚氨基二烷酸盐和氨基烷酸盐,通式为RN[(CH2)mCO2M]2和RNH(CH2)mCO2M,其中m为1-4,R为C8-C22烷基或烯基,M为H、碱金属、碱土金属、铵或烷醇铵。还包括咪唑啉鎓盐和铵盐的衍生物。适用的两性表面活性剂的特定实例包括3-十二烷基-氨基丙酸钠、3-十二烷基氨基丙烷磺酸钠、N-烷基-牛磺酸,如按照引入为参考的USP2658072中的方法,将十二烷基胺与羟乙磺酸钠反应制备;N-高级烷基天门冬氨酸,如按照引入本文为参考的USP2438091中的方法制备的;在引入本文为参考的USP2528378中描述的以商品名“Miranol”出售的产品。其它适用的两性表面活性剂包括磷酸酯(盐),如可可酰胺丙基氯化PG-dimonium磷酸盐(购自Mona公司的Monaquat PTC)。
阴离子表面活性剂
本发明包括约0.1%至约20%,更优选约0.2%至约10%,最优选约0.5%至约5%的阴离子表面活性剂
用于本发明组合物中的阴离子表面活性剂的非限制性实例公开于McCutcheon的
洗涤剂与乳化剂,北美版(1986),Allured PublishingCorporation出版;和McCutcheon的
功能物质,北美版(1992);两文献都全部引入作为参考。
各种阴离子表面活性剂都适用于本发明。阴离子表面活性剂的非限制性实例包括烷酰基羟乙磺酸盐和烷基硫酸盐与烷基醚硫酸盐。一般烷酰基羟乙磺酸盐可以式RCO-OCH2CH2SO3M表示,其中R是约10-约30个碳原子的烷基或链烯基,M是水溶性阳离子,如铵、钠、钾及三乙醇胺。这些羟乙磺酸盐的非限制性实例包括选自椰子酰基羟乙磺酸铵、椰子酰基羟乙磺酸钠、月桂酰基羟乙磺酸钠、硬脂酰基羟乙磺酸钠及它们的混合物的烷酰基羟乙磺酸盐。
烷基硫酸盐和烷基醚硫酸盐通常可用式ROSO3M和RO(C2H4O)xSO3M表示,式中R是约10-约30个碳原子的烷基或链烯基,x是约1-约10、M是水溶性阳离子如铵、钠、钾及三乙醇胺。另一类适用的阴离子表面活性剂是硫酸与有机物反应产物的水溶性盐,其通式为:
R1-SO3-M
式中R1是选自含约8-约24,优选约12-约18个碳原子直链或支链的饱和脂族烃基,M是阳离子。其它合成的阴离子表面活性剂还包括称为琥珀酰胺酸盐、含约12-约24个碳原子的烯烃磺酸盐及b-烷氧基链烷磺酸盐的一类。这类物质的实例有月桂基硫酸钠和月桂基硫酸铵。
其它的阴离子物质包括肌氨酸盐,其非限制性实例包括月桂酰肌氨酸钠、椰子酰肌氨酸钠和月桂酰肌氨酸铵。
适用于本发明的其它阴离子物质是通常含约8-约24个碳原子,优选约10-约20个碳原子的脂肪酸皂(即碱金属盐,如钠盐或钾盐)。制皂用脂肪酸可从天然来源如从植物或动物中取得的甘油酯(如棕榈油、椰子油、大豆油、蓖麻油、动物脂、猪脂等)中获得。脂肪酸也可由合成方法制得。上面引用的美国专利4557853已对皂类作了较详细的说明。
其它阴离子物质包括磷酸盐,如单烷基、二烷基和三烷基磷酸盐。
其它阴离子物质包括对应于式RCON(CH3)CH2CH2CO2M的链烷酰基肌氨酸盐,其中R是约10-约20个碳原子的烷基或链烯基,M是水溶性阳离子,如铵、钠、钾和三烷醇胺(如三乙醇胺),优选的实例是月桂酰基肌氨酸钠。
这里优选的阴离子表面活性剂的非限制性实例包括选自以下的物质:月桂基硫酸钠、月桂基硫酸铵、鲸蜡基硫酸铵、鲸蜡基硫酸钠、硬脂基硫酸钠、椰子酰羟乙磺酸铵、月桂酰羟乙磺酸钠、月桂酰肌氨酸钠及其混合物。
尤其优选月桂基硫酸钠。
阳离子表面活性剂
本发明组合物包含约0.1%至约15%,更优选约0.2%至约10%,最优选约0.5%至约5%的阳离子表面活性剂。
用于本发明组合物中的阳离子表面活性剂的非限制性实例公开于McCutcheon的
洗涤剂与乳化剂,北美版(1986),Allured PublishingCorporation出版;和McCutcheon的
功能物质,北美版(1992);两文献都全部引入作为参考。
这里有用的阳离子表面活性剂的非限制性实例包括有下列分子式的阳离子铵盐:
其中,R1选自含有大约12~22个碳原子的烷基,或者含有大约12~22个碳原子的芳香族的芳基或烷芳基;R2、R3和R4要各自从氢、含有大约1~22个碳原子的烷基或者含有大约12~22个碳原子的芳香族的芳基或烷芳基中选择;X是从由氯、溴、碘、乙酸根、磷酸根、硝酸根、硫酸根、甲基硫酸根、乙基硫酸根、甲苯磺酸根、乳酸根、柠檬酸根、甘醇酸酯以及它们的混合物构成的集合中选择。另外,烷基也可以含有醚键,或者羟基或氨基取代基(例如,烷基可以含有聚乙二醇和聚丙二醇部分)。
更优选的是,R1是一个含有大约12~22个碳原子的烷基;R2从H或含有大约1~22个碳原子的烷基中选择;R3和R4从氢、含有大约1~3个碳原子烷基中选取;X则如前所述。
最优选的是,R1是一个含有大约12~22个碳原子的烷基;R2、R3和R4从氢、含有大约1~3个碳原子烷基中选择;X则如前所述。
作为一个替代的办法,其它有用的阳离子乳化剂包括氨基酰胺,其中上述的结构中R1替换为R5CO-(CH2)n-,其中R5是含有大约12~22个碳原子的烷基,n是大约2~6的一个整数,优选的是大约2~4的一个整数,更优选的是大约2~3的一个整数。非限制性的这些阳离子乳化剂包括硬脂酰氨基丙基氯化磷酸PG-dimonium,硬脂酰氨基丙基乙硫酸(ethosulfate)乙基dimonium,硬脂酰氨基丙基二甲基(十四烷基乙酸)氯化铵,硬脂酰氨基丙基二甲基cetearyl甲苯磺酸铵,硬脂酰氨基丙基二甲基氯化铵、硬脂酰氨基丙基二甲基乳酸铵以及它们的混合物。
非限制性的季铵盐阳离子乳化剂几个例子可以是从由十六烷基氯化铵、十六烷基溴化铵、十二烷基氯化铵、十二烷基溴化铵、硬脂基氯化铵、硬脂基溴化铵、十六烷基二甲基氯化铵、十六烷基二甲基溴化铵、十二烷基二甲基氯化铵、十二烷基二甲基溴化铵、硬脂基二甲基氯化铵、硬脂基二甲基溴化铵、十六烷基三甲基氯化铵、十六烷基三甲基溴化铵、十二烷基三甲基氯化铵、十二烷基三甲基溴化铵、硬脂基三甲基氯化铵、硬脂基三甲基溴化铵、十二烷基二甲基氯化铵、硬脂基二甲基十六烷基二动物脂基二甲基氯化铵、二-十六烷基氯化铵、二-十六烷基溴化铵、二-十二烷基氯化铵、二-十二烷基溴化铵、二-硬脂基氯化铵、二-硬脂基溴化铵、二-十六烷基甲基氯化铵、二-十六烷基甲基溴化铵、二-十二烷基甲基氯化铵、二-十二烷基甲基溴化铵、二-硬脂基甲基氯化铵、二-硬脂基二甲基氯化铵、二-硬脂基甲基溴化铵以及它们的混合物构成的集合中选择的那些例子。其它的的季铵盐包括那些其中C12-C22烷基碳链是由动物脂脂肪酸或椰子脂肪酸衍生的。其中“动物脂基”一词是指一个由通常含C16~C18范围内的烷基的混合物的动物脂肪酸衍生的烷基(通常是加氢的动物脂肪酸),而“椰子”一词是指由通常含C12-C14的烷基混合物的椰子脂肪酸衍生的一个烷基。由这些动物脂和椰子得到的几个季铵盐的例子包括二动物脂基二甲基氯化铵,二动物脂基二甲基甲基硫酸铵、二(加氢动物脂基)二甲基氯化铵、二(加氢动物脂)二甲基醋酸铵、二动物脂二甲基磷酸铵、二动物脂二甲基硝酸铵、二(椰子烷基)二甲基氯化铵、二(椰子烷基)二甲基溴化铵、动物脂氯化铵、椰子基氯化铵、硬脂酰氨基丙基酸PG-dimonium、硬脂酰氨基丙基乙硫酸乙基dimonium、硬脂酰氨基丙基二甲基(十四烷基乙酸)氯化铵,硬脂酰氨基丙基二甲基cetearyl甲苯磺酸铵、硬脂酰氨基丙基二甲基氯化铵、硬脂酰氨基丙基二甲基乳酸铵以及它们的混合物构成的集合中选择。
优选的阳离子表面活性物可以从由二-十二烷基二甲基氯化铵、二-硬脂基二甲基氯化铵、二-十四烷基二甲基氯化铵、二-十六烷基二甲基氯化铵及其混合物构成的集合中选择。
水
本发明组合物包含约45%至约99.7%的水,更优选约60%至约95%,最优选约70%至约90%的水。具体的水含量取决于产品的形式及所需的水含量。
添加组分
本发明的组合物可以含多种添加组分。在本文中被完全引用作为参考的
CTFA Cosmetic Ingredient Handbook,Second Edition,1992中,描述了许多种常用于护肤品工业的化妆品和药品级组分,这些组分适用于本发明的组合物。在该参考内容的第537页描述了一些功能类组分的非限制性的例子。这些功能类的实例包括:磨料,吸收剂,防痤疮剂,防结块剂,防沫剂,灭菌剂,抗氧化剂,粘合剂,生物添加剂,缓冲剂,填充剂,螯合剂,化学添加剂,着色剂,化妆品收敛剂,化妆品生物杀伤剂,变性剂,药物收敛剂,外用止痛剂,成膜剂,香料组分,湿润剂,遮光剂,pH调节剂,增塑剂,防腐剂,推进剂,还原剂,皮肤增白剂,皮肤调理剂(软化剂,湿润剂,miscellaneous和闭塞剂),皮肤保护剂,溶剂,泡沫促进剂,水溶助长剂,加溶剂,悬浮剂(非表面活性剂),防晒剂,紫外线吸收剂增粘剂(含水或不含水)。这里的功能类物质为本领域技术人员已知的实例包括乳化剂、多价螯合剂和皮肤致敏剂(skin sensate)等。
在CTFA Cosmetic Ingredient Handbook中引用的这些添加组分的一些非限制性的例子也可以用于本发明,其中包括:维生素及其衍生物(即维生素C,维生素A(即视黄酸),视黄醇,视黄酸酯,视黄醇酯,类视色素,泛酰醇,泛酰醇酯,生育酚,生育酚酯,以及类似的物质);油和皮脂调节剂,如粘土、硅氧烷和药物活性物;防晒剂;其它硅氧烷:如二甲聚硅氧烷醇、二甲聚硅氧烷共多元醇和amodimethicone等;抗氧化剂;抗生物剂;防腐剂;乳化剂;聚乙二醇和聚丙二醇;有助于组合物成膜性质和亲和性的聚合物(如二十碳烯和乙烯基吡咯烷酮的共聚物,一个实例就是GAF Chemical Corporation出产的Ganex V-200);为保持组合物灭菌完整性的防腐剂;防痤疮药剂(如间苯二酚,硫磺,水杨酸,红霉素,锌,以及类似的物质);皮肤增白剂(或光亮剂),其中包括氢醌,曲酸,但不仅限于此;抗氧化剂;螯合剂和多价螯合剂;增稠剂如carbomers(用季戊四醇的烯丙基醚或蔗糖的丙基醚交联的丙烯酸的均聚物),交联和非交联的非离子和阳离子聚丙烯酰胺〔如SalcareSC92它具有CTFA命名聚季铵盐32(和)矿物油,SalcareSC95它具有CTFA命名聚季铵盐37(和)矿物油(和)PPG-1 trideceth-6,和非离子Seppi-Gel聚丙烯酰胺,购自Seppic公司〕;蛋白质和肽;酶;神经酰胺;以及美感组分,例如香料,色素,着色剂,芳香油,皮肤致敏剂,收敛剂,皮肤舒适剂,皮肤治疗剂及类似物质;这些美感组分的非限制性的例子包括丁子香油,薄荷醇,樟脑,桉树油,丁子香酚,乳酸酯,金缕梅馏出液,红没药醇,甘草酸二钾及类似的物质;皮肤调理剂如尿素和甘油以及1990年12月11日授权Orr等人的U.S.P No.4,976,953中描述的甘油的丙氧基化物,此文的内容在这里被完全引用作为参考。
这些其它成分中的一些成分在下面详细描述。
活性成份
本发明的组合物含有安全和有效量的一种或多种活性成份及其药物上可接受的盐。
这里所用的“安全和有效量”一词,是指以在完善的药品评判的范围内的一个合理的活性组分的用量,该活性成份的量要足够高,以致于可以改善要处理的条件,或者可以给皮肤带来所期望的好处,但是又要使其足够低,以致于可以避免严重的副作用。安全和有效量的活性成份的含义又将随着不同的活性物、活性物渗过皮肤的能力、使用者的年龄、健康状况以及皮肤条件和类似的其它因素而变化。
通常,本发明活性物占组合物重量的约0.001%至约20%,优选约0.01%至约15%,更优选约0.025%至约10%。
可以根据治疗作用和假设的作用模式给这里所用的活性物分类。然而,应该明白的是这里所用的活性物有时可以提供不止一种治疗作用或者是可以执行多种作用形式。因此,为方便起见,这里进行了分类,但不是为了将活性物限制在列出的特定的一种应用或一些应用中。另外,这里也可以使用这些物质的药物上可接受的盐。在本发明组合物中,下面的活性物是有用的。
抗痤疮活性物:有用的抗痤疮活性物的几个例子包括溶角蛋白剂,例如水杨酸(邻羟基苯甲酸)、水杨酸的衍生物例如5-辛酰水杨酸和间苯二酚;视黄酸类物质例如视黄酸和它的衍生物(例如顺式和反式视黄酸);含硫的D和L氨基酸及其衍生物和盐,尤其是其N-乙酰基衍生物,优选的例子为N-乙酰基-L-半胱氨酸;硫辛酸;抗菌素和灭菌剂例如过氧化苯甲酰、羟甲辛吡酮、四环素、2,4,4′-三氯-2′-羟基-二苯醚、3,4,4′-三氯对称二苯脲(3,4,4’-trichlorobanilide)、壬二酸及其衍生物、苯氧基乙醇、苯氧基丙醇、苯氧基异丙醇、乙酸乙酯,氯林肯霉素和甲氯环素;sebostats例如类黄酮;胆汁盐例如鲨胆淄醇硫酸盐及其衍生物、脱氧胆酸盐和胆酸盐。
抗皱和抗皮肤萎缩活性物:抗皱和抗皮肤萎缩活性物的几个例子包括视黄酸及其衍生物(顺式和反式);视黄醇、视黄酯、水杨酸及其衍生物;含硫的D和L氨基酸及其衍生物和盐,尤其是N-乙酰基衍生物,其优选的实例为N-乙酰基-L-半胱氨酸;硫醇,如乙硫醇;α-羟基酸,如乙醇酸和乳酸;肌醇六磷酸,硫辛酸、溶血磷脂酸和去皮剂(例如苯酚)。
非甾族抗炎活性物(NSAIDS):NSAIDS的例子包括下列类型:丙酸衍生物、乙酸衍生物、灭酸衍生物、联苯基羧酸衍生物和oxicams。所有这些NSAIDS都在1991年1月15日发表的Sunshine等人的美国专利4,985,459中有充分的说明,在这里作为参考。有用的NSAIDS的几个例子包括乙酰水杨酸、异丁苯丙酸、甲氧萘丙酸、苯恶丙芬、氟联苯丙酸、苯氧苯丙酸、联苯丁酮酸、酮苯丙酸、茚酮苯丙酸、吡丙芬、卡洛芬、恶哌拉嗪、双吡苯丙酸、咪洛芬、苯恶硫丙酸、噻丙吩、阿明洛芬、苯噻丙酸、氟苯丙酸和布氯酸。包括氢化可的松的甾族的抗炎药物也是有用的。
局部麻醉剂:几个局部麻醉剂的例子包括苯坐卡因、利度卡因、丁哌卡因、氯丙卡因、狄布卡因、衣铁卡因、甲哌卡因、丁卡因、达克罗宁、己卡因、普鲁卡因、可卡因、氯胺酮、丙吗卡因、苯酚和它们的药物上可以接受的盐。
人工鞣制剂和促鞣剂:人工的用于鞣制的促鞣剂包括二羟基丙酮、酪氨酸、酪氨酸酯,如酪氨酸乙酯,和phospho-DOPA。
抗菌和抗真菌活性物:抗菌和抗真菌活性物的例子有:β-内酰胺类药、喹诺酮类药物、环丙氟氯霉素、诺氟沙星、四环素、红霉素、阿米卡星、2,4,4′-三氯-2′-羟基二苯醚、3,4,4′-三氯对称二苯脲、苯氧基乙醇、苯氧基丙醇、苯氧基异丙醇、强力霉素、缠霉素、洗必汰、金霉素、土霉素、氯林肯霉素、乙氨丁醇、羟乙磺酸己脒定、甲哨唑、戊脒定、庆大霉素、卡那霉素、线霉素,甲烯土霉素、乌洛品托、二甲胺四环素、新霉素、奈替米星、巴龙霉素、链霉素、托普霉素、双氯苯咪唑、四环素、盐酸化物、红霉素、锌红霉素、无味红霉素、红霉素硬脂酸盐、硫酸阿米卡星、多西环素盐酸盐、硫酸卷曲霉素、葡萄糖酸洗必汰、盐酸洗必汰、盐酸金霉素、盐酸土霉素、盐酸氯林肯霉素、盐酸乙氨丁醇、盐酸甲哨唑、盐酸戊脒定、硫酸庆大霉素、硫酸卡那霉素、盐酸线霉素、盐酸甲烯土霉素、马尿酸乌洛托品、扁桃酸乌洛托品、盐酸二甲胺四环素、硫酸新霉素、硫酸奈替米星、硫酸巴龙霉素、硫酸链霉素、硫酸托普霉素、盐酸双氯苯咪唑、盐酸amanfadine、硫酸manfadine、羟甲辛吡酮、对氯间二甲苯酚、制霉菌素、癣退和克霉唑。
防晒活性物:在这里某些防晒剂是有用的。各种各样的防晒剂在下列文献中都有说明:1992年2月11日授权的Haffey等人的美国专利No.5,087,445;1991年12月17日授权的Turner等人的美国专利No.5,073,372;1991年12月17日授权的Turner等人的美国专利No.5,073,371;Segarin等人的Cosmetics Science and Technology一书中第八章第189页。所有上述文献全文在这里都全文作为参考。用于本发明的这些防晒剂的非限制性实例选自对甲氧基肉桂酸(2-乙基-己)酯、N,N-二甲基-对氨基苯甲酸(2-乙基己)酯、对氨基苯甲酸、2-苯基苯并咪唑-5-磺酸、奥克立林、羟苯甲酮、水杨酸高酯、水杨酸辛酯、4,4’-甲氧基-叔丁基二苯甲酰基甲烷、4-异丙基二苯甲酰基甲烷、3-亚苄基樟脑、3-(4-甲基亚苯基)樟脑、二氧化钛、氧化锌、二氧化硅、氧化铁及其混合物。其它一些有用的防晒剂公开于1990年6月26日授权Sabatelli的USP4937370;1991年3月12日授权Sabatelli等人的USP4999186;这两篇都结合入供参考。这里公开的防晒剂在一个分子中具有两个性质不同的发色团,它们体现不同的紫外辐射吸收光谱。一个生色团主要在UVB辐射范围内吸收,另一个在UVA辐射范围内强吸收。这些防晒剂与传统防晒剂相比具有更高的效力、更宽的UV吸收、更低的皮肤穿透性和更长的耐久效力。这些实例中尤其优选2,4-二羟基二苯酮的4-N,N-(2-乙基己基)甲基氨基苯甲酸酯、4-羟基二苯甲酰基甲烷的4-N,N-(2-乙基己基)甲基氨基苯甲酸酯、2-羟基-4-(2-羟基乙氧基)二苯酮的4-N,N-(2-乙基己基)甲基氨基苯甲酸酯、4-(2-羟基乙氧基)二苯甲酰基甲烷的4-N,N-(2-乙基己基)甲基氨基苯甲酸酯、及其混合物。通常,防晒剂占这里所用组合物的约0.5%至约20%。确切的使用量取决于所选防晒剂和所需的防晒因子(SPF)。SPF是防晒剂防止起红斑的光保护作用的常用量度方法。见Federal Register,卷43,No.166,第38206-38269页,8月25,1978,引入本文供参考。
这里有用的几个优选的活性物的例子包括水杨酸、3-羟基苯甲酸、乙醇酸、乳酸、4-羟基苯甲酸、乙酰基水杨酸、2-羟基丁酸、2-羟基戊酸、2-羟基己酸、顺-视黄酸、反-视黄酸、视黄醇、肌醇六磷酸、N-乙酰基-L-半胱氨酸、硫辛酸、壬二酸、花生四烯酸、过氧化苯甲酸、四环素、异丁苯丙酸、甲氧萘丙酸、氢化可的松、acetominophen、间苯二酚、苯氧基乙醇、苯氧基丙醇、苯氧基异丙醇、2,4,4′-三氯-2′-羟基二苯醚、3,4,4′-三氯对称二苯脲、羟甲辛吡酮、利度卡因盐酸盐、克霉唑、双氯苯咪唑、硫酸neocycin、对氨基苯甲酸、2-苯基苯并咪唑-5-磺酸、二羟基丙酮和它们的混合物。
在这里有用的更好的几个活性物的例子包括水杨酸、过氧化苯甲酰、乙酰基水杨酸、顺-视黄酸、反-视黄酸、视黄醇、肌醇六磷酸、N-乙酰基-L-半胱氨酸、硫辛酸、壬二酸、四环素、异丁苯丙酸、甲氧萘丙酸、acetominophen、氢化可的松、间苯二酚、苯氧基乙醇、苯氧基丙醇、苯氧基异丙醇、2,4,4′-三氯-2′-羟基二苯醚、3,4,4′-三氯对称二苯脲、羟甲辛吡酮、2-苯基苯并咪唑-5-磺酸、二羟基丙酮和它们的混合物。
在这里有用的最优选的几个活性物的例子包括水杨酸、过氧化苯甲酰、顺-视黄酸、反-视黄酸、视黄醇、肌醇六磷酸、N-乙酰基-L-半胱氨酸、硫辛酸、壬二酸、间苯二酚、乙醇酸、乳酸、异丁苯丙酸、甲氧萘丙酸、氢化可的松、苯氧基乙醇、苯氧基丙醇、苯氧基异丙醇、2,4,4′-三氯-2′-羟基二苯醚、3,4,4′-三氯对称二苯脲、对甲氧基肉桂酸2-(乙基己)酯、羟苯甲酮、2-苯基苯并咪唑-5-磺酸、二羟基丙酮和它们的混合物。
保湿剂和增湿剂
本发明组合物还包括一种或多种保湿剂和增湿剂。许多种这类物质都可被采用,每种的存在量可为约0.1%至约20%,更优选约0.5%至约15%,最优选约1%至约10%。保湿剂的非限制性实例包括:胍、乙醇酸和乙醇酸盐(如铵盐和烷基季铵盐);乳酸和乳酸盐(如铵盐和烷基季铵盐);各种形式的芦芸(如芦芸胶);多羟基醇如山梨醇、甘油、己三醇、丙二醇、丁二醇、己二醇等;聚乙二醇;糖和淀粉;糖和淀粉衍生物(烷氧基化葡萄糖);透明质酸;乳酰胺单乙醇胺;乙酰胺单乙醇胺;及其混合物。
另外,1990年12月11日授权Orr等人的USP4976953中描述的丙氧基化甘油也可用于本发明,该文献全文引入为参考。
这里特别优选的保湿剂是甘油。
不溶性颗粒
本发明的组合物包含约0.1%-约20%,更优选约0.25%-约15%,最优选约0.5%-约10%的不溶性颗粒(以组合物总重量计),该颗粒在以清洁组合物的形式时可增强清洁效果。
本文所用术语“不溶的”是指颗粒基本上不溶于本发明组合物中。具体地说,在25℃不溶性颗粒的溶解度为每100克组合物中应低于约1克,优选每100克组合物中低于约0.5克,更优选每100克组合物中低于约0.1克。
这里可以使用微粉化和常规粒径的不溶性颗粒。微粉化颗粒的绝大多数的粒径低于产生触觉的临界值,对皮肤几乎不产生磨蚀。常规粒径的颗粒是可触觉到的,加入后提供摩擦和磨蚀作用。
这些微粉化颗粒的平均粒径和粒度分布应低于大多数使用者的触觉阀限,但同时不能小到对除去油脂、污垢和碎屑(如化妆品)不起作用的程度。本发明还发现,平均粒径大于约75微米的颗粒在清洁过程中会有触感,因此,如果需要该种颗粒不被使用者察觉到,使组合物中这种较大颗粒的数量保持在最低限度是很重要的。反之,也发现平均粒径为小于约1-约5微米的颗粒一般来说清洁效果就差。如果不受理论束缚,可认为微粉化清洁用颗粒的大小应与待清除的污垢、油脂或碎屑层的厚度属同一数量级。据认为该层的厚度多数情况下是几微米数量级。本发明因此还发现微粉化颗粒的平均粒径应在约1-约75微米,更优选约15-约60微米,最优选约20-约50微米,这样的颗粒才能赋予组合物有效的去污性而没有触感。具有不同形状、表面特征及硬度特性的颗粒都可用于本发明中,只要粒度符合要求。本发明微粉化颗粒可从包括那些来自无机、有机、天然及合成源的各种物质中得到。这些物质的非限制性实例包括选自杏仁粉、矾土、氧化铝、硅酸铝、杏核粉、硅镁土、大麦粉、氯氧化铋、一氮化硼、碳酸钙、磷酸钙、焦磷酸钙、硫酸钙、纤维素、白垩、甲壳质、粘土、玉米穗轴粗粉、玉米穗轴粉、玉米粉、玉米粗粉、玉米淀粉、硅藻土、磷酸二钙、磷酸二钙二水合物、漂白土、水合二氧化硅、羟基磷灰石、氧化铁、希蒙得木种子粉、高岭土、丝瓜络、三硅酸镁、云母、微晶纤维素、蒙脱土、燕麦麦麸、燕麦粉、燕麦片、桃核粉、美洲山核桃壳粉、聚丁烯、聚乙烯、聚异丁烯、聚甲基苯乙烯、聚丙烯、聚苯乙烯、聚氨酯、尼龙、特氟隆(即聚四氟乙烯)、聚卤化烯烃、米糠、黑麦粉、丝云母、二氧化硅、玉米长须、碳酸氢钠、硅铝酸钠、大豆粉、合成水辉石、滑石、氧化锡、二氧化钛、磷酸三钙、核桃壳粉、小麦麦麸、小麦粉、小麦淀粉、硅酸锆以及它们的混合物。由混合的聚合物(如共聚物、三元共聚物等)制的微粉化颗粒也是适用的,如聚乙烯/聚丙烯共聚物、聚乙烯/丙烯/异丁烯共聚物、聚乙烯/苯乙烯共聚物等。通常,聚合物及混合的聚合物颗粒经氧化处理以破坏杂质等。聚合物及混合的聚合物颗粒也可任选地用各种常用交联剂交联,交联剂的非限制性实例包括丁二烯、二乙烯基苯、亚甲基双丙烯酰胺、蔗糖的烯丙基醚、季戊四醇的烯丙基醚,以及它们的混合物。适用的微粉化颗粒的其它实例包括蜡与树脂,如石蜡、巴西棕榈蜡、ozekerite蜡、小烛树蜡、脲-甲醛树脂等。当这类蜡及树脂用于本发明时,这些物质在室温和皮肤温度下应呈固态是很重要的。
选自聚丁烯、聚乙烯、聚异丁烯、聚甲基苯乙烯、聚丙烯、聚苯乙烯、聚氨酯、尼龙、特氟隆及它们混合物的合成聚合物颗粒是属于优选适用于本发明的水不溶微粉化颗粒状物质之中。聚乙烯和聚丙烯微粉化颗粒是最优选的,而这些物质经氧化后的变型态是尤其优选的。适用于本发明可商购的颗粒实例包括购自Allied Signal(Morristown,新泽西州)的AcumistTM微粉化聚乙烯蜡,可购到按5微米至60微米间的不同平均粒度分为A、B、C、及D四个系列的产品。平均粒径分别为25、30及45微米、经氧化的聚乙烯颗粒AcumistTMA-25、A-30及A-45是优选的。可商购的聚丙烯颗粒的实例包括购自Micro Powders(Dartek)的Propyltex系列。
常规粒径的不溶性颗粒对于本领域的配剂师来说是熟知的。这些粒子通常具有比这里所述的微粉化颗粒更大的粒径。这些颗粒的平均粒径通常大于约75微米或更大。处于触觉临界值之上。这些常规粒径颗粒通常可达约400微米或更大。这些颗粒可以使用制备所述微粉化颗粒的相同材料制得。这里优选使用的常规粒径颗粒物质为合成聚合物颗粒,选自:聚丁烯、聚乙烯、聚异丁烯、聚甲基苯乙烯、聚丙烯、聚苯乙烯、聚氨酯、尼龙、特氟隆及其混合物。最优选是聚乙烯和聚丙烯微粉化颗粒,尤其优选这些物质的氧化形态。这里使用的商购常规粒径颗粒的例子是ACuscrubTM51,Allied Signal(Morristown,NJ),平均粒径约125微米。
其它表面活性剂
本发明组合物除了所需的表面活性剂外,还可包括其它表面活性剂。尤其有用的是非离子表面活性剂。
用于本发明组合物中的非离子表面活性剂的非限制性实例公开于McCutcheon的
洗涤剂与乳化剂,北美版(1986),Allured PublishingCorporation出版;和McCutcheon的
功能物质,北美版(1992);两文献都全部引入作为参考。
那些可概括地定义为长链醇(如C8-C30醇)与糖或淀粉聚合物的缩合产物,即糖苷是属于适用于本发明非离子表面活性剂中的。这类化合物可用式(S)n-O-R表示,式中S是糖部分如葡萄糖、果糖、甘露糖和半乳糖,n是约1-约1000的整数,R是C8-C30烷基。衍生出烷基的长链醇实例包括癸醇、鲸蜡醇、硬脂醇、月桂醇、肉豆蔻醇、油醇等。这些表面活性剂优选的实例包括S是葡萄糖部分、R是C8-C20烷基、n是约1-约9整数的那些化合物。这些表面活性剂中可商购的实例包括癸基聚糖苷(可从Henkel公司购买的APG 325CS)和月桂基聚糖苷(可从Henkel公司购买的APG600CS及625CS)。
其它适用的非离子表面活性剂包括烯化氧与脂肪酸的缩合产物(即脂肪酸的烯化氧酯)。这些物质的通式为RCO(X)nOH,其中R是C10-C30烷基基团,X是-OCH2CH2-(即由乙二醇或氧化物衍生的)或-OCH2-CH-CH3-(即由丙二醇或氧化物衍生的),n是约1约100的整数。其它非离子表面活性剂是烯化氧与2摩尔脂肪酸的缩合产物(即烯化氧的二脂肪酸酯)。这类物质的通式为RCO(X)nOOCR,其中R是C10-C30烷基基团,X是-OCH2CH2-(即由乙二醇或氧化物衍生的),或-OCH2CHCH3-(即由丙二醇或氧化物衍生的),n是约1-约100的整数。其它非离子表面活性剂是烯化氧与脂肪醇的缩合产物(即脂肪醇的烯化氧醚)。这类物质的通式为R(X)nOR’,其中R是C10-C30烷基基团,X是-OCH2CH2-(即由乙二醇或氧化物衍生的)或-OCH2CHCH3-(即由丙二醇或氧化物衍生的),n是约1-约100的整数和R’是H或C10-C30烷基基团。还有其它非离子表面活性剂是烯化氧既与脂肪酸又与脂肪醇缩合的产物[即其中聚氧化烯部分的一端与脂肪酸酯化而另一端与脂肪醇醚化(即通过醚键连接)]。这类物质的通式为RCO(X)nOR’,其中R与R’是C10-C30烷基基团,X是-OCH2CH2-(即由乙二醇或氧化物衍生的)或-OCH2CHCH3-(即由丙二醇或氧化物衍生的),n是约1-约100整数。这些由烯化氧衍生的非离子表面活性剂的非限制性实例包括ceteth-1、ceteth-2、ceteth-6、ceteth-10、ceteth-12、ceteraeth-2、ceteraeth-6、ceteraeth-10、ceteraeth-12、steareth-1、steareth-2、steareth-6、steareth-10、steareth-12、steareth-21、PEG-2硬脂酸酯、PEG-4硬脂酸酯、PEG-6硬脂酸酯、PEG-10硬脂酸酯、PEG-12硬脂酸酯、PEG-20硬脂酸甘油脂、PEG-80动物脂酸甘油脂、PEG-10硬脂酸甘油脂、PEG-30椰子酸甘油脂、PEG-80椰子酸甘油脂、PEG-200动物脂酸甘油脂、PEG-8二月桂酸酯、PEG-10二硬脂酸酯以及它们的混合物。
其它适用的非离子表面活性剂还包括相应于下列结构式的多羟基脂肪酸酰胺表面活性剂:
式中R1是H、C1-C4烷基、2-羟乙基、2-羟基丙基,优选C1-C4烷基,更优选甲基或乙基,最优选甲基;R2是C5-C31烷基或链烯基,优选C7-C19烷基或链烯基,更优选C9-C17烷基或链烯基,最优选C11-C15烷基或链烯基;Z是至少有3个羟基直接连到链上的具有线型烃基链的多羟基烃基部分或它们的烷氧基化(优选乙氧基化或丙氧基化)衍生物。优选的Z选自葡萄糖、果糖、麦芽糖、乳糖、半乳糖、甘露糖、木糖及它们混合物的糖部分。相应于上述结构的特别优选的表面活性剂是椰子烷基N-甲基糖苷酰胺(即,其中R2CO-部分是由椰子油脂肪酸衍生得到的)。制备含多羟基脂肪酸酰胺组合物的方法已公开在例如英国专利说明书809060(ThomasHedley & Co.Ltd.1959年2月18日公布)、E.R.Wilson的美国专利2965576(1960年12月20日授权)、A.M Schwartz的美国专利2703798(1955年3月8日授权)、Piggott的美国专利1985424(1934年12月25日授权)中,这些内容已全部列入本文供参考。
乳化剂
这里的组合物可包含各种乳化剂。这些乳化剂用于乳化本发明组合物中的各种载体成分。适宜的乳化剂可包括现有技术中公开的任一种非离子、阳离子、阴离子和两性离子乳化剂。见McCutcheon的
洗涤剂与乳化剂,北美版(1986),Allued Publishing Corporation出版;1991年4月30日授权Ciotti等的USP5011681;1983年12月20日授权Dixon等人的USP4421769;和1973年8月28日授权Dickert等人的USP3755560;该四文献都全文引入作为参考。
适宜的乳化剂类型包括甘油酯、丙二醇酯、聚乙二醇脂肪酸酯、聚丙二醇脂肪酸酯、山梨醇酯、脱水山梨醇酐酯、羧酸共聚物、葡萄糖酯和醚、乙氧基醚、乙氧基醇、磷酸烷基酯、聚氧化乙烯脂肪醚磷酸酯、脂肪酰胺、酰基乳酸酯、皂类、及其混合物。
适宜的乳化剂可包括但不限于:聚乙二醇20脱水山梨醇单月桂酸酯(吐温20)、聚乙二醇5大豆甾醇、steareth-2、steareth-20、steareth-21、ceteareth-20、PPG-2甲基葡萄糖醚二硬脂酸酯、ceteth-10、吐温80、磷酸鲸蜡基酯、鲸蜡基磷酸钾、二乙醇胺鲸蜡基磷酸酯、吐温60、硬脂酸甘油酯、PEG-100硬脂酸酯、及其混合物。
乳化剂可以单独使用或以两种或多种混合物的形式使用,它可占本发明组合物的约0.1%至约10%,更优选约0.15%至约7%,最优选约0.2%至约5%。
油
本发明组合物含有约0.25至约40%,优选约0.5至约25%,更优选约0.75至约15%的油,选自:矿物油、矿脂、C7~C40支化链烃、C1~C30羧酸C1~C30醇酯、C2~C30二羧酸C1~C30醇酯、C1~C30羧酸单甘油酯、二甘油酯和三甘油酯、C1~C30羧酸乙二醇单酯和二酯、C1~C30羧酸丙二醇单酯和二酯、C1~C30羧酸糖单酯和多酯、聚二烷基硅氧烷、聚二芳基硅氧烷、聚烷芳基硅氧烷、3至9个硅原子的环甲基聚硅氧烷、植物油、氢化植物油、聚丙二醇、聚丙二醇C4~C20烷基醚、二C8~C30烷基醚及其混合物。
油物质在水中的溶解度通常比较低,通常低于约1wt%(25℃)。适用的油组分的非限定性实例包括但不限于以下物质。其中一些在USP4919934中有进一步的描述,该专利于1990年4月24日授权Deckner等人,本文引入作为参考。
矿物油,也称液态矿脂,是从矿脂中得到的液态烃的混合物。见“默克索引”,第10版,第7048条,第1033页(1983)和“国际化妆品成分词典”,第5版,卷1,第415-417页(1993),全部引入作为参考。
矿脂,也称石油胶,是胶体体系的非直链固态烃和高沸点的液态烃,其中绝大多数液态烃包含在胶束内。见“默克索引”,第10版,第7047条,第1033页(1983);Schindler的“Drug.Cosmet.Ind.”,89,36~37,76,78~80,82(1961)”;以及“国际化妆品成分词典”,第5版,卷1,第537页(1993),它们全部引入作为参考。
这里可以使用具有约7至约40个碳原子的直链和支链烃。这些烃物质的非限定性实例包括十二烷、异十二烷、角鲨烷、胆固醇、氢化聚异丁烯、二十二烷烃、十六烷、异十六烷(商购有Permethyl101A,Presperse公司,South Plainfield,NJ)。也可以用C7~C40异链烷烃,它们是C7~C40支化烃。
适用的油包括C1~C30羧酸和C2~C30二羧酸C1~C30醇酯,包括直链和支链化合物及其芳族衍生物。其它适用的酯包括C1~C30羧酸单甘油酯、二甘油酯和三甘油酯、C1~C30羧酸乙二醇单酯和二酯,C1~C30羧酸的丙二醇单酯和双酯。直链、支链和芳基羧酸也包括在内。也可以使用这些物质的丙氧基化和乙氧基化的衍生物。非限定实例包括癸二酸二异丙酯、己二酸二异丙酯、肉豆蔻酸异丙酯、棕榈酸异丙酯、丙酸肉豆蔻酯、二硬脂酸乙二醇酯、棕榈酸(2-乙基-己)酯、新戊酸异癸酯、苯甲酸C12~C15醇酯、马来酸二(2-乙基-己)酯、棕榈酸鲸蜡酯、肉豆蔻酸肉豆蔻酯、硬脂酸硬脂酯、硬脂酸鲸蜡酯、二十二烷酸二十二烷酯、马来酸二辛酯、癸二酸二辛酯、己二酸二异丙酯、辛酸鲸蜡醇、二亚油酸二异丙酯、辛酸/癸酸三甘油酯、PEG-6辛酸/癸酸三甘油酯、PEG-8辛酸/癸酸三甘油酯及其混合物。
也可以使用糖的各种C1-C30单酯和多酯及相关物质。这些酯衍生自一个糖或多元醇部分及一个或多个羧酸部分。取决于酸和糖成分,这些酯室温下可以呈液态或固态。液态酯的实例包括:葡萄糖四油酸酯、豆油脂肪酸的葡萄糖四酯(未饱和)、混合豆油脂肪酸的麦芽糖四酯、油酸半乳糖四酯、亚油酸阿拉伯糖四酯、四亚油酸木糖酯、五亚油酸半乳糖酯、四油酸山梨醇酯、不饱和豆油脂肪酸山梨醇六酯、五油酸木糖醇酯、四油酸蔗糖酯、五油酸蔗糖酸、六油酸蔗糖酯、七油酸蔗糖酯、八油酸蔗糖酯及其混合物。本发明的固态酯的例子是山梨醇六酯,其中的羧酸酯部分是摩尔比为1∶2的棕榈油酸酯和花生酸酯;蜜三糖的八酯,其中的羧酸酯部分是摩尔比为1∶3的亚油酸酯和二十二烷酸酯;麦芽糖的七酯,其中要酯化的羧酸部分是摩尔比为3∶4的向日葵籽油脂肪酸酯和二十四烷酸酯;蔗糖的八酯,其中要酯化的羧酸部分是摩尔比为2∶6的油酸酯和二十二烷酸酯;蔗糖的八酯,其中要酯化的羧酸部分是摩尔比为1∶3∶4的月桂酸酯、亚油酸酯和二十二烷酸酯。一种优选的原料是酯化度为7-8的蔗糖聚酯,而且其中的脂肪酸部分是C18单与/或二不饱和羧酸和二十二烷酸,不饱和羧酸与二十二烷酸的摩尔比为1∶7到3∶5。一种特别优选的固态糖多酯是分子中有约7个二十二烷酸脂肪酸部分和约1个油酸部分的蔗糖的八酯。酯在以下文献中有进一步的描述:1997年1月25日授予Jandacek的USP 2831854;USP4005196;USP4005195;1994年4月26日授权Letton等人的U.S.P.No.5,306,516;1994年4月26日授权Letton等人的U.S.P.No.5,306,515;1994年4月26日授权Letton等人的U.S.P.No.5,305,514;1989年1月10日授权Jandacek等人的U.S.P.No.4,797,300;1976年6月15日授权Rizzi等人的U.S.P.No.3,963,699;1985年5月21日授权Volpenhein的U.S.P.No.4,518,772;1985年5月21日授权Volpenhein的U.S.P.No.4,517,360;以上所有内容在此均被全部引用作为参考。
例如聚二烷基硅氧烷、聚二芳基硅氧烷、聚烷芳基硅氧烷和具有3至9个硅原子的环甲基聚硅氧烷的硅氧烷是适用的油。这些硅氧烷包括挥发性和非挥发性物质。这些硅氧烷公开在USP5069897中,1991年12月3日授予Orr,该专利全文引入本文作为参考。本发明中使用的聚烷基硅氧烷包括,例如,在25℃下粘度在大约0.5到约100,000厘沲(cs)之间的聚烷基硅氧烷。这样的聚烷基硅氧烷对应的通用化学式为R3SiO[R2SiO]xSiR3,式中R是烷基基团(优选的R是甲基或乙基,更优选甲基),x是0到大约500的整数,选择x可达到要求的分子量。市购聚烷基硅氧烷包括聚二甲基硅氧烷,又名二甲聚硅氧烷,其非限制性的例子包括General ElectricCompany出售的ViGasil系列和Dow Corning Corporation出售的DowCorning200系列。本发明中用作润肤剂的聚二甲基硅氧烷的具体的例子包括粘度为0.65cs,沸点为100℃的Dow Corning200流体;粘度为10cs,沸点高于200℃的Dow Corning225流体;以及粘度分别为50,350和12,500cs,沸点高于200℃的Dow Corning200流体。在此使用的环状聚烷基硅氧烷包括那些对应通用化学式为[SiR2O]n的物质,化学式中R为烷基基团(优选的R是甲基或乙基,更优选甲基),n是大约3到约9的整数,更优选的n是大约3到约7的整数,而最优选的n是大约4到约6的整数。当R是甲基时,这些物质通常是指环状聚甲基硅氧烷。市购环状聚甲基硅氧烷包括粘度为2.5cs,沸点为172℃的Dow Corning244流体,其中主要含四聚体的环状聚甲基硅氧烷(即n=4);粘度为2.5cs,沸点为178℃的Dow Corning344流体,其中主要含五聚体的环状聚甲基硅氧烷(即n=5);粘度为4.2cs,沸点为205℃的Dow Corning245流体,其中主要含环状聚甲基硅氧烷的四聚体和五聚体(即n=4和5);粘度为4.5cs,沸点为217℃的Dow Corning345流体,其中主要含环状聚甲基硅氧烷的四聚体,五聚体,六聚体的混合物(即n=4,5和6)。可使用的物质还有例如三甲基甲硅烷氧基硅酸酯,它是一种聚合物,相应的通用化学式为[(CH2)3SiO1/2]x[SiO2]y,式中x为大约1到约500的整数,y为大约1到约500的整数。市售三甲基甲硅烷氧基硅酸酯是以商品名Dow Corning593流体出售的与二甲聚硅氧烷的混合物。本发明中使用的还有二甲聚硅氧烷醇(dimethiconols),它是两端带羟基的聚二甲基硅氧烷。这些物质可以由通用化学式R3SiO[R2SiO]xSiR2OH和HOR2SiO[R2SiO]xSiR2OH表示,式中R为烷基基团(优选的R是甲基或乙基,更优选的是甲基),x是0到大约500的整数,通过选择x达到要求的分子量。市售二甲聚硅氧烷醇通常是以与二甲聚硅氧烷或环状聚甲基硅氧烷的混合物的形式出售(例如DowCorning 1401,1402和1403流体)。本发明中使用的还有聚烷基芳基硅氧烷,优选的是25℃下粘度在大约15到65cs之间的聚甲基苯基硅氧烷。这些物质都可获得,例如SF 1075甲基苯基流体(General Electric Company出售)和556 Cosmetic Grade聚苯基三甲基硅氧烷流体(Dow CorningCorporation出售)。
这里也可以使用植物油和氢化植物油,其实例包括红花油、蓖麻油、椰子油、棉子油、鲱油、棕榈仁油、棕榈油、花生油、豆油、菜子油、亚麻籽油、米糠油、松油、芝麻油、向日葵油、氢化红花油、氢化蓖麻油、氢化椰子油、氢化棉子油、氢化鲱油、氢化棕榈仁油、氢化棕榈油、氢化花生油、氢化豆油、氢化菜子油、氢化亚麻籽油、氢化米糠油、氢化松油、氢化芝麻油、氢化向日葵油及其混合物。
也可以使用聚丙二醇、聚丙二醇的C4~C20烷基醚、聚丙二醇的C1~C20羧酸酯和二C8~C30烷基醚。这些物质的非限定性实例包括PPG-14丁基醚、PPG-15硬脂基醚、PPG-9、PPG-12、PPG-15、PPG-17、PPG-20、PPG-26、PPG-30、PPG-34、二辛基醚、十二烷基辛基醚及其混合物。
形成复合物的方法
认为从本发明的两性、阴离子和阳离子表面活性剂形成的复合物优选由以下方法制备。
首先在水相中混合两性和阴离子表面活性剂,从而形成认为是处于这种物质间的复合物的分散体,然后将这一分散体直接与阳离子表面活性剂的水溶液混合。或者将该分散体直接加入到已含有所需阳离子表面活性剂的组合物中。
处理皮肤的方法
本发明也涉及一种方法,其中将有效量的本发明组合物施用于皮肤上。这些组合物用于调理和处理干燥皮肤并向皮肤输送活性成分。本发明组合物可以以多种用量使用,通常的施用量是约0.1mg/cm2至约25mg/cm2。
在另一实施方案中,本发明组合物用于个人清洁用,尤其是清洁脸部和颈部。通常将适当的或有效量的清洁用组合物施加于待清洁的区域。或者,将适当量的清洁用组合物施加到中间物如毛巾、海绵、垫片、棉球或其它施用工具上。如果需要,待清洁区域可用水预湿。已发现本发明组合物可以在清洁过程和从皮肤漂洗中与水结合。另外,组合物可以单独使用和用垫片、棉球、毛巾或其它类似工具从皮肤上擦去。漂洗过程通常是两步,涉及施用组合物,随后用水漂洗或无水擦去。通常使用的有效量取决于个人的需要及使用习惯。
实施例
以下实施例将进一步描述和说明本发明范围内的实施方案。实施例仅为说明目的,不解释为对本发明的限制,在不脱离本发明的精神和范围内的许多改动是可能的。
成分用化学名或CTFA命名。
实施例1
通过用常规混合设备将以下成分结合来制备含过氧化苯甲酰的留存液组合物。
成分
重量百分比
相A
水 适量至100
甘油 4.00
EDTA二钠 0.10
Carbomer 0.60
丙烯酸酯/丙烯酸C10-C30烷
基酯交联聚合物 0.05
(crosspolymer)
相B
硬脂醇 2.25
鲸蜡醇 2.25
Steareth-100 0.50
二硬脂基二甲基氯化铵 0.20
相C
三乙醇胺 0.50
相D
过氧化苯甲酰 2.50
相E
鲸蜡基二甲基甜菜碱 1.00
月桂基硫酸钠 0.50
在一适当容器中,将相A组分搅拌加热至约75℃,在另一容器中,将相B组分搅拌加热至约75℃,然后在搅拌下将相B加入至相A。然后在搅拌下加入相C,然后冷却混合物至35℃。在搅拌下加入过氧化苯甲酰。在另一容器中,混合相E成分,在搅拌下加入至其余混合物中。
所得的留存型组合物用于防止和治疗痤疮,它对皮肤温和。
另外,制备一组合物,其中用硬脂基二甲基甜菜碱代替鲸蜡基二甲基甜菜碱。
实施例2
通过用常规混合设备将以下成分结合来制备含水杨酸的个人清洗剂组
合物。
成分
重量百分比
相A
水 适量至100
甘油 3.00
EDTA二钠 0.01
相B
PPG-15硬脂醚 4.00
硬脂醇 2.88
水杨酸 2.00
二硬脂基二甲基氯化铵(Distearyl 1.50
Dimonium Chloride)
鲸蜡醇 0.80
Steareth-21 0.50
二十二烷醇 0.32
PPG-30 0.25
Steareth-2 0.25
相C
氧化聚乙烯粒1 1.00
香料 0.27
相D
可可酰胺丙基甜菜碱 2.00
月桂基硫酸钠 1.00
1购自Allied Signal Corp.的AcucscrubTM51
在一适当容器中,将相A组分搅拌加热至约75℃,在另一容器中,将相B组分搅拌加热至约75℃,然后在搅拌下将相B加入至相A。然后在搅拌下缓慢加入氧化聚乙烯粒以防止聚结。然后在搅拌下加入香料。然后冷却混合物至35℃。在另一容器中,混合相D成分,在搅拌下加入至其余混合物中(通常,这些成分可以水溶液形式获得并这样混合)。
所得的清洁组合物用于清洁皮肤。
另外,制备一组合物,其中用月桂酰羟乙磺酸钠代替月桂基硫酸钠。
实施例3
通过用常规混合设备将以下成分结合来制备个人清洁剂组合物。
成分
重量百分比
相A
水 适量至100
甘油 3.00
EDTA二钠 0.10
对羟苯甲酸甲酯 0.15
相B
PPG-15硬脂醚 4.00
硬脂醇 2.88
二硬脂基二甲基氯化铵 1.50
鲸蜡醇 0.80
Steareth-21 0.50
二十二烷醇 0.32
PPG-30 0.25
Steareth-2 0.25
对羟基苯甲酸丙酯 0.10
相C
香料 0.27
薄荷醇 0.05
相D
鲸蜡基二甲基甜菜碱 2.00
月桂基硫酸钠 1.00
在一适当容器中,将相A组分搅拌加热至约75℃,在另一容器中,将相B组分搅拌加热至约75℃,然后在搅拌下将相B加入至相A。然后在搅拌下加入香料和薄荷醇,然后冷却混合物至35℃。在另一容器中,混合相D成分,在搅拌下加入至其余混合物中(通常,这些成分可以水溶液形式获得并这样混合)。
所得的清洁组合物用于清洁皮肤。
另外,去掉薄荷醇并相应增加水含量来制备一种组合物。
另外,制备一种组合物,其中用月桂酰羟乙磺酸钠代替月桂基硫酸钠。
实施例4
通过用常规混合设备将以下成分结合来制备留存型乳膏组合物。
成分
重量百分比
相A
水 适量至100
甘油 5.00
EDTA二钠 0.10
对羟苯甲酸甲酯 0.20
相B
PPG-15硬脂醚 4.00
硬脂醇 1.44
二硬脂基二甲基氯化铵 0.50
鲸蜡醇 0.40
Steareth-21 0.50
二十二烷醇 0.16
Steareth-2 0.15
对羟基苯甲酸丙酯 0.10
相C
香料 0.12
相D
鲸蜡基二甲基甜菜碱 1.00
月桂基硫酸钠 0.50
在一适当容器中,将相A组分搅拌加热至约75℃,在另一容器中,将相B组分搅拌加热至约75℃,然后在搅拌下将相B加入至相A。然后在搅拌下加入香料,然后冷却混合物至35℃。在另一容器中,混合相D成分,在搅拌下加入至其余混合物中(通常,这些成分可以水溶液形式获得并这样混合)。
所得的留存乳膏用于调理皮肤和产生柔软光滑的皮肤感受。
另外,制备一组合物,其中用月桂酰羟乙磺酸钠代替月桂基硫酸钠。
实施例5
通过用常规混合设备将以下成分结合来制备个人清洁用凝胶组合物。
成分
重量百分比
相A
水 适量至100
甘油 4.00
EDTA二钠 0.10
PVM/MA癸二烯交联聚合物 1.00
氢氧化钠 0.14
对羟苯甲酸甲酯 0.20
二硬脂基二甲基氯化铵 0.50
相B
鲸蜡二甲基甜菜碱 0.75
月桂基硫酸钠 0.50
在一适当容器中,将相A组分剧烈搅拌。在另一容器中,混合相B成分,在搅拌下加入至其余混合物中。
所得的清洁用凝胶组合物用于有效清洁皮肤,它对皮肤温和。
另外,制备一组合物,其中用可可酰氨丙基甜菜碱代替鲸蜡基二甲基甜菜碱。
实施例6
通过用常规混合设备将以下成分结合来制备含水杨酸的留存液组合物。
成分
重量百分比
相A
水 适量至100
甘油 3.00
EDTA 四钠 0.02
相B
PPG-15硬脂醚 4.00
硬脂醇 0.75
水杨酸 2.00
鲸蜡醇 0.75
Steareth-21 0.45
Steareth-2 0.05
二硬脂基二甲基氯化铵 0.75
聚季铵盐-37和矿物油和PPG-
1Trideceth-6 0.75
相C
三乙醇胺 0.15
相D
香料 0.10
相E
鲸蜡基二甲基甜菜碱 2.00
月桂基硫酸钠 1.00
在一适当容器中,将相A组分搅拌加热至约75℃,在另一容器中,将相B组分搅拌加热至约75℃,然后在搅拌下将相B加入至相A。然后在搅拌下加入相C。在搅拌下加入香料。然后冷却混合物至35℃。在另一容器中,混合相E成分,在搅拌下加入至其余混合物中。
所得的留存组合物用于防止和治疗痤疮,它对皮肤温和并产生柔软光滑的皮肤感觉。
另外,制备一组合物,其中用月桂酰羟乙磺酸钠代替月桂基硫酸钠。
实施例7
通过用常规混合设备将以下成分结合来制备含水杨酸和薄荷醇的个人清洗剂。
成分
重量百分比
相A
水 适量至100
甘油 3.00
EDTA二钠 0.01
相B
PPG-15硬脂醚 4.00
硬脂醇 2.88
水杨酸 2.00
二硬脂基二甲基氯化铵 1.50
鲸蜡醇 0.80
Steareth-21 0.50
二十二烷醇 0.32
PPG-30 0.25
Steareth-2 0.25
相C
氧化聚乙烯粒1 1.00
香料 0.27
薄荷醇 0.05
相D
鲸蜡基二甲基甜菜碱 2.00
月桂基硫酸钠 1.00
1购自Allied Signal Corp.的AcucscrubTM51
在一适当容器中,将相A组分搅拌加热至约75℃,在另一容器中,将相B组分搅拌加热至约75℃,然后在搅拌下将相B加入至相A。然后在搅拌下缓慢加入聚乙烯粒以防止聚结。然后在搅拌下加入香料和薄荷醇。然后冷却混合物至35℃。在另一容器中,混合相D成分,在搅拌下加入至其余混合中(通常,这些成可以以水溶液形式获得并这样混合)。
所得的清洁用组合物用于清洁皮肤。
另外,制备含过氧化苯甲酰的组合物,其中用2.5%的过氧化苯甲酰代替水杨酸,并相应调节水含量。
另外,去掉薄荷醇并相应增加水含量来制备一种组合物。
另外,制备一组合物,其中用月桂酰羟乙磺酸钠代替月桂基硫酸钠。
Claims (18)
1.一种局部个人护理用组合物,包含:
(a)0.1%至20%重的下式两性表面活性剂:
其中R1为未取代的、饱和或未饱和的、直链或支化的C9至C22的烷基;m为1至3的整数;n为0或1;R2和R3分别选自C1至C3烷基和C1至C3的单羟基烷基;R4选自饱和或未饱和的C1至C5的烷基和饱和或未饱和的C1至C5的单羟基烷基;X选自CO2、SO3和SO4;及上述化合物的药物上可接受的盐;
(b)0.1%至20%重的阴离子表面活性剂,
(c)0.1%至15%重的下式的阳离子表面活性剂,
其中R1为C12到C22烷基,R2为C12到C22烷基,R3和R4各选自H或C1到C3烷基,X为阴离子,选自:氯离子、溴离子、碘离子、乙酸根、磷酸根、硝酸根、硫酸根、甲基硫酸根、乙基硫酸根、甲苯磺酸根、乳酸根、柠檬酸根、乙醇酸根及其混合物。
(d)0.001%至20%的活性成分,其选自:水杨酸、过氧化苯甲酰、顺-视黄酸、反-视黄酸、视黄醇、肌醇六磷酸、N-乙酰基-L-半胱氨酸、硫辛酸、壬二酸、间苯二酚、乙醇酸、乳酸、异丁苯丙酸、甲氧萘丙酸、氢化可的松、苯氧基乙醇、苯氧基丙醇、苯氧基异丙醇、2,4,4’-三氯-2’-羟基二苯醚、3,4,4’-三氯对称二苯脲、对甲氧基肉桂酸2-(乙基己)酯、羟苯甲酮、2-苯基苯并咪唑-5-磺酸、二羟基丙酮和它们的混合物。
(e)0.1%至99.7%重的水。
2.根据权利要求1的组合物,其中(a)中所述两性表面活性剂中,R2和R3选自CH3、CH2CH2OH和CH2CH2CH2OH;X选自CO2和SO3;m为2或3。
3.根据权利要求2的组合物,其中R2和R3选自CH3、CH2CH2OH和CH2CH2CH2OH;X选自CO2和SO3;m为2或3。
4.根据权利要求3的组合物,当X为CO2时,R4具有1至3个碳原子,当X为SO3时,R4具有2至4个碳原子。
5.根据权利要求4的组合物,其中R1具有11至18个碳原子;R2和R3为CH3;当X为CO2时,R4具有1个碳原子,当X为SO3时,R4具有3个碳原子。
6.根据权利要求5的组合物,其中R4具有1个碳原子,X为CO2,m为3,n为1。
7.根据权利要求5的组合物,其中R4具有3个碳原子,X为SO3,m为3和n为1。
8.根据权利要求1的组合物,其中所述两性表面活性剂选自鲸蜡基二甲基甜菜碱、可可酰胺丙基甜菜碱、可可酰胺丙基羟基磺内酰胺、硬脂基二甲基甜菜碱及其混合物。
9.根据权利要求1的组合物,其中两性表面活性剂是鲸蜡基二甲基甜菜碱。
10.根据权利要求1的组合物,其中所述阴离子表面活性剂选自:月桂基硫酸钠、鲸蜡基硫酸钠、可可酰基羟乙磺酸胺、月桂酰基羟乙磺酸钠、月桂酰基肌氨酸钠及其混合物。
11.根据权利要求10的组合物,其中所述阴离子表面活性剂为月桂基硫酸钠。
12.根据权利要求10的组合物,其中所述阳离子选自:二月桂基二甲基氯化铵、二硬脂基二甲基氯化铵、二肉豆蔻基二甲基氯化铵、二棕榈基二甲基氯化铵及其混合物。
13.根据权利要求1的组合物,其中所述组合物还包括0.1%至20%的保湿剂。
14.根据权利要求13的组合物,其中所述保温剂为甘油。
15.一种处理皮肤的方法,包括向皮肤施用0.5mg/cm2至25mg/cm2的权利要求1的组合物。
16.一种清洁皮肤的方法,它包括以下步骤:
(i)向皮肤施用0.5mg/cm2至25mg/cm2的权利要求1的组合物,和
(ii)从皮肤上漂洗去权利要求1的组合物。
17.一种清洁皮肤的方法,它包括以下步骤:
(i)向皮肤施用0.5mg/cm2至25mg/cm2的权利要求1的组合物,和
(ii)从皮肤上擦去权利要求1的组合物。
18.一种制备权利要求1的组合物的方法,包括以下步骤:
(i)将所述两性表面活性剂水溶液和所述阴离子表面活性剂水溶液结合形成所述两性的和阴离子的表面活性剂复合物的水分散体;和
(ii)将所述复合物的水分散体与所述阳离子表面活性剂的水溶液结合。
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US08/505,988 | 1995-07-24 | ||
US08/505,988 US5607980A (en) | 1995-07-24 | 1995-07-24 | Topical compositions having improved skin feel |
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CN1161100C true CN1161100C (zh) | 2004-08-11 |
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CNB961968753A Expired - Lifetime CN1161100C (zh) | 1995-07-24 | 1996-07-17 | 具有改进的皮肤感受的局部用组合物 |
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EP (1) | EP0841898B1 (zh) |
JP (1) | JPH11509552A (zh) |
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- 1996-07-17 PT PT96926729T patent/PT841898E/pt unknown
- 1996-07-17 AU AU66769/96A patent/AU706358B2/en not_active Expired
- 1996-07-17 CN CNB961968753A patent/CN1161100C/zh not_active Expired - Lifetime
- 1996-07-17 KR KR1019980700552A patent/KR19990035891A/ko not_active Ceased
- 1996-07-17 CA CA002227967A patent/CA2227967C/en not_active Expired - Lifetime
- 1996-07-17 AT AT96926729T patent/ATE212218T1/de not_active IP Right Cessation
- 1996-07-17 CZ CZ1998170A patent/CZ292677B6/cs not_active IP Right Cessation
Also Published As
Publication number | Publication date |
---|---|
EP0841898B1 (en) | 2002-01-23 |
WO1997003647A1 (en) | 1997-02-06 |
CZ17098A3 (cs) | 1998-06-17 |
DK0841898T3 (da) | 2002-03-25 |
DE69618787D1 (de) | 2002-03-14 |
PT841898E (pt) | 2002-06-28 |
DE69618787T2 (de) | 2002-10-10 |
CA2227967C (en) | 2002-06-04 |
KR19990035891A (ko) | 1999-05-25 |
CZ292677B6 (cs) | 2003-11-12 |
MX9800745A (es) | 1998-04-30 |
EP0841898A1 (en) | 1998-05-20 |
AU6676996A (en) | 1997-02-18 |
JPH11509552A (ja) | 1999-08-24 |
ATE212218T1 (de) | 2002-02-15 |
ES2171698T3 (es) | 2002-09-16 |
US5607980A (en) | 1997-03-04 |
AU706358B2 (en) | 1999-06-17 |
CN1200030A (zh) | 1998-11-25 |
CA2227967A1 (en) | 1997-02-06 |
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