MXPA96004033A - Low ph, hydrolically stable cosmetic compositions containing aci assets - Google Patents
Low ph, hydrolically stable cosmetic compositions containing aci assetsInfo
- Publication number
- MXPA96004033A MXPA96004033A MXPA96004033A MX PA96004033 A MXPA96004033 A MX PA96004033A MX PA96004033 A MXPA96004033 A MX PA96004033A
- Authority
- MX
- Mexico
- Prior art keywords
- mixtures
- group
- composition according
- further characterized
- acid
- Prior art date
Links
- 239000000203 mixture Substances 0.000 title claims abstract description 208
- 239000002537 cosmetic Substances 0.000 title claims abstract description 10
- RTZKZFJDLAIYFH-UHFFFAOYSA-N diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims abstract description 72
- 239000002253 acid Substances 0.000 claims abstract description 46
- -1 hydroxyl fatty acids Chemical class 0.000 claims abstract description 43
- 210000003491 Skin Anatomy 0.000 claims abstract description 42
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 33
- 150000001298 alcohols Chemical class 0.000 claims abstract description 31
- 239000004480 active ingredient Substances 0.000 claims abstract description 28
- 239000002736 nonionic surfactant Substances 0.000 claims abstract description 25
- 239000003795 chemical substances by application Substances 0.000 claims abstract description 21
- 239000004094 surface-active agent Substances 0.000 claims abstract description 18
- 235000014113 dietary fatty acids Nutrition 0.000 claims abstract description 14
- 239000000194 fatty acid Substances 0.000 claims abstract description 14
- 150000002191 fatty alcohols Chemical class 0.000 claims abstract description 13
- IAYPIBMASNFSPL-UHFFFAOYSA-N oxane Chemical compound C1CO1 IAYPIBMASNFSPL-UHFFFAOYSA-N 0.000 claims abstract description 13
- 150000002009 diols Chemical class 0.000 claims abstract description 12
- 230000002209 hydrophobic Effects 0.000 claims abstract description 12
- 125000002091 cationic group Chemical group 0.000 claims abstract description 9
- 238000002844 melting Methods 0.000 claims abstract description 7
- 230000037335 skin penetration Effects 0.000 claims abstract description 3
- YGSDEFSMJLZEOE-UHFFFAOYSA-N Salicylic acid Chemical compound OC(=O)C1=CC=CC=C1O YGSDEFSMJLZEOE-UHFFFAOYSA-N 0.000 claims description 53
- VEXZGXHMUGYJMC-UHFFFAOYSA-M chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 claims description 32
- DNIAPMSPPWPWGF-UHFFFAOYSA-N propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 claims description 30
- DUFKCOQISQKSAV-UHFFFAOYSA-N 2-(2-hydroxypropoxy)propan-1-ol Chemical compound CC(O)COC(C)CO DUFKCOQISQKSAV-UHFFFAOYSA-N 0.000 claims description 25
- 229960004889 salicylic acid Drugs 0.000 claims description 25
- 125000004432 carbon atoms Chemical group C* 0.000 claims description 24
- 125000000217 alkyl group Chemical group 0.000 claims description 21
- 230000002378 acidificating Effects 0.000 claims description 20
- ICIDSZQHPUZUHC-UHFFFAOYSA-N 2-octadecoxyethanol Chemical compound CCCCCCCCCCCCCCCCCCOCCO ICIDSZQHPUZUHC-UHFFFAOYSA-N 0.000 claims description 16
- DURPTKYDGMDSBL-UHFFFAOYSA-N 1-butoxybutane Chemical compound CCCCOCCCC DURPTKYDGMDSBL-UHFFFAOYSA-N 0.000 claims description 13
- WERYXYBDKMZEQL-UHFFFAOYSA-N 1,4-Butanediol Chemical compound OCCCCO WERYXYBDKMZEQL-UHFFFAOYSA-N 0.000 claims description 12
- QGZKDVFQNNGYKY-UHFFFAOYSA-O ammonium Chemical compound [NH4+] QGZKDVFQNNGYKY-UHFFFAOYSA-O 0.000 claims description 12
- GLDOVTGHNKAZLK-UHFFFAOYSA-N Stearyl alcohol Chemical compound CCCCCCCCCCCCCCCCCCO GLDOVTGHNKAZLK-UHFFFAOYSA-N 0.000 claims description 10
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 10
- QIQXTHQIDYTFRH-UHFFFAOYSA-M stearate Chemical compound CCCCCCCCCCCCCCCCCC([O-])=O QIQXTHQIDYTFRH-UHFFFAOYSA-M 0.000 claims description 10
- BXWNKGSJHAJOGX-UHFFFAOYSA-N Cetyl alcohol Chemical compound CCCCCCCCCCCCCCCCO BXWNKGSJHAJOGX-UHFFFAOYSA-N 0.000 claims description 9
- 239000002202 Polyethylene glycol Substances 0.000 claims description 9
- 229940098760 STEARETH-2 Drugs 0.000 claims description 9
- 239000003093 cationic surfactant Substances 0.000 claims description 9
- 229960000541 cetyl alcohol Drugs 0.000 claims description 9
- 229920001223 polyethylene glycol Polymers 0.000 claims description 9
- 229920005862 polyol Polymers 0.000 claims description 9
- 125000003118 aryl group Chemical group 0.000 claims description 8
- 150000004665 fatty acids Chemical class 0.000 claims description 8
- 239000001257 hydrogen Substances 0.000 claims description 8
- 229910052739 hydrogen Inorganic materials 0.000 claims description 8
- 125000004435 hydrogen atoms Chemical group [H]* 0.000 claims description 8
- 229940100458 STEARETH-21 Drugs 0.000 claims description 7
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 7
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 7
- NLXLAEXVIDQMFP-UHFFFAOYSA-N Ammonium chloride Substances [NH4+].[Cl-] NLXLAEXVIDQMFP-UHFFFAOYSA-N 0.000 claims description 6
- BDJRBEYXGGNYIS-UHFFFAOYSA-N Azelaic acid Chemical compound OC(=O)CCCCCCCC(O)=O BDJRBEYXGGNYIS-UHFFFAOYSA-N 0.000 claims description 6
- 240000007170 Cocos nucifera Species 0.000 claims description 6
- 235000013162 Cocos nucifera Nutrition 0.000 claims description 6
- 229920005628 alkoxylated polyol Polymers 0.000 claims description 6
- 150000002170 ethers Chemical class 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
- 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
- BTSZTGGZJQFALU-UHFFFAOYSA-N Piroctone olamine Chemical compound NCCO.CC(C)(C)CC(C)CC1=CC(C)=CC(=O)N1O BTSZTGGZJQFALU-UHFFFAOYSA-N 0.000 claims description 5
- 235000019270 ammonium chloride Nutrition 0.000 claims description 5
- 229960001680 ibuprofen Drugs 0.000 claims description 5
- 229960002009 naproxen Drugs 0.000 claims description 5
- 229950001046 piroctone Drugs 0.000 claims description 5
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 5
- VRBLNWVVFVBNRK-UHFFFAOYSA-N 1,6-diphenylhexane-1,6-dione Chemical compound C=1C=CC=CC=1C(=O)CCCCC(=O)C1=CC=CC=C1 VRBLNWVVFVBNRK-UHFFFAOYSA-N 0.000 claims description 4
- CUVLMZNMSPJDON-UHFFFAOYSA-N 1-(1-butoxypropan-2-yloxy)propan-2-ol Chemical compound CCCCOCC(C)OCC(C)O CUVLMZNMSPJDON-UHFFFAOYSA-N 0.000 claims description 4
- HBXWUCXDUUJDRB-UHFFFAOYSA-N 1-octadecoxyoctadecane Chemical compound CCCCCCCCCCCCCCCCCCOCCCCCCCCCCCCCCCCCC HBXWUCXDUUJDRB-UHFFFAOYSA-N 0.000 claims description 4
- QDHHCQZDFGDHMP-UHFFFAOYSA-N monochloramine Chemical compound ClN QDHHCQZDFGDHMP-UHFFFAOYSA-N 0.000 claims description 4
- JYGXADMDTFJGBT-VWUMJDOOSA-N Cortisol 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 3
- SHGAZHPCJJPHSC-NUEINMDLSA-N Isotretinoin Chemical compound OC(=O)C=C(C)/C=C/C=C(C)C=CC1=C(C)CCCC1(C)C SHGAZHPCJJPHSC-NUEINMDLSA-N 0.000 claims description 3
- SHGAZHPCJJPHSC-NWVFGJFESA-N Tretinoin Chemical compound OC(=O)/C=C(\C)/C=C/C=C(C)C=CC1=C(C)CCCC1(C)C SHGAZHPCJJPHSC-NWVFGJFESA-N 0.000 claims description 3
- 229960001727 Tretinoin Drugs 0.000 claims description 3
- 125000004429 atoms Chemical group 0.000 claims description 3
- 229960000890 hydrocortisone Drugs 0.000 claims description 3
- WSEBKJRVPMLGFV-UHFFFAOYSA-M (3-chloro-2-hydroxypropyl)-(2-hydroxyethyl)-dimethylazanium;chloride Chemical compound [Cl-].OCC[N+](C)(C)CC(O)CCl WSEBKJRVPMLGFV-UHFFFAOYSA-M 0.000 claims description 2
- 206010040880 Skin irritation Diseases 0.000 claims description 2
- 229960001138 acetylsalicylic acid Drugs 0.000 claims description 2
- 150000001450 anions Chemical class 0.000 claims description 2
- BSYNRYMUTXBXSQ-UHFFFAOYSA-N aspirin Chemical compound CC(=O)OC1=CC=CC=C1C(O)=O BSYNRYMUTXBXSQ-UHFFFAOYSA-N 0.000 claims description 2
- 229960002255 azelaic acid Drugs 0.000 claims description 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 2
- 229910052799 carbon Inorganic materials 0.000 claims description 2
- LYCAIKOWRPUZTN-UHFFFAOYSA-N glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 claims description 2
- 150000003872 salicylic acid derivatives Chemical class 0.000 claims description 2
- 230000036556 skin irritation Effects 0.000 claims description 2
- 231100000475 skin irritation Toxicity 0.000 claims description 2
- XXMIOPMDWAUFGU-UHFFFAOYSA-N 1,6-Hexanediol Chemical compound OCCCCCCO XXMIOPMDWAUFGU-UHFFFAOYSA-N 0.000 claims 1
- 101700015466 Cat-1 Proteins 0.000 claims 1
- 239000005977 Ethylene Substances 0.000 claims 1
- PCSMJKASWLYICJ-UHFFFAOYSA-N Succinaldehyde Chemical compound O=CCCC=O PCSMJKASWLYICJ-UHFFFAOYSA-N 0.000 claims 1
- 239000000956 alloy Substances 0.000 claims 1
- 229910045601 alloy Inorganic materials 0.000 claims 1
- REDXJYDRNCIFBQ-UHFFFAOYSA-N aluminium(3+) Chemical class [Al+3] REDXJYDRNCIFBQ-UHFFFAOYSA-N 0.000 claims 1
- 101700021616 catA1 Proteins 0.000 claims 1
- GUTLYIVDDKVIGB-UHFFFAOYSA-N cobalt Chemical compound [Co] GUTLYIVDDKVIGB-UHFFFAOYSA-N 0.000 claims 1
- 229910052803 cobalt Inorganic materials 0.000 claims 1
- 239000010941 cobalt Substances 0.000 claims 1
- VGGSQFUCUMXWEO-UHFFFAOYSA-N ethene Chemical group C=C VGGSQFUCUMXWEO-UHFFFAOYSA-N 0.000 claims 1
- 239000002563 ionic surfactant Substances 0.000 claims 1
- 150000004671 saturated fatty acids Chemical class 0.000 claims 1
- 235000003441 saturated fatty acids Nutrition 0.000 claims 1
- 230000002500 effect on skin Effects 0.000 abstract description 5
- 125000001931 aliphatic group Chemical group 0.000 abstract 1
- 125000000129 anionic group Chemical group 0.000 abstract 1
- 235000019441 ethanol Nutrition 0.000 description 31
- 239000000839 emulsion Substances 0.000 description 24
- 239000012071 phase Substances 0.000 description 23
- 210000004027 cells Anatomy 0.000 description 18
- 239000004615 ingredient Substances 0.000 description 17
- 229920001451 Polypropylene glycol Polymers 0.000 description 16
- 239000003921 oil Substances 0.000 description 14
- 150000001875 compounds Chemical class 0.000 description 13
- PEDCQBHIVMGVHV-UHFFFAOYSA-N glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 13
- 239000000463 material Substances 0.000 description 13
- 235000013772 propylene glycol Nutrition 0.000 description 13
- CPELXLSAUQHCOX-UHFFFAOYSA-M bromide Chemical compound [Br-] CPELXLSAUQHCOX-UHFFFAOYSA-M 0.000 description 11
- QAOWNCQODCNURD-UHFFFAOYSA-L sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 description 10
- XSQUKJJJFZCRTK-UHFFFAOYSA-N urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 description 10
- 210000000434 stratum corneum Anatomy 0.000 description 9
- 210000002615 Epidermis Anatomy 0.000 description 8
- VEXZGXHMUGYJMC-UHFFFAOYSA-N HCl Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 8
- 239000003995 emulsifying agent Substances 0.000 description 8
- 239000003906 humectant Substances 0.000 description 8
- 239000010410 layer Substances 0.000 description 8
- 150000003077 polyols Chemical group 0.000 description 8
- 235000011187 glycerol Nutrition 0.000 description 7
- 229960005150 glycerol Drugs 0.000 description 7
- 229940114926 stearate Drugs 0.000 description 7
- 239000003760 tallow Substances 0.000 description 7
- 229960005323 Phenoxyethanol Drugs 0.000 description 5
- QCDWFXQBSFUVSP-UHFFFAOYSA-N Phenoxyethanol Chemical compound OCCOC1=CC=CC=C1 QCDWFXQBSFUVSP-UHFFFAOYSA-N 0.000 description 5
- 239000000654 additive Substances 0.000 description 5
- 230000000996 additive Effects 0.000 description 5
- 230000015572 biosynthetic process Effects 0.000 description 5
- 239000004202 carbamide Substances 0.000 description 5
- 239000003974 emollient agent Substances 0.000 description 5
- 238000005755 formation reaction Methods 0.000 description 5
- 239000004973 liquid crystal related substance Substances 0.000 description 5
- 238000000034 method Methods 0.000 description 5
- 239000000126 substance Substances 0.000 description 5
- 230000000475 sunscreen Effects 0.000 description 5
- 239000000516 sunscreening agent Substances 0.000 description 5
- 238000009834 vaporization Methods 0.000 description 5
- SVTBMSDMJJWYQN-UHFFFAOYSA-N 2-Methyl-2,4-pentanediol Chemical compound CC(O)CC(C)(C)O SVTBMSDMJJWYQN-UHFFFAOYSA-N 0.000 description 4
- RXKJFZQQPQGTFL-UHFFFAOYSA-N Dihydroxyacetone Chemical compound OCC(=O)CO RXKJFZQQPQGTFL-UHFFFAOYSA-N 0.000 description 4
- 229940120503 Dihydroxyacetone Drugs 0.000 description 4
- 229940015001 Glycerin Drugs 0.000 description 4
- 102000011782 Keratins Human genes 0.000 description 4
- 108010076876 Keratins Proteins 0.000 description 4
- 206010039509 Scab Diseases 0.000 description 4
- 150000007513 acids Chemical class 0.000 description 4
- 230000000845 anti-microbial Effects 0.000 description 4
- 239000003599 detergent Substances 0.000 description 4
- 238000009472 formulation Methods 0.000 description 4
- AEMRFAOFKBGASW-UHFFFAOYSA-N glycolic acid Chemical compound OCC(O)=O AEMRFAOFKBGASW-UHFFFAOYSA-N 0.000 description 4
- 229940051250 hexylene glycol Drugs 0.000 description 4
- 150000002500 ions Chemical class 0.000 description 4
- 239000007788 liquid Substances 0.000 description 4
- 150000003839 salts Chemical class 0.000 description 4
- 239000011780 sodium chloride Substances 0.000 description 4
- UCSJYZPVAKXKNQ-HZYVHMACSA-N 1-[(1S,2R,3R,4S,5R,6R)-3-carbamimidamido-6-{[(2R,3R,4R,5S)-3-{[(2S,3S,4S,5R,6S)-4,5-dihydroxy-6-(hydroxymethyl)-3-(methylamino)oxan-2-yl]oxy}-4-formyl-4-hydroxy-5-methyloxolan-2-yl]oxy}-2,4,5-trihydroxycyclohexyl]guanidine Chemical compound CN[C@H]1[C@H](O)[C@@H](O)[C@H](CO)O[C@H]1O[C@@H]1[C@](C=O)(O)[C@H](C)O[C@H]1O[C@@H]1[C@@H](NC(N)=N)[C@H](O)[C@@H](NC(N)=N)[C@H](O)[C@H]1O UCSJYZPVAKXKNQ-HZYVHMACSA-N 0.000 description 3
- 206010013786 Dry skin Diseases 0.000 description 3
- OMPJBNCRMGITSC-UHFFFAOYSA-N Incidol Chemical compound C=1C=CC=CC=1C(=O)OOC(=O)C1=CC=CC=C1 OMPJBNCRMGITSC-UHFFFAOYSA-N 0.000 description 3
- OFVLGDICTFRJMM-WESIUVDSSA-N Tetracycline Chemical compound C1=CC=C2[C@](O)(C)[C@H]3C[C@H]4[C@H](N(C)C)C(O)=C(C(N)=O)C(=O)[C@@]4(O)C(O)=C3C(=O)C2=C1O OFVLGDICTFRJMM-WESIUVDSSA-N 0.000 description 3
- 229960002180 Tetracycline Drugs 0.000 description 3
- 239000004098 Tetracycline Substances 0.000 description 3
- QTBSBXVTEAMEQO-UHFFFAOYSA-M acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 description 3
- XEKOWRVHYACXOJ-UHFFFAOYSA-N acetic acid ethyl ester Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 description 3
- 125000005210 alkyl ammonium group Chemical group 0.000 description 3
- 239000003814 drug Substances 0.000 description 3
- 229940079593 drugs Drugs 0.000 description 3
- 230000037336 dry skin Effects 0.000 description 3
- AEMRFAOFKBGASW-UHFFFAOYSA-M glycolate Chemical compound OCC([O-])=O AEMRFAOFKBGASW-UHFFFAOYSA-M 0.000 description 3
- ACCCMOQWYVYDOT-UHFFFAOYSA-N hexane-1,1-diol Chemical compound CCCCCC(O)O ACCCMOQWYVYDOT-UHFFFAOYSA-N 0.000 description 3
- 230000036571 hydration Effects 0.000 description 3
- 238000006703 hydration reaction Methods 0.000 description 3
- 238000002156 mixing Methods 0.000 description 3
- 239000007764 o/w emulsion Substances 0.000 description 3
- 230000035515 penetration Effects 0.000 description 3
- ISWSIDIOOBJBQZ-UHFFFAOYSA-N phenol Chemical compound OC1=CC=CC=C1 ISWSIDIOOBJBQZ-UHFFFAOYSA-N 0.000 description 3
- 229920000642 polymer Polymers 0.000 description 3
- GOOHAUXETOMSMM-UHFFFAOYSA-N propylene oxide Chemical compound CC1CO1 GOOHAUXETOMSMM-UHFFFAOYSA-N 0.000 description 3
- 108090000623 proteins and genes Proteins 0.000 description 3
- 102000004169 proteins and genes Human genes 0.000 description 3
- 150000003242 quaternary ammonium salts Chemical class 0.000 description 3
- 235000019364 tetracycline Nutrition 0.000 description 3
- 230000001225 therapeutic Effects 0.000 description 3
- GPLRAVKSCUXZTP-UHFFFAOYSA-N 3-(2,3-dihydroxypropoxy)propane-1,2-diol Chemical compound OCC(O)COCC(O)CO GPLRAVKSCUXZTP-UHFFFAOYSA-N 0.000 description 2
- YDCSFYSJEYSCBP-UHFFFAOYSA-N 3-hexadecoxypropan-1-ol Chemical compound CCCCCCCCCCCCCCCCOCCCO YDCSFYSJEYSCBP-UHFFFAOYSA-N 0.000 description 2
- POJWUDADGALRAB-PVQJCKRUSA-N Allantoin Natural products NC(=O)N[C@@H]1NC(=O)NC1=O POJWUDADGALRAB-PVQJCKRUSA-N 0.000 description 2
- 239000004342 Benzoyl peroxide Substances 0.000 description 2
- 229960003260 Chlorhexidine Drugs 0.000 description 2
- SNPLKNRPJHDVJA-ZETCQYMHSA-N D-panthenol Chemical compound OCC(C)(C)[C@@H](O)C(=O)NCCCO SNPLKNRPJHDVJA-ZETCQYMHSA-N 0.000 description 2
- 210000004207 Dermis Anatomy 0.000 description 2
- 239000003109 Disodium ethylene diamine tetraacetate Substances 0.000 description 2
- RRAFCDWBNXTKKO-UHFFFAOYSA-N Eugenol Chemical compound COC1=CC(CC=C)=CC=C1O RRAFCDWBNXTKKO-UHFFFAOYSA-N 0.000 description 2
- GHXZTYHSJHQHIJ-UHFFFAOYSA-N Exidine 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 2
- BEJNERDRQOWKJM-UHFFFAOYSA-N Kojic acid Chemical compound OCC1=CC(=O)C(O)=CO1 BEJNERDRQOWKJM-UHFFFAOYSA-N 0.000 description 2
- 229940101267 Panthenol Drugs 0.000 description 2
- 210000004927 Skin cells Anatomy 0.000 description 2
- 206010040844 Skin exfoliation Diseases 0.000 description 2
- 229920002472 Starch Polymers 0.000 description 2
- 125000000218 acetic acid group Chemical group C(C)(=O)* 0.000 description 2
- 230000001153 anti-wrinkle Effects 0.000 description 2
- 239000008346 aqueous phase Substances 0.000 description 2
- QIGBRXMKCJKVMJ-UHFFFAOYSA-N benzohydroquinone Chemical compound OC1=CC=C(O)C=C1 QIGBRXMKCJKVMJ-UHFFFAOYSA-N 0.000 description 2
- 235000019400 benzoyl peroxide Nutrition 0.000 description 2
- PUPZLCDOIYMWBV-UHFFFAOYSA-N butylene glycol Chemical compound CC(O)CCO PUPZLCDOIYMWBV-UHFFFAOYSA-N 0.000 description 2
- 239000011248 coating agent Substances 0.000 description 2
- 125000000118 dimethyl group Chemical group [H]C([H])([H])* 0.000 description 2
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 2
- 235000019301 disodium ethylene diamine tetraacetate Nutrition 0.000 description 2
- ZGTMUACCHSMWAC-UHFFFAOYSA-L disodium;2-[2-[carboxylatomethyl(carboxymethyl)amino]ethyl-(carboxymethyl)amino]acetate Chemical compound [Na+].[Na+].OC(=O)CN(CC([O-])=O)CCN(CC(O)=O)CC([O-])=O ZGTMUACCHSMWAC-UHFFFAOYSA-L 0.000 description 2
- 150000002148 esters Chemical class 0.000 description 2
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 description 2
- KIWBPDUYBMNFTB-UHFFFAOYSA-M ethyl sulfate Chemical compound CCOS([O-])(=O)=O KIWBPDUYBMNFTB-UHFFFAOYSA-M 0.000 description 2
- SFNALCNOMXIBKG-UHFFFAOYSA-N ethylene glycol monododecyl ether Chemical compound CCCCCCCCCCCCOCCO SFNALCNOMXIBKG-UHFFFAOYSA-N 0.000 description 2
- 238000010438 heat treatment Methods 0.000 description 2
- VLKZOEOYAKHREP-UHFFFAOYSA-N hexane Chemical compound CCCCCC VLKZOEOYAKHREP-UHFFFAOYSA-N 0.000 description 2
- 125000004356 hydroxy functional group Chemical group O* 0.000 description 2
- JVTAAEKCZFNVCJ-UHFFFAOYSA-M lactate Chemical compound CC(O)C([O-])=O JVTAAEKCZFNVCJ-UHFFFAOYSA-M 0.000 description 2
- 150000003893 lactate salts Chemical class 0.000 description 2
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 description 2
- 239000004310 lactic acid Substances 0.000 description 2
- 235000014655 lactic acid Nutrition 0.000 description 2
- 150000002632 lipids Chemical class 0.000 description 2
- 230000003020 moisturizing Effects 0.000 description 2
- NHNBFGGVMKEFGY-UHFFFAOYSA-N nitrate Chemical compound [O-][N+]([O-])=O NHNBFGGVMKEFGY-UHFFFAOYSA-N 0.000 description 2
- 235000020957 pantothenol Nutrition 0.000 description 2
- 239000011619 pantothenol Substances 0.000 description 2
- 230000037368 penetrate the skin Effects 0.000 description 2
- 229930002330 retinoic acid Natural products 0.000 description 2
- 150000003870 salicylic acids Chemical class 0.000 description 2
- 239000002904 solvent Substances 0.000 description 2
- 235000019698 starch Nutrition 0.000 description 2
- 230000003637 steroidlike Effects 0.000 description 2
- 235000000346 sugar Nutrition 0.000 description 2
- JOXIMZWYDAKGHI-UHFFFAOYSA-M toluene-4-sulfonate Chemical compound CC1=CC=C(S([O-])(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-M 0.000 description 2
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- ZWGTVKDEOPDFGW-UHFFFAOYSA-N hexadecylazanium;chloride Chemical compound [Cl-].CCCCCCCCCCCCCCCC[NH3+] ZWGTVKDEOPDFGW-UHFFFAOYSA-N 0.000 description 1
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- 239000011591 potassium Substances 0.000 description 1
- 229910052700 potassium Inorganic materials 0.000 description 1
- ANBFRLKBEIFNQU-UHFFFAOYSA-M potassium;octadecanoate Chemical compound [K+].CCCCCCCCCCCCCCCCCC([O-])=O ANBFRLKBEIFNQU-UHFFFAOYSA-M 0.000 description 1
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- XBDQKXXYIPTUBI-UHFFFAOYSA-N propionic acid Chemical class CCC(O)=O XBDQKXXYIPTUBI-UHFFFAOYSA-N 0.000 description 1
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- 150000003856 quaternary ammonium compounds Chemical class 0.000 description 1
- LISFMEBWQUVKPJ-UHFFFAOYSA-N quinolin-2(1H)-one Chemical compound C1=CC=C2NC(=O)C=CC2=C1 LISFMEBWQUVKPJ-UHFFFAOYSA-N 0.000 description 1
- 229920005989 resin Polymers 0.000 description 1
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- YGSDEFSMJLZEOE-UHFFFAOYSA-M salicylate Chemical compound OC1=CC=CC=C1C([O-])=O YGSDEFSMJLZEOE-UHFFFAOYSA-M 0.000 description 1
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- 125000005373 siloxane group Chemical group [SiH2](O*)* 0.000 description 1
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- 150000005621 tetraalkylammonium salts Chemical class 0.000 description 1
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- 235000010384 tocopherol Nutrition 0.000 description 1
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- 235000010493 xanthan gum Nutrition 0.000 description 1
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- GVJHHUAWPYXKBD-IEOSBIPESA-N α-tocopherol Chemical compound OC1=C(C)C(C)=C2O[C@@](CCC[C@H](C)CCC[C@H](C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-IEOSBIPESA-N 0.000 description 1
Abstract
The present invention relates to spreadable skin care compositions comprising: (A) from about 0.05% to about 20% of an active ingredient, preferably having a solubility parameter of from about 6 to about 12; ) from about 0.1% to about 25% alcohols; (C) from about 1% to about 20% of a stable, hydrophobic, stable aliphatic agent selected from the group consisting of saturated C16 to C30 fatty alcohols, fatty alcohols from saturated C16 to C30 containing from about 1 to about 5 moles of ethylene oxide, saturated C16 to C30 diols, saturated C16 to C30 mono-glycol ether, saturated C16 to C30 hydroxyl fatty acids, and mixtures thereof, having a melting point of at least about 45 ° C; (D) from about 0.05% to about 10% of a stable hydrophilic surfactant acid selected from the group consisting of age nte anionic, cationic, zwitterionic, nonionic surfactant and mixtures thereof, and (F) from about 25% to about 99.7% water, wherein the pH of the composition is about 3.5 or less; these cosmetic compositions provide improved physicochemical stability, while providing good skin deposition and good skin penetration of the active ingredients while also providing dermal irritation
Description
COSMETIC COMPOSITIONS OF PHOSPHONIC, HYDROLYTICAL, OESTABLE_S_ OUE CONTAIN ACTIVE ACIDS
TECHNICAL CAGE
The present invention relates to stable, low pH, hydrolytically stable skin care compositions containing acidic active ingredients such as salicylic acid. In particular, it relates to stable low pH cosmetic compositions having liquid crystalline phases, providing improved wetting and hydration as well as improved chemical and physical stability, while providing low dermal irritation.
BACKGROUND OF THE INVENTION
A wide variety of acidic active ingredients are currently known to treat various skin conditions. Unfortunately, it is more difficult to formulate these acidic assets in oil-in-water emulsions that are stable, due in part to their acidic nature and limited solubility characteristics. Representative of some of these active ingredients is saiicí lico acid. Cosmetic compositions containing salicylic acid are known in the art, and help to increase the replenishment of skin cells and ultimately provide a
skin that you see as young, fresher and healthier. Acrylic acid is a well-known keratolytic agent that is believed to help remove keratin plugs and aid in the skin exfoliation procedure described below. Salicylic acid is also known for its anti-acne, anti-aging effects on the skin, etc., described in C. Huber et al., 1992, Derrn Res. 257, p. 293-297, 1977 which is incorporated herein by reference. See also PCT patent application No. 9310756 of Blank, published June 10, 1993. The skin is composed of two layers: the epidermis (or cuticle) and the dermis. The epidermis is a thin outer layer composed of stratified epithelium. The outermost layer of the epidermis is the stratum corneum which is composed of quera + ina, flattened cells containing protein surrounded by thin layers of lipids. He believes that cells can attach to each other by connections of proteins (denosnosines) on cells. The cells in the deepest part of the epidermis, the basal layer, multiply and grow, pushing the older cells of the epidermis up and towards the surface. As these cells move upward they flatten. The epidermis is usually devoid of blood vessels and depends on vessels found in the dermis for nutrition. The cells that are more superficially of the epidermis, which are removed from the nutrient supply, gradually differentiate,
transforming its proteins into keratin. This keratin procedure results in the death of the cells. Keratin is a proteinaceous and soluble material and gives the corneal stratum a material of corneal material. Dead stratum corneum cells that are more outwardly are gradually detached and replaced by freshly implanted cells. Typically, approximately 30 days are required for a cell to migrate from the basal layer from the epidermis, crust and discard in the outer layers of the stratum cerneum. F? As the cell migrates outward from the basal layer, pfogresi varnente keratinizes until it becomes relatively impermeable. The result is the stratum corneum, an ex-finely thin surface layer (10 microns) with substantial barrier properties. The cell covers in the stratum corneum tend to be pristine polar lipids, such as cerainid, sterols and fatty acids, whereas the cytoplasm of the stratum corneum cells remains polar and aqueous. In normal skin, the stratum corneum crusts as individual cells or as small agglomerates of cells. Skin problems such as dry skin, etc., are keratization disorders in which the crust formation of the stratum corneum cell on the surface of the skin is altered in relation to normal, young and healthy skin. . This alteration results in large groupings of
cells that tend to visible scalding of the skin, an accumulation of kerati material on the surface of the skin or in follicles or ducts and / or a rough texture to the surface of the skin. These conditions can be improved by applying cosmetic compositions, that is, containing salicylic acid, which can aid in the removal of the more efficient keratomaceous material. Although attempts have been made to partially neutralize these acidic assets in order to improve the formulation capacity and reduce the potential for skin irritation, this approach appears to reduce the penetration of the active acidic ingredients into the skin. Therefore, effective cosmetic compositions are required which stabilize acidic actives such as salicylic acid, for removal of surface chases from the stratum corneum. Therefore, an object of the present invention is to provide oil-in-water, low pH emulsions. , novel, containing active acids, these compositions being physically active, while providing good deposition and good penetration into the skin of the active ingredient, while also providing low dermal irritation. Therefore, an object of the present invention is to provide novel compositions to increase skin moisturization and hydration for the removal of dry skin cells or scabs of the stratum corneum.
A further object of the present invention is to provide such compositions with low dermal irritation, especially in compositions that require low pH. A further object of the present invention is to provide such compositions with low dermal irritation, especially in compositions that require an active ingredient. A further object of the present invention is to provide said compositions having good stability of the acidic active components in cosmetically elegant form.
BRIEF DESCRIPTION OF THE INVENTION
The present invention relates to spreadable skin care compositions comprising: (A) from about 0.05% to about 20% of an acid active ingredient, preferably having a solubility parameter of from about 6 to about 12; (B) from about 0.1% to about 25% of alkoxylated alcohols, alkoxylated polyols and mixtures of the same, of the phónu1:
R 0
wherein R is selected from the group consisting of alcohols, polyols, diolee and mixtures thereof, which have a
chain length from about 2 to about 10 carbon atoms; n is an integer of about 3 to about 40; X is selected from the group consisting of hydrogen, methyl, ethyl, propyl and mixtures thereof; (C) from about 1% to about 20% of a hydrophobic, acid-stable structuring agent selected from the group consisting of saturated fatty alcohols from C30 to saturated C30 to saturated C30 to saturated fatty alcohols containing from about 5 moles of ethylen oxide, diols from Cie to saturated O30, rnonoglycerol ethers of saturated C30 to C30, saturated C30 to C30 hydroxy fatty acids, and mixtures thereof, having a melting point of at least approx 1rnadament e 5 ° C; (D) from about 0.05% to about 10% of a stable hydrophilic surfactant agent selected from the group consisting of ammonium, catonic, zwitterionic, nonionic surfactant and mixtures thereof; and (F) from about 25% to about 99.7% water, wherein the pH of the composition is about 3.5 or less, preferably about * 2.5 to about 3.5, preferably about * 2.8 to about 3.2. . In additional embodiments, the present invention relates to spreadable skin care compositions comprising:
(A) from about 0.1% to about 5% salicylic acid; (B) from about 0.1% to about 25% of alkoxylated alcohols, alkoxylated polyols, and mixtures thereof, of the fopnule:
R 0
wherein R is selected from the group consisting of alcohols, poiols, diols, and mixtures thereof, having a chain length of from about 2 to about 10 carbon atoms; n is an integer of about 3 to about 40; X is selected from the group consisting of hydrogen, methyl, ethyl, propyl and mixtures thereof; (0) «about 1% to about 20% of a sterically stable, acid-stable, acid-forming agent selected from the group consisting of fatty alcohols of Cié a (.30 saturated, fatty alcohols of Ci6 to C30 saturates containing from about 1 to about 5 moles of full oxide, diols from saturated C30 to C30, saturated rnonogl 1 ceroli from Cie to saturated C30, hydroxy fatty acids from Cie to saturated C30, and mixtures thereof, which have a minor melting point * of approximately 45 ° C; (D) from about 0.05% to about 10% of a hydrophilic surfactant stable to the acid selected from the group consisting of ammonium surfactant, ionic cation, zwiterio co, nonionic and mixtures of the same;
(F) from about * 25% to about 99.7% water, wherein the pH of the composition is about
3. 5 or less, preferably from about 2.5 to about 3.5, most preferably from about 2.8 to about 3.2. All percentages and ratios used are by weight with respect to the total composition. All measurements made are at 5 ° C, unless otherwise indicated. The present invention may comprise, consists of or consists essentially of the essential ingredients and components as well as optionals described herein.
DETAILED DESCRIPTION OF THE INVENTION
The cosmetic compositions of the present invention are useful for moisturizing and moisturizing the skin and for the position of acidic active ingredients on the skin. These compositions are in the form of oil-water emulsions by which the oil phase and the water phase must contain, in addition to the essential components described herein, a variety of ingredients known in the art. The acidic active ingredients are preferably deposited on the skin in the oil phase of the oil-in-water emulsion. The active ingredients cited for use herein will preferably have a solubility parameter of from about 6 to about 12.
In particular, the present invention relates to spreadable skin care compositions which are oil-in-water emulsions, comprising: (0) from about 0.05% to about 20% of an acid active ingredient, preferably having a parameter of solubility from about 6 to about 12; (B) from about 0.1% to about 25% of alkoxylated alcohols, alkoxy side polyols and mixtures of the nos, from 1 to for 1:
R 0
wherein R is selected from the group consisting of alcohols, polyols, daols and mixtures thereof, which have a
Chain length from about 2 to about 10 carbon atoms; n is an integer around * 3 to about 40; X is selected from the group consisting of
Hydrogen, methyl, ethyl, propyl and mixtures thereof; (Or from about 1% to about 20% of a hydrophobic, stable, structuring agent selected from the group consisting of fatty alcohols from saturated C 0 to O 30, saturated C 30 C 1 fatty alcohols containing from about 1 to about 5 moles of ethylene oxide, gave saturated C30 to C30, nonoglycerol ethers of saturated C1 to C30, hydroxy fatty acids from C1 to C30 saturated, and mixtures of the same, which have a lower melting point than 45 ° C;
(D) from about 0.05% to approximately 10% of a stable hydrophilic surfactant to the acid selected from the group consisting of ammonium, cationic, zwitterionic, nonionic surfactant and mixtures thereof; and (F) from about 25% to approximately 99.7% water, wherein the pH of the composition is about 3.5 or less, preferably from about 2.5 to about 3.5, most preferably from about 2.8 to about 3.2. Preferably, the ratio of component (C) to component (D) is from about 20: 1 to about 1: 1, preferably from about 10: 1 to about 1: 1, most preferably from about * 5: 1 to about 1: 1, and most preferably still about 3: 1. These relationships allow the formation of laminate liquid crystalline phases, which contribute to the physical and chemical stability of the compositions at temperatures of about ~ 10 ° to about 50 ° C at a pH of about 3.5 to less. The compositions of the present invention have complex rheological characteristics. These compositions have characteristics of physical properties of oil-in-water emulsions, liquid crystals, as well as crystal gel networks. the nature of liquid crystals, the formation of liquid crystals, the properties and advantages of liquid crystals are also described in G. Dahrns, Properties of O / U
Emulsions with Amsotropic Lamellar Phases, 101 Cosrnetics 8. loiletries 113-115, (1986); P. Loll, Liquid Crystals in Cosmetics Emulsions, IC? urfactants' Publication RP94-93E; and G.M. Eccleston, Muí tiple-Phase Oil-Tn-Uater Emulsion, 41 3. Soc Cosrnet. Chem. 1-22, (January / February 1990); all of which are incorporated herein by reference in their entirety. The oil-in-water emulsions of the present have desirable aesthetic and elegant properties, such as a rich and creamy, more non-greasy skin feel. These emulsions can cover a wide range of consistencies from thin lotions to thick creams. These emulsions typically have viscosities ranging from about 100 cps to about 500,000 cps, preferably from about 3,000 to about 200,000, most preferably from about 5,000 cps to about 150,000 cps, and still about 5,000 cps. at approximately 100,000 cps as measured at a temperature of 25 ° C with a viscosity mirror of Broo f leld ynchro-Lectpc, Model D. The oil-in-water emulsion compositions herein have a low pH. The compositions of the present invention have a pH value of about 3.5 or less, preferably from about 2.5 to about 3.5, preferably from about 2.8 to about 3.2. The preferred pH value depends on the active component or particular assets employed. in the composition of the present invention. For example, for acid assets of the
present invention, the pH of the composition should be carefully chosen so that it is at or below the pKa of the active ingredient. By normal definitions, the pKa value for a compound is that pKa value in which the material is 50% dissociated ionized to produce a conjugated base and a proton (or proton hydrate). Without being limited by theory, when the phl of the formulation is below the pKa of the asset, it is believed that the active will exist primarily in its non-ionized form which must increase its subsequent deposition on the skin. For example, salicylic acid has a pKa reported from 2.97 to 19 ° C in aqueous solution, therefore, it will be useful to formulate salicylic acid comprising compositions at or below a pH of about 2.97 to suppress ionization and increase the Maximum deposition on the skin from the emulsion. See CRC Handbook »'of Chemistry and Physics, 57th edition, page D-150 (1976). a when pH regulators can be used to help maintain the pH of the emulsion compositions, these are not required components, but are simply optional ingredients.
(A) Active Ingredients
The compositions of the present invention comprise a safe and effective amount of an acidic active ingredient, and mixtures thereof, which are preferably soluble in the
oil phase of the composition of the present invention and which are deposited on the surface of the skin. The term "safe and effective amount" as used herein means an amount of active ingredient sufficiently high to modify the conditions to be treated or to provide the benefit of the desired skin, but low enough to avoid effects different sides, at a ratio of benefit to reasonable risk within the scope of solid medical judgment. What is a safe and effective amount of the active ingredient will vary with the specific active, the ability of the active to penetrate the skin, the age, the health condition and condition of the user's skin, and other similar factors. Typically, the active compounds of the present invention comprise from about 0.05% to about 20%, preferably from about 0.1% to about 10% and most preferably from about 1% to about 5% by weight of the composition. The active ingredients useful herein preferably have a solubility parameter of from about 6 to about 12, preferably from about 7 to about 12, and most preferably from about 9 to about 12. The solubility parameters are well known for The formulation chemistry of the ordinary technique is used routinely as a guide to determine the capacities and solubilities of materials in the formulation process. Without being limited to the theory,
believes that by choosing active ingredients with solubility parameters in the above-mentioned scales, the active compounds will tend to be hydrophobic, that is to say lipophilic, and therefore more soluble in the oil phase of the present oil-in-water emulsions. The lipophilic nature of the active ingredients should help to increase the deposition of active ingredients on the skin from an oil-in-water emulsion during the emulsion of water emulsion. Generally, the preferred actives useful herein with the solubility parameters outlined above will have a solubility in water at 25 ° C or less than about 1 g per about 100 g of water. The solubility parameter of a chemical compound, 6, is defined as the square root of the cohesive energy density for that compound. Typically, a par-solubility parameter for a compound is calculated from the ablated values of the additive group contributions for the heat-vaporization and molar volume of the components of that compound, using the following equation:
1/2 Li
S i mi S where i Ei - the sum of heat of contributions of the group S vaporization additive i rm - the sum of the contributions of the additive group of
molar volume The normal tabulations of additive group contributions for vaporization heat and volume for a wide variety of atoms and groups of atoms are collected in Barton, fl.F.M. Handbook or Solubility Pararneters, CRC Press, chapter 5, Table 3, pp. 64-66 (1985), which is incorporated herein by reference in its entirety. The above solubility parameter equation is described in Fedors, R.F., "Method for Estimation of Both the Solubility Parameters and Molar Volumes of Liquids," Polymer Engineering and Science. vol. 14, no. 2, pp. 147-154 (February 1974), which is incorporated herein by reference in its entirety. The calculated solubility parameters obey the Law of mixtures in such a way that the parameter of solubility calculated for a mixture of materials is given by the weighted average of the solubility parameters calculated for each component of that mixture. See Handbook of Chen stry and Phisics, 57th edition, CRC Press, p. C-726 (1976-1977), which is incorporated herein by reference in its entirety. Chemists who make formulations typically report and use parameters of solubility in units of (cal / cm3 / 1/2) Tabulated values of additive group contributions for vaporization in Handbook of Solubility
Pararne ers, repoi so in units of kj / ol. However, these heat-vaporization values are easily converted to cal / mol using the following good ratios.
known: 1 J / rnol - 0.239006 cal / rnol and 1000 3 = 1 kJ See Gordon, A.3. and others The Chernist's Compa ion,
John liley to Sons, pp. 56-463, (1972), which is incorporated herein by reference in its entirety. The solubility parameters have also been tabulated for a wide variety of chemical compounds. Tabulations of solubility parameters are found in
Handbook of Solubility For ether, supr. The assets useful herein can be categorized by their therapeutic benefit or their postulated mode of action. However, it is important to understand the assets that are useful in the present, in some cases they can provide more than one therapeutic benefit or operate through more than one action method. Therefore, ratings are hereby made for convenience purposes and are not intended to limit the asset to the particular application or particular applications listed. In the useful asset classes herein based on a therapeutic benefit or mode of action are described in the co-pending patent application of P &G Series No. 00 / 161,104, filed on December 2, 1993, Deckner et al., on pages 10-14, these pages are incorporated here by reference. In addition to the following acidic assets which preferably have the parameters of solubility outlined above are useful to the compositions of the present invention. R ive an iacné: Examples of useful ant acne assets
they include ceratoli, such as salicylic acid (o-hydroxybenzoic acid), salicylic acid derivatives such as 5-octane-1-olic acid, and resormyol; retinoids such as retinoic acid and its derivatives (e.g., cis and trans), antibiotics and anti-microbials such as benzoyl peroxide, octopirox, t-traciclma, 2, 4, 4 '-tr? chlor-2' -hydroxy ether diphenyl, 3,4,4'-tpclorobamlid, azelaic acid and its derivatives, phenoxyethanol, phenoxy propanol, phenoxy isopropanol, ethyl acetate, cindarnicm and rneclosicline; seboestates such as flavonoids; and bile salts such as cirnnol sulfate and its derivatives, deoxycholate and cholate. Anti-wrinkle and Anti-Atrophy Assets of the Skin: Examples of anti-wrinkle and skin anti-antria actives include retinoic acid, salicylic acid and skin-detaching agents (eg, phenol and the like), Inflammatory flnti Steroidal active (NSflIDS) :
Derivatives of propionic acid; acetic acid derivatives; phenaic acid derivatives; diphenylcarboxylic acid derivatives; and oxicams. All of those NSDAIDS are fully described in the U.S. Patent. 4,985,459 to Sunshme et al., Issued January 15, 1991, incorporated herein by reference. Examples of useful NSATDS include acetyl alicylic acid, abuprofen, naproxen, benoxaprofen, f Lurbiprofen, fencoprofen, fenbutene, ketoprofen, indoprofen, pirprofen, carprofen, oxaprozm, pranoprofen, rn? R * oprofen, thioxaprofen, suprofen, alminoprofen, tiaprofe co,
fluprofen and bucloxic acid. Also useful are steroidal anti-n-alpha drugs including hydrocortezone and the like. Topical Anesthetics: Examples of topical anesthetic drugs include benzocama, 1 idocaine, bupivacaine, chloroprocama, dibucaine, etidocaine, rnepivacam, tetracaine, diclomna, hexilcama, procaine, cocaine, cetar ina, pramoxma enoL, and pharmaceutically acceptable salts thereof. Tanning Accelerators: Examples of artificial tanning ingredients and tanning accelerators include dihydroxyacetone. Antimicrobial and Antimicrobial Assets: Examples of antimicrobial and anti-icotic agents include b-lactam drugs, quinolone drugs, ciprofloxacin, norfloxacin, tetracycline, entromromic, arnicacin, ether 2, 4, 4 '-tr? Chloro- 2 '-Differential hydroxy, 3, 4, 4'-t ncJorobaml Lda, phenoxyethanol, (enoxipropanol, phenoxanopropanol, doxycycline, capreornicin, chlorhexidine, chlor-tetr-aciclma, oxytetracycline, cindamicma, ethambutol, hexamid isothionate, metromdazole, pentamidine , gentane, Cananicin, Lineo Icma, Rnetacycline, Rnetenami na, Imnocycline, Noomycin, Net il i ciña, Parornomycin, Streptomycin, Cynazole, Rniconazole, Tetracycline Hydrochloride, Epidermal Acid, Zynecromide , potassium phthalate, potassium stearate, anhydrous sulfate, doxycycline hydrochloride, capreium sulfate, chlorhexidine glucanate, chlorhexidine hydrochloride, hydrochloride
chlortetracycline, oxytetracycline hydrochloride, clindamycin hydrochloride, ethambutol hydrochloride, etronidazole hydrochloride, pentranicin hydrochloride, gentani sulfate, cananicin sultafo, lineornicin hydrochloride, rnetacycline hydrochloride, rnetanarin hippurate, rnetanamine mandalate, hydrochloride of rninocycline, neomycin sulfate, netiir icine sulfate, paranomycin sulfate, streptomycin sulfate, toina icine sulfate, rniconazole hydrochloride, ananfadine hydrochloride, arnanfadine sulfate, octopirox, parachlorornetaxylene, statin, tolnaftate and c lotprnazole. Sunscreen assets: Certain sunscreen assets - are useful in the present. Active sunscreen filters are described in the U.S. Patent. No. 5,087,445, Haffey et al., Issued February 11, 1992; Patent of E.U.A. Do not.
5,073,372, of furner et al., Issued December 17, 1991; Patent of F.U.A. No. 5,073,371, Turner et al. Issued December 17, 1991; and Segapn, and others, in chapter VTIT, pages 189 and subsequent of Cosrnet i es Sci nce and Technology, all of which are incorporated herein by reference and in their entirety. Some non-limiting examples of sunscreen assets include those selected from the group consisting of acid? ~ Am? Nobenzo? co, 2 - (- in? lbenz? m? dazol-5-sulfone? co and mixtures thereof.) Other useful sunscreens are those described in
Patent of E.U.P. No. 4,937,370, of Sabatelli, issued on 26
June 1990, and Patent of E.U.A. No. 4,999,186, of Sa atelli et al., Issued March 12, 1991; these two references are incorporated herein by reference in their entirety. The term "salicylic acid" herein includes derivatives of salicylic acid, such as 5-octane acid or ethyl salt. Preferred examples of active agents useful herein include those selected from the group consisting of salicylic acid, 3-hydroxy acid? enzoic, acid 4-h? droxybenzoic, acetylsalicylic acid, 2-hydroxy-2-hydroxy acid, 2-hydroxypentanoic acid, 2-hydroxy-hexane acid? co, cis-retinoic acid, rans-retinoic acid, azelaic acid, aracidonic acid, benzoyl peroxide, tetracycline, ibuprofen, naproxen, hydrocort isone, acetorninophen, resorcmol, phenoxyethanol, phenoxypropanol, phenoxanopropanol, ether 2,4,4'- tp citor ~ o -2 'hidro iifeico, 3,4,4' -t plorocarba lida, octopirox, chlor * hidode of lidocama, clotprnazole, nuconazole, neo-icine sulfate, p-arnidenebenzoic acid, 2-Fem lbenz irnidazole-5-sulfonyl acid, dihydroxyacetone, and mixtures thereof. Highly preferred examples of active ingredients useful in the present include those selected from the group consisting of salicylate acid, acetyl acid, cis-retinoic acid, t-reoic acid, azelaic acid, tetracycline, ibuprofen, oxen, acetopunofen, h? dr * ocort i sona, resorcmol, phenoxyethanol, phenoxypropanol, f-enox usopr-opanol, ether 2,4,4'-
tpcloro-2'-h? drox? d? phenyl ?, 3,4, 4 '-t riclorocarbamide, octopirox, 2-phenolbenz? rn? dazol-5-sulphonic acid, dihydroxy-acetone, and mixtures thereof. Very preferred examples even useful herein include those selected from the group consisting of salicylic acid, cis-retmoic acid, trans-retmoic acid, azelaic acid, resorcmol, ibuprofen, naproxen, hydrocortisone, phenoxyethanol, phenoxy propanol, phenoxanopropanol, ether 2, 4,4'-tp chloro-2'-hydroxydiphenilic acid, 3, 4.4'-tbear riba lida rock, acid 2-phenolbenz? Rn? Dazol-5-sulphon? Dihydroxyacetone, and mixtures thereof. An especially preferred active useful herein is salicylic acid or a level of from about 0.1% to about 5% by weight, preferably from about 1% to about 3% by weight, most preferably from about-1.5% to about 2.5% by weight of the composition. The above list of acidic actives also includes salts of these acidic active substances provided that these salts remain acidic in the compositions of the present invention.
(B) ALCOXYL ALCOHOLS
The compositions of the present invention comprise from about 0.1% to about 25%, preferably from about 0.1% to about 15%, and preferably even from about 6% to about 10% of alcohols.
alkoxylates and / or alkoxylated polyols, which are useful as solubilizing agents for the acidic active ingredients in the oil phase of the oil-in-water emulsions. The alkoxylated alcohols and polyols useful herein are generally hydrophobic, having a solubility in water of less than about 1 gram per about 100 grams of water at 25 ° C. Preferably, these solvents have a minimum of 10-20 moles of propylene oxide. These compounds are typically formulated in the oil phase of oil-in-water emulsions as described in the examples given below. Mixtures of alkoxylated alcohols and alkoxylated polyols can be used herein. The alkoxylated alcohols useful herein may be described by the following general formula:
R 0
wherein R is selected from the group consisting of alcohols, polyols, diols, and mixtures thereof, having a chain length of about? to approximately 10 carbon atoms; n is an integer of about 3 to about 40; X is selected from the group consisting of hydrogen, methyl, ethyl, propyl and mixtures thereof. Preferably, R is selected from the group consisting of alcohols, polyols, diols or mixtures thereof, having a chain length of about 4 to
about 16 carbon atoms; X is methyl; and n is an integer of about * 6 to about 35. Most preferably, R is selected from the group consisting of alcohols, polyols, diols or mixtures thereof, having a chain length of from about 4 to about 6 carbon atoms. carbon; X is methyl; and n is an integer of from about 10 to about 20. Non-limiting examples of classes of alkoxylated alcohols useful herein include propoxylated and butoxylated ethers and alcohols and polyols. These compounds can be described as alkyl ethers of PPG and PBG where PPG and PBG are commonly used designations for polypropylene glycol and polyalkylene glycol, respectively. The average number of PPG or PBG groups in these ethers is commonly given by a designation. of number after PPG or PBG. For example, butyl ether of PPG-14, would designate a polypropylene glycol ether of butane! where the molecule has on average 14 units of propylene glycol. Non-limiting examples of alkoxylated alcohols useful in the present include butyl ether of PPG-10, butyl ether of PPG-11, butyl ether of PPG-12, butyl ether of PPG-13, butyl ether of PPG-14, butyl ether of PPG -15, butyl ether of PPG-J6, butryonic ether of PPG-17, butyl ether of PPG-18, ether-butyl of PPG-19, tert butyl of PPG-20, butyl ether of PPG-22, ether * butyl of PPG-24, butyl ether of PPG-30, stearyl ether of PPG-11, stearic ether of PPG-
15, PPG-10 oleyl ether, PPG-7 lacrylic ether, PPG-30 isocyclic ether, PPG-10 glyceryl ether, PPG-15 glyclic ether, PPG-10 butylene glycol ether, PPG-butyl ether - 15, PPG-27 glyceryl ether, PPG-30 cetyl ether, PPG-28 ce-ethyl ether, PPG-10 cetyl ether, PPG-10 hexylene glycol ether, PPG-15 hexylene glycol ether, ether 1, 2, 6-hexanotrol of PPG-10, 1,2,6-hexanotpol ether of PPG-15, and mixtures thereof. The preferred alkoxylated alcohols are those selected from the group consisting of bu lyl ether of PPG-14, stearal ether of PPG-15, stearate ether of PPG-11, oleyl ether of PPG-20 and mixtures thereof. The most preferred alkoxy alcohols are those selected from the group consisting of PPG-14 butyl ether, PPG-15 stearyl ether, and mixtures thereof. The butyl ether of PPG-14 is available under the name Fluid AP from Union Carbide Corporation, stearyl ether from PPG-15 is available under the tradename Arlarnol E frorn TCI Amen cas Coporat ion. Non-limiting examples of alkoxylated polyolenes useful herein include those selected from the group consisting of 1,4-butanediol of PPG-10, 1,4-butanediol of PPG-12, 1,4-butanediol of PPG- 14, butanediol of PPG-2, 1,6-hexanedione of PPG-10, 1,6-hexanedione of PPG-12, hexanediol of PPG-14, hexanediol of PPG-20, and mixtures thereof. Preferred are those selected from the group consisting of 1,4-butanediol
of PPG-10, 1,4-butanediol of PPG-12, 1, 6-hexanedione of PPG-10, and hexanediol of PPG-12, and mixtures thereof. Most preferred is 1-butanediol from PPG-10. This compound is commercially available under the tradename Macol 57 from PPG / Mazer Corporation.
(OR STABLE HIDROFQBICQ STRUCTURING AGENT TO THE ACID
The present invention also comprises about * 1% to about 20%, preferably about 1% to about 10%, most preferably about 3% about 9% of a stable hydrophobic structuring agent to the acid selected from the group consisting of of C 1 to C 30 saturated fatty alcohols, saturated C 6 to C 30 fatty alcohols containing from about 1 to about 5 moles of ethylene oxide, diols of C 1 a
- ^ 30 saturates, hydrological ions from Cie to C30 saturated, you. C 1 to C 30 saturated hydroxy fatty acids, and mixtures thereof, which have a melting point of at least about 45 ° C. These binding agents are useful in assisting in the formation of the rheological characteristic of the composition which contributes to the hydrolytic stability of the composition of the present invention. In particular, the coating agents assist in the formation of liquid gel net structures. The preferred sterilizing agents of the present
invention are selected from the group consisting of osteaprylic alcohol, ethyl alcohol, ether glycol ether stearyl alcohol having an average of about 5 ethylene oxide units, polyethylene glycol ether of cetyl alcohol having an average of about 1 to about 5 otiien oxide units, and mixtures thereof. The highly preferred structuring agents of the present invention are selected from the group consisting of stearyl alcohol, cetyl alcohol, polyethylene glycol ether and stearate alcohol having an average of about 2 units of ethylene oxide (is earet-2), the polyethylene glycol of cetyl alcohol having an average of about 2 units of oxide do full and mixtures of the same. Very preferred structuring agents which are selected from the group consisting of stearate alcohol LCO, cetyl alcohol, steareth-2 and mixtures thereof. Very preferred is steareth-2, available under the name BpjR 72 from TCI Amen cas.
(D) HIDRQFILICQ TENSIOACTIVE AGENT STABLE TO THE ACID
The compositions of the present invention comprise from about 0.05% to about 10%, preferably from
I X to about 6%, and most preferably from about J% to about 3% of at least one hydrophobic surfactant stable to the acid which can disperse the materials
hydrophobic in the water phase. The surfactant, to a minimum, must be sufficiently hydrophilic to disperse in water. The surfactant is used herein to emulsify the oil and water phase ingredients and to stabilize the resulting emulsion. The surfactants useful herein may include any of a wide variety of nonionic, cationic, ammonic and zwitterionic surfactants described in US Patents and other references. See McCutcheon's, Detergents and Ernulsi fers, North American Edition (1986), published by Allured Publishmg Corporation; Patent of E.U.A. DO NOT. 5,011,681 to Ciotti et al., Issued Apr. 30, J991; Patent of E.U.A. No. 4,421,769 of Dixon et al., Issued December 20, 1983; and Patent of E.U.A. No. 3,755,560 to Dickert et al., Issued August 28, 1973; Four references are incorporated herein for reference purposes in their entirety. The exact chosen emulsifier will depend on the pl-. of the composition and other components present. Suitable types of surfactants include tetraalkylammonium salts, ethoxylated alcohols, fatty acid amides, and ions? if we. Presently, cationic furants, especially dialkylamino quaternary compounds, are proffered. A wide variety of cationic surfactants useful herein are described in the US Pat.
E.U.A. No. 5,151,209 to McCall et al. Issued September 29, 1992; Patent of E.U.A. No. 5,151,210 of Steuri et al. Issued September 29, 1992; Patent of E.U.A. No. 5,120,532, of CJells et al. Issued June 9, 1992; Patent of E.U.A. No. 4,387,090, issued by Bolich on June 7, 1983; Patent of E.U.A. DO NOT. 3,155,591, Hilfer, issued November 3, 1964; Patent of E.U.A. No. 3,929,678, Laughlin et al. Issued December 30, 1975; Patent of E.U.A. No. 3,959,461 to Bailey and others
10 issued on May 25, 1976; McCut-cheon's, Detergent to Ernulsifiers, (North American edition 1979) M.C. Publishing Co .; and Schwaitz, and others, Surface Active Agents, Their Chemistry and Techonology, New York; Interscience Publishers, 1949; All these documents are incorporated herein by reference in their
15 totality Cationic surfactants useful herein include catonic ammonium salts such as those having the formula:
? p where Ri is an alkyl group having from about 12 to approximately 30 carbon atoms, or groups aplo or alkalo
aromatics having about 1 2 to about 30 carbon atoms; R2, 3, VR * are independently selected from hydrogen, an alkyl group having from about 1 to about 22 carbon atoms, an aplo or aromatic aplo group having from about 12 to about 22 carbon atoms; and X is any compatible anion, preferably from the group consisting of chloride, bromide, iodide, acetate, phosphate, nitrate, sulfate, ethyl sulfate, ethyl sulfate, tosylate, lactate, citrate, glycolate and mixtures thereof. Ada citonally, The alkyl groups of Ri. 2 R3 and R4 may also contain ester and / or ether bonds,
0 substituents of hydroxy or arnine group (eg, the alkyl groups may contain polyethylene glycol and poly propylene glycol moieties). Most preferably, Ri is an alkyl group having from about J2 to about 22 carbon atoms; R2 - or select from H or an alkyl group that ^? e e of alr-ededor de
1 to about 22 carbon atoms; R3 and R1 are independently selected from H or an alkyl group that is from about 1 to about 3 carbon atoms; and X is as described above. Highly effective, Ri is an alkyl group having from about 12 to about 22 carbon atoms; R2,
R3 and R4 are selected from H an alkyl group having from about 1 to about 3 carbon atoms; and X is as described above.
Alternatively, other useful cationic emulsifiers include ino-arnides, wherein in the above structure Ri is alternatively R5CO- (CH2) n- wherein Rs is an alkyl group having from about 12 to about 22 carbon atoms, and n is an integer from about 2 to about 6, preferably from about 2 to about 4, and most preferably even from 2 to about 3. Non-limiting examples of these cationic chewing liquors include stearate of the stearate idoproate. PG-d is as stearynipropyl erythropyl ether ethosulfate, stearamidopropyl dimethyl ammonium acetate acetate, steararnidoprop ldirnetii eetap larnomo tosylate, idopropyl dimethyl tin stearic acid, Jacta or stearamidopropyl dimyl propionium chloride and mixtures thereof. Non-limiting examples of quaternary ammonium salt surfactants include those selected from the group consisting of cetylammonium chloride, cetylammonium bromide, lauryl or lauryl chloride, lauryl ammonium bromide or, stearmanium chloride, bromide stearate Larnoruo, laupldimethalolamine chloride, cetildirnetanedium bromide or, laupldiinethyl ammonium chloride, laupldimethylammonium bromide, stearylmethylmethyl chloride, steamedimemide bromide 1, cetyltrirnetimiammonium chloride, cethamethylmethylene bromide, laupltprimethyl-ammonium, lauryltriinetiiamomo bromide, stearate-
tprnethylamino, stearyl-p-methyl-ammonium bromide, "Jaupldirneta lamomo" chloride, stearyldirnethyl-ethyl-di-methyl-d-methylalenonium chloride, dicetiamine-chloride, dicetyl-bromide bromide, dLlaur-1-laronium chloride, dilauryl-anmon bromide, desteap-larnom chloride, bromide destelanilonium, diceti irneti lamono chloride, dicetyl bromide, ammonium chloride, laurylmethyl lammonium chloride, dilaultile netium bromide, desteap lne and larnome chloride, paraffinyl bromide bromide, and mixtures thereof. Additional quaternary ammonium salts include those wherein the alkyl carbon chain of
C 2 to C 30 is derived from a fatty acid of tallow or of a coconut fatty acid. The term "tallow" refers to an alkyl group derived from tallow fatty acids (generally hydrogenated tallow fatty acids), which generally has mixtures of alkyl chains on the Cie to Cie scale. The term "coco" refers to an alkyl group derived from a coconut fatty acid, which generally has mixtures of alkyl chains on the C? 2 to C14 scale. Examples of quaternary ammonium salts derived from these sources of tallow and coconut include sebodirnetilanyl chloride, di sebodine ammonium rnetilsulfate, dihydrogenated dihydrogen chloride or di-tallow acetate, has been hydrogenated), dinethylamine acetate, di-propylammonium phosphate, disodium-1-nitrate nitrate, di (cocoalkyl) d? rnet 1 larnome, di bromide (cocoalqui L)) dirneti i-ammonium, tallow chloride, ammonium chloride, fat chloride or stearamidopropyl di-propyleneamine, stearamidopropyl lactate
d i rnet 11 ammonium, and mixtures thereof. An example of a quaternary ammonium compound having an alkyl group with an ester linkage is ditallowoxydiurethyl ammonium chloride. Preferred cationic surfactants are those selected from the group consisting of dialryldimethyl onium chloride, dimethyl arnide chloride, dimethyl styrene chloride, dipalkyrityl dimethyl ammonium chloride, dirnethylammonium chloride, stearamidopropyl PG-dirnomethylphosphate, stearate doparatile ethosulfate l-diaronium, stearanidopropyl-di-methyl-ureteapic lamellate chloride, stearamidopropyldirnethylammonium chloride, stearamidopropyl-dirnethylaminonium lactate, and mixtures of the same. The most preferred cationic surfactants are those selected from the group consisting of ammonium dilaupldirnetium chloride, disteapldimethylarnmonium chloride, rhamidimide dihydride chloride, dipalnitryl-dunetyl chloride, and mixtures thereof. Also, certain nonionic surfactants are preferred for use herein, especially when used in conjunction with the cationic emulsifiers described above. It has been found that a mixture of a nonionic surfactant of hydrophilic equilibrium Lipophilic (EHL) with a nonionic surfactant agent of low EHl is especially preferred. Without being limited by theory, it is believed that this combination of high and low μH nonionic surfactants in compositions that
demonstrate increased emulsion stability. The abbreviation "EHL" means lipophilic hydrophilic balance. The EHL system is well known in the art and is described in detail in "The EHL System, A Time Savmg Guide to E ulsifier Selection", ICI Amencas In. , August 1984, which is incorporated herein by reference. As defined herein, the nonionic surfactants of EHL include any of the well-known nonionic surfactants having an EHL of at least about 6 to about 18, preferably about 8 to about 18, and most preferably still from about 10 to about 18. These nonionic surfactants of EHI. Highs do not include those with high EHL values below 6, as described below. Typical of these high EHL nonionic emulsifiers are ethoxy or propoxylated alcohols, preferably ethoxy sides and alkyl phenols, with the alcohol derivatives being preferred. These alcohol derivatives contain a straight or branched chain alkyl group on the C8-C30 scale, preferably C? Or-C22 / rnuy preferably Ci2-C2o, and generally contain about 30, preferably about 6, about 25, ethylene oxide or propylene oxide groups. Among these ethoxylated alcohols and propoxy Sides, the eloxyl derivatives are most preferred. Preferred to be used herein are the polyethylether 1 ethers
der *? lauryl alcohol, cetyl alcohol, oleyl alcohol, esteapyl alcohol, alcohol to soesterial, myristyl alcohol, behenyl alcohol and mixtures thereof. Very preferred for use in the present are polyoxyethylene cetyl ether 10, known by the CTFA designation as ceteth-10; esteaplico ether de polloxietileño 21, known by the CTFA designation as steareth-21; alkylpoliet coconut oxylate (6.5), deci lpolyethoxy lato (6); and mixtures thereof. Very preferred for use in the present are ceteth-10, steareth-21, and mixtures thereof. Detailed lists of non-ionic eLsificants of EHL can be found in McCutcheon, EMULSTFIERS AND DETERGENTS,
North American Edition, 1984, McCutcheon Division, MC
Publishing Company, which has already been incorporated here by reference. The non-ionic EHL coating agents are defined herein as any of the well known nonionic surfactants having an EHL value of from about 1 to less than about 6. These non-ionic surfactants of low EHL do not include the EHL nonionic surfactant described above. Examples of these non-ionic emulsifiers of EHL ba or are ethoxylated alcohols wherein these alcohol derivatives contain a straight or branched chain alkyl group on the C8-C30 scale, preferably C? or ~ C22, rnuy preferably C? 2-C2o. and generically they contain around
from 1 to about 5 ethylene oxide groups per molecule. Some non-limiting examples of these non-ionic emulsifiers of EHL to or useful herein include ethoxylated lacrylic alcohol with one mole of ethane oxide (ie, laureth-1), laureth-2, the? Reth-3, laureth ~ 4, laur-eth-5, and mixtures thereof. Detailed lists of EHL emulsifiers can be found in McCutcheon, EMULSIFIERS AND DETERGENTS, North American Edition, 1984, McCutcheon Division, MC Publishmg Cornpany, which has already been incorporated herein by reference. In the present invention, it has been found that when a combination of high and low EHL nonionic ernulsifiers are used together, the combination of esteret-2l and / or ceteth-10 with steareth-2 is preferred.
(E) WATER Compositions of the present invention comprise from about 25% to about 99.7%, most preferably from about 65% to about 95%, and I very much prefer to still be about 70% to about
90% water
OPTIONAL COMPONENTS Each of the water and oil phases of the emulsions can comprise a wide variety of optional components. Typical of such optional components are:
Popropylene glycols - Polypropylene glycols and propylene glycol are useful herein, at a level of from about 1% to about 5% by weight of the composition, preferably from about 2% to about 3.5% by weight of the composition , to increase the penetration of the acid active ingredient of the present invention. Polypropylene glycols are polymers that are typically formed from the polymerization of propylene oxide, propylene glycol, propylchlorohydrin, propylbromohydrin, and other related materials. The propylene glycols are represented by the following formula:
where n is about 10 to about 50, preferably about 15 to about 40, and most preferably about 20 about 34. In the above structure, even though an isomeric orientation is illustrated by covenience, this illustration is not intended to exclude other isomeric structures. Polypropylene glycols are commonly referred to as PPG followed by a number that indicates the average number of units repealed in the structure. For example, PPG-30 corresponds to the previous structure where it has an average value of approximately 30. Based on this nomenclature, the polypropylene glycols useful in the
present encompass those designated PPG-10 through PPG-50, most preferably those designated PPG-15 through PPG-40, and most preferably those designated PPG-20 through PPG-34. Humectants - Another optional component of the compositions of the present invention is a humectant. When used herein, the humectant may comprise from about 0.1% to about 20%, and preferably from about 0.5% to about 10%, and most preferably still from about 1% to about 5% by weight of the composition. Although these materials are defined herein as humectants, they may also possess fermentation, skin conditioning and other related properties. Examples of humectants useful herein include materials such as urea; guanidine; α-hydroxy saturated or unsaturated alkyl acids such as glycolic acid and salts of glycolate (eg quaternary ammonium and alkylanonium) and lactic acid and lactate salts (eg, ammonium and quaternary alkylammonium); zabila in any of its varieties of forms (v. gr., zabila gel); polyhydric alcohols such as sorbitol, glycerol, low molecular weight propylene glycols (eg, propylene glycol and tripropylene glycol), hexanotriol, propylene glycol, butylene glycol, hexylene glycol and the like; polyethylene glycol; sugars and starches; sugar and starch derivatives (eg, alkoxylated glucose); hyaluronic acid; chitin; sodium polyacrylates with starch graft such
such as Sanwet (RTM) IM-1000, TM-1500, and IM-2500 (available from CeJanese Superabsorbent Materials, Portsmouth, VA); lactarin-rnonoethanolarnin; aceta-monoethanolamine acetates; propoxylated glycerol (as described in U.S. Patent No. 4,976,953 by Orr et al., issued December 11, 1990, which is incorporated herein by reference in its entirety); and mixtures thereof. Preferred humectants useful in the compositions of the present invention are urea, diols and triols of C3-6, polypropylene glycols of low molecular weight and propoxylated glycerin. Preferred humectants include those materials selected from the group consisting of urea, polyethylene glycol, 1,3-d? hydroxypropopane, glycepna, propylene glycol, hexylene glycol, 1,4-d? hydrox? hexane, 1,2,6-hexanotropic acid, dipropylene glycol, t-propylene glycol and mixtures thereof. Very preferred are those selected from the group consisting of urea, glycerol, propylene glycol, hex Llengl 1 col, glycepna, propylene glycol, t-propylene glycol, and mixtures thereof. Most preferred is propylene glycol, urea, glycepine and mixtures thereof. Emollients - The compositions of the present invention may also include an emollient. Examples of suitable emollients include, but are not limited to, volatile and non-volatile silicon oils (v.gr, duneta cona, cicio eti cona, dimethiconone, and the like) highly branched hydrocarbons, and mixtures thereof. Emollients useful in the present invention are the
which are described in the patent of E.U.A. No. 4,919,934, Decner et al., Issued April 24, 1990, which is hereby incorporated in its entirety. The emollients may typically comprise in total from 0.1% to about 25% by weight, most preferably from about 0.5% to about 10%, and most preferably from about 0.5% to about 5% by weight of the composition. Additional ingredients A variety of additional ingredients can be incorporated into the compositions of the present invention. These additional ingredients, at least, must be acid-stable, non-limiting examples of these additional ingredients include vitamins and derivatives thereof (e.g., tocopherol panthenol, and the like), other thickening agents (e.g., polyaplanarin) and isoparaffin of C13-14 and laureth-7, available from Sepigel 305 of Seppic Corp., Fairfield, NJ; and branched polysaccharides such as sclycollucans available under the tradename Clearogel® CS 11 from Michel Mercier Products Inc., Mountainside, NJ); unsaturated alkyl alpha hydroxy acids; resins; gums, (e.g., guar gum, xanthan gum and the like); waxes (both natural and synthetic), polymers to aid in the film-forming properties and substantivity of the composition (such as a copolymer of eicosene and vinylpyrrolidone, an example of which is available from GAF Chemical Corporation as Ganex V-220R);
abrasive scrubbing particles for cleansing and exfoliating the skin Cv.gr., ACuscrubR soft abrasives (e.g., ACuscrub 30, 31, 32, 40, 41, 42, 43, 44, 50, 51 and 52) available from Allied Signal Inc, Morpstown, NJ; and mineral oil encapsulated in capsules < e 3M brand PMU available from 3M Corporation, St. Paul, MN3; preservatives to maintain the microbial integrity of the compositions; skin penetration aids such as DMSO, 1-dodecylazac? cloheptane-2-one (available from Azsne * of Upjohn Co.) and the like; artificial bronzing ingredients and tanning accelerators such tyrosine, tyrosine esters such as ethyl tyroside, phospho-DOPA) skin whitening agents (c brighteners) including but not limited to hydroquinone, kojic acid and sodium rnetabisulfite; chelators and kidnappers; and components such as fragrances, pigments, dyes, essential oils, skin sensitizers, astringents skin sedative agents, skin scarring agents and the like, non-limiting examples of these aesthetic components include panthenol and derivatives; v.gr., and ilpantenol), savila, pantotemco acid and its derivatives, clover oil, menthol, camphor, eucalyptus oil, eugenol, methyl lactate, with hazelnut destaining, allantoin, bisabalol, potassium glycyrrhizin and the like. Preferred ingredients are saturated and / or saturated aminoalkyl hydroxyacids at a level of about
0. 05 to about 5% by weight of the composition, such as lactic acid, lactate salts (e.g., ammonium and quaternary alkylammonium), glycolic acid, glycolate salts (e.g., ammonium and quaternary alkylammonium) and acids of fruits. A discussion of alpha-hydroxyamics is described in Ualter. Sputh, Bydroxy, Acids and Skin Agmg, Siap / Cosrnetics / Chernical Specialties, PO, 54-59 (Sept. J993), which is incorporated herein by reference in its entirety.
DISCHARGE METHODS
The present invention also relates to methods wherein an effective amount of an acidic active ingredient is deposited on the skin to modify the condition being treated or to provide the desired benefit. A definite amount is a suitable quantity to provide the desired benefit but low enough to avoid serious side effects to a ratio of benefit to reasonable risk within the scope of the sound financial judgment. What is a safe and effective amount of the acid asset will vary with the specific asset, the ability of active L to penetrate the skin, the age of the user, the health condition of the user and the skin condition of the user, and other factors Similar. Said methods comprise applying topically to the skin and scalp an effective amount of the composition of the present invention. For example, an effective amount of a
The composition containing a composition containing salicylic acid means a sufficient amount to provide a flake replacement benefit, generally from about 0.004 RNG / cm2 to about 0.1 RNG / cm2, very preferably about 0.02 RNG / CrN2. to approximately
0. 06 rng / crn2, and most preferably still 0.04 mg / c 2. The composition can be applied for several days consecutively, weeks, months or years at an appropriate interval. Appropriate ranges are from about 3 times a day to about 10 times every 3 days, preferably from about 2 times a day to about 1 time a day, and one day, and preferably about once a day, until Desquamation, moisturization, hydration is achieved. J5 EXAMPLES
The following examples are described and demonstrate embodiments within the scope of the present invention. The examples are given solely for purposes of illustration and are not intended to be construed as limiting the present invention, since many variations can be made without departing from the spirit and scope of the invention. The ingredients are identified by the chemical name CTFA.
EXAMPLES I-II Spread moisturizers containing salicylic acids
An oil emulsion in spreadable humectant water containing salicylic acids is prepared by combining the following ingredients using conventional mixing techniques as described below.
Ingredients II% by weight% by weight Salicylic acid 2 1.5 PPG-14 butyl ether 8.00 8.00 Glycerin 4.00 4.00 Stearic alcohol 1.5 1.5 Cetyl alcohol 3.00 3.0 Distearyl chloride 0.1 0.1 irnet.il ammonium ropilenglicol 3.00 3.00 Steareth -211 2.0 2.0 Steareth-22 1.0 1.0 Dimeticone3 1.0 1.0 Chloro-cyclic * 1.0 1.0 Disodium EDTA 0.02 0.02 Minor components 0.07 0.07 water CBP 100 CBP 100
polyethylene glycol ether of stearyl alcohol with a
average of approximately 21 moles of ethylene oxide. 2 Polyethylene glycol ether of stearyl alcohol with an average of about 2 moles of ethylene oxide. 3 A polymer mixture of linear siloxanes completely blocked and blocked with trimethyldyloxy units. 4 A cyclic dimethylpolysium loxane compound. The above compositions are prepared in the following manner: First a water phase is prepared by heating the water to a temperature of about 82 ° C and adding the diesteryl dimethyl lamomo chloride, glycerin and propylene glycol.
This mixture is maintained at a temperature of about 65 ° C to about 75 ° C. The oil phase is prepared in a separate vessel by mixing the alcohol, stearate alcohol, steareth-2, steareth-21, dunethicone, and the cyclomethylene, and the mixture is heated to a temperature of about 65 ° C to 100 ° C. 75 ° C. In a separate container, the salicylic acid phase is prepared by searching for the salicylic acid in the beryllic ether.
PPG-14 at a temperature of about 65 ° C to about
75 ° C. Subsequently, the salicylic acid phase in the oil phase is mixed at a temperature of about 65 ° C to about 75 ° C. The oil phase mixture is added to the aqueous phase mixture and milled at a temperature around
from 65 ° C to approximately 75 ° C. The resulting mixture is cooled to a temperature of about 40 ° C to about 50 ° C. Subsequently, a mixture comprising the minor ingredients of the disodium EDTA to the emulsion is added. It is cooled to room temperature. In the above compositions the following can be prepared: First an aqueous phase is prepared by heating the water to a temperature of about 82 ° C and adding the distearyldirnethylammonium chloride, glycerin, propylene glycol, cetyl alcohol, stearyl alcohol, steareth-2, and steareth ~ 21 .. This mixture is maintained at a temperature of about 65 ° C to about 75 ° C. In a separate vessel, the salicylic acid phase is prepared by mixing salicylic acid, PPG-14 butyl ether, dimethicone and cyclodimicone at a temperature of about 65 ° C to about 75 ° C. Subsequently, the salicylic acid phase mixture is mixed in the water phase mixture and milled at a temperature of about 65 ° C to approximately 75 ° C. The resulting mixture is cooled to a temperature of about 40 ° C to about 50 ° C. Subsequently, a mixture comprising the minor ingredients and EDTA of disodium is added to the emulsion. It is cooled to room temperature. The resulting compositions are useful for applying to the skin to supply salicylic acid and are useful
for the treatment of wrinkles, dry skin and other skin conditions related to age.
Claims (3)
1. - A spreadable composition for skin care consisting of: (A) from about 0.05% to about 20% of an acid active ingredient, preferably having a solubility parameter of from about 6 to about 12; (B) from about 0.1% to about 25% of alkoxyl alcohols, an alkoxylated polyol and mixtures thereof, of the formula: R o wherein R is selected from the group consisting of alcohols, polyo] es, diols, and mixtures thereof, having a chain length of from about 2 to about 10 carbon atoms; n is an integer of about 3 to about 40; X is selected from the group consisting of hydrogen, methyl, ethyl, propyl and mixtures thereof; (C) of from about 1% to about 20% of a hydrophobic, stable, structuring agent to the acid selected from the group consisting of saturated fatty acids from C a to C 30, saturated C 6 to C 30 fatty alcohols containing from of about 5 moles of ethylen oxide, diols of saturated C30 to C30, saturated cycloalkyl ether of C30 to saturated C30, hydroxylic fatty acids of Ci6 to C30 saturated, and mixtures thereof, which have a melting point of at least about 45 ° C; (D) from about 0.05% to about 10% of a hydrophilic surfactant stable to the acid selected from the group consisting of surfactant to ionic, cationic, zwitepomco, nonionic and mixtures thereof; and (F) from about 25% to about 99.7% water, wherein the pH of the composition is about 3.5 or less. 2. The composition according to claim 1, further characterized in that the pH is from about 2.5 to about 3.5. 3. The composition according to claim 2, further characterized in that the pH is from about 2.8 to about 3 2. 4. The composition according to claim 1, further characterized in that the acidic active is selected from the group consisting of salicylic acid, acetylsalicylic acid, cis-retinoic acid trans-retinoic acid, azelaic acid, tet raciclma, ibuprofen, naproxen, acetonanophen, hydrocortisone, resorcmol, phenoxyethanoi, phenoxypropanol, phenoxanopropanol, ether 2, 4, 4 ' -tr? chlor-o-2 '-hydroxydifemlico, 3, 4, 4'- tnclorocarbaní lida, octopirox, acid 2-femlbenz? m? dazol-5-sulfomco, dihLdroxiacetona, and mixtures thereof. 5. The composition according to claim 4, further characterized in that the acid active it is about 0.1% to about .10% with respect to the composition. 6. The composition according to claim 5, further characterized in that the hydrophobic structuring agent is selected from the group consisting of stearyl alcohol, cetyl alcohol, polyethylene glycol ether stearyl alcohol having an average of about 2 units of ethylene and mixtures thereof. 7. The composition according to claim 4, further characterized in that the acid stable hydrophilic surfactant is selected from the group consisting of cationic surfactants, nonionic surfactants and mixtures thereof. 8. The composition according to claim 7, further characterized in that the cat ionic surfactant has the formula: wherein Ri is an alkyl group having from about 12 to about 30 carbon atoms, or groups aplo or alloy the aromatic having about 12 to about 30 carbon atoms; R2, R3, and R4 are independently selected from hydrogen, an alkyl group having from about 1 to about 22 carbon atoms, an aryl or aromatic aryl group having from about 12 to about 22 carbon atoms; and X is any companion ani n. 9. The composition according to claim 8, further characterized in that the cationic surfactant is selected from the group consisting of dilandyl chloride, dimethylammonium chloride, dimistyldimethylammonium chloride, dipalnitryldimethylammonium chloride, and mixtures thereof. 10. The composition according to claim 7, further characterized in that the nonionic surfactant is selected from the group consisting of a high EHL nonionic surfactant having an EHL of at least about 6 to about 18. , a nonionic surfactant of EHL ba or having an EHL of about 1 to about 6 and mixtures thereof. 11. The composition according to claim 10, further characterized in that the nonionic surfactant agent is selected from the group consisting of ceteth-10, steareth-21, cobalt alkopolylate 1 (6.5) coconut, deci lpolethoxylate ( 6), steareth-2 and mixtures of the same. 12. The composition according to claim J1, further characterized in that the agent Nonionic surfactant is selected from the group consisting of ceteth-10, steareth-21, steareth-2 and mixtures thereof. 13. The composition according to claim 5, further characterized in that the ratio of component (C) to component (D) is from about 20: 1 to about 1: 1. 14. The composition according to claim 13, further characterized in that the ratio of component (C) to component (D) is from about 10: 1 to about 1: 1. 15. The composition according to claim. 1.4, further characterized in that the ratio of component (C) to component (D) is from about 5: 1 to about 1: 1. 16. The composition according to claim 1, further characterized in that the acid active has a solubility parameter of about 9 to about 12. 17. The composition according to claim 16, further characterized in that the acid active is selects from the group consisting of salicylic acid, salicylic acid derivative, cis-retinoic acid-trans-retinoic acid, azelaic acid, ibuprofen, naproxen, 2-phenylbenzylnidazo-l-5-sulfonic acid and mixtures thereof. 18. The composition according to claim 17, further characterized by the alcohols alkoxylates and coxyl-side-polyols are selected from the group consisting of butyl ether of PPG-14, stearyl ether of PPG-15, stearal stearyl ether of PPG-11, oleyl ether of PPG-20, 1,4-t > utanod? ol of PPG-10, 1, 4-butanedione of PPG-12, 1,6-hexanedione of PPG-10 and 1,6-hexanediol of PPG-12, and mixtures thereof. 19. The composition according to claim 18, further characterized in that the alkoxylated alcohols and alkoxylated polyols are selected from the group consisting of PPG-14 butyl ether, stearate ether of PPG-15, 1,4-butanediol? ol of PP6-10 and mixtures thereof. 20. The composition according to claim 19, further characterized in that the acidic active is salicylic acid at a level of about 0.1% to about 5% with respect to the composition. 21. The composition according to claim 17, further characterized in that the hydrophobic structuring agent is selected from the group consisting of stearate alcohol, cetyl alcohol, ether with a stearate alcohol glycol having an average of about? ethylene oxide units and mixtures thereof. 22. The composition according to claim 17, further characterized in that the acid-stable hydrophilic surfactant is selected from the group consisting of cationic surfactants, nonionic surfactants and mixtures thereof.
23. - The composition according to claim 22, further characterized in that the cationic surfactant has the formula: wherein Ri is an alkyl group having from about 12 to about 30 carbon atoms, or aromatic alkalo or alkalo groups having from about 12 to about 30 carbon atoms; R2, R3, and 4 are independently selected from hydrogen, an alkyl group having from about 1 to about 22 carbon atoms, an aryl or aromatic group having from about 12 to about 22 atoms. of carbon; and X is any compatible anion. 24. The composition according to claim 23, further characterized in that the cationic ionic surfactant is selected from the group consisting of dilauryl diirnetium chloride lamomo, distearyl disiryl ammonium chloride, dirnip stilyrnethiyl chloride or dipalrnite chloride Ldirneta. lamonium and mixtures thereof. 25. The composition according to claim 22, further characterized in that the agent Nonionic surfactant is selected from the group consisting of a high EHL nonionic surfactant having an EHL of at least about 6 to about 18, a low EHL nonionic surfactant having an EHL of about 1 to about 6 and mixtures thereof. 26. The composition according to claim 25, further characterized in that the nonionic surfactant is selected from the group consisting of ceteth-10, steareth-21, coconut polypolyethoxylate (6.5), decylpolyethoxylate (6), steareth-2 and mixtures thereof. 27. The composition according to claim 26, further characterized in that the nonionic surfactant is selected from the group consisting of ceteth-10, steareth-21, steareth-2 and mixtures thereof. 28. The composition according to claim 17, characterized adornas because the ratio of component (C) to component (D) is about 20: 1"about 1: 1. 29. The composition according to claim 28, further characterized in that the ratio of component (C) to component (D) is from about 10: 1 to about 1: 1. 30. The composition according to claim 29, further characterized in that the ratio of component (C) to component (D) is from about 5.1 to approximately 1: 1.
3. The composition according to claim 1, further characterized in that the viscosity of the composition is from about 3,000 to about 200,000 cps. 32. The composition according to claim 20, further characterized in that the composition additionally comprises from about 1% to about 5% by weight with respect to the propylene glycol composition. 33. The composition according to claim 32, further characterized in that the propylene glycol level is from about 2% to about 3.5% by weight with respect to the composition. SUMMARY OF THE INVENTION The present invention relates to spreadable compositions for skin care comprising: (A) from about 0.05% to about 20% of an acidic active ingredient, preferably having a solubility parameter of from about 6 to about 12; (B) around 0.1% to about 25% alcohols; (C) from about 1% to about 20% of a hydrophobic, stable acid-stable agent selected from the group consisting of saturated C C to C C gras fatty alcohols, saturated Ci 6 to C 30 fatty alcohols containing from from 1 to about 5 moles of ethylene oxide, saturated C30 C22 diols, saturated C30 to C30 onoglycerol ethers, saturated C30 to C20 hydroxy fatty acids, and mixtures thereof, which have a melting point of at least approximately 45 ° C; (D) from about 0.05% to about 10% of a stable hydrophilic surfactant to the acid selected from the group consisting of ammonium surfactant, cat1 orneo, zwiter-iomco, nonionic and mixtures thereof; and (F) from about 25% to about 99.7% water, wherein the pH of the composition is about 3.5 or less; These cosmetic compositions provide improved physicochemical stability, while providing good skin deposition and good skin penetration of the active ingredients while also providing low skin irritation. JJ / crrn * cgt * cpm * rnvs P96-584F
Family
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