CA2564077A1 - Mequinol-based dermatological depigmenting composition - Google Patents
Mequinol-based dermatological depigmenting composition Download PDFInfo
- Publication number
- CA2564077A1 CA2564077A1 CA002564077A CA2564077A CA2564077A1 CA 2564077 A1 CA2564077 A1 CA 2564077A1 CA 002564077 A CA002564077 A CA 002564077A CA 2564077 A CA2564077 A CA 2564077A CA 2564077 A1 CA2564077 A1 CA 2564077A1
- Authority
- CA
- Canada
- Prior art keywords
- composition
- mequinol
- acid
- skin
- depigmenting
- 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.)
- Abandoned
Links
- 239000000203 mixture Substances 0.000 title claims abstract description 53
- NWVVVBRKAWDGAB-UHFFFAOYSA-N p-methoxyphenol Chemical compound COC1=CC=C(O)C=C1 NWVVVBRKAWDGAB-UHFFFAOYSA-N 0.000 title claims abstract description 47
- 229960003505 mequinol Drugs 0.000 title claims abstract description 22
- 239000002537 cosmetic Substances 0.000 claims abstract description 18
- 229940061720 alpha hydroxy acid Drugs 0.000 claims abstract description 14
- 150000001280 alpha hydroxy acids Chemical class 0.000 claims abstract description 13
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims description 12
- 239000002253 acid Substances 0.000 claims description 11
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 claims description 10
- BJEPYKJPYRNKOW-UHFFFAOYSA-N alpha-hydroxysuccinic acid Natural products OC(=O)C(O)CC(O)=O BJEPYKJPYRNKOW-UHFFFAOYSA-N 0.000 claims description 7
- 230000000694 effects Effects 0.000 claims description 6
- 235000011090 malic acid Nutrition 0.000 claims description 6
- BJEPYKJPYRNKOW-REOHCLBHSA-N (S)-malic acid Chemical compound OC(=O)[C@@H](O)CC(O)=O BJEPYKJPYRNKOW-REOHCLBHSA-N 0.000 claims description 5
- 239000004310 lactic acid Substances 0.000 claims description 5
- 235000014655 lactic acid Nutrition 0.000 claims description 5
- 239000001630 malic acid Substances 0.000 claims description 5
- 230000000475 sunscreen effect Effects 0.000 claims description 5
- 239000000516 sunscreening agent Substances 0.000 claims description 5
- 206010008570 Chloasma Diseases 0.000 claims description 4
- AEMRFAOFKBGASW-UHFFFAOYSA-N Glycolic acid Chemical compound OCC(O)=O AEMRFAOFKBGASW-UHFFFAOYSA-N 0.000 claims description 4
- 208000003351 Melanosis Diseases 0.000 claims description 4
- 208000012641 Pigmentation disease Diseases 0.000 claims description 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 4
- 238000000034 method Methods 0.000 claims description 4
- 230000019612 pigmentation Effects 0.000 claims description 4
- 239000003814 drug Substances 0.000 claims description 3
- 235000015165 citric acid Nutrition 0.000 claims description 2
- 229940079593 drug Drugs 0.000 claims description 2
- 239000007844 bleaching agent Substances 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 239000007854 depigmenting agent Substances 0.000 abstract description 7
- 210000003491 skin Anatomy 0.000 description 12
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 10
- LXCFILQKKLGQFO-UHFFFAOYSA-N methylparaben Chemical compound COC(=O)C1=CC=C(O)C=C1 LXCFILQKKLGQFO-UHFFFAOYSA-N 0.000 description 10
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 10
- QELSKZZBTMNZEB-UHFFFAOYSA-N propylparaben Chemical compound CCCOC(=O)C1=CC=C(O)C=C1 QELSKZZBTMNZEB-UHFFFAOYSA-N 0.000 description 9
- YXFVVABEGXRONW-UHFFFAOYSA-N Toluene Chemical compound CC1=CC=CC=C1 YXFVVABEGXRONW-UHFFFAOYSA-N 0.000 description 6
- 239000008213 purified water Substances 0.000 description 6
- 239000002994 raw material Substances 0.000 description 6
- HRZFUMHJMZEROT-UHFFFAOYSA-L sodium disulfite Chemical compound [Na+].[Na+].[O-]S(=O)S([O-])(=O)=O HRZFUMHJMZEROT-UHFFFAOYSA-L 0.000 description 6
- 229940001584 sodium metabisulfite Drugs 0.000 description 6
- 235000010262 sodium metabisulphite Nutrition 0.000 description 6
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 6
- GWEVSGVZZGPLCZ-UHFFFAOYSA-N Titan oxide Chemical compound O=[Ti]=O GWEVSGVZZGPLCZ-UHFFFAOYSA-N 0.000 description 5
- 150000001875 compounds Chemical class 0.000 description 5
- 235000011187 glycerol Nutrition 0.000 description 5
- 235000010270 methyl p-hydroxybenzoate Nutrition 0.000 description 5
- 239000004292 methyl p-hydroxybenzoate Substances 0.000 description 5
- 229960002216 methylparaben Drugs 0.000 description 5
- GLDOVTGHNKAZLK-UHFFFAOYSA-N octadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCCCO GLDOVTGHNKAZLK-UHFFFAOYSA-N 0.000 description 5
- 229940100460 peg-100 stearate Drugs 0.000 description 5
- 235000010232 propyl p-hydroxybenzoate Nutrition 0.000 description 5
- 239000004405 propyl p-hydroxybenzoate Substances 0.000 description 5
- 229960003415 propylparaben Drugs 0.000 description 5
- XUMBMVFBXHLACL-UHFFFAOYSA-N Melanin Chemical compound O=C1C(=O)C(C2=CNC3=C(C(C(=O)C4=C32)=O)C)=C2C4=CNC2=C1C XUMBMVFBXHLACL-UHFFFAOYSA-N 0.000 description 4
- GSEJCLTVZPLZKY-UHFFFAOYSA-N Triethanolamine Chemical compound OCCN(CCO)CCO GSEJCLTVZPLZKY-UHFFFAOYSA-N 0.000 description 4
- 150000007513 acids Chemical class 0.000 description 4
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 3
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 3
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 description 3
- XLOMVQKBTHCTTD-UHFFFAOYSA-N Zinc monoxide Chemical compound [Zn]=O XLOMVQKBTHCTTD-UHFFFAOYSA-N 0.000 description 3
- 239000002671 adjuvant Substances 0.000 description 3
- XNEFYCZVKIDDMS-UHFFFAOYSA-N avobenzone Chemical compound C1=CC(OC)=CC=C1C(=O)CC(=O)C1=CC=C(C(C)(C)C)C=C1 XNEFYCZVKIDDMS-UHFFFAOYSA-N 0.000 description 3
- 229960005193 avobenzone Drugs 0.000 description 3
- 229940073669 ceteareth 20 Drugs 0.000 description 3
- 229940081733 cetearyl alcohol Drugs 0.000 description 3
- 239000006185 dispersion Substances 0.000 description 3
- 208000000069 hyperpigmentation Diseases 0.000 description 3
- 230000003810 hyperpigmentation Effects 0.000 description 3
- 239000002480 mineral oil Substances 0.000 description 3
- 235000010446 mineral oil Nutrition 0.000 description 3
- 235000019333 sodium laurylsulphate Nutrition 0.000 description 3
- UITSPQLTFPTHJZ-UHFFFAOYSA-N 2-[[3,4,5-tris(2-hydroxyethoxy)-6-methoxyoxan-2-yl]methoxy]ethanol Chemical compound COC1OC(COCCO)C(OCCO)C(OCCO)C1OCCO UITSPQLTFPTHJZ-UHFFFAOYSA-N 0.000 description 2
- OUYCCCASQSFEME-QMMMGPOBSA-N L-tyrosine Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-QMMMGPOBSA-N 0.000 description 2
- 235000021355 Stearic acid Nutrition 0.000 description 2
- 102000003425 Tyrosinase Human genes 0.000 description 2
- 108060008724 Tyrosinase Proteins 0.000 description 2
- YKTSYUJCYHOUJP-UHFFFAOYSA-N [O--].[Al+3].[Al+3].[O-][Si]([O-])([O-])[O-] Chemical compound [O--].[Al+3].[Al+3].[O-][Si]([O-])([O-])[O-] YKTSYUJCYHOUJP-UHFFFAOYSA-N 0.000 description 2
- 239000000654 additive Substances 0.000 description 2
- 239000003963 antioxidant agent Substances 0.000 description 2
- 239000008346 aqueous phase Substances 0.000 description 2
- 125000004432 carbon atom Chemical group C* 0.000 description 2
- 230000035614 depigmentation Effects 0.000 description 2
- 208000035475 disorder Diseases 0.000 description 2
- 239000000839 emulsion Substances 0.000 description 2
- 150000002148 esters Chemical class 0.000 description 2
- 239000000945 filler Substances 0.000 description 2
- 239000000499 gel Substances 0.000 description 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 2
- 239000004615 ingredient Substances 0.000 description 2
- 239000007788 liquid Substances 0.000 description 2
- 229940100485 methyl gluceth-10 Drugs 0.000 description 2
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 description 2
- FMJSMJQBSVNSBF-UHFFFAOYSA-N octocrylene Chemical group C=1C=CC=CC=1C(=C(C#N)C(=O)OCC(CC)CCCC)C1=CC=CC=C1 FMJSMJQBSVNSBF-UHFFFAOYSA-N 0.000 description 2
- 229960000601 octocrylene Drugs 0.000 description 2
- 230000007170 pathology Effects 0.000 description 2
- 239000012071 phase Substances 0.000 description 2
- 239000003755 preservative agent Substances 0.000 description 2
- 230000002265 prevention Effects 0.000 description 2
- 150000003839 salts Chemical class 0.000 description 2
- GEHJYWRUCIMESM-UHFFFAOYSA-L sodium sulfite Chemical compound [Na+].[Na+].[O-]S([O-])=O GEHJYWRUCIMESM-UHFFFAOYSA-L 0.000 description 2
- 239000007787 solid Substances 0.000 description 2
- 239000000243 solution Substances 0.000 description 2
- 239000008117 stearic acid Substances 0.000 description 2
- 239000004408 titanium dioxide Substances 0.000 description 2
- 230000000699 topical effect Effects 0.000 description 2
- 230000009466 transformation Effects 0.000 description 2
- OUYCCCASQSFEME-UHFFFAOYSA-N tyrosine Natural products OC(=O)C(N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-UHFFFAOYSA-N 0.000 description 2
- 239000011787 zinc oxide Substances 0.000 description 2
- NIXOWILDQLNWCW-UHFFFAOYSA-N Acrylic acid Chemical compound OC(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-N 0.000 description 1
- QGZKDVFQNNGYKY-UHFFFAOYSA-O Ammonium Chemical compound [NH4+] QGZKDVFQNNGYKY-UHFFFAOYSA-O 0.000 description 1
- 239000004475 Arginine Substances 0.000 description 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 description 1
- 201000004624 Dermatitis Diseases 0.000 description 1
- KCXVZYZYPLLWCC-UHFFFAOYSA-N EDTA Chemical compound OC(=O)CN(CC(O)=O)CCN(CC(O)=O)CC(O)=O KCXVZYZYPLLWCC-UHFFFAOYSA-N 0.000 description 1
- 102000004190 Enzymes Human genes 0.000 description 1
- 108090000790 Enzymes Proteins 0.000 description 1
- 208000016311 Freckling Diseases 0.000 description 1
- 206010020751 Hypersensitivity Diseases 0.000 description 1
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 1
- KDXKERNSBIXSRK-UHFFFAOYSA-N Lysine Natural products NCCCCC(N)C(O)=O KDXKERNSBIXSRK-UHFFFAOYSA-N 0.000 description 1
- 239000004472 Lysine Substances 0.000 description 1
- 239000004909 Moisturizer Substances 0.000 description 1
- 208000007256 Nevus Diseases 0.000 description 1
- YBGZDTIWKVFICR-JLHYYAGUSA-N Octyl 4-methoxycinnamic acid Chemical compound CCCCC(CC)COC(=O)\C=C\C1=CC=C(OC)C=C1 YBGZDTIWKVFICR-JLHYYAGUSA-N 0.000 description 1
- 206010036229 Post inflammatory pigmentation change Diseases 0.000 description 1
- ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 description 1
- 229920002125 Sokalan® Polymers 0.000 description 1
- 206010064127 Solar lentigo Diseases 0.000 description 1
- 101710147108 Tyrosinase inhibitor Proteins 0.000 description 1
- 206010047642 Vitiligo Diseases 0.000 description 1
- 238000005299 abrasion Methods 0.000 description 1
- 230000009471 action Effects 0.000 description 1
- 239000004480 active ingredient Substances 0.000 description 1
- 239000013543 active substance Substances 0.000 description 1
- 230000000996 additive effect Effects 0.000 description 1
- 230000032683 aging Effects 0.000 description 1
- 208000026935 allergic disease Diseases 0.000 description 1
- 230000007815 allergy Effects 0.000 description 1
- 150000001408 amides Chemical class 0.000 description 1
- 150000001413 amino acids Chemical class 0.000 description 1
- ODKSFYDXXFIFQN-UHFFFAOYSA-N arginine Natural products OC(=O)C(N)CCCNC(N)=N ODKSFYDXXFIFQN-UHFFFAOYSA-N 0.000 description 1
- 239000002585 base Substances 0.000 description 1
- 238000004061 bleaching Methods 0.000 description 1
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 229960001631 carbomer Drugs 0.000 description 1
- 239000002738 chelating agent Substances 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 238000004040 coloring Methods 0.000 description 1
- 239000000470 constituent Substances 0.000 description 1
- 239000006071 cream Substances 0.000 description 1
- WZHCOOQXZCIUNC-UHFFFAOYSA-N cyclandelate Chemical compound C1C(C)(C)CC(C)CC1OC(=O)C(O)C1=CC=CC=C1 WZHCOOQXZCIUNC-UHFFFAOYSA-N 0.000 description 1
- 125000004122 cyclic group Chemical group 0.000 description 1
- 229940000033 dermatological agent Drugs 0.000 description 1
- 239000003241 dermatological agent Substances 0.000 description 1
- 210000004207 dermis Anatomy 0.000 description 1
- 235000014113 dietary fatty acids Nutrition 0.000 description 1
- MCPKSFINULVDNX-UHFFFAOYSA-N drometrizole Chemical compound CC1=CC=C(O)C(N2N=C3C=CC=CC3=N2)=C1 MCPKSFINULVDNX-UHFFFAOYSA-N 0.000 description 1
- 229960000979 drometrizole Drugs 0.000 description 1
- 239000000975 dye Substances 0.000 description 1
- 239000003792 electrolyte Substances 0.000 description 1
- 239000003995 emulsifying agent Substances 0.000 description 1
- 238000005886 esterification reaction Methods 0.000 description 1
- JAPKVFCSJTZIAU-UHFFFAOYSA-N ethanol;1-phenoxyethanol Chemical compound CCO.CC(O)OC1=CC=CC=C1 JAPKVFCSJTZIAU-UHFFFAOYSA-N 0.000 description 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 1
- 239000000194 fatty acid Substances 0.000 description 1
- 229930195729 fatty acid Natural products 0.000 description 1
- 150000004665 fatty acids Chemical class 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 239000003205 fragrance Substances 0.000 description 1
- 239000003349 gelling agent Substances 0.000 description 1
- 230000002068 genetic effect Effects 0.000 description 1
- 229910052736 halogen Inorganic materials 0.000 description 1
- 150000002367 halogens Chemical group 0.000 description 1
- 125000004051 hexyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 description 1
- 239000003906 humectant Substances 0.000 description 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 description 1
- 150000004679 hydroxides Chemical class 0.000 description 1
- 150000001261 hydroxy acids Chemical class 0.000 description 1
- 229910052500 inorganic mineral Inorganic materials 0.000 description 1
- 230000007794 irritation Effects 0.000 description 1
- JJTUDXZGHPGLLC-UHFFFAOYSA-N lactide Chemical compound CC1OC(=O)C(C)OC1=O JJTUDXZGHPGLLC-UHFFFAOYSA-N 0.000 description 1
- 206010024217 lentigo Diseases 0.000 description 1
- 230000003902 lesion Effects 0.000 description 1
- 150000002632 lipids Chemical class 0.000 description 1
- 239000006210 lotion Substances 0.000 description 1
- 230000007246 mechanism Effects 0.000 description 1
- 229940126601 medicinal product Drugs 0.000 description 1
- 230000008099 melanin synthesis Effects 0.000 description 1
- 210000002752 melanocyte Anatomy 0.000 description 1
- 201000001441 melanoma Diseases 0.000 description 1
- 230000002503 metabolic effect Effects 0.000 description 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 1
- 239000004530 micro-emulsion Substances 0.000 description 1
- 239000003094 microcapsule Substances 0.000 description 1
- 239000011859 microparticle Substances 0.000 description 1
- 235000013336 milk Nutrition 0.000 description 1
- 239000008267 milk Substances 0.000 description 1
- 210000004080 milk Anatomy 0.000 description 1
- 239000011707 mineral Substances 0.000 description 1
- 230000001333 moisturizer Effects 0.000 description 1
- 210000004400 mucous membrane Anatomy 0.000 description 1
- GOQYKNQRPGWPLP-UHFFFAOYSA-N n-heptadecyl alcohol Natural products CCCCCCCCCCCCCCCCCO GOQYKNQRPGWPLP-UHFFFAOYSA-N 0.000 description 1
- 238000006386 neutralization reaction Methods 0.000 description 1
- 229960001679 octinoxate Drugs 0.000 description 1
- 229960003921 octisalate Drugs 0.000 description 1
- WCJLCOAEJIHPCW-UHFFFAOYSA-N octyl 2-hydroxybenzoate Chemical compound CCCCCCCCOC(=O)C1=CC=CC=C1O WCJLCOAEJIHPCW-UHFFFAOYSA-N 0.000 description 1
- 125000002347 octyl 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])[H] 0.000 description 1
- 239000003921 oil Substances 0.000 description 1
- 150000007530 organic bases Chemical class 0.000 description 1
- 239000007800 oxidant agent Substances 0.000 description 1
- DXGLGDHPHMLXJC-UHFFFAOYSA-N oxybenzone Chemical compound OC1=CC(OC)=CC=C1C(=O)C1=CC=CC=C1 DXGLGDHPHMLXJC-UHFFFAOYSA-N 0.000 description 1
- 229960001173 oxybenzone Drugs 0.000 description 1
- 125000001147 pentyl group Chemical group C(CCCC)* 0.000 description 1
- 239000002304 perfume Substances 0.000 description 1
- 239000008194 pharmaceutical composition Substances 0.000 description 1
- 239000000049 pigment Substances 0.000 description 1
- 239000011591 potassium Substances 0.000 description 1
- 229910052700 potassium Inorganic materials 0.000 description 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 230000001012 protector Effects 0.000 description 1
- 230000004044 response Effects 0.000 description 1
- 229920006395 saturated elastomer Polymers 0.000 description 1
- 231100000241 scar Toxicity 0.000 description 1
- 239000003352 sequestering agent Substances 0.000 description 1
- 210000002966 serum Anatomy 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- 235000010265 sodium sulphite Nutrition 0.000 description 1
- 150000003408 sphingolipids Chemical class 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- OGIDPMRJRNCKJF-UHFFFAOYSA-N titanium oxide Inorganic materials [Ti]=O OGIDPMRJRNCKJF-UHFFFAOYSA-N 0.000 description 1
- LENZDBCJOHFCAS-UHFFFAOYSA-N tris Chemical group OCC(N)(CO)CO LENZDBCJOHFCAS-UHFFFAOYSA-N 0.000 description 1
- ZQTYRTSKQFQYPQ-UHFFFAOYSA-N trisiloxane Chemical compound [SiH3]O[SiH2]O[SiH3] ZQTYRTSKQFQYPQ-UHFFFAOYSA-N 0.000 description 1
- 239000011782 vitamin Substances 0.000 description 1
- 229930003231 vitamin Natural products 0.000 description 1
- 235000013343 vitamin Nutrition 0.000 description 1
- 229940088594 vitamin Drugs 0.000 description 1
- 230000002087 whitening effect Effects 0.000 description 1
- 239000000230 xanthan gum Substances 0.000 description 1
- 229920001285 xanthan gum Polymers 0.000 description 1
- 229940082509 xanthan gum Drugs 0.000 description 1
- 235000010493 xanthan gum Nutrition 0.000 description 1
- -1 α-hydroxy acid ester Chemical class 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q19/00—Preparations for care of the skin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
- A61K8/34—Alcohols
- A61K8/347—Phenols
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
- A61K8/36—Carboxylic acids; Salts or anhydrides thereof
- A61K8/365—Hydroxycarboxylic acids; Ketocarboxylic acids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q19/00—Preparations for care of the skin
- A61Q19/02—Preparations for care of the skin for chemically bleaching or whitening the skin
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Dermatology (AREA)
- Emergency Medicine (AREA)
- Birds (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Cosmetics (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
L~invention se rapporte à une composition dépigmentante de la peau comprenant, dans un milieu physiologiquement acceptable, du méquinol associé à un autre agent dépigmentant tel que les acides alpha-hydroxylés en vue d~une utilisation pharmaceutique ou cosmétique. The invention relates to a depigmenting composition of the skin comprising in a physiologically acceptable medium, mequinol associated with another depigmenting agent such as alpha-hydroxy acids for pharmaceutical or cosmetic use.
Description
COMPOSITION DERMATOLOGIQUE DEPIGMENTANTE A BASE DE MEQUINOL
La présente invention concerne une nouvelle composition cosmétique ou dermatologique comprenant en association le méquinol (ou 4-hydroxyanisole) et un acide alpha-hydroxylé
(ou alpha hydroxy-acide ou AHA), utilisable par application topique pour la dépigmentation de la peau. La composition selon l'invention peut également contenir un filtre solaire.
La pigmentation de la peau résulte de la synthèse de la mélanine dans les mélanocytes 1o du derme par la transformation de la tyrosine sous l'influence d'une enzyme cupro-protéique la tyrosinase.
On peut donc obtenir un effet de dépigmentation de la peau en utilisant un composé qui dégrade la mélanine ou un inhibiteur de la tyrosinase qui bloque le mécanisme de transformation de la tyrosine en mélanine.
Le méquinol ou 4-hydroxyanisole est connu de longue date comme étant un composé
ayant une activité dépigmentant (Brun R, Journal of the society of cosmetic chemists (1960), 11, 571-9).
Le mode d'action du méquinol en tant que dépigmentant étant d'agir comme un substrat 2o de la tyrosinase (Riley P, Journal of Pathology (1969), 97(2)1 185-91 et Journal of Pathology (1969), 97(2), 193-206.
L'acide citrique ou l'acide malique sont connus dans l'art antérieur dans les compositions cosmétiques et pharmaceutiques comme des agents chélatants ou oxydants à des concentrations faibles, inférieures à 0.01 % par rapport au poids total de la composition.
La Demanderesse a découvert de manière surprenante que la combinaison du méquinol et d'un acide alpha hydroxylé permettait d'obtenir une réponse dépigmentante beaucoup plus rapide et efficace que celle obtenue avec le méquinol seul et ce avec des quantités plus faibles que celles nécessaires lors de l'utilisation de l'actif seul.
Cette synergie de l'activité dépigmentante obtenue à des quantités moindres des deux actifs permet en outre de diminuer de manière significative les effets secondaires néfastes (rougeurs, irritations) liés à l'utilisation d'un dépigmentant. DEPIGMENTING DERMATOLOGICAL COMPOSITION BASED ON MEQUINOL
The present invention relates to a novel cosmetic composition or dermatological comprising mequinol (or 4-hydroxyanisole) in combination with an alpha-hydroxylated (or alpha hydroxy acid or AHA), usable by topical application for the depigmentation of the skin. The composition according to the invention may also contain a solar filter.
The pigmentation of the skin results from the synthesis of melanin in the melanocytes 1o dermis by the transformation of tyrosine under the influence of an enzyme cupro protein tyrosinase.
It is therefore possible to obtain a depigmentation effect on the skin by using a compound that degrades melanin or a tyrosinase inhibitor that blocks the mechanism of transformation of tyrosine into melanin.
Mequinol or 4-hydroxyanisole has been known for a long time as a compound having a depigmenting activity (Brown R, Journal of the Society of Cosmetic chemists (1960), 11, 571-9).
Mequinol's mode of action as a depigmenting agent is to act as a substratum 2o tyrosinase (Riley P, Journal of Pathology (1969), 97 (2) 1 185-91 and Journal of Pathology (1969), 97 (2), 193-206.
Citric acid or malic acid are known in the prior art in the compositions cosmetics and pharmaceuticals as chelating or oxidizing agents to low concentrations, less than 0.01% in relation to the total weight of the composition.
The Applicant has surprisingly discovered that the combination of the mequinol and an alpha hydroxylated acid allowed to obtain a depigmenting response a lot faster and more effective than mequinol alone, with quantities lower than those required when using the asset alone.
This synergy of depigmenting activity obtained at lower amounts both assets can also significantly reduce the effects of harmful side effects (redness, irritation) related to the use of a depigmenting agent.
2 L'invention se rapporte donc à une composition dépigmentante de la peau comprenant dans un milieu physiologiquement acceptable, du méquinol et au moins un acide alpha hydroxylé.
On entend par milieu physiologiquement acceptable, un milieu compatible avec la peau, les muqueuses et/ou les phanères.
Les a-hydroxyacides auxquels s'applique l'invention peuvent être linéaires, ramifiés ou cycliques, saturés ou insaturés. Les atomes d'hydrogène de la chaîne carbonée peuvent, 1o en outre, être substitués par des halogènes, des radicaux halogénés, alkylés, acylés, acyloxylés, alcoxy carbonylés ou alcoxylés ayant de 2 à 28 atomes de carbone.
L'a-hydroxyacide utilisable selon l'invention peut consister en un acide mono-ou polycarboxylique comportant une ou plusieurs fonctions hydroxy, l'une au moins de ces fonctions hydroxy devant occuper une position a sur ledit acide.
De préférence, les a-hydroxy-acides de l'invention sont des a-hydroxy-alcanoïques ayant de 2 à 18 atomes de carbone.
Comme a-hydroxy-acides utilisables dans l'invention, on peut citer notamment les acides glycolique (ou a-hydroxyéthanoïque), lactique (ou a-hydroxypropanoïque), malique (ou hydroxybutanedioïque), tartrique (ou dihydroxybutanedioïque), citrique, mandélique, a-hydroxycaprylique (ou (x-hydroxyoctanoïque), a-hydroxy-hexanoïque, a-hydroxydécanoïque, a-hydroxydodécanoïque, a-hydroxy-tétradécanoïque, a-hydroxyhexadécanoïque, a-hydroxyoctadécanoïque, a-hydroxyeisanoïque, a-hydroxydocosanoïque, a-hydroxyhexacosanoïque, a-hydroxyoctacosanoïque.
Ces acides peuvent se présenter dans la composition sous forme d'acide libre et/ou sous la forme de l'un de leurs sels associés ou bien sous la forme de l'un de leurs esters ou de leurs amides correspondants, ou bien encore éventuellement sous la forme du lactide correspondant (forme obtenue par autoestérification des molécules).
Les sels peuvent être préparés par les procédés connus, par exemple par neutralisation d'un a-hydroxyacide avec une base appropriée telles que les hydroxydes de sodium, de WO 2005/115322 The invention thus relates to a depigmenting composition of the skin comprising in a physiologically acceptable medium, mequinol and at least one acid alpha hydroxylated.
The term "physiologically acceptable medium" means a medium that is compatible with the skin, mucous membranes and / or integuments.
The α-hydroxy acids to which the invention applies may be linear, branched or cyclic, saturated or unsaturated. The hydrogen atoms of the carbon chain can In addition, be substituted by halogens, halogenated radicals, alkylated, acylated, acyloxylated, alkoxycarbonylated or alkoxylated having from 2 to 28 carbon atoms.
The α-hydroxy acid which can be used according to the invention may consist of a monohydric acid or polycarboxylic compound having one or more hydroxy functions, at least one of these hydroxy functions to occupy a position a on said acid.
Preferably, the α-hydroxy acids of the invention are α-hydroxy-alkanoids having from 2 to 18 carbon atoms.
As α-hydroxy acids that may be used in the invention, mention may in particular be made of the acids glycolic (or α-hydroxyethanoic), lactic (or α-hydroxypropanoic), malic (or hydroxybutanedioic acid), tartaric (or dihydroxybutanedioic), citric, mandelic, a-hydroxycaprylic (or (x-hydroxyoctanoic), α-hydroxy-hexanoic, a-hydroxydecanoic, α-hydroxydodecanoic, α-hydroxy-tetradecanoic, a-hydroxyhexadecanoic, α-hydroxyoctadecanoic, α-hydroxyeisanoic, a-hydroxydocosanoic, α-hydroxyhexacosanoic, α-hydroxyoctacosanoic.
These acids can be present in the composition in free acid form and / or the form of one of their associated salts or in the form of one of their esters or their corresponding amides, or possibly also in the form of the lactide corresponding (form obtained by self-esterification of the molecules).
The salts can be prepared by known methods, for example by neutralization of an α-hydroxy acid with a suitable base such as hydroxides of sodium, WO 2005/11532
3 PCT/FR2005/001212 potassium ou d'ammonium, ou une base organique telle que la triéthanolamine ou les acides aminés (lysine, arginine).
Quand on utilise un ester d'a-hydroxyacide, il peut s'agir notamment d'un ester de méthyle, d'éthyle, de propyle, de butyle, de pentyle, d'hexyle ou d'octyle.
On utilisera de préférence comme acides alpha hydroxylés utiles selon l'invention, l'acide malique, l'acide citrique, l'acide lactique ou l'acide glycolique.
1o L'application d'une composition contenant l'association selon l'invention permet d'obtenir un net blanchiment de la peau.
L'invention se rapporte aussi à une composition dépigmentante de la peau comprenant dans un milieu physiologiquement acceptable, du méquinol, au moins un agent dépigmentant tel qu'un AHA et au moins un filtre solaire.
La composition selon l'invention comprend avantageusement entre 0,0001 et 20 %
en poids de méquinol par rapport au poids total de la composition et entre 0,025 et 20 % en poids d'agent dépigmentant par rapport au poids total de la composition, et de préférence, 2o respectivement, entre 0,001 et 10 % en poids de méquinol par rapport au poids total de la composition et entre 0,05 et 10 % en poids d'agent dépigmentant par rapport au poids total de la composition.
La composition peut également comprendre au moins un filtre solaire dans des concentrations préférentielles allant de 0.001 à 30.00 % en poids par rapport au poids total de la composition.
Parmi les filtres solaires, on peut citer à titre d'exemple non limitatif, les filtre solaires physiques tels que le dioxyde de titane, l'oxyde de zinc et les filtres solaires chimiques tels que l'octocrylene, l'ethylhexyl methoxycinnamate, l'octyl salicylate, l'avobenzone, l'oxybenzone ou le drometrizole trisiloxane ou leurs mélanges.
Dans une variante de réalisation de la présente invention, la composition pourra comprendre plusieurs filtres solaires. Auquel cas, chaque filtre solaire pourra être ajouté à
une concentration allant de 0.001 à 20% en poids par rapport au poids total de la composition. 3 PCT / FR2005 / 001212 potassium or ammonium, or an organic base such as triethanolamine or the amino acids (lysine, arginine).
When an α-hydroxy acid ester is used, it may be in particular a ester of methyl, ethyl, propyl, butyl, pentyl, hexyl or octyl.
It is preferable to use as useful hydroxylated alpha acids according to the invention, the acid malic acid, citric acid, lactic acid or glycolic acid.
The application of a composition containing the combination according to the invention provides a clear whitening of the skin.
The invention also relates to a depigmenting composition of the skin comprising in a physiologically acceptable medium, mequinol, at least one agent depigmenting agent such as an AHA and at least one sunscreen.
The composition according to the invention advantageously comprises between 0.0001 and 20%
in weight of mequinol relative to the total weight of the composition and between 0.025 and 20%
weight of depigmenting agent relative to the total weight of the composition, and preference, 2o, respectively, between 0.001 and 10% by weight of mequinol relative to total weight of the composition and between 0.05 and 10% by weight of depigmenting agent with respect to weight total of the composition.
The composition may also comprise at least one sunscreen in preferential concentrations ranging from 0.001 to 30.00% by weight relative to by weight total of the composition.
Among the sunscreens, mention may be made by way of non-limiting example, the solar filters such as titanium dioxide, zinc oxide and solar chemical such octocrylene, ethylhexyl methoxycinnamate, octyl salicylate, avobenzone, oxybenzone or trisiloxane drometrizole or mixtures thereof.
In an alternative embodiment of the present invention, the composition will include several sunscreens. In which case, each solar filter can be added to a concentration ranging from 0.001% to 20% by weight relative to the total weight of the composition.
4 Les compositions selon l'invention peuvent comprendre en outre tout additif usuellement utilisé dans le domaine cosmétique ou pharmaceutique, tel que des séquestrants, des antioxydants, des conservateurs, des charges, des électrolytes, des humectants, des colorants, de bases ou d'acides usuels, minéraux ou organiques, des parfums, des huiles essentielles, des actifs cosmétiques, des hydratants, des vitamines, des acides gras essentiels, des sphingolipides, des composés auto-bronzants, des agents apaisants et protecteurs de la peau. Bien entendu l'homme du métier veillera à choisir ce ou ces éventuels composés complémentaires, et/ou leur quantité, de manière telle que les propriétés avantageuses de la composition selon l'invention ne soient pas, ou lo substantiellement pas, altérées.
Ces additifs peuvent être présents dans la composition à raison de 0,001 à 20 % en poids par rapport au poids total de la composition.
La présente invention a aussi pour objet une composition pharmaceutique telle que décrite précédemment à titre de médicament.
La présente invention a également pour objet une composition cosmétique.
2o Les compositions contenant l'association selon l'invention peuvent présenter toutes les formes galéniques normalement utilisées pour une application topique, par exemple sous forme de solutions, de gels, de dispersions du type lotion ou sérum, d'émulsions de consistance liquide ou semi-liquide du type lait, obtenues par dispersion d'une phase grasse dans une phase aqueuse (H/E) ou inversement (E/H), ou de suspensions ou émulsions de consistance molle, semi-solide ou solide du type crème ou gel, ou encore de microémulsions, de microcapsules, de microparticules ou de dispersions vésiculaires de type ionique et/ou non ionique. Ces compositions sont préparées selon les méthodes usuelles.
3o De façon connue, les compositions cosmétiques ou dermatologiques de l'invention peuvent contenir des adjuvants habituels dans le domaine cosmétique ou dermatologique, tels que les émulsionnants, les gélifiants hydrophiles ou lipophiles, les actifs hydrophiles ou lipophiles différents de l'oxyde de titane et de l'a-hydroxyacide, les conservateurs, les antioxydants, les parfums, les charges, les filtres et les matières colorantes. Les quantités de ces différents adjuvants sont celles classiquement utilisées dans les domaines cosmétique et/ou dermatologique, et par exemple de 0,01 % à
20 %
du poids total de la composition. Ces adjuvants, selon leur nature, peuvent être introduits dans la phase grasse, dans la phase aqueuse et/ou dans les vésicules lipidiques.
L'invention se rapporte également à l'utilisation de la composition selon l'invention telle 4 The compositions according to the invention may furthermore comprise any additive usually used in the cosmetic or pharmaceutical field, such as sequestrants, antioxidants, preservatives, fillers, electrolytes, humectants, dyes, bases or usual acids, mineral or organic, perfumes, oils essential ingredients, cosmetic active ingredients, moisturizers, vitamins, Fatty acids essential ingredients, sphingolipids, self-tanning compounds, soothing and skin protectors. Of course, the person skilled in the art will take care to choose this or these possible additional compounds, and / or their quantity, in such a way that the advantageous properties of the composition according to the invention are not, or lo not substantially, altered.
These additives may be present in the composition in a proportion of 0.001 to 20 % in weight relative to the total weight of the composition.
The present invention also relates to a pharmaceutical composition such than previously described as a drug.
The present invention also relates to a cosmetic composition.
The compositions containing the combination according to the invention can present all galenic forms normally used for topical application, for example example under form of solutions, gels, dispersions of the lotion or serum type, of emulsions liquid or semi-liquid consistency of the milk type, obtained by dispersion of a phase fat in an aqueous phase (O / W) or vice versa (W / O), or suspensions or emulsions of soft, semi-solid or solid consistency of the cream or gel type, or again microemulsions, microcapsules, microparticles or dispersions vesicular ionic and / or nonionic type. These compositions are prepared according to methods usual.
In known manner, the cosmetic or dermatological compositions of the invention may contain adjuvants usual in the cosmetic field or dermatological agents, such as emulsifiers, hydrophilic gelling agents or lipophilic hydrophilic or lipophilic active agents different from titanium oxide and hydroxyacid, the preservatives, antioxidants, fragrances, fillers, filters and Contents coloring. The amounts of these various adjuvants are those classically used in the cosmetic and / or dermatological fields, and for example from 0.01% to 20%
of the total weight of the composition. These adjuvants, depending on their nature, may to be introduced in the fatty phase, in the aqueous phase and / or in the vesicles lipid.
The invention also relates to the use of the composition according to the invention
5 que décrite précédemment dans le domaine pharmaceutique et cosmétique.
Les compositions de l'invention conviennent particulièrement bien au traitement et à la prévention des désordres de la pigmentation. Préférentiellement, les compositions de l'invention conviennent au traitement et à la prévention des désordres hyperpigmentaires 1o tels que le melasma, le chloasma, les lentigines, le lentigo sénile, le vitiligo, les taches de rousseur, les hyperpigmentations post-inflammatoires dues à une abrasion, une brûlure, une cicatrice, une dermatose, une allergie de contact; les nevi, les hyperpigmentations à
déterminisme génétique, les hyperpigmentations d'origine métabolique ou médicamenteuse, les mélanomes ou toutes autres lésions pigmentaires, notamment celles induites par le vieillissement photo induit ou chronologique de la peau et des phanères.
Plus préférentiellement les compositions selon l'invention conviennent au traitement du mélasma.
Les compositions selon l'invention trouvent également une application dans le domaine cosmétique, en particulier dans la protection contre les aspects néfastes du soleil, en particulier, contre les taches pigmentaires.
L'invention porte également sur un procédé de traitement cosmétique non thérapeutique d'embellissement de la peau et/ou d'amélioration de son aspect de surface, caractérisé
par le fait que l'on applique sur la peau et/ou ses phanères une composition comprenant du méquinol et au moins un agent dépigmentant.
Le méquinol et l'a.-hydroxyacide sont utilisés en quantité efficace de façon à
voir visiblement un blanchiment de la peau dès l'application de ladite composition.
Les exemples de formulations ci-dessous permettent d'illustrer les compositions selon l'invention, sans toutefois en limiter la portée. 5 as previously described in the pharmaceutical and cosmetic field.
The compositions of the invention are particularly suitable for treatment and to prevention of disorders of pigmentation. Preferentially, compositions of the invention are suitable for the treatment and prevention of disorders hyperpigmentation 1o such as melasma, chloasma, lentigines, senile lentigo, vitiligo, the spots of freckling, post-inflammatory hyperpigmentations due to abrasion, burn, a scar, dermatitis, contact allergy; the nevi, the hyperpigmentations to genetic determinism, hyperpigmentations of metabolic origin or medicinal products, melanomas or any other pigmented lesions, in particular those induced by aging photo induced or chronological skin and appendages.
More preferentially, the compositions according to the invention are suitable for treatment of melasma.
The compositions according to the invention also find an application in the field cosmetics, in particular in the protection against the harmful aspects of sun, in particular, against the pigment spots.
The invention also relates to a non-cosmetic cosmetic treatment method therapeutic beautifying the skin and / or improving its surface appearance, characterized in that a composition is applied to the skin and / or its integuments comprising mequinol and at least one depigmenting agent.
Mequinol and the α-hydroxy acid are used in an effective amount so as to see visibly a bleaching of the skin from the application of said composition.
The sample formulations below illustrate the compositions according to the invention without limiting its scope.
6 Dans les compositions ci-après (exemples 1 à 6), les proportions des différents constituants sont exprimées en pourcentage en poids par rapport au poids total de la composition.
Exemple 1 :
Matières premières Quantités en % poids pour poids Eau purifiée Qsp 100 EDTA 0.1 Carbomer 0.6 Gomme de xanthane 0.4 Solution.aqueuse de trisamino 10% (qsp pH 5.5-6.0) 4 Métabisulfite de sodium 0.2 Sulfite de sodium 0.2 Méquinol 4 Phenoxyethanol 1 Ethanol 20 Propylène glycol 5 Glycérine 5 Acide citrique 0.05 Exemple 2:
Matières premières Quantités en % poids pour poids Méquinol 0.10 Silicate d'aluminium ma nesium 3.00 But lh drox toluene 0.04 Methyl paraben 0.18 Propyl paraben 0.02 Alcool cet li ue 4 Acide stéarique 3 Alcool stea li ue 4 GI ce I stearate / PEG 100 stearate 3.5 Methyl gluceth 10 5 Métabisulfite de sodium 0.2 Glycérine 4 Acide malique 0.05 Eau purifiée qsp 100 1o Exemple 3:
Matières premières Quantités en % poids pour poids Eau purifiée qsp 100 6 In the compositions below (Examples 1 to 6), the proportions of the different constituents are expressed as a percentage by weight relative to the total weight of the composition.
Example 1 Raw materials Quantities in% by weight for weight Purified water Qs 100 EDTA 0.1 Carbomer 0.6 0.4 xanthan gum 10% trisamino solution (qsp pH 5.5-6.0) 4 Sodium metabisulfite 0.2 Sodium sulphite 0.2 Mequinol 4 Phenoxyethanol 1 Ethanol 20 Propylene glycol 5 Glycerin 5 Citric acid 0.05 Example 2 Raw materials Quantities in% by weight for weight Mequinol 0.10 Aluminum silicate ma nesium 3.00 But lh drox toluene 0.04 Methyl paraben 0.18 Propyl paraben 0.02 Alcohol this liu 4 Stearic acid 3 Steal alcohol 4 GI this I stearate / PEG 100 stearate 3.5 Methyl gluceth 10 5 Sodium metabisulfite 0.2 Glycerin 4 Malic acid 0.05 Purified water qs 100 1o Example 3:
Raw materials Quantities in% weight for weight Purified water qs 100
7 Methyl paraben 0.20 Glycérine 5 GI cer I stearate / PEG 100 stearate 2.30 GI ce I stearate / sodium lauryl sulfate 8.00 Cetearyl alcohol / ceteareth 20 1.00 Mineral oil 9.00 Propyl paraben 0.10 Métabisulfite de sodium 0.15 Méquinol 2 Acide lactique 0.06 Triéthanolamine Qs pH 4.5 Exemple 4:
Matières premières Quantités en % poids pour poids Mé uinol 0.10 Silicate d'aluminium ma nesium 3.00 But Ih drox toluene 0.04 Methyl paraben 0.18 Propyl paraben 0.02 Alcool cet li ue 4 Acide stéarique 3 Alcool stearylique 4 GI ce I stearate / PEG 100 stearate 3.5 Methyl gluceth 10 5 Métabisulfite de sodium 0.2 Dioxyde de titane 5 GI cérine 4 Acide malique 0.05 Eau purifiée qsp 100 Exemple 5:
Matières premières Quantités en % poids pour poids Eau purifiée s 100 Methyl paraben 0.20 Glycérine 5 GI cer I stearate / PEG 100 stearate 2.30 GI ce I stearate / sodium lauryl sulfate 8.00 Cetearyl alcohol / ceteareth 20 1.00 Mineral oil 9.00 Avobenzone 2 Oxyde de zinc 2 Propyl paraben 0.10 Métabisulfite de sodium 0.15 Mé uinol 2 Acide lactique 0.06 7 Methyl paraben 0.20 Glycerin 5 GI cer I stearate / PEG 100 stearate 2.30 GI this I stearate / sodium lauryl sulfate 8.00 Cetearyl alcohol / ceteareth 20 1.00 Mineral oil 9.00 Propyl paraben 0.10 Sodium metabisulfite 0.15 Mequinol 2 Lactic acid 0.06 Triethanolamine Qs pH 4.5 Example 4 Raw materials Quantities in% by weight for weight Meinol 0.10 Aluminum silicate ma nesium 3.00 Goal Ih drox toluene 0.04 Methyl paraben 0.18 Propyl paraben 0.02 Alcohol this liu 4 Stearic acid 3 Stearyl alcohol 4 GI this I stearate / PEG 100 stearate 3.5 Methyl gluceth 10 5 Sodium metabisulfite 0.2 Titanium dioxide 5 GI cerine 4 Malic acid 0.05 Purified water qs 100 Example 5 Raw materials Quantities in% weight for weight Purified water 100 Methyl paraben 0.20 Glycerin 5 GI cer I stearate / PEG 100 stearate 2.30 GI this I stearate / sodium lauryl sulfate 8.00 Cetearyl alcohol / ceteareth 20 1.00 Mineral oil 9.00 Avobenzone 2 Zinc oxide 2 Propyl paraben 0.10 Sodium metabisulfite 0.15 Me uinol 2 Lactic acid 0.06
8 Triéthanolamine Qs H 4.5 Exemple 6:
Matières premières Quantités en % poids pour poids Eau purifiée gsp 100 Methyl paraben 0.20 Glycérine 5 GI ce I stearate / PEG 100 stearate 2.30 GI ce I stearate / sodium lauryl sulfate 8.00 Cetearyl alcohol / ceteareth 20 1.00 Mineral oil 9.00 Avobenzone 2 Octocrylène 10 Propyl paraben 0.10 Métabisulfite de sodium 0.15 Mé uinol 2 Acide lactique 0.06 Triéthanolamine Qs pH 4.5 8 Triethanolamine Qs H 4.5 Example 6 Raw materials Quantities in% weight for weight Purified water gsp 100 Methyl paraben 0.20 Glycerin 5 GI this I stearate / PEG 100 stearate 2.30 GI this I stearate / sodium lauryl sulfate 8.00 Cetearyl alcohol / ceteareth 20 1.00 Mineral oil 9.00 Avobenzone 2 Octocrylene 10 Propyl paraben 0.10 Sodium metabisulfite 0.15 Me uinol 2 Lactic acid 0.06 Triethanolamine Qs pH 4.5
Claims (10)
- le méquinol (ou 4-hydroxyanisole) et - au moins un alpha-hydroxy acide à une concentration comprise entre 0,025 et 20 % en poids par rapport au poids total de la composition, dans un véhicule physiologiquement acceptable. 1. Composition comprising an association with depigmenting activity constituted by:
mequinol (or 4-hydroxyanisole) and at least one alpha-hydroxy acid at a concentration of between 0.025 and 20% by weight relative to the total weight of the composition, in a physiologically acceptable vehicle.
prévenir ou à traiter des désordres de la pigmentation. 6. Use of a depigmenting composition of the skin comprising mequinol and a alpha hydroxylated acid for the manufacture of a pharmaceutical preparation destined to to prevent or treat disorders of pigmentation.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| FR0405281A FR2870123A1 (en) | 2004-05-14 | 2004-05-14 | DEPIGMENTING DERMATOLOGICAL COMPOSITION BASED ON MEQUINOL |
| FR0405281 | 2004-05-14 | ||
| PCT/FR2005/001212 WO2005115323A1 (en) | 2004-05-14 | 2005-05-13 | Mequinol-based dermatological depigmenting composition |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA2564077A1 true CA2564077A1 (en) | 2005-12-08 |
Family
ID=34945900
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA002564077A Abandoned CA2564077A1 (en) | 2004-05-14 | 2005-05-13 | Mequinol-based dermatological depigmenting composition |
Country Status (5)
| Country | Link |
|---|---|
| EP (1) | EP1755542A1 (en) |
| JP (1) | JP2007537217A (en) |
| CA (1) | CA2564077A1 (en) |
| FR (1) | FR2870123A1 (en) |
| WO (1) | WO2005115323A1 (en) |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5389677B1 (en) * | 1986-12-23 | 1997-07-15 | Tristrata Inc | Method of treating wrinkles using glycalic acid |
| US5874463A (en) * | 1994-10-24 | 1999-02-23 | Ancira; Margaret | Hydroxy-kojic acid skin peel |
| US6353029B1 (en) * | 2000-08-24 | 2002-03-05 | Bristol-Myers Squibb Company | Storage stable tretinoin and 4-hydroxyanisole containing topical composition |
-
2004
- 2004-05-14 FR FR0405281A patent/FR2870123A1/en active Pending
-
2005
- 2005-05-13 JP JP2007512292A patent/JP2007537217A/en active Pending
- 2005-05-13 EP EP05771158A patent/EP1755542A1/en not_active Withdrawn
- 2005-05-13 CA CA002564077A patent/CA2564077A1/en not_active Abandoned
- 2005-05-13 WO PCT/FR2005/001212 patent/WO2005115323A1/en not_active Ceased
Also Published As
| Publication number | Publication date |
|---|---|
| JP2007537217A (en) | 2007-12-20 |
| FR2870123A1 (en) | 2005-11-18 |
| EP1755542A1 (en) | 2007-02-28 |
| WO2005115323A1 (en) | 2005-12-08 |
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