FR2894481A1 - USE OF A DERMATOLOGICAL COMPOSITION COMPRISING A COMBINATION OF HYDROQUINONE, FLUOCINOLONE ACETONIDE AND TRETINOINE FOR THE TREATMENT OF HYPERPIGMENTATION OF NON-CAUCASIAN SKINS - Google Patents
USE OF A DERMATOLOGICAL COMPOSITION COMPRISING A COMBINATION OF HYDROQUINONE, FLUOCINOLONE ACETONIDE AND TRETINOINE FOR THE TREATMENT OF HYPERPIGMENTATION OF NON-CAUCASIAN SKINS Download PDFInfo
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- FR2894481A1 FR2894481A1 FR0512679A FR0512679A FR2894481A1 FR 2894481 A1 FR2894481 A1 FR 2894481A1 FR 0512679 A FR0512679 A FR 0512679A FR 0512679 A FR0512679 A FR 0512679A FR 2894481 A1 FR2894481 A1 FR 2894481A1
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- composition
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- use according
- hydroquinone
- skin
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- QIGBRXMKCJKVMJ-UHFFFAOYSA-N Hydroquinone Chemical compound OC1=CC=C(O)C=C1 QIGBRXMKCJKVMJ-UHFFFAOYSA-N 0.000 title claims abstract description 31
- 239000000203 mixture Substances 0.000 title claims abstract description 28
- SHGAZHPCJJPHSC-YCNIQYBTSA-N all-trans-retinoic acid Chemical compound OC(=O)\C=C(/C)\C=C\C=C(/C)\C=C\C1=C(C)CCCC1(C)C SHGAZHPCJJPHSC-YCNIQYBTSA-N 0.000 title claims abstract description 15
- FEBLZLNTKCEFIT-VSXGLTOVSA-N fluocinolone acetonide Chemical compound C1([C@@H](F)C2)=CC(=O)C=C[C@]1(C)[C@]1(F)[C@@H]2[C@@H]2C[C@H]3OC(C)(C)O[C@@]3(C(=O)CO)[C@@]2(C)C[C@@H]1O FEBLZLNTKCEFIT-VSXGLTOVSA-N 0.000 title claims abstract description 14
- 229960001347 fluocinolone acetonide Drugs 0.000 title claims abstract description 14
- 208000000069 hyperpigmentation Diseases 0.000 title claims abstract description 9
- 230000003810 hyperpigmentation Effects 0.000 title claims abstract description 9
- 229960004337 hydroquinone Drugs 0.000 claims abstract description 13
- 229960001727 tretinoin Drugs 0.000 claims abstract description 13
- 239000002537 cosmetic Substances 0.000 claims abstract description 6
- VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 claims description 9
- 239000006071 cream Substances 0.000 claims description 6
- 239000003795 chemical substances by application Substances 0.000 claims description 5
- BXWNKGSJHAJOGX-UHFFFAOYSA-N n-hexadecyl alcohol Natural products CCCCCCCCCCCCCCCCO BXWNKGSJHAJOGX-UHFFFAOYSA-N 0.000 claims description 4
- GLDOVTGHNKAZLK-UHFFFAOYSA-N n-octadecyl alcohol Natural products CCCCCCCCCCCCCCCCCCO GLDOVTGHNKAZLK-UHFFFAOYSA-N 0.000 claims description 4
- LXCFILQKKLGQFO-UHFFFAOYSA-N p-hydroxybenzoic acid methyl ester Natural products COC(=O)C1=CC=C(O)C=C1 LXCFILQKKLGQFO-UHFFFAOYSA-N 0.000 claims description 4
- 235000010262 sodium metabisulphite Nutrition 0.000 claims description 4
- 239000004322 Butylated hydroxytoluene Substances 0.000 claims description 3
- 235000021355 Stearic acid Nutrition 0.000 claims description 3
- 238000004061 bleaching Methods 0.000 claims description 3
- 235000010354 butylated hydroxytoluene Nutrition 0.000 claims description 3
- 229940095259 butylated hydroxytoluene Drugs 0.000 claims description 3
- 229960000541 cetyl alcohol Drugs 0.000 claims description 3
- 235000010270 methyl p-hydroxybenzoate Nutrition 0.000 claims description 3
- 239000004292 methyl p-hydroxybenzoate Substances 0.000 claims description 3
- 229960002216 methylparaben Drugs 0.000 claims description 3
- GOQYKNQRPGWPLP-UHFFFAOYSA-N n-heptadecyl alcohol Natural products CCCCCCCCCCCCCCCCCO GOQYKNQRPGWPLP-UHFFFAOYSA-N 0.000 claims description 3
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 claims description 3
- 229940100460 peg-100 stearate Drugs 0.000 claims description 3
- 239000004405 propyl p-hydroxybenzoate Substances 0.000 claims description 3
- 229960003415 propylparaben Drugs 0.000 claims description 3
- 239000008213 purified water Substances 0.000 claims description 3
- 239000008117 stearic acid Substances 0.000 claims description 3
- 230000000699 topical effect Effects 0.000 claims description 3
- 239000002253 acid Substances 0.000 claims description 2
- YQEMORVAKMFKLG-UHFFFAOYSA-N glycerine monostearate Natural products CCCCCCCCCCCCCCCCCC(=O)OC(CO)CO YQEMORVAKMFKLG-UHFFFAOYSA-N 0.000 claims description 2
- SVUQHVRAGMNPLW-UHFFFAOYSA-N glycerol monostearate Natural products CCCCCCCCCCCCCCCCC(=O)OCC(O)CO SVUQHVRAGMNPLW-UHFFFAOYSA-N 0.000 claims description 2
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 claims description 2
- 238000002360 preparation method Methods 0.000 claims description 2
- XAGFODPZIPBFFR-UHFFFAOYSA-N aluminium Chemical compound [Al] XAGFODPZIPBFFR-UHFFFAOYSA-N 0.000 claims 1
- 229910052782 aluminium Inorganic materials 0.000 claims 1
- SRMHVPHBKYGDRR-UHFFFAOYSA-N benzene-1,4-diol;2-hydroxypropane-1,2,3-tricarboxylic acid Chemical compound OC1=CC=C(O)C=C1.OC(=O)CC(O)(C(O)=O)CC(O)=O SRMHVPHBKYGDRR-UHFFFAOYSA-N 0.000 claims 1
- 229910052919 magnesium silicate Inorganic materials 0.000 claims 1
- 235000019792 magnesium silicate Nutrition 0.000 claims 1
- 239000000391 magnesium silicate Substances 0.000 claims 1
- 239000004296 sodium metabisulphite Substances 0.000 claims 1
- 230000035614 depigmentation Effects 0.000 abstract description 3
- 230000002087 whitening effect Effects 0.000 abstract 1
- 210000003491 skin Anatomy 0.000 description 34
- 239000003814 drug Substances 0.000 description 13
- 229940079593 drug Drugs 0.000 description 7
- 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 6
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 6
- -1 defoamers Substances 0.000 description 4
- 239000000126 substance Substances 0.000 description 4
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 3
- 230000002209 hydrophobic effect Effects 0.000 description 3
- 239000012071 phase Substances 0.000 description 3
- QELSKZZBTMNZEB-UHFFFAOYSA-N propylparaben Chemical compound CCCOC(=O)C1=CC=C(O)C=C1 QELSKZZBTMNZEB-UHFFFAOYSA-N 0.000 description 3
- 229940001584 sodium metabisulfite Drugs 0.000 description 3
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 3
- AZQWKYJCGOJGHM-UHFFFAOYSA-N 1,4-benzoquinone Chemical compound O=C1C=CC(=O)C=C1 AZQWKYJCGOJGHM-UHFFFAOYSA-N 0.000 description 2
- 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
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 description 2
- 201000004624 Dermatitis Diseases 0.000 description 2
- 208000012641 Pigmentation disease Diseases 0.000 description 2
- 239000012455 biphasic mixture Substances 0.000 description 2
- 150000001875 compounds Chemical class 0.000 description 2
- 239000007854 depigmenting agent Substances 0.000 description 2
- 230000000694 effects Effects 0.000 description 2
- 235000011187 glycerol Nutrition 0.000 description 2
- 210000004209 hair Anatomy 0.000 description 2
- BJRNKVDFDLYUGJ-RMPHRYRLSA-N hydroquinone O-beta-D-glucopyranoside Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@H]1OC1=CC=C(O)C=C1 BJRNKVDFDLYUGJ-RMPHRYRLSA-N 0.000 description 2
- 208000014674 injury Diseases 0.000 description 2
- 238000000034 method Methods 0.000 description 2
- 229940100485 methyl gluceth-10 Drugs 0.000 description 2
- 230000003647 oxidation Effects 0.000 description 2
- 238000007254 oxidation reaction Methods 0.000 description 2
- 230000019612 pigmentation Effects 0.000 description 2
- 235000010232 propyl p-hydroxybenzoate Nutrition 0.000 description 2
- HRZFUMHJMZEROT-UHFFFAOYSA-L sodium disulfite Chemical compound [Na+].[Na+].[O-]S(=O)S([O-])(=O)=O HRZFUMHJMZEROT-UHFFFAOYSA-L 0.000 description 2
- 239000002904 solvent Substances 0.000 description 2
- 239000000516 sunscreening agent Substances 0.000 description 2
- 229940051117 tri-luma Drugs 0.000 description 2
- ATTPXNCCXYEULE-JOBJWGHLSA-N triluma Chemical compound OC1=CC=C(O)C=C1.OC(=O)\C=C(/C)\C=C\C=C(/C)\C=C\C1=C(C)CCCC1(C)C.C1([C@@H](F)C2)=CC(=O)C=C[C@]1(C)[C@]1(F)[C@@H]2[C@@H]2C[C@H]3OC(C)(C)O[C@@]3(C(=O)CO)[C@@]2(C)C[C@@H]1O ATTPXNCCXYEULE-JOBJWGHLSA-N 0.000 description 2
- 208000002874 Acne Vulgaris Diseases 0.000 description 1
- NLZUEZXRPGMBCV-UHFFFAOYSA-N Butylhydroxytoluene Chemical compound CC1=CC(C(C)(C)C)=C(O)C(C(C)(C)C)=C1 NLZUEZXRPGMBCV-UHFFFAOYSA-N 0.000 description 1
- QWOJMRHUQHTCJG-UHFFFAOYSA-N CC([CH2-])=O Chemical compound CC([CH2-])=O QWOJMRHUQHTCJG-UHFFFAOYSA-N 0.000 description 1
- 206010033546 Pallor Diseases 0.000 description 1
- 206010040829 Skin discolouration Diseases 0.000 description 1
- DWAQJAXMDSEUJJ-UHFFFAOYSA-M Sodium bisulfite Chemical compound [Na+].OS([O-])=O DWAQJAXMDSEUJJ-UHFFFAOYSA-M 0.000 description 1
- 208000027418 Wounds and injury Diseases 0.000 description 1
- 238000005299 abrasion Methods 0.000 description 1
- 239000003082 abrasive agent Substances 0.000 description 1
- 239000002250 absorbent Substances 0.000 description 1
- 230000002745 absorbent Effects 0.000 description 1
- 239000006096 absorbing agent Substances 0.000 description 1
- 230000035508 accumulation Effects 0.000 description 1
- 238000009825 accumulation Methods 0.000 description 1
- 150000007513 acids Chemical class 0.000 description 1
- 206010000496 acne Diseases 0.000 description 1
- 239000000654 additive Substances 0.000 description 1
- 239000003470 adrenal cortex hormone Substances 0.000 description 1
- 230000002411 adverse Effects 0.000 description 1
- 230000016571 aggressive behavior Effects 0.000 description 1
- SNAAJJQQZSMGQD-UHFFFAOYSA-N aluminum magnesium Chemical compound [Mg].[Al] SNAAJJQQZSMGQD-UHFFFAOYSA-N 0.000 description 1
- 229940035676 analgesics Drugs 0.000 description 1
- 239000000730 antalgic agent Substances 0.000 description 1
- 239000000058 anti acne agent Substances 0.000 description 1
- 230000003110 anti-inflammatory effect Effects 0.000 description 1
- 229940124340 antiacne agent Drugs 0.000 description 1
- 239000004599 antimicrobial Substances 0.000 description 1
- 239000003963 antioxidant agent Substances 0.000 description 1
- 235000006708 antioxidants Nutrition 0.000 description 1
- 239000008346 aqueous phase Substances 0.000 description 1
- 229960000271 arbutin Drugs 0.000 description 1
- 235000010323 ascorbic acid Nutrition 0.000 description 1
- 229960005070 ascorbic acid Drugs 0.000 description 1
- 239000011668 ascorbic acid Substances 0.000 description 1
- 239000003212 astringent agent Substances 0.000 description 1
- 239000011230 binding agent Substances 0.000 description 1
- 239000003139 biocide Substances 0.000 description 1
- 239000006172 buffering agent Substances 0.000 description 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 description 1
- 239000002738 chelating agent Substances 0.000 description 1
- 229960004106 citric acid Drugs 0.000 description 1
- 239000003086 colorant Substances 0.000 description 1
- 239000000470 constituent Substances 0.000 description 1
- 230000006378 damage Effects 0.000 description 1
- 230000007547 defect Effects 0.000 description 1
- 230000008021 deposition Effects 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 208000035475 disorder Diseases 0.000 description 1
- 239000000975 dye Substances 0.000 description 1
- 235000013399 edible fruits Nutrition 0.000 description 1
- 239000003974 emollient agent Substances 0.000 description 1
- 239000003995 emulsifying agent Substances 0.000 description 1
- 239000000839 emulsion Substances 0.000 description 1
- 229940043075 fluocinolone Drugs 0.000 description 1
- 239000012634 fragment Substances 0.000 description 1
- 229960005150 glycerol Drugs 0.000 description 1
- 229940075529 glyceryl stearate Drugs 0.000 description 1
- 239000003906 humectant Substances 0.000 description 1
- 150000002433 hydrophilic molecules Chemical class 0.000 description 1
- 208000031066 hyperpigmentation of the skin Diseases 0.000 description 1
- 239000005414 inactive ingredient Substances 0.000 description 1
- 230000002757 inflammatory effect Effects 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 230000007794 irritation Effects 0.000 description 1
- 239000003410 keratolytic agent Substances 0.000 description 1
- BEJNERDRQOWKJM-UHFFFAOYSA-N kojic acid Chemical compound OCC1=CC(=O)C(O)=CO1 BEJNERDRQOWKJM-UHFFFAOYSA-N 0.000 description 1
- 229960004705 kojic acid Drugs 0.000 description 1
- WZNJWVWKTVETCG-UHFFFAOYSA-N kojic acid Natural products OC(=O)C(N)CN1C=CC(=O)C(O)=C1 WZNJWVWKTVETCG-UHFFFAOYSA-N 0.000 description 1
- 239000002932 luster Substances 0.000 description 1
- 230000036244 malformation Effects 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 210000002752 melanocyte Anatomy 0.000 description 1
- 230000008450 motivation Effects 0.000 description 1
- 210000004400 mucous membrane Anatomy 0.000 description 1
- 230000009965 odorless effect Effects 0.000 description 1
- BJRNKVDFDLYUGJ-UHFFFAOYSA-N p-hydroxyphenyl beta-D-alloside Natural products OC1C(O)C(O)C(CO)OC1OC1=CC=C(O)C=C1 BJRNKVDFDLYUGJ-UHFFFAOYSA-N 0.000 description 1
- 239000002304 perfume Substances 0.000 description 1
- 239000000049 pigment Substances 0.000 description 1
- 239000004014 plasticizer Substances 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 108090000623 proteins and genes Proteins 0.000 description 1
- 206010037844 rash Diseases 0.000 description 1
- 235000020945 retinal Nutrition 0.000 description 1
- 239000011604 retinal Substances 0.000 description 1
- 229930002330 retinoic acid Natural products 0.000 description 1
- 210000004761 scalp Anatomy 0.000 description 1
- 239000003352 sequestering agent Substances 0.000 description 1
- 230000009759 skin aging Effects 0.000 description 1
- 210000004927 skin cell Anatomy 0.000 description 1
- 230000037370 skin discoloration Effects 0.000 description 1
- 239000003009 skin protective agent Substances 0.000 description 1
- 210000003625 skull Anatomy 0.000 description 1
- 235000010267 sodium hydrogen sulphite Nutrition 0.000 description 1
- 230000036561 sun exposure Effects 0.000 description 1
- 230000000475 sunscreen effect Effects 0.000 description 1
- 239000004094 surface-active agent Substances 0.000 description 1
- 230000008733 trauma Effects 0.000 description 1
- 229930003231 vitamin Natural products 0.000 description 1
- 239000011782 vitamin Substances 0.000 description 1
- 235000013343 vitamin Nutrition 0.000 description 1
- 229940088594 vitamin Drugs 0.000 description 1
- 150000003722 vitamin derivatives Chemical class 0.000 description 1
Classifications
-
- 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
- A61K8/35—Ketones, e.g. benzophenone
- A61K8/355—Quinones
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/045—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
- A61K31/05—Phenols
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/20—Carboxylic acids, e.g. valproic acid having a carboxyl group bound to a chain of seven or more carbon atoms, e.g. stearic, palmitic, arachidic acids
- A61K31/203—Retinoic acids ; Salts thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
- A61K31/585—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin containing lactone rings, e.g. oxandrolone, bufalin
-
- 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
- A61K8/37—Esters of carboxylic acids
-
- 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
- A61K8/63—Steroids; Derivatives thereof
-
- 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
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)
- Epidemiology (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Birds (AREA)
- Emergency Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Dermatology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Cosmetics (AREA)
Abstract
La présente invention concerne une composition comprenant une association d'hydroquinone, de trétinoïne et d'acétonide de fluocinolone, destinée au traitement de l'hyperpigmentation des peaux non caucasiennes ou à la dépigmentation ou au blanchiment des peaux non caucasiennes. L'invention concerne également les applications cosmétiques d'une telle composition.The present invention relates to a composition comprising a combination of hydroquinone, tretinoin and fluocinolone acetonide, for the treatment of hyperpigmentation of non-Caucasian skin or depigmentation or whitening of non-Caucasian skin. The invention also relates to the cosmetic applications of such a composition.
Description
E.E.
La présente invention se rapporte à une composition, notamment dermatologique, comprenant une association d'hydroquinone, de trétinoïne et d'acétonide de fluocinolone, destinée au traitement de l'hyperpigmentation des peaux non caucasiennes ou à la dépigmentation ou au blanchiment des peaux non caucasiennes. L'invention se rapporte également aux utilisations cosmétiques d'une telle composition, tel que le rafraîchissement du teint des peaux non caucasiennes. The present invention relates to a composition, especially dermatological, comprising a combination of hydroquinone, tretinoin and fluocinolone acetonide, for the treatment of hyperpigmentation of non-Caucasian skin or depigmentation or bleaching of non-Caucasian skin . The invention also relates to the cosmetic uses of such a composition, such as refreshing the complexion of non-Caucasian skin.
L'hyperpigmentation de la peau est un trouble courant se manifestant par l'apparition de taches brunes ou colorées sur des fragments de peau. Hyperpigmentation of the skin is a common disorder manifested by the appearance of brown or colored spots on skin fragments.
L'hyperpigmentation se produit lors d'accumulations de mélanine sur la peau, conférant à la peau une hétérogénéité. Les taches pigmentées peuvent apparaître sur toutes les parties du corps, en particulier sur le dos des mains, sur le visage, le décolleté et le crâne des hommes. Il s'agit de malformations cutanées, de multiplications locales et bénignes des cellules de la peau formant le pigment (mélanocytes), et qui peuvent apparaître sous différentes couleurs. La prédisposition familiale joue un rôle dans l'apparition des taches pigmentées, ainsi que l'exposition au soleil fréquente. Ainsi, les gènes, le soleil et le vieillissement cutané sont les principaux facteurs qui influencent l'hyperpigmentation. En outre, des taches pigmentées peuvent apparaître suite à des agressions ou à des inflammations cutanées. Une augmentation de la production de mélanine peut ainsi être provoquée par un processus inflammatoire cutané entraînant des pigmentations induites par exemple après traumatismes, éruptions eczémateuses, ou d'autres irritations cutanées. Environ 30% des taches brunes sont ainsi dues à des inflammations de la peau. Hyperpigmentation occurs during accumulations of melanin on the skin, giving the skin a heterogeneity. Pigmented spots can appear on all parts of the body, especially on the backs of hands, on the face, décolleté and skull of men. These are cutaneous malformations, local and benign multiplications of skin cells forming the pigment (melanocytes), and which can appear in different colors. Familial predisposition plays a role in the appearance of pigmented spots, as well as frequent sun exposure. Thus, genes, sun and skin aging are the main factors that influence hyperpigmentation. In addition, pigmented spots may appear following aggression or skin inflammation. An increase in the production of melanin can thus be caused by an inflammatory skin process resulting in pigmentations induced for example after trauma, eczematous eruptions, or other cutaneous irritations. About 30% of brown spots are thus due to inflammation of the skin.
Les problèmes pigmentaires sont d'autant plus importants chez les phototypes foncés tels que les peaux non caucasiennes, en particulier les peaux asiatiques, noires, ou métisses. En effet, les peaux foncées telles que les peaux noires marquent très facilement. En cas de blessures, elles cicatrisent souvent très mal et en relief. De plus, toutes les petites affections cutanées, les imperfections, l'acné, les petites écorchures sont suivies d'une phase de réparation qui se traduit par l'apparition de taches brunes. En l'absence de traitement adapté, elles s'installent pendant plusieurs années. Pigmentary problems are especially important in dark phototypes such as non-Caucasian skin, especially Asian, black, or mixed skin. Indeed, dark skin such as black skin mark very easily. In case of injuries, they often heal very badly and in relief. In addition, all the small skin conditions, imperfections, acne, small abrasions are followed by a repair phase that results in the appearance of brown spots. In the absence of appropriate treatment, they settle for several years.
Divers produits du type vitamine C, acides de fruits, et filtres solaires ont été développés pour traiter ces problèmes de pigmentation, mais la plupart d'entre eux renferment des mélanges instables qui risquent de remplacer les taches sombres par des taches claires, plus visibles. Various vitamin C-type products, fruit acids, and sunscreens have been developed to treat these pigmentation problems, but most of them contain unstable mixtures that may replace dark spots with clear, more visible spots.
Il existe ainsi un besoin de traiter les taches d'hyperpigmentation et d'éliminer les défauts de la peau généralement dus au dépôt de quantités excessives de mélanine chez les sujets de phototype foncé, notamment les peaux non caucasiennes, telles que les peaux asiatiques, noires, ou métisses. There is thus a need to treat hyperpigmentation spots and to eliminate skin defects generally due to the deposition of excessive amounts of melanin in dark phototype subjects, especially non-Caucasian skin, such as Asian skin, black skin. , or mestizos.
Par ailleurs, il existe un besoin de pouvoir décolorer une peau non caucasienne normalement pigmentée afin d'accroître l'éclat du teint, ou afin d'uniformiser l'apparence de la peau. Les motivations qui poussent à décolorer la peau peuvent être diverses. L'éclaircissement franc du teint est souvent recherché en Afrique Noire ainsi que dans les pays asiatiques, avec des solutions traditionnelles ou chimiques qui présentent généralement des effets secondaires néfastes importants sur l'aspect et la structure de la peau. La pâleur ou la blancheur du visage asiatique est obtenue avec des molécules, telles que l'arbutine, l'acide kojique, ou l'acide ascorbique, qui peuvent être mal tolérées ou irritantes. On the other hand, there is a need to be able to discolor normally pigmented non-Caucasian skin to increase the radiance of the complexion, or to even out the appearance of the skin. The motivations that drive skin discoloration can be diverse. The clear lightening of the complexion is often sought in Black Africa as well as in Asian countries, with traditional or chemical solutions that generally have significant adverse side effects on the appearance and structure of the skin. The pallor or whiteness of the Asian face is obtained with molecules, such as arbutin, kojic acid, or ascorbic acid, which may be poorly tolerated or irritating.
Il existe donc un besoin de disposer de compositions présentant une activité dépigmentante ou éclaircissante et qui soient bien tolérées par la peau, notamment pour des peaux non caucasiennes, telles que les peaux hispaniques, indiennes, noires, asiatiques ou métisses. There is therefore a need for compositions having a depigmenting or lightening activity and which are well tolerated by the skin, especially for non-Caucasian skin, such as Hispanic, Indian, black, Asian or mixed skin.
Or, de façon surprenante, les inventeurs ont découvert que l'association d'hydroquinone, de trétinoïne, et d'acétonide de fluocinolone permettait de traiter efficacement l'hyperpigmentation des peaux non caucasiennes, et permettait également de dépigmenter ou de blanchir efficacement les peaux non caucasiennes, et d'augmenter l'éclat du teint de ces types de peaux. Surprisingly, the inventors have discovered that the combination of hydroquinone, tretinoin, and fluocinolone acetonide effectively treated the hyperpigmentation of non-Caucasian skin, and also effectively depigmented or whitened the skin. non-Caucasian, and increase the radiance of the complexion of these types of skin.
La présente invention a donc pour objet l'utilisation d'une association d'hydroquinone, de trétinoïne, et d'acétonide de fluocinolone, pour la préparation d'une composition destinée au traitement de 1'hyperpigmentation des peaux non caucasiennes ou au blanchiment des peaux non caucasiennes. Une telle composition est également destinée à la dépigmentation des peaux non caucasiennes. The present invention therefore relates to the use of a combination of hydroquinone, tretinoin, and fluocinolone acetonide, for the preparation of a composition intended for the treatment of hyperpigmentation of non-Caucasian skin or the bleaching of skin. non-caucasian skin. Such a composition is also intended for the depigmentation of non-Caucasian skin.
De façon avantageuse, les peaux non caucasiennes sont choisies parmi les peaux hispaniques, indiennes, noires, asiatiques ou métisses. Advantageously, non-Caucasian skins are chosen from Hispanic, Indian, Black, Asian or Métis skins.
Avantageusement, la composition selon l'invention est un médicament ; elle est de préférence destinée à une application topique. Advantageously, the composition according to the invention is a medicament; it is preferably intended for topical application.
Le médicament selon la présente invention comprend également un milieu physiologiquement acceptable, c'est-à-dire qui est compatible avec la peau, y compris le cuir chevelu, les muqueuses, les cheveux, les poils et/ou les yeux, et peut constituer une composition dermatologique. Cette composition peut comprendre tous les constituants habituellement présents dans le type d'application envisagé. The medicament according to the present invention also comprises a physiologically acceptable medium, that is to say which is compatible with the skin, including the scalp, the mucous membranes, the hair, the hairs and / or the eyes, and may constitute a dermatological composition. This composition may comprise all the constituents usually present in the type of application envisaged.
Le médicament selon la présente invention peut comprendre une grande variété de composants additionnels, en particulier il peut s'agir d'absorbants, d'abrasifs, d'agents anti-acné, d'agents anti-mousse, d'agents anti-microbiens, d'anti-oxydants, de liants, d'additifs biologiques, d'agents tampons, d'agents chélatants, de colorants, d'astringents cosmétiques, de biocides cosmétiques, d'analgésiques externes, d'agents formateur de films, de composants parfumés, d'agents opacifiants, de plastifiants, de conservateurs, d'autres agents dépigmentants, d'agents émollients, d'agents protecteurs de la peau, de solvants, d'agents solubilisants, d'agents surfactants, d'agents absorbant la lumière ultra-violette, d'agents écrans solaires, d'agents augmentant la viscosité (aqueux ou non aqueux), d'humectants, de séquestrants, etc. The drug according to the present invention may comprise a wide variety of additional components, in particular it may be absorbents, abrasives, anti-acne agents, defoamers, anti-microbial agents , antioxidants, binders, biological additives, buffering agents, chelating agents, dyes, cosmetic astringents, cosmetic biocides, external analgesics, film-forming agents, perfume components, opacifying agents, plasticizers, preservatives, other depigmenting agents, emollients, skin-protecting agents, solvents, solubilizing agents, surfactants, absorbing agents ultraviolet light, sunscreen agents, viscosity increasing agents (aqueous or non-aqueous), humectants, sequestering agents, etc.
Ces composants additionnels peuvent être présents dans le médicament selon la présente invention en une quantité comprise entre 0,001 et 20 % en poids par rapport au poids total de la composition. These additional components may be present in the drug according to the present invention in an amount of between 0.001 and 20% by weight relative to the total weight of the composition.
L'homme du métier sera évidemment attentif à choisir les composés additionnels possibles et/ou leur quantité de façon à ce que les propriétés avantageuses du médicament selon la présente invention ne soient pas totalement ou pas substantiellement diminuées par l'ajout envisagé. Those skilled in the art will obviously be careful to choose the possible additional compounds and / or their amount so that the advantageous properties of the drug according to the present invention are not totally or not substantially reduced by the envisaged addition.
La présente invention a également pour objet l'utilisation cosmétique d'une association d'hydroquinone, de trétinoine, et d'acétonide de fluocinolone, comme agent pour éclaircir le teint des peaux non caucasiennes, ou en augmenter l'éclat. Par augmenter l'éclat du teint, on entend un embellissement de l'aspect de la peau, et un éclaircissement préférentiellement uniforme de sa couleur. The present invention also relates to the cosmetic use of a combination of hydroquinone, tretinoin, and fluocinolone acetonide, as an agent for lightening the complexion of non-Caucasian skin, or increase its luster. By increasing the radiance of the complexion is meant an embellishment of the appearance of the skin, and a preferentially uniform lightening of its color.
L'hydroquinone est un agent dépigmentant connu. Il est préparé par réduction de la p-benzoquinone avec du bisulfite de sodium. Le nom chimique de l'hydroquinone est le 1,4-benzènediol. De façon avantageuse, l'hydroquinone est présente dans le médicament selon la présente invention à une concentration comprise entre 1 et 10% en poids, avantageusement entre 2 et 7%, et encore plus avantageusement d'environ 4% en poids, par rapport au poids total de la composition. Hydroquinone is a known depigmenting agent. It is prepared by reducing p-benzoquinone with sodium bisulfite. The chemical name of hydroquinone is 1,4-benzenediol. Advantageously, the hydroquinone is present in the drug according to the present invention at a concentration of between 1 and 10% by weight, advantageously between 2 and 7%, and still more advantageously of approximately 4% by weight, relative to total weight of the composition.
Le nom chimique de la trétinoïne est : l'acide (all-E)-3,7-diméthyl-9-(2,6,6-triméthyl-l-cyclohexèn-l-yl)-2,4,6, 8-nonatétraénoique. C'est un acide all-trans rétinoïque formé par l'oxydation du groupe aldéhyde du rétinène en groupe carboxyle. Il est très réactif à la lumière et à l'humidité. Il s'agit d'un agent kératolytique. Dans un mode de réalisation particulier, la trétinoine est présente dans le médicament selon la présente invention à une concentration comprise entre 0,025 et 2% en poids, avantageusement entre 0,025% et 1% en poids, encore plus avantageusement d'environ 0,05% en poids, par rapport au poids total de la composition. The chemical name of tretinoin is: (all-E) -3,7-dimethyl-9- (2,6,6-trimethyl-1-cyclohexen-1-yl) -2,4,6,8 -nonatétraénoique. It is an all-trans retinoic acid formed by the oxidation of the retinene aldehyde group to the carboxyl group. It is very reactive to light and moisture. It is a keratolytic agent. In a particular embodiment, tretinoin is present in the medicament according to the present invention in a concentration of between 0.025 and 2% by weight, advantageously between 0.025% and 1% by weight, and still more advantageously of approximately 0.05%. by weight, relative to the total weight of the composition.
Le nom chimique de l'acétonide de fluocinolone est le (6,11,16)-6,9-difluoro-11,21-dihydroxy-16,17-[(1-méthyléthylidène)bis(oxy) ] -pregna- l ,-4-diène-3,20-dione. II s'agit d'une poudre cristalline blanche qui est sans odeur et stable à la lumière. L'acétonide de fluocinolone est un corticostéroïde synthétique fluoré destiné à une utilisation dermatologique topique, et il est utilisé en tant qu'anti-inflammatoire. Dans un mode de réalisation particulier, 1' acétonide de fluocinolone est présent dans le médicament selon la présente invention à une concentration comprise entre 0,005 et 0,1% en poids, avantageusement entre 0,005 et 0,05% en poids, encore plus avantageusement d'environ 0,01 % en poids, par rapport au poids total de la composition. The chemical name of fluocinolone acetonide is (6,11,16) -6,9-difluoro-11,21-dihydroxy-16,17 - [(1-methylethylidene) bis (oxy)] -pregna-1 , -4-diene-3,20-dione. It is a white crystalline powder that is odorless and light stable. Fluocinolone acetonide is a synthetic fluorinated corticosteroid for topical dermatological use and is used as an anti-inflammatory. In a particular embodiment, the fluocinolone acetonide is present in the medicament according to the present invention at a concentration of between 0.005 and 0.1% by weight, advantageously between 0.005 and 0.05% by weight, and even more advantageously with about 0.01% by weight, based on the total weight of the composition.
Avantageusement, le médicament selon la présente invention contient du 15 metabisulfite de sodium pour prévenir l'oxydation de l'hydroquinone. Advantageously, the drug according to the present invention contains sodium metabisulfite to prevent the oxidation of hydroquinone.
Le médicament selon la présente invention peut être fourni sous toutes les formes galéniques normalement utilisées dans le domaine de la dermatologie. De manière préférentielle, le médicament se présentera sous forme de crème. 20 La forme crème peut être avantageusement préparée comme indiqué dans la demande de brevet WO 2004/037201, par un procédé comprenant les étapes de : a) mélange des composés hydrophiles avec l'eau pour former une phase aqueuse ; b) mélange des composés hydrophobes pour former une phase hydrophobe ; 25 c) mélange des phases hydrophobes et hydrophiles pour former un mélange biphasique et, d) addition d'un émulsifiant au mélange biphasique pour former une émulsion. The medicament according to the present invention may be provided in any galenical form normally used in the field of dermatology. Preferably, the drug will be in the form of cream. The cream form may advantageously be prepared as indicated in the patent application WO 2004/037201, by a process comprising the steps of: a) mixing the hydrophilic compounds with the water to form an aqueous phase; b) mixing the hydrophobic compounds to form a hydrophobic phase; C) mixing the hydrophobic and hydrophilic phases to form a biphasic mixture, and d) adding an emulsifier to the biphasic mixture to form an emulsion.
De plus, elles peuvent contenir d'autres ingrédients habituels des crèmes et être 30 fabriquées de façon bien connue de l'homme du métier. 10 De manière avantageuse, le médicament selon la présente invention contient au moins un ingrédient inactif choisi parmi l'hydroxytoluène butylé, l'alcool cétylique, l'acide citrique, la glycérine, le stéarate de glycéryle, le silicate de magnésium et d'aluminium, le méthyl gluceth-10, le méthyl parabène, le stéarate de PEG-100, le propylparabène, l'eau purifiée, le métabisulfite de sodium, l'acide stéarique et l'alcool stéarylique. In addition, they may contain other usual cream ingredients and be manufactured in a manner well known to those skilled in the art. Advantageously, the medicament according to the present invention contains at least one inactive ingredient selected from butylated hydroxytoluene, cetyl alcohol, citric acid, glycerin, glyceryl stearate, magnesium aluminum silicate and the like. , methyl gluceth-10, methyl paraben, PEG-100 stearate, propylparaben, purified water, sodium metabisulfite, stearic acid and stearyl alcohol.
Avantageusement, le médicament selon la présente invention est la crème Tri-Luma vendue par la société Galderma, telle que présentée dans l'exemple 1. Exemple 1 : composition de la crème Tri-Luma La crème a la formule suivante, en pourcentage en poids par rapport au poids total : -silicate de magnésium et d'aluminium 3,00% - hydroxytoluène butylé 0,04% -alcool cétylique 4,00% - acide stéarique 3,00% - alcool stéarylique 4, 00% - methylparaben 0,18% - propylparaben 0,02% - Arlacel 165 [stéarate de glycérol et 3,50% monostéarate de glycerol stéarate de PEG-100] méthyl gluceth-10 5,00% - glycérine 4,00% trétinoïne 0,05% acétonide de fluocinolone 0,01% acide citrique 0,05% - hydroquinone 4,00% -métabisulfite de sodium 0,20% eau purifiée 68,95% Advantageously, the drug according to the present invention is the Tri-Luma cream sold by Galderma, as shown in Example 1. EXAMPLE 1 Composition of Tri-Luma Cream The cream has the following formula, in percentage by weight relative to the total weight: - magnesium aluminum silicate 3.00% - butylated hydroxytoluene 0.04% - cetyl alcohol 4.00% - stearic acid 3.00% - stearyl alcohol 4.00% - methylparaben 0, 18% - propylparaben 0.02% - Arlacel 165 [glycerol stearate and 3.50% glycerol monostearate PEG-100 stearate] methyl gluceth-10 5.00% - glycerin 4.00% tretinoin 0.05% acetonide fluocinolone 0.01% citric acid 0.05% - hydroquinone 4.00% - sodium metabisulfite 0.20% purified water 68.95%
Claims (12)
Priority Applications (2)
Application Number | Priority Date | Filing Date | Title |
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FR0512679A FR2894481A1 (en) | 2005-12-14 | 2005-12-14 | USE OF A DERMATOLOGICAL COMPOSITION COMPRISING A COMBINATION OF HYDROQUINONE, FLUOCINOLONE ACETONIDE AND TRETINOINE FOR THE TREATMENT OF HYPERPIGMENTATION OF NON-CAUCASIAN SKINS |
PCT/FR2006/051294 WO2007068843A1 (en) | 2005-12-14 | 2006-12-06 | Use of a dermatological composition comprising an association of hydroquinone, fluocinolone acetonide and tretinoin, for whitening non-caucasian skin types |
Applications Claiming Priority (1)
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FR0512679A FR2894481A1 (en) | 2005-12-14 | 2005-12-14 | USE OF A DERMATOLOGICAL COMPOSITION COMPRISING A COMBINATION OF HYDROQUINONE, FLUOCINOLONE ACETONIDE AND TRETINOINE FOR THE TREATMENT OF HYPERPIGMENTATION OF NON-CAUCASIAN SKINS |
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FR2894481A1 true FR2894481A1 (en) | 2007-06-15 |
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FR0512679A Withdrawn FR2894481A1 (en) | 2005-12-14 | 2005-12-14 | USE OF A DERMATOLOGICAL COMPOSITION COMPRISING A COMBINATION OF HYDROQUINONE, FLUOCINOLONE ACETONIDE AND TRETINOINE FOR THE TREATMENT OF HYPERPIGMENTATION OF NON-CAUCASIAN SKINS |
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WO (1) | WO2007068843A1 (en) |
Citations (2)
Publication number | Priority date | Publication date | Assignee | Title |
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US3856934A (en) * | 1970-06-24 | 1974-12-24 | A Kligman | Skin depigmentation |
WO2004037201A2 (en) * | 2002-10-25 | 2004-05-06 | Hill Dermaceuticals, Inc. | Topical skin care composition |
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2005
- 2005-12-14 FR FR0512679A patent/FR2894481A1/en not_active Withdrawn
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2006
- 2006-12-06 WO PCT/FR2006/051294 patent/WO2007068843A1/en active Application Filing
Patent Citations (2)
Publication number | Priority date | Publication date | Assignee | Title |
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US3856934A (en) * | 1970-06-24 | 1974-12-24 | A Kligman | Skin depigmentation |
WO2004037201A2 (en) * | 2002-10-25 | 2004-05-06 | Hill Dermaceuticals, Inc. | Topical skin care composition |
Non-Patent Citations (4)
Title |
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"Efficacy and safety of triple-combination cream versus vehicle cream in the treatment of patients with postinflammatory hyperpigmentation", JOURNAL OF THE AMERICAN ACADEMY OF DERMATOLOGY, C.V. MOSBY, ST. LOUIS, MO, US, vol. 52, no. 3, March 2005 (2005-03-01), pages P168, XP004788713, ISSN: 0190-9622 * |
CALLENDER V D: "Acne in ethnic skin: Special considerations for therapy", DERMATOLOGIC THERAPY 2004 UNITED STATES, vol. 17, no. 2, 2004, pages 184 - 195, XP000238242, ISSN: 1396-0296 * |
COOK-BOLDEN F ET AL: "THE USE OF A TRIPLE-DRUG COMBINATION PRODUCT AND PROCEDURES FOR THE TREATMENT OF HYPERPIGMENTARY DISORDERS", COSMETIC DERMATOLOGY, KNOLLS PUB. GROUP, CEDAR KNOLLS, NJ, US, vol. 18, no. 8, August 2005 (2005-08-01), pages 589 - 594, XP009066078, ISSN: 1041-3766 * |
TOROK HELEN MARY ET AL: "Hydroquinone 4%, tretinoin 0.05%, fluocinolone acetonide 0.01%: a safe and efficacious 12-month treatment for melasma.", CUTIS; CUTANEOUS MEDICINE FOR THE PRACTITIONER. JAN 2005, vol. 75, no. 1, January 2005 (2005-01-01), pages 57 - 62, XP009067213, ISSN: 0011-4162 * |
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