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US5164185.Pdf ||||||||||||||| USOO564185A United States Patent (19) 11 Patent Number: 5,164,1859 9. Charpin et al. (45) Date of Patent: Nov. 17, 1992 54 PHARMACEUTICAL AND COSMETIC 56) References Cited DEPIGMENTATION COMPOSITIONS WITH A CAFFEIC ACID BASE U.S. PATENT DOCUMENTS 3,982,999 9/1976 Kharasch ........................... 424/94.3 75) Inventors: Isabelle Charpin, St Maur Dess y w r 7 E. acquetI et al. ms:... SEElegin Men, 4,824,865 4/1989 Bowser et al. ... ... 514/858 Christiane Montastier, Maisons 4,990,330 2/199i Oyama .................................. 424/62 Laffitte; Francois Milecamps, Paris, FOREIGN PATENT DOCUMENTS all of France 1533371 7/1968 France . 26l3622 12/1978 F A. 73 Assignee: L'Oreal, Paris, France 239.060 10/1988 E. A. 2-55607 10/1990 Japan. 21 Appl. No.: 691,045 OTHER PUBLICATIONS 22 PCT Filed: Oct. 19, 1990 Patent Abstracts of Japan, vol. 11, No. 349 (C-456)(2796), Nov. 14, 1987. 86 PCT No.: PCT/FR90/00760 Patent Abstract of Japan, vol. 6, No. 44, (C-95)(922), S371 Date: Aug. 13, 1991 Mar. 19, 1982, S 102(e) Date: Aug. 31, 1991 Primary Examiner-Thurman K. Page Assistant Examiner-D. Colucci 87). PCT Pub. No.: WO91/05543 Attorney, Agent, or Firm-Cushman, Darby & Cushman PCT Pub. Date: May 2, 1991 57 ABSTRACT s A pharmaceutical or cosmetic depigmenting composi 30 Foreign Application Priority Data tion for application to the skin so as to improve the Oct. 20, 1989 FR France ................................ 89 13774 aesthetic appearance of the skin or to treat pathological or accidental hyperpigmentation contains caffeic acid 5ll Int. Cl............................................... A61K 7/135 or an ester or amide thereof in an amount effective to 52 U.S. Cl. ....................................... 424/401; 424/62 depigment the skin. 58) Field of Search ........................ 424/401, 62, 94.3; 514/852, 858 19 Claims, 5 Drawing Sheets NBION OF TE YROSNEATYROSNASE ACT WITY EFFECT OF CAFFEIC ACID O O S O 15 20 2s 30 35 40 Tie in minutes corro 1) as so caffec acid (2) eases 25 Caffeic acid U.S. Patent Nov. 17, 1992 Sheet 1 of 5 5,164,185 FG.1 INHIBITION OF THE TYROSINE/TYROSINASE ACT WITY EFFECT OF CAFFEIC ACID 160 150 140 130 120 110 - 1OO K g 90 (2) O O SS BO g 3 (1) g 70 60 SO 40 30 20 10 O O S O 15 20 25 30 35 40 Time in minutes Control (1) r 50 Caffeic acid (2) e-elease 25 Caffeic acid U.S. Patent Nov. 17, 1992 Sheet 2 of 5 5,164,185 FG.2 : INHIBITION OF THE TYROSINE/TYROSINASE ACTIVITY 160 DERIVATIVE OF CAFFEIC ACID 150 140 130 120 (2) 110 - 100 90 o (1) 70 60 50 40 30 20 10 O 0 5 10 15 20 25 30 35 40 4.5 SO 55 60 Time in minutes Control (1) -x-x-x-x 50 C6 Caffeic acid amide C6 (2) -- 50 Ca Caffeic acid amide C8 U.S. Patent Nov. 17, 1992 Sheet 3 of 5 5,164,185 FIG.3 INHIBITION OF TYROSINE/TYROSINASE ACTIVITY COMBINATION OF CAFFEIC ACIC AND COPPER GLUCONATE 160 150 140 130 120 90 w (1) (2) 15 20 25 30 35 40 Time in minutes CONTROL (1) K---- 50 CAFFEIC ACID (2)-3:25 COPPERCAFFEIC GLUCONATEACID + U.S. Patent Nov. 17, 1992 Sheet 4 of 5 5,164,185 FG. A. INHIBITION OF TYROSINE/TYROSINASE ACTIVITY COMBINATIONS BASED ON CAFFEIC ACID 100 95 90 85 80 75 70 65 60 55 4. (3) SO45 Ss. 1)2) 40 35 30 25 20 15, 00 0.5 10 1.5 20 TIME INDEX (TIME INDEX 1 FOR THE MAXIMAL CONCENTRATION OF THE CONTROL) CONTROL (1) +----- 25 CAFFEIC ACID + 25 COPPER GLULuATE (2) 25 CAFFEIC ACID + 25. HYDROQUINONE (3)--------- 25 CAFFEIC ACID + 5. KOJIC ACID U.S. Patent Nov. 17, 1992 Sheet 5 of 5 5,164,185 FIG.5 INHIBITION OF TYROSINE/TYROSINASE ACITIWTY COMBINATION HAVING 3 AND 4 COMPONENTS CONTAINING CAFFEIC ACID ( ) O 5 10 15 20 25 30 35 40 Time in minutes CONTROL - 15 CAFFEICHYDROQUINONE ACID + 15, KOJIC ACID (2)-------. 20. HYDROQUINONE + 10 CAFFEIC ACID + 10. KOJIC ACID + 10% COPPER GLUCONATE (3) ---- (16.5 CAFFEIC ACID + 16.5 KOJIC ACID + 17.5 COPPER GLUCONATE 5,164,185 2 ring, as well as certain leucodermas such as vitiligo, in PHARMACEUTICAL AND COSMETIC which, because pigmentation cannot be restored to the DEPIGMENTATION COMPOSITIONS WITH A injured skin, the areas of remaining normal skin are CAFFEIC ACID BASE depigmented so as to impart to the total skin area a homogeneous white color. The present invention relates to a pharmaceutical or Following various studies conducted on numerous cosmetic depigmenting composition which contains, as substances used either singly or in combination, it was an active ingredient, caffeic acid or one of its deriva found, surprisingly and unexpectedly, that caffeic acid tives. or its derivatives, and especially its esters and amides, It will be remembered that the mechanism which O produced an especially interesting depigmenting action, forms skin pigmentation, i.e., the formation of melanins, their efficacy being mainly the result of an inhibition of is especially complex and involves the triggering of the tyrosinasic activity leading to the limited formation of main steps diagrammed below: dopachrome and thus, of melanins. TYROSINE-DOPA-DOPAQUINONE 15 This new property of caffeic acid and its derivatives DOPACHROME-MELANINS had heretofore never been brought to light, despite the many studies conducted on this acid. tyrosinase being the main enzyme involved in this series Therefore, the present invention relates to a pharma of reactions. ceutical or cosmetic depigmenting composition used in The depigmenting agents currently used in cosmetol a topical application and containing, in a vehicle suit ogy are, more specifically, phenolic derivatives, and, 20 most notably, hydroquinone or a hydroquinone ether able for such an application, an effective quantity of such as hydroquinone monomethyl ether. caffeic acid or of one of its esters or amides. While these compounds have a certain level of effec Among the esters of caffeic acid, mention may be tiveness, they are not, unfortunately, free from side made especially of the compounds corresponding to the effects that make their use a sensitive, and even danger 25 formula: Ous, matter. Thus, hydroquinone, whose use is restricted, more (1) over, to a 2% concentration, is especially irritating and HO cytotoxic for melanocytes. Many authors have contem plated its total or partial replacement. 30 Thus, French Patent No. 87.08236 (2,616,325) pro HO posed a composition containing a combination of hy droquinone and kojic acid or of its derivatives, in partic R representing an alkyl radical of from 1 to 8 carbon ular its salts and esters. atoms, and preferably the methyl radical. International Application WO 85/0401 proposes, in 35 Among the caffeic acid amides, mention may be addition and for the same purpose, a depigmenting com made, in particular, of the compounds corresponding to position containing a combination of hydroquinone or its benzylic monoether and salicylic acid. the formula: Moreover, among the compositions producing a pro nounced depigmenting action, mention must also be (2) made of the Kligman trio, generally chosen as the com HO pound of reference, which is based on a combination of acidic Vitamin A, hydroquinone, and a steroid, either dexamethasone or hydrocortisone. The use of this com HO position has, however, been restricted to the extent that 45 it exhibits a high level of irritation caused by acidic R" representing an alkyl radical of from 1 to 8 carbon Vitamin A as well as undesirable effects caused by hy atoms, and preferably an alkyl of from 6 to 8 carbon pervitaminosis A. atoms. The amide having 6 carbon atoms is most espe It has now been well established that a substance cially preferred. produces a depigmenting action if it acts directly on the 50 In compositions according to the invention, the con vitality of the epidermal melanocytes where melano centration of caffeic acid or of one of its derivatives genesis normally takes place, and/or if it interferes with one of the stages of melanin biosynthesis, either by generally ranges between 0.1 and 8%, and preferably inhibiting one of the enzymes involved or by its inser between 1 and 3% by weight. tion as a structural analogue in the synthesis pathway, 55 The vehicle for the compositions according to the which can thus become blocked, thereby producing the invention may be, in particular, an aqueous or hydroal depigmenting effect. coholic solution, an oil-in-water or water-in-oil emul The use of harmless topical depigmenting substances sion, an emulsified gel, or a diphase system. exhibiting a high degree of efficacy is most especially The compositions according to the invention prefera sought in order to treat regional hyperpigmentation bly exist as lotions, creams, gels, masks, microspheres or caused by melanocytic hyperactivity, such as idiopathic nanospheres, or vesicular dispersions. In these latter, at melasmas occurring during pregnancy ('mask of preg least one of the active ingredients may be liposomes. nancy' or chloasma) or melasmas secondary to estro Moreover, it was discovered, surprisingly, that when gen-progesterone contraception, cases of localized hy caffeic acid or one of its derivatives was associated with perpigmentation caused by hyperactivity and benign 65 a substance chosen from among the following: hydro melanocytic proliferation, such as senile pigmentary quinone or one of its ethers, kojic acid (hydroxy-5 hy spots, termed actinic lentigos, accidental hyperpigmen droxymethyl-2H-4 pyranone-4), a water-soluble copper tation such as photosensitization and post-lesion scar salt, or a mixture of these substances, increased efficacy 5,164,185 3 4.
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