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Lllllllllllllllllllllllllllillllllllllllllllllllllllllllllll lllllllllllllllllllllllllllIlllllllllllllllllllllllllllllllllllllllllllllll Unlted States Patent [19] [11] Patent Number: 5,164,185 Charpin et a1. [45] Date of Patent: Nov. 17, 1992 [54] PHARMACEUTICAL AND COSMETIC [56] References Cited DEPTGMENTATION 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 Des ghment at all giijs’l?l§l,‘guca?daggyshfn’. - - 1 4,824,865, , 4/1989 Bowseracque eet a.al. 514/858 . g. ' ye ’. 0 .3” 4,990,330 2/1991 Oyama ................................ .. 424/62 Christiane Montastler, Maisons Laf?tte; Francois Millecamps, Paris, FOREIGN PATENT DOCUMENTS 3“ °f France 1533371 7/1968 France . _ 2613622 12/1978 F . [73] Ass1gnee: L’Oreal, Pans, France 2390160 10/1988 F222: _ 2-55607 10/1990 Japan . [2]] Appl. No.: 691,045 OTHER PUBLICATIONS [22] PCT Filed: 091- 19, 1990 Patent Abstracts of Japan, vol. 11, No. 349 . (C*4S6)(2796), Nov. 14, 1987. [86] PCT N°-= PCT/FR90/00760 Patent Abstract of Japan, vol. 6, No. 44, (C-95)(922), §371 Date: Aug. 13, 1991 Mar- 19, 1982. § 102(5) Date; Aug 31’ 1991 Primary Examiner-Thurman K. Page Assistant Examiner-D. Colucci [87] PCT Pub, No,; W091 /05543 Attorney, Agent, or Firm-—Cushman, Darby & Cushman PCT Pub. Date: May 2, 1991 [57] ABSTRACT . _ ‘ ' A pharmaceutical or cosmetic depigmenting composi-' [30] Forelg" Apphc‘mon Pnomy 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 [51] Int. Cl.5 ............................................ .. 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 INHIBITION OF THE TYROSINE/TYROSINASE “:0 ACTIVITY EFFECT OF CAFFEIC ACID ‘I50 140. ~ 130 120 119 (21 O ‘ 1 ' D S I) 15 2O 2 S 30 35 40 The in Ilnutes Control (lb-- 50: cmele we (21% Z51 Caffelc ICTd US. Patent Nov. 17,1992 Sheet 1 of 5 5,164,185 FIG.1 INHIBITION OF THE TYROSINE/TYROSINASE ACTIVITY EFFECT OF CAFFEIC ACID 1601 150 . 140. 130. 120W 110. T?»0000 mm 3153 071030 78 mu0 w 35 40 Time in minutes Control I1) -—*--~- 50% Caffeic acid (2)--- 25% Caffeic acid US. Patent Nov. 17, 1992 Sheet 2 of 5 5,164,185 vINHIBITION OF THE TYROSINE/TYROSINASE ACTIVITY DERIVATIVE 0F CAFFEIC ACID 1 F58 025910303 mwwm mu” 4 W. l 0 0I. 5 1'0 1'5 2‘0 2'5 3'0 3'5 4'0 45 50I 5'5 50 Time in minutes Control (1) H495 50% C6 Caffeic acid amide (2) ........._.. 50% C8 Caffeic acid amide C6 US. Patent Nov. 17, 1992 Sheet 3 of 5 5,164,185 Fl6.3 INHIBITION OF TYROSINE/TYROSINASE ACTIVITY COMBINATION OF CAFFEIC ACIC ANO COPPER GLUCONATE w m w. .1... U All 2 O m m... 1 12.52. 03007303 0 25 30 35 40 Time in minutes wwmwwmnmnm CONTROL (1) H44‘ 50% CAFFEIC ACID {251 CAFFEIC ACID + (2) 25x COPPERGLUCONATE US. Patent Nov. 17, 1992 Sheet 4 of 5 5,164,185 INHIBITION OF TYROSINE/TYROSINASE ACTIVITY COMBINATIONS BASED ON CAFFEIC ACID 9 5 9 0 nozqxor._.:m 2..aon3533:: .HDAULJOLJOPTUHJIQJU.»_ a0 ofs 1.5 TIME INDEX (TIME INDEX - 1 FOR THE MAXIMAL CONCENTRATION OF THE CONTROL) CONTROL (1) m**-BBTTIDDSSIAwBDJwDmrADmNSO 25% CAFFEIC ACID + 25% COPPER GLULONATE (2) 25X CAFFEIC ACID + 25% NYDROQUINONE (MW 25% CAFFEIC ACID + 51 KOJIC ACID US. Patent Nov. 17, 1992 Sheet 5 of 5 5,164,185 FIGS INHIBITION OF TYROSINE/TYROSINASE ACITIVTY COMBINATION HAVING 3 AND 4 COMPONENTS CONTAINING CAFFEIC ACID 160‘ 150 140 13)‘ 120 > 110 pauuogw‘ awouqoodoq ‘[D 90 80 (1) 70 a), 50‘ 40 30 20‘ ‘n. 0 I 4‘ ? ; 2 . ; ; 0 5 10 15 20 25 30 35 40 Time in minutes comm (1) {2oz15x CAI-'FEICmunoqumous ACID + 15% mm ACID (2) {20%1oz NYDROQUINONECAFFEIC ACID + 10x KOJIC ACID + m; COPPER GLUCONATE (3) H-**'{16.5%16.5% CAFFEICKOJIC ACID ACID + + + 17.5% COPPER GLUCONATE 5,164,185 1 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 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 main steps diagrammed below: tyrosinasic activity leading to the limited formation of dopachrome and thus, of melanins. This new property of caffeic acid and its derivatives TYROSINE—>DOPA->DOPAQUINONE-s 15 DOPACHROMEqMELANINS 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 20 a topical application and containing, in a vehicle suit ogy are, more speci?cally, phenolic derivatives, and, able for such an application, an effective quantity of most notably, hydroquinone or a hydroquinone ether caffeic acid or of one of its esters or amides. such as hydroquinone monomethyl ether. Among the esters of caffeic acid, mention may be While these compounds have a certain level of effec made especially of the compounds corresponding to the tiveness, they are not, unfortunately, free from side formula: effects that make their use a sensitive, and even danger 25 ous, matter. Thus, hydroquinone, whose use is restricted, more (1) over, to a 2% concentration, is especially irritating and cytotoxic for melanocytes. Many authors have contem HO O-R 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. 35 atoms, and preferably the methyl radical. International Application WO 85/0401 proposes, in 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 the formula: its benzylic monoether and salicylic acid. 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 composition 5 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 generally ranges between 0.1 and 8%, and preferably one of the stages of melanin biosynthesis, either by between 1 and 3% by weight. inhibiting one of the enzymes involved or by its inser The vehicle for the compositions according to the tion as a structural analogue in the synthesis pathway, 55 invention may be, in particular, an aqueous or hydroal which can thus become blocked, thereby producing the depigmenting effect. coholic solution, an oil-in-water or water-in-oil emul The use of harmless topical depigmenting substances sion, an emulsi?ed 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-S hy spots, termed actinic lentigos, accidental hyperpigmen droxymethyl-2 H-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 of the depigmenting action was observed, and this ac tion could be attributed only to a synergistic effect.
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