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(12) United States Patent (10) Patent No.: US 9,364,424 B2 Caetano Et Al

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(12) United States Patent (10) Patent No.: US 9,364,424 B2 Caetano Et Al US009364424B2 (12) United States Patent (10) Patent No.: US 9,364,424 B2 Caetano et al. (45) Date of Patent: *Jun. 14, 2016 (54) TOPICAL COSMETIC SKIN LIGHTENING (56) References Cited COMPOSITIONS AND METHODS OF USE THEREOF U.S. PATENT DOCUMENTS 5,609,875 A 3, 1997 Hadas (71) Applicant: Stiefel Laboratories, Inc., New Castle, 6,090,369 A 7/2000 Stewart DE (US) 2001 OO16213 A1 8/2001 Singh-Verma 2003. O198612 A1 10/2003 Chaudhuri et al. 2004/0028642 A1 2/2004 Hansenne et al. (72) Inventors: Joao Paulo Caetano, Sao Paulo (BR): 2004/0175439 A1 9/2004 Cyr Monica Alves Mariani De Oliveira, Sao 2005, 0163731 A1* 7, 2005 PeliSSon ................. A61K 8,347 Pauloa (BR) 424,59 2006, OO18867 A1 1/2006 Kawasaki et al. 2006/0280704 A1 12/2006 John (73) Assignee: Stiefel Laboratories, Inc., Wilmington, 2007/0020203 A1* 1/2007 Chaudhuri ............. A61K 8,675 New Castle, DE (US) 424,59 2007/O122492 A1 5, 2007 Behr (*) Notice: Subject to any disclaimer, the term of this 2008, OOSO459 A1 2/2008 Elie et al. patent is extended or adjusted under 35 U.S.C. 154(b) by 0 days. FOREIGN PATENT DOCUMENTS This patent is Subject to a terminal dis FR WO2005/063.191 * 7, 2005 ............... A61K 7.48 claimer. JP 01-311011 A 12/1989 JP 06-271442 A 9, 1994 JP 09-077638 A 3, 1997 (21) Appl. No.: 14/950,395 JP 2003-063925. A 3, 2003 JP 2003-081749 A 3, 2003 (22) Filed: Nov. 24, 2015 JP 2004-352697 A 12, 2004 JP 2005-139070 A 6, 2005 (65) Prior Publication Data WO WO 2003/0593.13 A1 T 2003 WO WO 2005/025532 A1 3, 2005 US 2016/OO743 15 A1 Mar. 17, 2016 WO WO 2005/063.191 A1 7/2005 WO WO 2005/067885 A1 7/2005 WO WO 2006/053912 5, 2006 Related U.S. Application Data WO WO 2007/107268 A1 9, 2007 (63) Continuation-in-part of application No. 12/743,353, OTHER PUBLICATIONS filed as application No. PCT/US2008/012952 on Nov. Halder, et al. Skin Therapy Letter, 9(6): 1 (2004). 19, 2008, now Pat. No. 9,241,893, which is a Masato Suzuki (Editorial Supervisor), Functional Cosmetics III, continuation-in-part of application No. CMC Limited, Jan. 1, 2000, pp. 27-35 (in Japanese). Masato Suzuki (Editorial Supervisor), Functional Cosmetics III, PCT/US2007/024109, filed on Nov. 19, 2007. CMC Limited, Jan. 1, 2000 (English translation). (51) Int. Cl. A 6LX8/97 (2006.01) * cited by examiner A61O 1704 (2006.01) Primary Examiner — Sean Basquill A61O 19/08 (2006.01) (74) Attorney, Agent, or Firm — Dara L. Dinner; Theodore A61O 19/02 (2006.01) R. Furman A6 IK 8/35 (2006.01) A6 IK S/37 (2006.01) (57) ABSTRACT A6 IK 8/49 (2006.01) Topical cosmetic compositions are provided that can com (52) U.S. Cl. prise a Phyllanthus extract, a Bellis extract, and a licorice CPC. A61K 8/97 (2013.01); A61K 8/35 (2013.01); (Glycyrrhiza) extract. These compositions are used for topi A61K 8/355 (2013.01); A61 K8/37 (2013.01); cal cosmetic applications, particularly to lighten skin. Meth A61K 8/496 (2013.01); A61O 1704 (2013.01); ods for lightening skin are also provided and can comprise A61O 19/02 (2013.01); A61O 19/08 (2013.01) topically administering a therapeutically effective amount of (58) Field of Classification Search a topical cosmetic composition comprising a Phyllanthus CPC ........... A61K 8/97: A61K 8/35; A61K 8/355; extract, a Bellis extract, and a licorice extract, to skin of a A61K 8/37; A61K 8/496; A61Q 17/04; subject in need thereof. A61Q 19/08: A61Q 19/02 See application file for complete search history. 17 Claims, 5 Drawing Sheets U.S. Patent Jun. 14, 2016 Sheet 1 of 5 US 9,364,424 B2 Hydroquinone F.G. U.S. Patent Jun. 14, 2016 Sheet 2 of 5 US 9,364,424 B2 New Formation : New Fontatio: FG, 2 U.S. Patent Jun. 14, 2016 Sheet 3 of 5 US 9,364,424 B2 F.G. 3 U.S. Patent Jun. 14, 2016 Sheet 4 of 5 US 9,364,424 B2 3.Hydroquinone & New Formula Control F.G. 4 U.S. Patent Jun. 14, 2016 Sheet 5 of 5 US 9,364,424 B2 . 5a & b. Photogrgraph ic Register ; Hydroqui O at T0 (day 0) and T2 (day 21) Fig. 5 c & d. Photographic Register New Formulation at T0 and T21 ig. 5 e & f. Photograph C egister Control at T0 and T2 FG. 5 US 9,364,424 B2 1. 2 TOPCAL COSMETC SKN LIGHTENING present in Phyllanthus extract, Bellis extract, or licorice COMPOSITIONS AND METHODS OF USE extract. In a further embodiment, the cosmetic composition THEREOF does not comprise oligopeptide-4 (pro-collagen oligopep tide) or oligopeptide-5 (pro-elastin oligopeptide). In another FIELD OF THE INVENTION embodiment, the cosmetic composition does not comprise at least one oligopeptide having a suitable molecular weight So The presently described subject matter relates to topical that it is able to act as carrier of Phyllanthus Embilica extract cosmetic or dermatological compositions comprising plant and penetrate skin to maximize the efficacy. extracts. These compositions are used for topical cosmetic In an embodiment, the present Subject matter relates to a applications, particularly to treat undesired skin pigmenta 10 topical cosmetic composition, comprising, consisting essen tion. tially of, or consisting of a Phyllanthus embilica extract; a Bellis perennis extract; and a licorice extract. BACKGROUND OF THE INVENTION In another embodiment, the present Subject matter relates to a topical cosmetic composition, comprising, consisting Topical cosmetic skin lightening compositions that are safe 15 essentially of, or consisting of a skin-lightening active com and effective are particularly desirable for treating undesir ponent comprising, consisting essentially of or consisting of able skin pigmentation, including for example, regional a Phyllanthus extract, a Bellis extract, and a licorice extract; at hyperpigmentation caused by melanocytic hyperactivity Such least one Sunscreen; and a cosmetically acceptable carrier. as idiopathic melasma occurring during pregnancy (mask of In another embodiment, the present Subject matter relates pregnancy or chloasma) or secondary to estrogen-progester to a topical cosmetic composition, comprising, consisting one contraception; local hyperpigmentation caused by benign essentially of, or consisting of a skin-lightening active com melanocytic hyperactivity and proliferation Such as lentigo ponent comprising, consisting essentially of or consisting of senilis, known as liver spots; accidental hyperpigmentation a Phyllanthus embilica extract, a Bellis perennis extract, and Such as post-lesional photosensitization and scarring, skin a licorice extract; at least one Sunscreen; and a cosmetically ageing (for example lentigines seniles); and certain forms of 25 acceptable carrier. leukoderma Such as vitiligo where, if the injured skin cannot In an embodiment, the present Subject matter relates to a be repigmented, the residual Zones of normal skin are light topical cosmetic composition, comprising, consisting essen ened or depigmented to impart a homogeneous color to the tially of, or consisting of a skin-lightening active component entire skin. comprising, consisting essentially of, or consisting of a Phyl Several active ingredients and preparations that lighten 30 lanthus extract, a Bellis extract, and a licorice extract; and a skin, i.e., counteract skin pigmentation, are currently known. non-skin lightening component comprising at least one Sun These products that are currently used contain hydroquinone, SCC. but such products have recently been deemed unacceptable In an embodiment, the present Subject matter relates to a for toxicological reasons. In fact, RDC 215 forbids the use of topical cosmetic composition, comprising, consisting essen hydroquinone in cosmetic products after December, 2007. 35 tially of, or consisting of a skin-lightening active component U.S. Published Patent Application No. 2008/0050459 comprising, consisting essentially of, or consisting of a Phyl describes a cosmetic composition comprising an extract of lanthus embilica extract, a Bellis perennis extract, and a lico Phyllanthus Embilica, an extract of Bellis Perrenis, an extract rice extract; and a non-skin lightening component comprising of Glycyrrhiza Glabra, and requiring at least one oligopep at least one Sunscreen. tide to achieve its cosmetic effect for the combined cosmetic 40 In another embodiment, the present Subject matter relates treatment of fine lines and wrinkles, and/or skin brightening. to a method of lightening skin pigmentation in a Subject, Suitable oligopeptides are described as those having a Suit comprising topically administering to skin of a subject in able molecular weight so that they are able to act as carriers of need thereof, a therapeutically effective amount of a topical Phyllanthus Embilica extract and penetrate skin to maximize cosmetic composition in accordance with the presently the efficacy. The only oligopeptides described in the publica 45 described subject matter. tion for achieving the cosmetic composition are oligopep In yet another embodiment, the present Subject matter tide-4 (pro-collagen oligopeptide) and oligopeptide-5 (pro relates to a method of treating a skin disorder or condition in elastin oligopeptide). a Subject, comprising topically administering to skin of a There remains a need in the art for improved topical cos subject in need thereofatherapeutically effective amount of a metic compositions containing agents that safely and effec 50 topical cosmetic composition in accordance with the pres tively lighten skin. ently described subject matter. SUMMARY OF THE INVENTION BRIEF DESCRIPTION OF THE FIGURES The present Subject matter relates generally to topical cos 55 FIG. 1 illustrates progressive lightening over time that metic compositions useful for treating various skin disorders becomes statistically significant after 21 days for Site B or conditions associated with undesired skin pigmentation.
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