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(19) United States (12) Patent Application Publication (10) Pub US 20130289102A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2013/0289102 A1 Singh et al. (43) Pub. Date: Oct. 31, 2013 (54) AMYRIS ALCOHOL AND ITS ESTER FOR Publication Classi?cation TREATING ACNE (5 1) Int. Cl. (75) Inventors: Chandra Ulagaraj Singh; San Antonio; A61K 31/22 (200601) TX (US);_ Jagaveerabhadra Rao Nulu; A61K 31/12 (2006.01) Austin TX (Us) A61K31/352 (2006.01) ’ A61K 31/045 (2006.01) _ _ _ _ _ (52) US. Cl. (73) Asslgneei Trlnlty Laboratorlesa Inc-3 San Ammo, CPC ............. .. A61K 31/22 (2013.01); A61K 31/045 TX (US) (201301); A61K31/12 (2013.01); A61K ' 31/352 (2013.01) (21) APPl- N°~~ 13/996,636 USPC ......... .. 514/450; 514/510; 514/729; 514/454; (22) PCT Filed: Dec. 22, 2011 514/453; 514/679 (57) ABSTRACT (86) PCT NO‘: PCT/Us2011/066751 The P resent invention relates to formulations comP rising § 371 (0X1), amyris alcohol or an ester of amyris alcohol or combinations (2); (4) Date; Jul, 2, 2013 thereof to treat acne in humans. These formulations can fur ther comprise a phytoestrogen such as glabridin and Related U‘s‘ Application Data miroestrol; an antloxidant such as tetrahydrocurcumin 'and naturally occurring peroxides such as artem1s1n1n and dihy (60) Provisional application No. 61/425,916; ?led on Dec. droartemisinin and combinations thereof for improved effec 22, 2010. tiveness in treating acne. Illuu... Valerianol Bcta-cudcsmol i Epi-gamma-eudesmol Elemol Alpha-eudesmol Patent Application Publication Oct. 31, 2013 Sheet 1 0f 6 US 2013/0289102 A1 EDGEH Patent Application Publication Oct. 31, 2013 Sheet 2 0f 6 US 2013/0289102 A1 WMDUEN o?xopomowcmomwtm Patent Application Publication Oct. 31, 2013 Sheet 3 0f 6 US 2013/0289102 A1 FIGURE3 Patent Application Publication Oct. 31, 2013 Sheet 4 0f 6 US 2013/0289102 A1 EDGEw HobmoobzA20MH Bbmmoacbmxoo?.NMIH Patent Application Publication Oct. 31, 2013 Sheet 5 0f 6 US 2013/0289102 A1 QMDUEm O O\/O EEEEQEPEQEF 0IIO Patent Application Publication Oct. 31, 2013 Sheet 6 0f 6 US 2013/0289102 A1 FIGURE6 US 2013/0289102 A1 Oct. 31,2013 AMYRIS ALCOHOL AND ITS ESTER FOR Would thus be advantageous to provide relief from all of the TREATING ACNE above four principal causes of acne. [0007] Topical products used to remove comedones are CROSS REFERENCE TO RELATED knoWn as comedolytics, the most effective being tretinoin, APPLICATIONS marketed as a prescription product (Retin A) and by several [0001] This application claims the bene?t of U.S.Appl. No. generic companies (http://WWWdrugs.com/pro/tretinoin. html). Tretinoin or all-trans retinoic acid is the naturally 61/425,916, ?led Dec. 22, 2010. The content of the aforesaid occurring metabolite of Vitamin A. Tretinoin increases epi application is relied upon and incorporated by reference in its dermal cell turnover, thus causing comedolysis and most entirety. importantly prevents the formation of neW keratinous plugs. Applications of tretinoin are normally once a day at bedtime. FIELD OF THE INVENTION Dryness, stinging and redness sometimes accompany the [0002] The ?eld of the invention relates generally to thera applications. Importantly, improvement is usually not seen peutics. More speci?cally, the ?eld of the invention relates to for 6-8 Weeks. Adapalene 0.1% (Differin) is a topical retinoid treatments for acne. like tretinoin. Available by prescription only, the gel is usually applied once nightly. Side effects include frequent scaling, BACKGROUND OF THE INVENTION burning, redness and dryness. Improvement is delayed and is not evident for 4-8 Weeks. Sodium sulfacetamide 10%/ sulfur [0003] There are approximately 45 million people Who suf 5% (Sulfacet-R) is also available by prescription only. It is a fer from acne in America alone (http://WWW.aad.org/media lotion With antibacterial and comedolytic action. As With resources/stats-and-facts/conditions/acne). The disease is so tretinoin, improvement is seen in 4-8 Weeks. Salicylic acid common in youth at their puberty that it often has been termed 2% is an over the counter product that exhibits mild come physiological. Although acne stops appearing for most dolytic activity. people by the age of 25, some people, the majority of them are [0008] The only products that have anti-sebum activity are Women, experience the disease Well into their adult life. This estrogens and 13 cis-retinoic acid (isotretinoin) and these “adult acne” differs from teenage acne in location and that it must be used systemically to be effective (Strauss, 1., et al., tends to be more in?ammatory With feWer comedones. As the (2007); Guidelines of care for acne vulgaris management, human concern for facial beauty continues to receive height Journal of the American Academy ofDermaZology 56 (4): ened marketing attention, the cure for various forms of acne 651-63). Isotretinoin (Accutane) is a metabolite of VitaminA has received much attention, as evidenced by the number of available by prescription only. Isotretinoin is used to treat patents and patent applications that have appeared recently. only severe cystic or conglobate acne. Because of its terato From 1975 to January 2003, there Were over 9000 patents genic properties, birth defects can occur. Isotretinoin is a issued by the US. Patent Of?ce that had some reference to poWerful drug and can elevate triglycerides, total cholesterol acne. From these data, it Would become obvious that a suit and decrease high-density lipoproteins (HDL). Other side able solution to this problem has eluded past efforts. effects include dry skin, dry eyes, itching, headaches, nose [0004] The acne process results from a cascade of events. bleed, and photosensitivity. It is generally taken for 4-5 First, at puberty a spike in androgen production heralds an months to see improvement. Recently, one brand of oral con increase in sebum production and begins the hyperkeratini traceptive has been approved for the treatment of acne for Zation process causing microcomedones and sebum block patients Who request birth control. ade. With this blockage, the number of resident follicular ?ora [0009] A number of topical and systemic agents are used to increases dramatically. These bacteria produce in?ammatory loWer the number of bacteria that coloniZe the follicular duct. products, Which permeate through thin Walls of dilated These include benZoyl peroxide (BP), BP 5%/erythromycin sebum-?lled duct. Once in the perifollicular dermis, they 3% (BenZamycin). BP has antibacterial activity and drying trigger the body’s oWn immune defenses (both acute and effects and is available over the counter or by prescription. granulaomatous) to produce the characteristic in?ammatory Moreover, it has been recently reported that benZoyl peroxide papules, pustules and nodules characteristic of in?ammatory seems to induce free radical production that can produce skin acne. changes that qualitatively resemble ultraviolet B damage, [0005] Thus, there are four factors that are believed to be e.g., increases in epidermal thickness, and deleterious the contributors of acne: (1) Increased sebum production; (2) changes in elastin and glycosaminoglycans content (Ibbot Comedo formation, in Which the follicular infundibulum son, S H., et al., J. Inves. Derm, 1999, 112: 933-938). In hypercorni?es, hyperkeratiniZes, and hypodesquamates; (3) addition, BenZoyl peroxide is highly reactive, and is thus ColoniZation of the follicule by anaerobic Propionibacle di?icult to stabiliZe in practical compositions. BP is applied rium, mainly R acnes; and (4) The host’s in?ammatory once or tWice daily for 1-2 months. BP can produce erythema response. The above four factors are interrelated to each other. and peeling of skin. BP is often tried ?rst for both non Sebum is comedogenic and causes in?ammation by itself. in?ammatory and mild in?ammatory acne. Other topical Propionibaclerium acnes is a relatively sloW groWing, (typi antibiotics include clindamycin and erythromycin. These are cally) obligate anaerobe gram positive bacterium that is used as solutions, lotions or gels by prescription only. Usually linked to the skin condition acne. they are applied once or tWice daily and results are seen in 1-2 [0006] The Propionibaclerium has high lipolytic activity months. AZelaic acid 20% (AZelex) also has mild antibacte and liberates free fatty acids from sebum lipids. The free fatty rial effects. Systemic antibiotics include tetracycline and its acids have been shoWn to cause marked in?ammation. The analogs, Which are used in loW doses for years or until the end microorganisms also produce other extracellular enZymes of the acne prone years. Most patients With mild in?amma such as proteases and hyaluronidases, and chemotactic fac tory acne receive a combination of topical antibiotics and tors, Which may be important in the in?ammatory process. It tretinoin or other retinoid. Bacterial resistance does occur so US 2013/0289102 A1 Oct. 31,2013 antibiotics may be changed or BP is substituted since resis selves; and (6) An enhancement of the topical bioavailability tance does not occur With BP. More severe acne requires of anti-acne and anti-rosacea compositions. systemic antibiotics and topical retinoid. The most severe [0016] Since the resistance to bacteria is becoming a prob must receive oral isotretinoin for 4-5 months. lem, it Would be advantageous to control bacteria Without [0010] There are no drugs that directly affect the in?am using an antibacterial agent. Also, salicylic acid is being one matory acne. The retinoids do have some anti-in?ammatory of the most favored and inexpensive ingredients to control properties, but these are poorly described. Topical steroid and acne, albeit its irritation causing side effects, it Would be even systemic steroids have been used to abort a severe ?are advantageous to devise methodologies to increase both topi of fulminant acne, but these are limited uses because of the cal bioavailability and anti-acne e?icacy of salicylic acid With side effects.
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