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IIHHHHHHHHHHHHH US005094.857A United States Patent (19) 11) Patent Number: 5,094,857 Luderschmidt (45) Date of Patent: Mar

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IIHHHHHHHHHHHHH US005094.857A United States Patent (19) 11) Patent Number: 5,094,857 Luderschmidt (45) Date of Patent: Mar IIHHHHHHHHHHHHH US005094.857A United States Patent (19) 11) Patent Number: 5,094,857 Luderschmidt (45) Date of Patent: Mar. 10, 1992 54 TREATMENT OF ACNE OR AND 163490 12/1985 European Pat. Off. ROGENETICALOPECA BY TOPICAL 285563 10/1988 European Pat. Off. 316780 5/1989 European Pat. Off. ADMINISTRATION OF ETHISTERONE 356382 2/1990 European Pat. Off. 76 Inventor: Christoph Luderschmidt, Orthstrasse 3338339 4/1984 Fed. Rep. of Germany . 22, D-8000 Munchen, Fed. Rep. of 3738620 5/1989 Fed. Rep. of Germany . Germany 3836862 5/1990 Fed. Rep. of Germany . 2131292A 6/1984 United Kingdom . (21) Appl. No.: 606,949 2131292B 3/1987 United Kingdom. (22 Filed: Oct. 31, 1990 OTHER PUBLICATIONS Luder Schmidt CA.112:133196w (1989). Related U.S. Application Data Schmidt CA106:149804e (1987). 63 Continuation of Ser. No. 268,153, Nov. 7, 1988, aban Mortimer CA.104:136092e(1985). doned. Mortimer GA. 104:136094c (1985). 30 Foreign Application Priority Data Luderschmidt GA.104:6216ic (1985). Luderschmidt GA. 102:143355e (1984). Nov. 13, 1987 (DEl Fed. Rep. of Germany ....... 3738620 Mortimer GA.101:1370455(1984). 51) Int. Cl.......................... A61K 7/06; A61K 7/48; Mortimer GA. 101:116766n(1984). A61K 31/565; A61L 15/03 Schmidt, J. B. et al., Med. Welt. 36:1 122 (1985). 52 U.S. C. .................................... 424/449; 514/859; Schmidt, J. B. et al., Hautarzt 38(3):470-473 Aug. 514/947; 514/169 (1987). 58) Field of Search ................................ 514/169-182, Toth, F et al., Z. Arztl. Fortbild (Jena) 64(3):122-131 514/859, 947; 424/449 Feb. 1, 1990. 56 References Cited Neumann, F. et al., J. Steroid Biochem. 25(5B):885-895 Nov. 1986. U.S. PATENT DOCUMENTS Schmidt, J. B. et al., Endocrinol Exp. 21 (1): 71-78 Mar. 4,540,564 9/1985 Bodor .................................. 5.14/176 1987. 4,824,850 4/1989 ... 514/176 4,829,070 5/1989 Bodor .................................. 514/307 Primary Examiner-Shep K. Rose 4,867,982 9/1989 Campbell et al. ................... 424/449 Attorney, Agent, or Firm-Omri M. Behr 4,880,921 1 1/1989 Bodor .................................. 540/110 4,895,727 1/1990 Allen ................................... 514/947 57 ABSTRACT 4,900,837 2/1990 Bodor .................................. 54.6/285 There is disclosed the use of ethisterone its nor analogs 4,913,905 4/1990 Fankhauser et al. ... 424/449 as well as their corresponding 17-esters formed with 4,994,278 2/1991 Sablotsky et al. ... ... 424/449 pharmaceutically acceptable carboxylic acids, for the 5,008,257 4/199 Bodor ............... ... 514/192 reduction of lipids, in particular waxy solids in the seba 5,032,403 7/1991 Sinnreich O. 424/449 ceous glands. Such removal facilitates the topical treat FOREIGN PATENT DOCUMENTS ment of acne vulgaris or androgenetic alopezia. 114003 7/1984 European Pat. Off. 163489 12/1985 European Pat. Off. 7 Claims, 1 Drawing Sheet U.S. Patent Mar. 10, 1992 5,094,857 X x Spironolactone dpm OR-88 IOO% a ethisterOne O dexomethoSOne v cyproteronacetat O I7-O-propylmesterolone 8O 4O FIG. IoIO IO-5 IO dpm O O ethisterOne O O ... O progesterone OO % W v norethindrone FG.2 O-IO IO-5 IO 5,094,857 1 2 tion which leads to the formation of acne, acne itself can TREATMENT OF ACNE OR ANDROGENETIC be readily avoided. ALOPECIA BY TOPCAL ADMINISTRATION OF It will be understood by those skilled in the art that ETHISTERONE hereinbelow, the terms ethisterone or nor-ethisterone 5 when utilized alone should be considered to include the . This application is a continuation of application Ser. 17-esters thereof with pharmaceutically acceptable car No. 07/268,153, filed 1 1/7/88, now abandoned. boxylic acids suitably lower alkanoic acids containing from 1 to 10 carbon atoms such as formates, acetates, FIELD OF THE INVENTION propionates, butyrates, valerates, oenanthates and the The invention is directed to the use of certain ste O corresponding structural isomers thereof. roids, notably ethisterone its nor analogs as well as their Ethisterone has been known for thirty years as a corresponding 17-esters formed with pharmaceutically gestogenic component which has been widely used as acceptable carboxylic acids, for the topical treatment of an oral contraceptive. The specific chemical name for acne vulgaris or androgenetic alopezia. ethisterone is 17-alpha-hydroxypregen-4-en-20-yn 15 3-one (17-alpha-ethynyl testosterone); the nor-analog of DESCRIPTION OF THE PRIOR ART ethisterone is known as ethindrone or 17-hyroxy-19 Acne is a well known inflammatory skin disease of norpregn-4-en-20-yn-3-one (17-alpha-ethynyl-19-nor adolescence in which a substantial number of postules testosterone). are formed in the face. In particularly serious cases the This latter material is described for example, in U.S. acne may continue over several years, and lead to a 20 Pat. Nos. 2,744,122 and 2,949,462. The utilizable esters, permanent scarring of portions of the skin. in particular, those of the nor-components are described Because of the influence of endocrinological action, in U.S. Pat. No. 2,964,537. These are formed from the the sebaceous glands of the skin are stimulated to an corresponding carboxylic acids having C1 to C10 carbon over-production of sebum which brings about the satu atoms reacting with the 17 hydroxy group. These car ration of the follicles which with this material, which 25 boxylic acids are, in particular, those which are listed in forms the komedo. This material is formed from numer U.S. Pat. No. 2,964,537 among these acelic acid is par ous components which range from sebaceous residues ticularly preferred. The disclosures of the foregoing to keratinous material. The growth of bacteria in these materials and the destruction of the follicles, gives rise patents are incorporated herein by reference. to the different symptoms of acne in particular, acne 30 DESCRIPTION OF THE PREFERRED vulgaris. EMBODIMENTS A substantial number of therapeutic treatment meth ods of acne have been suggested heretofore which, The topical consumption of ethisterone is generally while they offer a certain measure of relief, do not lead speaking determined by the applied amount rather than to the cure of this condition. Antibiotics have been 35 the formulation of the applied composition. Hence, the applied both topically and systemically to acne patients concentration of ethisterone in an transdermal form can which had the disadvantage that, because of the buildup be substantially less (i.e. up to a factor of 10) than the of resistance to the applied antibiotics, the treating conventional oil-in-water emulsions which show sub agent had to be changed after a certain time interval. stantially no transdermal activity. Furthermore, conventional modes of treatment such as 40 It is generally preferred to apply the ethisterone in a scraping cures, are known wherein layers of skin are concentration of between 0.001 through 1, in particular, removed and thereby the skin channels having oc 0.01 to 0.1 mg/cm2 of skin surface area, the latter cluded sebaceous glands are cleaned. Finally, adminis amount is the one which should reach the receptor tration of natural and synthetic hormones was at position. The composition is generally applied one to tempted to treat both acne and androgenetically caused 45 three times daily in the usual amounts whereby under loss of hair without achieving a decisive break-through usual amounts those amounts are understood which will since the side effects i.e. viralization, fertility problems, lead to the formation of a thin film on the treated skin. and the like were to great. The treatment is continued so long as necessary until The purpose of the present invention is to provide a the symptoms of the disease disappear. Ethisterone can material for the treatment of acne and/or androgeneti 50 be dissolved in the usual topical formulations and ap cally caused alopezia. plied to the skin surface in question in such formulations for example, creams, lotions, solutions, sprays and the SUMMARY OF THE INVENTION like. The solution to the problem lies in the provision of Among applicable transdermal systems there may be ethisterone, 19-norethisterone and/or the correspond 55 utilized alcoholic solution systems, which usually com ing esters of pharmaceutically acceptable carboxylic prise ethanol or propanol. The solubility of the ethister acids thereof, or mixtures thereof in a topically accept one in alcoholic systems can be improved, by the provi able formulation. sion thereto of surfactant materials such as polyethylene It is the surprising finding of this invention that ethis glycols. Especially suitable as polyethylene glycols are terone which is usually dissolved in an oil-in-water 60 those sold in commerce under the Trademark of emulsion, when applied to the skin, reduces the total "Tween' 20-80. Similarly surface active agents such as lipid content of the skin by a factor of about 25% from sorbitan esters may be utilized which are known in the initial value. It is also noted that there is a reduction commerce under the Trademarks of "Tegan' or of 75% by weight of those lipids which comprise waxy "Span". substances which generally have a carbon skeleton of 65 As liquid formulation there may similarly be used between about C20 to about C28. By elimination of these alcohols, in particular, ethanol, isopropanol; acetone; waxy substances which are the substantial cause of the glycerine; glycols, such as propylene glycol; mineral closure of the skin pores, the bacteriological degrada oils, aqueous cellulose containing derivatives as well as 5,094,857 3 4. liquid fluorinated hydrocarbons (freons) of these com cm2 nor-ethisterone through the skin barrier to the re ponents ethanol or isopropanol is preferred.
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