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(12) United States Patent (10) Patent No.: US 8,486,374 B2 Tamarkin Et Al

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(12) United States Patent (10) Patent No.: US 8,486,374 B2 Tamarkin Et Al USOO8486374B2 (12) United States Patent (10) Patent No.: US 8,486,374 B2 Tamarkin et al. (45) Date of Patent: Jul. 16, 2013 (54) HYDROPHILIC, NON-AQUEOUS (56) References Cited PHARMACEUTICAL CARRIERS AND COMPOSITIONS AND USES U.S. PATENT DOCUMENTS 1,159,250 A 11/1915 Moulton 1,666,684 A 4, 1928 Carstens (75) Inventors: Dov Tamarkin, Maccabim (IL); Meir 1924,972 A 8, 1933 Beckert Eini, Ness Ziona (IL); Doron Friedman, 2,085,733. A T. 1937 Bird Karmei Yosef (IL); Alex Besonov, 2,390,921 A 12, 1945 Clark Rehovot (IL); David Schuz. Moshav 2,524,590 A 10, 1950 Boe Gimzu (IL); Tal Berman, Rishon 2,586.287 A 2/1952 Apperson 2,617,754 A 1 1/1952 Neely LeZiyyon (IL); Jorge Danziger, Rishom 2,767,712 A 10, 1956 Waterman LeZion (IL); Rita Keynan, Rehovot (IL); 2.968,628 A 1/1961 Reed Ella Zlatkis, Rehovot (IL) 3,004,894 A 10/1961 Johnson et al. 3,062,715 A 11/1962 Reese et al. 3,067,784. A 12/1962 Gorman (73) Assignee: Foamix Ltd., Rehovot (IL) 3,092.255. A 6, 1963 Hohman 3,092,555 A 6, 1963 Horn 3,141,821 A 7, 1964 Compeau (*) Notice: Subject to any disclaimer, the term of this 3,142,420 A 7/1964 Gawthrop patent is extended or adjusted under 35 3,144,386 A 8/1964 Brightenback U.S.C. 154(b) by 1180 days. 3,149,543 A 9, 1964 Naab 3,154,075 A 10, 1964 Weckesser 3,178,352 A 4, 1965 Erickson (21) Appl. No.: 12/014,088 3,236,457 A 2, 1966 Kennedy et al. (22) Filed: Jan. 14, 2008 (Continued) FOREIGN PATENT DOCUMENTS (65) Prior Publication Data AU 19878O257 9, 1986 CA 2422244 9, 2003 US 2008/029922O A1 Dec. 4, 2008 (Continued) OTHER PUBLICATIONS Related U.S. Application Data Alcohol SDA 40B.http://www.pharmco-prod.com/pages/MSDS/ SDA 40B 200.pdf Accessed Dec. 9, 2008, 2 pages. (63) Continuation-in-part of application No. 1 1/430,599, Ambrose, Ursual et al., “In Vitro Studies of Water Activity and filed on May 9, 2006, now Pat. No. 7,704,518, which is Bacterial Growth Inhibition of Sucrose-Polyethylene Glycol 400 a continuation-in-part of application No. 10/835,505, Hydrogen Peroxide and Xylose-Polyethylene Glycol 400-Hydrogen Peroxide Pastes Used to Treat Infected Wounds.” Antimicrobial filed on Apr. 28, 2004, now Pat. No. 7,820,145, Agents and Chemotherapy, vol. 35. No. 9, pp. 1799-1803, 1991. application No. 12/014,088, which is a Arisan, http://www.arisankimya.com/kozmetik.htm Accessed Dec. continuation-in-part of application No. 1 1/653,205, 10, 2008, 8 pages. filed on Jan. 12, 2007. Barry, B.W. et al. Comparative bio-availability and activity of pro prietary topical corticosteroid preparations: vasoconstrictor assays (60) Provisional application No. 60/919,303, filed on Mar. on thirty-one ointments, British Journal of Dermatology, 93, 563 21, 2007. 571, 1975. (Continued) (51) Int. Cl. Primary Examiner — Ernst Arnold A6 IK33/00 (2006.01) (74) Attorney, Agent, or Firm — Fish & Richardson P.C. A6 IK 47/34 (2006.01) A 6LX3L/375 (2006.01) (57) ABSTRACT A 6LX3L/355 (2006.01) A waterless composition suitable for delivery of an active A6 IK3I/35 (2006.01) agent to a body Surface or cavity includes a vehicle having A6 IK3I/442 (2006.01) about 70% to about 99% by weight of a hydrophilic polar A6 IK3I/47 (2006.01) Solvent, said hydrophilic solvent selected from the group A 6LX3/57 (2006.01) consisting of (i) a mixture of two or more different polyeth ylene glycols (PEGs), wherein at least one PEG is a high A6 IK 9/12 (2006.01) molecular weight PEG having a melting point greater than A6 IK3I/522 (2006.01) 25° C.; and (ii) propylene glycol (PG); about 0% to about A6 IK3I/35 (2006.01) 10% of at least one surface active agent; about 0% to about A6 IK3I/00 (2006.01) 5% of a polymeric agent; about 0% to about 30% of a sec (52) U.S. Cl. ondary hydrophilic solvent; and about 0% to about 5% of a USPC ........ 424/45; 424/600: 514/178; 514/263.38: silicone oil; and about 3% to about 25% hydrophobic propel 514/345; 514/458: 514/460: 514/474: 514/649; lant. The composition is otherwise substantially free of a 514/772.7 hydrophobic solvent and includes at least one of a surface (58) Field of Classification Search active agent and a polymeric agent. The vehicle and the pro USPC .................... 514/178,263.38, 345, 458, 474, pellant are sufficiently miscible that the components may be 514/649, 772.7 homogeneously distributed with mild shaking. See application file for complete search history. 22 Claims, 4 Drawing Sheets US 8,486,374 B2 Page 2 U.S. PATENT DOCUMENTS 4,305,936 12, 1981 Klein 4,309,995 1, 1982 Sacco 3,244,589 4, 1966 Sunnen 4,310,510 1, 1982 Sherman et al. 3,252,859 5, 1966 Silver 4.323,694 4, 1982 Scala, Jr. 3,261,695 T. 1966 Sienkiewicz 4.325,939 4, 1982 Shah 3,263,867 8, 1966 Lehmann 4.329,990 5, 1982 Sneider 3,263,869 8, 1966 Corsette 4,335,120 6, 1982 Holick et al. 3,298.919 1, 1967 Bishop et al. 4,352,808 10, 1982 Rane et al. 3,301.444 1, 1967 Wittke 4.385, 161 5, 1983 Caunt et al. 3,303,970 2, 1967 Breslau et al. 4,386,104 5, 1983 Nazzaro-Porro 3,330,730 7, 1967 Hernandez 4,393,066 T. 1983 Garrett et al. 3,333,333 8, 1967 Noack 4.427,670 1, 1984 Ofuchi et al. 3,346,451 10, 1967 Collins et al. 4,439,416 3, 1984 Cordon et al. 3,366,494 1, 1968 Bower et al. 4,439,441 3, 1984 Hallesy et al. 3,369,034 2, 1968 Chalmers 4,440,320 4, 1984 Wernicke 3,377,004 4, 1968 Wittke 4,447,486 5, 1984 Hoppe et al. 3,384.541 5, 1968 Clark et al. 4,469,674 9, 1984 Shah et al. 3,395,214 T. 1968 Mummert 4,508,705 4, 1985 Chaudhuri et al. 3,395,215 T. 1968 Schubert 4,522,948 6, 1985 Walker 3,401,849 9, 1968 Weber, III 4,529,601 7, 1985 Broberg et al. 3.419,658 12, 1968 Sanders 4,529,605 7, 1985 Lynch et al. 3.456,052 T. 1969 Gordon 4.552,872 11, 1985 Cooper et al. 3,527.559 9, 1970 Sliwinski 4,574,052 3, 1986 Gupte et al. 3,540,448 11, 1970 Sunnen 4,576,961 3, 1986 Lorck et al. 3,559,890 2, 1971 Brooks et al. 4.595,526 6, 1986 Lai 3,561,262 2, 1971 Borucki 4,603,812 8, 1986 Stoesser et al. 3,563,098 2, 1971 Weber, III 4,627,973 12, 1986 Moran et al. 3,574,821 4, 1971 Pfirrmann 4,628,063 12, 1986 Haines et al. 3,577,518 5, 1971 Shepherd 4,661.524 4, 1987 Thomson et al. 3,667,461 6, 1972 Zamarra 4,672,078 6, 1987 Sakai et al. 3,751,562 8, 1973 Nichols 4,673,569 6, 1987 Shernov et al. 3,770,648 11, 1973 Mackles 4,678.463 7, 1987 Millar 3,787,566 1, 1974 Gauvreau 4,701,320 10, 1987 Hasegawa et al. 3,819,524 6, 1974 Schubert et al. 4,725,609 2, 1988 Kull, Jr. et al. 3,841,525 10, 1974 Siegel 4,738,396 4, 1988 Doi et al. 3,849,580 11, 1974 Weinstein et al. 4,741,855 5, 1988 Grote et al. 3,865,275 2, 1975 De Nunzio 4,752.465 6, 1988 Mackles 3,866,800 2, 1975 Schmitt 4,770,634 9, 1988 Pellico 3,882,228 5, 1975 Boncey et al. 4,780.309 10, 1988 Geria et al. 3,886,084 5, 1975 Vassiliades 4,784.842 11, 1988 London et al. 3,890,305 6, 1975 Weber et al. 4,792,062 12, 1988 Goncalves 3,912,665 10, 1975 Spitzer et al. 4,798,682 1, 1989 Ansmann 3,923,970 12, 1975 Breuer 4,804.674 2, 1989 Curtis-Prior et al. 3,929,985 12, 1975 Webb, Jr. 4,806,262 2, 1989 Snyder 3,952,916 4, 1976 Phillips 4,808,388 2, 1989 Beutler et al. 3,959,160 5, 1976 Horsler et al. 4,822,613 4, 1989 Rodero 3,962,150 6, 1976 Viola 4,822,614 4, 1989 Rodero 3,963,833 6, 1976 DeSalva et al. 4,826,048 5, 1989 Skorka et al. 3,966,090 6, 1976 Prussin et al. 4,827,378 5, 1989 Gillan et al. 3,966,632 6, 1976 Colliopoulos et al. 4,828,837 5, 1989 Uster et al. 3,970,219 7, 1976 Spitzer et al. 4,836,217 6, 1989 Fischer et al. 3,970,584 7, 1976 Hart et al. 4,837,019 6, 1989 Georgalas et al. 3,993,224 11, 1976 Harrison 4,837,378 6, 1989 Borgman 3,997,467 12, 1976 Jederstrom 4,844,902 7, 1989 Grohe 4,001,391 1, 1977 Feinstone et al. 4,847,068 7, 1989 Dole et al. 4,001,442 1, 1977 Stahlberger et al. 4,849,117 7, 1989 Bronner et al.
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