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(12) Patent Application Publication (10) Pub. No.: US 2015/0025060A1 Tamarkin Et Al

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(12) Patent Application Publication (10) Pub. No.: US 2015/0025060A1 Tamarkin Et Al US 2015.0025060A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2015/0025060A1 Tamarkin et al. (43) Pub. Date: Jan. 22, 2015 (54) FOAMABLE COMPOSITIONS AND KITS (30) Foreign Application Priority Data COMPRISING ONE ORMORE OF A CHANNEL AGENT, ACHOLINERGICAGENT, Oct. 25, 2002 (IL) .......................................... 1524.86 A NITRC OXDE DONOR AND RELATED AGENTS AND THEIR USES Publication Classification (71) Applicant: Foamix Pharmaceuticals Ltd., Rehovot (51) Int. Cl. (IL) A613 L/554 (2006.01) A 6LX3 L/505 (2006.01) (72) Inventors: Dov Tamarkin, Macabim (IL); Meir A647/10 (2006.01) Eini, Ness Ziona (IL); Doron Friedman, A613 L/4422 (2006.01) Karmei Yosef (IL); Tal Berman, Rishon (52) U.S. Cl. Le Ziyyon (IL); Alex Besonov, Rehovot CPC ........... A6 IK3I/554 (2013.01); A61 K3I/4422 (IL) (2013.01); A61 K3I/505 (2013.01); A61 K 47/10 (2013.01) (21) Appl. No.: 14/448,670 USPC ....................... 514/211.03: 514/356; 514/275 (22) Filed: Jul. 31, 2014 (57) ABSTRACT Related U.S. Application Data The present invention relates to a foamable therapeutic com position comprising: (a) a therapeutically effective concen (63) Continuation of application No. 1 1/767,442, filed on tration of at least one active agent selected from the group Jun. 22, 2007, which is a continuation-in-part of appli consisting of a channel agent, a cholinergic agent, and a nitric cation No. 10/911.367, filed on Aug. 4, 2004, said oxide donor; and (b) a foamable carrier comprising: application No. 1 1/767,442 is a continuation-in-part of i. about 50% to about 98% of a solvent selected from the application No. 10/532,618, filed on Dec. 22, 2005, group consisting of water, a hydrophilic solvent; a filed as application No. PCT/IB2003/005527 on Oct. hydrophobic solvent; a potent solvent; a polar solvent, a 24, 2003, said application No. 1 1/767,442 is a contin silicone, an emollient, and mixtures thereof; uation-in-part of application No. 10/835,505, filed on ii. 0% to about 48% of a secondary solvent selected from Apr. 28, 2004, now Pat. No. 7.820,145, which is a the group consisting of water, a hydrophilic solvent; a continuation-in-part of application No. 1 1/430,437, hydrophobic solvent; a potent solvent; a polar solvent, a filed on May 9, 2006, now Pat. No. 7,645,803, said silicone, an emollient, a co-solvent, a penetration application No. 1 1/767,442 is a continuation-in-part of enhancer and mixtures thereof. application No. 11/430,599, filedon May 9, 2006, now iii. a surface-active agent; Pat. No. 7.704,518, which is a continuation-in-part of iv. about 0% to about 5% by weight of at least one poly application No. 10/835,505, filed on Apr. 28, 2004, meric agent; and now Pat. No. 7,820,145. V. a liquefied or compressed gas propellant at a concentra (60) Provisional application No. 60/492.385, filed on Aug. tion of about 3% to about 25% by weight of the total 4, 2003, provisional application No. 60/429.546, filed composition; on Nov. 29, 2002, provisional application No. 60/679, wherein the composition is housed in a container and is 020, filed on May 9, 2005, provisional application No. substantially flowable, and 60/784,793, filed on Mar. 21, 2006, provisional appli which upon release expands to form a breakable foam; and cation No. 60/492.385, filed on Aug. 4, 2003, provi wherein the foamable carrier is selected to generate a foam sional application No. 60/530,015, filed on Dec. 16, of good to excellent quality. 2003, provisional application No. 60/679,020, filed on The invention further provides a method of treating, alleviat May 9, 2005, provisional application No. 60/784,793, ing or preventing a disorder of mammalian Subject, compris filed on Mar. 21, 2006, provisional application No. ing administering Such a composition to an afflicted target 60/815,948, filed on Jun. 23, 2006. site. Patent Application Publication Jan. 22, 2015 Sheet 1 of 5 US 2015/0O25060A1 Figure 1 Patent Application Publication Jan. 22, 2015 Sheet 2 of 5 US 2015/0O25060A1 Figure 3 Fig 3.1 Fig 3.2 Fig 3.3 X200 X400 Patent Application Publication Jan. 22, 2015 Sheet 3 of 5 US 2015/0O25060A1 X400 Patent Application Publication Jan. 22, 2015 Sheet 4 of 5 US 2015/0O25060A1 Patent Application Publication Jan. 22, 2015 Sheet 5 of 5 US 2015/0O25060A1 Figure 6 Figure 7 WNXOO2 US 2015/0025060A1 Jan. 22, 2015 FOAMABLE COMPOSITIONS AND KITS 0008 External topical administration is an important COMPRISING ONE OR MORE OFA route for the administration of drugs in disease treatment. CHANNEL AGENT, A CHOLINERGICAGENT, Many groups of drugs, including, for example, antibiotic, A NITRIC OXDE DONOR AND RELATED anti-fungal, anti-inflammatory, anesthetic, analgesic, anti-al AGENTS AND THEIR USES lergic, corticosteroid, retinoid and anti-proliferative medica tions are preferably administered in hydrophobic media, CROSS REFERENCE TO RELATED namely ointment; or in semi-solid creams. However, oint APPLICATIONS ments and creams often form an impermeable barrier, so that 0001) This application claims the benefit of priority under metabolic products and excreta from the wounds to which 35 U.S.C. S 119(e) to U.S. Patent Application No. 60/815,948, they are applied are not easily removed or drained away. filed on Jun. 23, 2006, entitled "Foamable Compositions Furthermore, it is difficult to administer creams and oint Comprising a Calcium Channel Blocker, a Cholinergic Agent ments onto damaged tissues, so the efficacy of the drug is and a Nitric Oxide Donor,” which is incorporated herein in its reduced. In addition, ointments and creams often do not cre entirety. ate an environment for promoting respiration of the wound 0002 This application is a continuation-in-part applica tissue and it is not favorable to the normal respiration of the tion of co-pending U.S. patent application Ser. No. 10/835, skin. Foam offers an alternative form of products for topical 505, filed on Apr. 28, 2004, which claims the benefit of administration, which is more convenient to use and does not priority under 35 U.S.C. S 119(e) to U.S. Patent Application require rubbing in order to facilitate drug spreading and No. 60/530,015, filed on Dec. 16, 2003, and U.S. Patent absorption. Application No. 60/492.385, filed on Aug. 4, 2003, all 0009 Foams and, in particular, foams that are substan entitled “Oleaginous Pharmaceutical and Cosmetic Foam. tially based on non-aqueous solvents are complicated sys and all hereby incorporated in their entirety by reference. tems which do not form under all circumstances. U.S. patent 0003) This application is a continuation-in-part applica application Ser. No. 10/835,505 entitled “Oleaginous Phar tion of co-pending U.S. patent application Ser. No. 1 1/430, maceutical and Cosmetic Foam describes stable oleaginous 437, filed on May 9, 2006, entitled “Saccharide Foamable cosmetic or therapeutic foam compositions containing cer Compositions,” which claims the benefit under 35 U.S.C. tain active agents, having unique therapeutic properties and S119(e) of U.S. Provisional Patent Application No. 60/679, methods of treatment using such compositions. The foamable 020, filed on May 9, 2005, entitled “Hygroscopic Anti-Infec carrier includes at least one solvent selected from a hydro tive Compositions.” and both of which are hereby incorpo phobic solvent, a silicone oil, an emollient, a co-solvent, and rated in their entirety by reference. mixtures thereof, wherein the solvent is present at a concen 0004) This application is a continuation-in-part applica tration of about 70% to about 96.5% by weight of the total tion of co-pending U.S. patent application Ser. No. 1 1/430, composition, at least a non-ionic surface-active agent at a 599, filed on May 9, 2006, entitled “Foamable Vehicle and concentration of about 0.1% to less than about 10% by weight Pharmaceutical Compositions Thereof.” which claims the of the total composition; at least one gelling agent at a con benefit under 35 U.S.C. S 119(e) of U.S. Provisional Patent centration of about 0.1% to about 5% by weight of the total Application No. 60/784,793, filed on Mar. 21, 2006, entitled composition; a therapeutically effective amount of at least “Polyol Foamable Vehicle and Pharmaceutical Compositions one active agent; and at least one liquefied or compressed gas Thereof.” both of which are herein incorporated by reference propellant, at a concentration of about 3% to about 25% by in its entirety. weight of the total composition. 0005. This application is a continuation-in-part applica 10010 Huggins et al. describes hydroalcoholic foam com tion of co-pending U.S. patent application Ser. No. 10/532, positions in WO 2004/071479. 618, filed on Dec. 22, 2005, entitled “Cosmetic and Pharma ceutical Foam.” which is a 371 application of International 10011. A fissure is a split in the skin of the distal anal canal. Patent Application No. IB03/005527, designating the United It is a common complaint in young adults with a roughly States and filed on Oct. 24, 2003, which claims the benefit of equal incidence in both sexes. Acute fissures are very com priority under 35 U.S.C. S 119(e) to U.S. Patent Application mon and most heal spontaneously, but a proportion progress No. 60/492.546, filed on Nov. 29, 2002, both entitled “Cos to form a chronic linear ulcer in the anal canal and show great metic and Pharmaceutical Foam and which claims the ben reluctance to heal without intervention.
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