US2014161889A1PendingUtilityA1

Transdermal formulation containing cox inhibitors

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Assignee: EGIS PHARMACEUTICALS PLCPriority: Jul 31, 2012Filed: Feb 13, 2014Published: Jun 12, 2014
Est. expiryJul 31, 2032(~6 yrs left)· nominal 20-yr term from priority
Inventors:Endre MikulásikTamás SpaitsÁgota Szakálynè Sinka
A61K 31/635A61K 9/06A61K 47/32A61K 9/0014A61K 47/10A61K 31/415A61K 9/10
48
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Claims

Abstract

Disclosed are gel compositions suitable for the topical administration of an active compound having poor solubility and skin penetration, for example, of a COX-2 inhibitor compounds, processes of preparation thereof and methods of use thereof for the treatment of indications treatable by the active compound.

Claims

exact text as granted — not AI-modified
1 . A pharmaceutical composition, comprising:
 a selective COX-2 inhibitor, forming a plurality of solid particles;   a penetration enhancing compound;   at least one solubilizer;   a wetting agent;   a gel forming agent;   a solvent comprising water; and   at least one volatile siloxane agent coating the selective COX-2 inhibitor,   wherein the solid particles are dispersed in the composition, and   wherein the composition comprises a suspension gel.   
     
     
         2 . The composition of  claim 1 , wherein the solubilizer comprises polyethylene glycol hexadecyl ether. 
     
     
         3 . The composition of  claim 2 , wherein the polyethylene glycol hexadecyl ether comprises about 4-15% of the composition. 
     
     
         4 . (canceled) 
     
     
         5 . (canceled) 
     
     
         6 . The composition of  claim 1 , wherein the solubilizer comprises at least one of polyethylene glycol hexadecyl ether, poly(ethylene glycol)-block-poly(propylene glycol)-block-poly(ethylene)glycol, polyethylene glycol 1000, polyoxyethylene (20) sorbitan monostearate, span 60, and emulsifier 10. 
     
     
         7 . The composition of  claim 1 , wherein the solubilizer comprises polyethylene glycol hexadecyl ether and polyethylene glycol 1000. 
     
     
         8 . The composition of  claim 1 , wherein the wetting agent comprises polyethylene glycol. 
     
     
         9 . The composition of  claim 1 , wherein the gel forming agent comprises polymerized prop-2-enoic acid ester. 
     
     
         10 . The composition of  claim 9 , wherein the polymerized prop-2-enoic acid ester comprises about 0.2-1.5% of the composition. 
     
     
         11 . The composition of  claim 1 , wherein the volatile siloxane agent comprises at least one of hexamethyldisiloxane and decamethylcyclopentasiloxane. 
     
     
         12 . The composition of  claim 11 , wherein the hexamethyldisiloxane comprises about 5-20% of the composition. 
     
     
         13 . The composition of  claim 11 , wherein the decamethylcyclopentasiloxane comprises about 4-10% of the composition. 
     
     
         14 . The composition of  claim 1 , wherein the selective COX-2 inhibitor comprises celecoxib. 
     
     
         15 . The composition of  claim 1 , wherein the selective COX-2 inhibitor comprises about 0.5-10% of the composition. 
     
     
         16 . The composition of  claim 1 , further comprising a precipitation agent. 
     
     
         17 . The composition of  claim 16 , wherein the precipitation agent comprises NaOH solution. 
     
     
         18 . The composition of  claim 16 , wherein the precipitation agent comprises about 0.7-1.5% of the composition. 
     
     
         19 . The composition of  claim 1 , wherein the penetration enhancing compound comprises a terpene. 
     
     
         20 . The composition of  claim 1 , wherein the solvent consists essentially of an aqueous solvent. 
     
     
         21 . The composition of  claim 1 , comprising
 celecoxib in an amount of from about 1.5% to about 3%;   menthol in an amount of about 0.7-5%;   polyethylene glycol hexadecyl ether in an amount of 5%;   polyethylene glycol 1000 in an amount of 10%;   polymerized prop-2-enoic acid ester in an amount of about 0.3-1%;   a 10% NaOH solution in an amount of about 0.7-1.5%;   hexamethyldisiloxane in an amount of 5%;   decamethylcyclopentasiloxane in an amount of 5%; and   purified water.   
     
     
         22 . The composition of  claim 21 , wherein the amount of celecoxib is about 1.5%. 
     
     
         23 . The composition of  claim 21 , wherein the amount of celecoxib is about 2%. 
     
     
         24 . The composition of  claim 21 , wherein the amount of celecoxib is about 3%. 
     
     
         25 . The composition of  claim 8 , wherein the polyethylene glycol comprises about 8-15% of the composition. 
     
     
         26 . The composition of  claim 19 , wherein the terpene is menthol. 
     
     
         27 . The composition of  claim 1 , wherein the penetration enhancing compound comprises 0.5-10% of the composition.

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