Transdermal formulation containing cox inhibitors

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.

What is claimed is: 
     
         1 . A pharmaceutical composition for application to the skin, comprising:
 celecoxib comprising about 3.0% of the composition;   carbopol 980 NF comprising about 0.3-1% of the composition;   menthol comprising about 1-2% of the composition;   Brij 58 comprising about 5.0% of the composition;   polyethylene glycol 1000 comprising about 10% of the composition;   Silicone fluid 0.65 cSt comprising about 5% of the composition;   ST Cyclomethicone 5-NF comprising about 5% of the composition;   NaOH;   and   purified water comprising an amount sufficient to raise the formulation to 100%.   
     
     
         2 . The pharmaceutical composition of  claim 1 , wherein the carbopol 980 NF comprises about 0.3% of the composition. 
     
     
         3 . The pharmaceutical composition of  claim 1 , wherein the NaOH comprises about 0.07 to about 0.12% of the composition. 
     
     
         4 . The pharmaceutical composition of  claim 1 , wherein the NaOH comprises about 0.08% of the composition. 
     
     
         5 . The pharmaceutical composition of  claim 1 , wherein the NaOH comprises an amount sufficient to bring the pH of the composition to about 5.5-7.5. 
     
     
         6 . The composition according to  claim 1 , wherein the celecoxib comprises a suspension form. 
     
     
         7 . The pharmaceutical composition of  claim 1 , wherein the celecoxib is coated with the Silicone Fluid 0.65 cSt and the ST-Cyclomethicone 5-NF. 
     
     
         8 . A pharmaceutical composition for application to the skin, comprising:
 celecoxib comprising about 1.5% of the composition;   carbopol 980 NF comprising about 0.3-1% of the composition;   menthol comprising about 0.7-5.0% of the composition;   Brij 58 comprising about 5.0% of the composition;   polyethylene glycol 1000 comprising about 10% of the composition;   Silicone fluid 0.65 cSt comprising about 5% of the composition;   ST Cyclomethicone 5-NF comprising about 5% of the composition;   NaOH;   and   purified water comprising an amount sufficient to raise the formulation to 100%.   
     
     
         9 . The pharmaceutical composition of  claim 8 , wherein the carbopol 980 NF comprises about 0.3% of the composition. 
     
     
         10 . The pharmaceutical composition of  claim 8 , wherein the NaOH comprises about 0.07 to about 0.12% of the composition. 
     
     
         11 . The pharmaceutical composition of  claim 8 , wherein the NaOH comprises about 0.08% of the composition. 
     
     
         12 . The pharmaceutical composition of  claim 8 , wherein the NaOH comprises an amount sufficient to bring the pH of the composition to about 5.5-7.5. 
     
     
         13 . The composition according to  claim 8 , wherein the celecoxib comprises a suspension form. 
     
     
         14 . The pharmaceutical composition of  claim 8 , wherein the celecoxib is coated with the Silicone Fluid 0.65 cSt and the ST-Cyclomethicone 5-NF. 
     
     
         15 . The pharmaceutical composition of  claim 8 , wherein the menthol comprises about 0.7% of the composition.