Oral formulations

Abstract

A solid pharmaceutical composition containing AP23573 suitable for oral administration is disclosed.

1 . A solid pharmaceutical composition suitable for oral administration which comprises:
 2-35% by weight of AP23573,   0.01-3% by weight of an antioxidant and   70-97% by weight a carrier material comprising at least one cellulose polymer, optionally containing one or more additional pharmaceutically acceptable excipients.   
     
     
         2 . The solid composition of  claim 1  in which the carrier material comprises microcrystalline cellulose, hydroxypropyl cellulose and lactose monohydrate. 
     
     
         3 . The solid composition of  claim 1  in which the antioxidant is butylated hydroxytoluene. 
     
     
         4 . The solid composition of  claim 1  containing one or both of croscarmellose sodium and magnesium stearate as the optional excipient(s). 
     
     
         5 . The solid composition of any of  claims 1 - 4  which further comprises a pharmaceutically acceptable film or enteric coating. 
     
     
         6 . The solid composition of any of  claims 1 - 5  which contains 10-40 mg of AP23573. 
     
     
         7 . A process for preparing a solid pharmaceutical composition of  claim 1 , which comprises:
 (a) providing a solution of AP23573 in a selected solvent;   (b) combining the solution with the carrier to form a wet mass;   (c) granulating the wet mass to generate wet granules;   (d) drying the wet granules to generate dried granules;   (e) compressing said dried granules into tablets; and   (f) optionally coating the resulting tablets with a film-coating polymer;   wherein the solution in step (a) further comprises an antioxidant, or the carrier in step (b) is combined with an antioxidant prior to combining with the solution of AP23573.   
     
     
         8 . The process of  claim 7 , wherein one or more additional excipients are combined in step (b) and incorporated in the wet mass. 
     
     
         9 . The process of either of  claims 7  and  8 , wherein one or more additional excipients are added to the granules before or after drying in step (d). 
     
     
         10 . The process of  claim 9  wherein the one or more additional excipients comprise one or both of croscarmellose sodium and magnesium stearate. 
     
     
         11 . The solid pharmaceutical composition prepared by the method of any of  claims 7 - 10 . 
     
     
         12 . The solid pharmaceutical composition of  claim 11  which contains 10-40 mg of AP23573.