Process for preparing spray dried formulation of tmc125

Abstract

This invention relates to a process for producing a spray-dried powder comprising microcrystalline cellulose in a solid dispersion of the anti-HIV compound etravirine (TMC125) in a water-soluble polymer.

1 . A process for producing a solid pharmaceutical powder, comprising the steps of:
 (a) providing a feed mixture of microcrystalline cellulose and a solution of a water-soluble polymer and TMC125;   (b) spray-drying the feed mixture from step (a) to form a solid dispersion of the pharmaceutical agent and the polymer by introducing the feed mixture as droplets into a spray-drying chamber via an atomizing means.   
   
   
       2 . The process of  claim 1 , wherein the microcrystalline cellulose has an average effective particle size of 5-50 μm, in particular 10-30 μm. 
   
   
       3 . The process of  claim 1 , wherein the water-soluble polymer is selected from hydroxypropylmethyl cellulose, polyvinyl pyrrolidone, and copolyvidone. 
   
   
       4 . The process of  claim 3 , wherein the polymer is hydroxypropylmethyl cellulose. 
   
   
       5 . The process of  claim 1 , wherein the ratio of the polymer to pharmaceutical agent is in the range of from 10:1 to 1:1, in particular in the range of from 5:1 to 1:1. 
   
   
       6 . The process of  claim 5 , wherein the ratio of MCC to TMC125 is in the range of from 1:1 to 1:3, in particular about 1:2. 
   
   
       7 . The process of  claim 1 , wherein the solvent is selected from acetone, dichloromethane, ethanol, methanol and combinations thereof. 
   
   
       8 . The process of  claim 1 , wherein the atomizing means comprises a high-pressure nozzle. 
   
   
       9 . A solid dispersion of TMC125 in powder form obtainable by the process of  claim 1 . 
   
   
       10 . A pharmaceutical formulation comprising a powder as defined in  claim 9  and further excipients. 
   
   
       11 . A solid dosage form comprising a powder as defined in  claim 9  and further excipients.