Method for the preparation of a pharmaceutical composition comprising 5-aminosalicylic acid for use in treatment of ulcerative colitis and crohn's disease

Abstract

The present invention concerns a new method of preparing granules comprising 5-aminosalicylic acid and a new method of preparing a pharmaceutical composition for the treatment of ulcerative colitis or Crohn's disease by oral administration comprising as active ingredient 5-aminosalicylic acid.

1 - 27 . (canceled) 
     
     
         28 . A composition comprising dry extruded strong, smooth non-spherical granules comprising 5-aminosalicylic acid (5-ASA) and a pharmaceutically acceptable binder, wherein:
 the weight ratio of the binder to 5-ASA in the granules is up to 6.5:100 and   the granules are made by a process comprising extruding a wet mass comprising the binder, 5-ASA, and a solvent comprised of at least 50% w/w water through an extruder.   
     
     
         29 . The composition of  claim 28 , wherein the weight ratio of the binder to 5-ASA in the granules is up to 5:100. 
     
     
         30 . The composition of  claim 28 , wherein the binder is selected from the group consisting of polyvinylpyrrolidone, pregelatinized cornstarch, and cellulose derivative binders. 
     
     
         31 . The composition of  claim 28 , wherein the binder comprises polyvinylpyrrolidone. 
     
     
         32 . The composition of  claim 28 , wherein the solvent is comprised of at least 85% w/w water. 
     
     
         33 . The composition of  claim 28 , wherein more than 85% of the granules have a particle size of 850 to 1000 μm as measured by sieve analysis. 
     
     
         34 . The composition of  claim 28 , wherein the granules exhibit a strength that makes them resistant to wear during further processing. 
     
     
         35 . The composition of  claim 34 , wherein the percent of granules in the composition having a particle size of 850 to 1000 μm as measured by sieve analysis before and after processing for one hour in a laboratory fluid bed does not differ by more than 1%. 
     
     
         36 . The composition of  claim 28 , wherein the granules exhibit a smoothness that permits a reproducible coating process to achieve a target dissolution rate profile. 
     
     
         37 . The composition of  claim 28 , wherein the granules are provided with a pharmaceutically acceptable coating. 
     
     
         38 . The composition of  claim 37 , wherein the coating is selected from the group consisting of enteric coatings and delayed release coatings. 
     
     
         39 . The composition of  claim 37 , wherein the coating provides a dissolution rate-limiting barrier on the granules. 
     
     
         40 . The composition of  claim 39 , wherein the barrier is semipermeable. 
     
     
         41 . The composition of  claim 38 , wherein the coating comprises a polymer selected from the group consisting of polymethacrylate polymers and ethyl cellulose polymers. 
     
     
         42 . A tablet formed from the granules of  claim 28 . 
     
     
         43 . A tablet formed from the granules of  claim 37 .