Fast-dissolving pharmaceutical composition

Abstract

A fast-dissolving pharmaceutical composition comprising micronized (R)-2-(4-bromo-2-fluorobenzyl)-1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine-4-spiro-3′-pyrrolidine-1,2′,3,5′-tetrone (hereinafter, referred to as AS-3201). The present pharmaceutical composition has improved dissolution characteristics as well as a good bioavailability.

1 - 12 . (canceled)  
   
   
       13 . A fast-dissolving pharmaceutical composition comprising micronized (R)-2-(4-bromo-2-fluorobenzyl)-1,2,3,4-tetrahydropyrrolo [1,2-a]pyrazine-4-spiro-3′-pyrrolidine-1,2′,3,5′-tetrone (hereinafter, referred to as “AS-3201”).  
   
   
       14 . The fast-dissolving pharmaceutical composition according to  claim 13 , wherein the mean particle size of the micronized AS-3201 is less than about 10 μm.  
   
   
       15 . The fast-dissolving pharmaceutical composition according to  claim 13 , wherein the mean particle size of the micronized AS-3201 is less than about 5 μm.  
   
   
       16 . The fast-dissolving pharmaceutical composition according to  claim 13 , wherein the mean particle size of the micronized AS-3201 is in the range of about 0.5 μm-about 3 μm.  
   
   
       17 . The fast-dissolving pharmaceutical composition according to any one of  claims 13  to  16 , which has a dissolution percentage of the active substance 50% or more for 15 minutes after the start of the dissolution test.  
   
   
       18 . The fast-dissolving pharmaceutical composition according to  claim 17 , which has a dissolution percentage of the active substance 80% or more for 15 minutes after the start of the dissolution test.