Pharmaceutical formulation of n-[5-[2-(3,5-dimethoxyphenyl)ethyl]-2h-pyrazol-3-yl]-4-[(3r,5s)-3,5-dimethylpiperazin-1-yl]benzamide

Abstract

There are provided pharmaceutical compositions comprising a compound of Formula (I) as defined herein and an amount of an alkaline effervescent agent that is sufficient to provide satisfactory in vitro dissolution; and further comprising one or more pharmaceutically acceptable ingredients; and to processes for obtaining them.

1 . A pharmaceutical composition comprising greater than 10% w/w of the compound of Formula (I): 
       
         
           
           
               
               
           
         
       
       and an amount of an alkaline effervescent agent that is sufficient to provide satisfactory in vitro dissolution; and further comprising one or more pharmaceutically acceptable ingredients. 
     
     
         2 . A pharmaceutical composition according to  claim 1  comprising 15% w/w to 40% w/w of the compound of Formula (I). 
     
     
         3 . A pharmaceutical composition according to any of the preceding claims comprising 15% to 25% w/w of the alkaline effervescent agent. 
     
     
         4 . A pharmaceutical composition according to any of the preceding claims comprising 15% w/w to 25% w/w of the compound of Formula (I) and 15% w/w to 25% w/w of the effervescent agent; and further comprising one or more pharmaceutically acceptable ingredients. 
     
     
         5 . A pharmaceutical composition according to any of the preceding claims wherein the effervescent agent is magnesium carbonate. 
     
     
         6 . A pharmaceutical composition according to any of the preceding claims wherein the composition comprises between 0.25% w/w and 8% w/w of an alternative lubricant. 
     
     
         7 . A pharmaceutical composition according to any of the preceding claims wherein the composition comprises between 2.5% w/w and 3.5% w/w of an alternative lubricant 
     
     
         8 . A pharmaceutical composition according to  claims 7  and  8  wherein the alternative lubricant is glyceryl dibehenate. 
     
     
         9 . A wet granulation formulation comprising the compound of Formula (I), water, an alkaline effervescent agent, additional filler(s), binding agent(s) and disintegrant(s). 
     
     
         10 . A wet granulation formulation comprising 15% w/w to 25% w/w of the compound of Formula (I) and 15% w/w to 25% w/w of an alkaline effervescent agent; and further comprising one or more pharmaceutically acceptable ingredients. 
     
     
         11 . A roller compaction formulation comprising 15% w/w to 25% w/w of the compound of Formula (I) and 15% w/w to 25% w/w of an alkaline effervescent agent; and further comprising one or more pharmaceutically acceptable ingredients. 
     
     
         12 . A direct compression formulation comprising 15% w/w to 25% w/w of the compound of Formula (I) and/or hydrate thereof and 15% w/w to 25% w/w of an alkaline effervescent agent; and further comprising one or more pharmaceutically acceptable ingredients.