Pharmaceutical compositions containing a dgat1 inhibitor

Abstract

The present invention relates to a pharmaceutical composition comprising a therapeutically effective amount of a compound of formula (I), or a pharmaceutically acceptable salt thereof, one or more surfactants with lubricant properties, one or more dry binders with disintegrant properties, one or more fillers and one or more disintegrants.

1 : A pharmaceutical composition comprising
 a) a therapeutically effective amount of a compound of formula (I), or a pharmaceutically acceptable salt thereof,   
       
         
           
           
               
               
           
         
         b) one or more surfactants with lubricant properties; 
         c) one or more dry binders with disintegrant properties; 
         d) one or more fillers and 
         e) one or more disintegrants. 
       
     
     
         2 : The pharmaceutical composition according to  claim 1 , further comprising one or more lubricants. 
     
     
         3 : The pharmaceutical composition according to  claim 1 , wherein the surfactant is selected from sodium lauryl sulfate, stearic acid, palmitic acid, myristic acid, poloxamers, polyethylene glycols, the Tween series of surfactants, the Brij series of surfactants, Triton X-100, and combinations thereof. 
     
     
         4 : The pharmaceutical composition according  claim 1 , wherein the surfactant is present in an amount which is 0.1 to 5% by weight of the composition. 
     
     
         5 : The pharmaceutical composition according to  claim 1 , wherein the dry binder is selected from polyethylene glycols, pregelatinized starch, starch; chitosan, guar gum, microcrystalline cellulose, methyl cellulose, calcium carboxymethylcellulose, sodium carboxymethylcellulose, alginic acid, alginic acid sodium salt, hydroxypropylmethyl cellulose, hydroxypropyl cellulose and combinations thereof. 
     
     
         6 : The pharmaceutical composition according to  claim 1 , wherein the dry binder is present in an amount which is 5 to 15% by weight of the composition. 
     
     
         7 : The pharmaceutical composition according to  claim 1 , wherein the filler is selected from microcrystalline cellulose, Anhydrous Dicalcium Phosphate, Anhydrous Lactose, and a mixture thereof. 
     
     
         8 : The pharmaceutical composition according to  claim 7 , wherein the filler is a mixture of Anhydrous Lactose and microcrystalline cellulose wherein the ratio of microcrystalline cellulose and Anhydrous Lactose is between 1:5 and 1:1. 
     
     
         9 . The pharmaceutical composition according to  claim 1 , wherein the disintegrant is selected from crosscarmellose sodium, cross-linked polyvinyl pyrrolidone and Sodium Starch Glycollate. 
     
     
         10 : The pharmaceutical composition according to  claim 9 , wherein the disintegrant is present in an amount which is 2-10% by weight of the tablet. 
     
     
         11 : The pharmaceutical composition according to  claim 10 , wherein the disintegrant is present in an amount which is 2, 6 or 9% by weight of the tablet. 
     
     
         12 : The pharmaceutical composition according to  claim 1 , wherein the salt of the compound of formula (I) is the sodium salt. 
     
     
         13 : The pharmaceutical composition according to  claim 1  in the form of a tablet. 
     
     
         14 : A method for treating or preventing a condition or disorder associated with DGAT1 activity, comprising administering to an animal in need of such treatment a therapeutically effective amount of a pharmaceutical composition according to  claim 1 . 
     
     
         15 . A pharmaceutical composition according to  claim 1  for treating or preventing a condition or disorder associated with DGAT1 activity. 
     
     
         16 : A process for preparing a pharmaceutical composition according to  claim 1  comprising the steps of:
 (a) mixing the compound of the formula (I), or a pharmaceutically acceptable salt thereof, with at least one pharmaceutically acceptable excipient to form a blend; 
 (b) roller compacting, then milling said blend; 
 (c) lubricating the resulting mixture, and 
 (d) compressing the resulting mixture into a solid oral dosage form. 
 
     
     
         17 : The composition of  claim 5 , wherein the hydroxypropylmethyl cellulose or hydroxypropyl cellulose is of medium to high viscosity. 
     
     
         18 : The composition of  claim 17 , wherein the viscosity grades are approximately 3 to 6 cps. 
     
     
         19 : The composition of  claim 17 , wherein the hydroxypropylmethyl cellulose or hydroxypropyl cellulose is low substituted hydroxypropyl cellulose (L-HPC LH-21). 
     
     
         20 : The method of  claim 14 , wherein the animal is a human.