Pharmaceutical compositions containing a dgat1 inhibitor

Abstract

The present invention relates to 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, e.g. 1, 2 or 3, surfactants with lubricant properties; c) one or more, e.g. 1, 2 or 3, dry binders with disintegrant properties; d) one or more, e.g. 1, 2 or 3, fillers, and e) one or more, e.g. 1, 2 or 3, disintegrants.

1 . A pharmaceutical composition in the form of a tablet comprising
 a) a therapeutically effective amount of the sodium salt of the compound trans-(4-{4-[5-(6-trifluromethyl-pyridin-3-ylamino)-pyridin-2-yl]-phenyl}-cyclohexyl)-acetic acid   
       
         
           
           
               
               
           
         
         b) 0.1 to 5% of sodium lauryl sulfate by weight of the tablet prior to any optional film coating; 
         c) 2 to 20% of hydroxypropyl cellulose by weight of the tablet prior to any optional film coating; 
         d) 15-50% of microcrystalline cellulose by weight of the tablet prior to any optional film coating; 
         e) 0.1-1.0% of colloidal silica by weight of the tablet prior to any optional film coating; 
         f) 0.1-10% of sodium stearyl fumarate by weight of the table prior to any optional film coating; 
         g) 4 to 85% of anhydrous lactose by weight of the tablet prior to any optional film coating of; 
         h) 0.5 to 10% of sodium starch glycolate by weight of the tablet prior to any optional film coating; and 
         i) an optional film coating. 
       
     
     
         2 . The pharmaceutical composition according to  claim 1 , further comprising 0.1 to 10% of magnesium stearate by weight of the tablet prior to any optional film coating. 
     
     
         3 . The pharmaceutical composition according to  claim 1 , further comprising a surfactant selected from the group consisting of 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 to  claim 1  further comprising a binder selected from the group consisting of polyethylene glycols, pregelatinized starch, starch, chitosan, guar gum, methyl cellulose, calcium carboxymethylcellulose, sodium carboxymethylcellulose, alginic acid, alginic acid sodium salt, hydroxypropylmethyl cellulose, hydroxypropyl cellulose and combinations thereof. 
     
     
         5 . The pharmaceutical composition according to  claim 1 , wherein the wherein the ratio of microcrystalline cellulose to anhydrous lactose is between 1:5 and 1:1. 
     
     
         6 . The pharmaceutical composition according to  claim 1 , further comprising crosscarmellose sodium or cross-linked polyvinyl pyrrolidone as a disintegrant. 
     
     
         7 . The composition of  claim 1 , wherein the hydroxypropyl cellulose has a viscosity from 3 to 6 cps. 
     
     
         8 . The composition of  claim 1 , wherein the hydroxypropyl cellulose is low substituted hydroxypropyl cellulose (L-HPC LH-21). 
     
     
         9 . The composition of  claim 1  further comprising 0.05 to 5% of one or more glidants selected from the group consisting of magnesium trisilicate, powdered cellulose, starch, talc and combinations thereof by weight of the tablet prior to any optional film coating. 
     
     
         10 . The composition of  claim 1 , wherein the film coating is comprised of hydroxypropyl methyl cellulose, polyethylene glycol and talc. 
     
     
         11 . The composition of  claim 10 , wherein the film coating further comprises iron oxide. 
     
     
         12 . The composition of  claim 10 , wherein the film coating further comprises titanium dioxide. 
     
     
         13 . 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.