Pharmaceutical compositions

Abstract

The invention provides lipid-based pharmaceutical compositions comprising alisporivir.

1 . A pharmaceutical composition for oral administration comprising alisporivir in an amount of about 15% to about 20% by weight of the composition, and water in an amount of about 2% to about 15% by weight of the composition. 
     
     
         2 . A pharmaceutical composition according to  claim 1  comprising a lipophilic component, a surfactant, and a hydrophilic component, and wherein the water is in an amount of about 4% to about 15% by weight of the composition. 
     
     
         3 . A composition according to  claim 1  wherein the water is in an amount of about 4% to about 5% by weight of the composition. 
     
     
         4 . A composition according to  claim 1  wherein alisporivir is in an amount of about 19% to about 20% by weight of the composition. 
     
     
         5 . A pharmaceutical composition according to  claim 1  in form of a pre-concentrate for oral administration comprising:
 1) alisporivir in an amount of about 15% to about 20% by weight of the composition, 
 2) a lipophilic component, 
 3) a surfactant, 
 4) a polyethylene glycol, and 
 5) water in an amount of about 2% to about 15% by weight of the composition. 
 
     
     
         6 . A pharmaceutical composition according to  claim 1  in form of a pre-concentrate for oral administration comprising:
 1) alisporivir in an amount of about 19% to about 20% by weight of the composition, 
 2) a lipophilic component, 
 3) a surfactant, 
 4) ethanol, and 
 5) water in an amount of about 4% to about 5% by weight of the composition. 
 
     
     
         7 . A composition according to  claim 1  wherein the hydrophilic component is selected from the group consisting of ethanol, polyethyleneglycol, triethylcitrate, diethylene glycol monoethyl ether and propylene glycol, preferably selected from the group consisting of ethanol, polyethyleneglycol, and propylene glycol. 
     
     
         8 . A composition according to  claim 2  wherein the lipophilic component is selected from the group consisting of medium chain triglycerides, corn oil mono-di-triglycerides, sorbitan monooleate, linoleoyl macrogolglycerides and oleic acid, preferably selected from the group consisting of medium chain triglycerides and sorbitan monooleate. 
     
     
         9 . A composition according to  claim 2  wherein the surfactant is selected from the group consisting of Macrogolglycerol hydroxystearate, Caprylocaproyl Macrogol-8 glycerides, Vitamin E Polyethylene Glycol Succinate and Glyceryl caprylate, preferably selected from the group consisting of Macrogolglycerol hydroxystearate, Caprylocaproyl Macrogol-8 glycerides and Vitamin E Polyethylene Glycol Succinate. 
     
     
         10 . A pharmaceutical composition for oral administration comprising:
 1) alisporivir in an amount of about 5% to about 15% by weight of the composition;   2) a lipophilic component selected from the group consisting of medium chain triglycerides, corn oil mono-di-triglycerides, sorbitan monooleate, linoleoyl macrogolglycerides and oleic acid;   3) a surfactant selected from the group consisting of Macrogolglycerol hydroxystearate, Caprylocaproyl Macrogol-8 glycerides, Vitamin E Polyethylene Glycol Succinate and Glyceryl caprylate;   4) a hydrophilic component selected from the group consisting of ethanol, polyethyleneglycol, triethylcitrate, diethylene glycol monoethyl ether and propylene glycol.   
     
     
         11 . A composition according to  claim 1  in unit dosage form. 
     
     
         12 . A composition according to  claim 11  which contains from about 50 to about 400 mg alisporivir, preferably about 100 or about 200 mg alisporivir. 
     
     
         13 . A capsule comprising the composition according to  claim 1 . 
     
     
         14 . A capsule according to  claim 13  wherein the capsule is a soft gelatin capsule, a hard gelatin capsule or a HPMC-based capsule or a Vegicap. 
     
     
         15 . A composition according to  claim 1  which is a drinkable solution.