New pharmaceutical compositions

Abstract

Spontaneously dispersible pharmaceutical compositions comprising a piperidine, e.g. 1-acyl-piperidine Substance P Antagonist and its use in the treatment of CNS disorders, e.g. depression and social phobia, and respiratory diseases, e.g. asthma and chronic bronchitis.

1 . A spontaneously dispersible pharmaceutical composition comprising a piperidine substance P antagonist.  
     
     
         2 . A spontaneously dispersible pharmaceutical composition comprising a piperidine substance P antagonist and a carrier medium comprising 
 1) a hydrophilic component and    2) a surfactant.    
     
     
         3 . A composition as claimed in  claim 1  or  2  for oral administration.  
     
     
         4 . A composition as claimed in any preceding claim comprising a lipophilic component.  
     
     
         5 . A pharmaceutical composition comprising (2R,4S)-N-(1-(3,5-bis(trifluoromethyl) -benzoyl)-2-(4-chlorobenzyl)-4-piperidinyl)-quinoline-4-carboxamide as active agent and a carrier medium comprising 
 1) a hydrophilic phase,    2) a lipophilic phase, and    3) a surfactant.    
     
     
         6 . A pharmaceutical composition of any one of  claims 1  to  4  comprising (2R,4S)-N-(1-(3,5-bis(trifluoromethyl)-benzoyl)-2-(4-chlorobenzyl)-4-piperidinyl)-quinoline-4-carboxamide.  
     
     
         7 . A composition as claimed in any preceding claim in the form of a microemulsion preconcentrate.  
     
     
         8 . A composition as claimed in any preceding claim wherein the hydrophilic component comprises triethyl citrate or propylene glycol, wherein the surfactant comprises a reaction product of a natural or hydrogenated castor oil with ethylene oxide or a polyoxyethylene fatty acid ester, and wherein the lipophilic component comprises a transesterified ethoxylated vegetable oil, a C 8  to C 10  fatty acid mono-, di and/or tri-glyceride, a medium chain fatty acid triglyceride or a refined glycerol-transesterified corn oil.  
     
     
         9 . A spontaneously dispersible pharmaceutical composition comprising about 0.05 to about 20% by weight of (2R,4S)-N-(1-(3,5-bis(trifluoromethyl)-benzoyl)-2-(4-chlorobenzyl) -4-piperidinyl)-quinoline-4-carboxamide, about 5 to about 50% by weight of a hydrophilic component, about 5 to about 80% by weight of a surfactant, and optionally about 5 to about 85% by weight of a lipophilic component, all weights based on the total composition.  
     
     
         10 . A composition as claimed in any preceding claim in the form of a microemulsion.  
     
     
         11 . A composition according to any preceding claim in unit dosage form.  
     
     
         12 . A composition according to  claim 11  in soft or hard gelatin encapsulated form.  
     
     
         13 . A method of treatment of a subject suffering from a disorder treatable with aa piperidine substance P antagonist comprising administering a therapeutically effective amount of a pharmaceutical composition as claimed in any preceding claim to a subject in need of such treatment.