Pharmaceutical delivery systems for hydrophobic drugs and compositions comprising same

Abstract

A drug delivery system for oral administration of hydrophobic drugs with enhanced and extended absorption and improved pharmacokinetics is provided. In one embodiment, formulations comprising testosterone and testosterone esters, e.g., testosterone palmitate, are disclosed. Methods of treating a hormone deficiency or effecting male contraception with the inventive formulations are also provided.

1 . An oral pharmaceutical formulation comprising
 (a) 10-20 wt. % of a testosterone ester selected from the group consisting of testosterone enanthate, testosterone undecanoate, testosterone cypionate and testosterone palmitate,   (b) surfactant having a HLB value of from 1 to less than 10 selected from the group consisting of mono- and/or di-glycerides of fatty acids, transesterification products of natural or hydrogenated vegetable oil triglyceride and a polyalkylene polyol, and mixtures thereof, and   (c) polyoxyethylene 40 hydrogenated castor oil,   wherein the weight ratio of the surfactant having a HLB value of 1 to less than 10 to polyoxyethylene 40 hydrogenated castor oil is 3.9:1.   
     
     
         2 . The oral formulation of  claim 1 , wherein the testosterone ester is present in the formulation at 15 wt. % thereof. 
     
     
         3 . The oral pharmaceutical formulation of  claim 1 , wherein the testosterone ester is testosterone undecanoate. 
     
     
         4 . The oral pharmaceutical formulation of  claim 1 , wherein the surfactant having a HLB value of from 1 to less than 10 includes a mono- and/or di-glyceride of a fatty acid. 
     
     
         5 . The oral pharmaceutical formulation of  claim 4 , wherein the surfactant having a HLB value of from 1 to less than 10 is glyceryl monolinoleate. 
     
     
         6 . The oral pharmaceutical formulation of  claim 5 , wherein the testosterone ester is present in the formulation at 15 wt. % thereof. 
     
     
         7 . The oral pharmaceutical formulation of  claim 1 , wherein the formulation is encased in a capsule.