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) about 23 wt. % or less of a testosterone ester selected from the group consisting of testosterone enanthate, testosterone undecanoate, testosterone cypionate and testosterone palmitate,   (b) lipophilic surfactant, and   (c) polyoxyethylene 40 hydrogenated castor oil,   wherein the weight ratio of the lipophilic surfactant to polyoxyethylene 40 hydrogenated castor oil ranges from 3.8:1 to 4.2:1.   
     
     
         2 . The oral pharmaceutical formulation of  claim 1 , wherein the lipophilic surfactant is selected from the group consisting of glyceryl palmitostearate, glyceryl monolinoleate and mixtures thereof. 
     
     
         3 . The oral pharmaceutical formulation of  claim 2 , wherein the lipophilic surfactant is glyceryl monolinoleate. 
     
     
         4 . The oral pharmaceutical formulation of  claim 1 , wherein the testosterone ester is present in the formation at from about 10 wt. % to about 23 wt. % thereof. 
     
     
         5 . The oral pharmaceutical formulation of  claim 1 , wherein the testosterone ester is testosterone undecanoate. 
     
     
         6 . The oral pharmaceutical formulation of  claim 1 , wherein the formulation is encased in a capsule.