Oral testosterone ester formulations and methods of treating testosterone deficiency comprising same

Abstract

A pharmaceutical formulation of testosterone undecanoate is provided. Methods of treating a testosterone deficiency or its symptoms with the inventive formulations are also provided.

58 . An oral pharmaceutical composition comprising testosterone undecanoate solubilized in a carrier comprising at least one lipophilic surfactant and at least one hydrophilic surfactant in a total lipophilic surfactant to total hydrophilic surfactant ratio (w/w) falling in the range of about 6:1 to 3.5:1, wherein said solubilized testosterone undecanoate comprises 18 to 22 percent by weight of the composition. 
     
     
         59 . The oral pharmaceutical composition of  claim 58  in which the at least one hydrophilic surfactant comprises Cremophor RH 40 (polyoxyethyleneglycerol-trihydroxy-stearate). 
     
     
         60 . The oral pharmaceutical composition of  claim 58  in which the at least one lipophilic surfactant comprises oleic acid. 
     
     
         61 . The oral pharmaceutical composition of  claim 58  in which the testosterone undecanoate is solubilized in a carrier substantially free of ethanol. 
     
     
         62 . The oral pharmaceutical composition of  claim 58  which comprises 15 to 17 percent by weight of the at least one hydrophilic surfactant. 
     
     
         63 . The oral pharmaceutical composition of  claim 58  which comprises 50 to 55 percent by weight of the at least one lipophilic surfactant. 
     
     
         64 . A method of treating testosterone deficiency or its symptoms comprising orally administering to a subject suffering from testosterone deficiency or its symptoms an effective amount of a pharmaceutical composition comprising testosterone undecanoate solubilized in a carrier comprising at least one lipophilic surfactant and at least one hydrophilic surfactant in a total lipophilic surfactant to total hydrophilic surfactant ratio (w/w) falling in the range of about 6:1 to 3.5:1 to provide an average serum testosterone concentration at steady state falling in the range of about 300 to about 1100 ng/dL. 
     
     
         65 . The method of  claim 64  in which the composition is administered once daily. 
     
     
         66 . The method of  claim 64  in which the composition is administered twice daily.