ORAL TESTOSTERONE ESTER FORMULATIONS AND METHODS OF TREATING TESTOSTERONE DEFICIENCY COMPRISING SAME
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.