Proliposomal testosterone formulations

摘要

Novel testosterone formulations are disclosed where testosterone is incorporated into a phospholipid/cholesterol system to produce a proliposomal powder dispersion. The proliposomal powder dispersions of the invention may be formulated with phamarceutically acceptable excipients to form pharmaceutical compositions. Enterically coated oral dosage forms are disclosed as are methods of treatment for testosterone replacement therapy.

主权项

1. A method of preparing a proliposomal powder dispersion, wherein the powder dispersion consists essentially of native testosterone, cholesterol, and at least one phospholipid, the method comprising:
(a) dissolving native testosterone in a water miscible solvent until the solution is clear; (b) obtaining a dispersion of native testosterone, phospholipid and cholesterol by adding a phospholipid to the clear solution of native testosterone and water miscible solvent, and subsequently adding cholesterol to the mixture of the solution of native testosterone and water miscible solvent and phospholipid to obtain a dispersion of testosterone, phospholipid and cholesterol, wherein the native testosterone and cholesterol are added in a weight ratio (native testosterone):(cholesterol) ranging from 1.0:0.05 to 1.0:0.30, and the phospholipid is added such native testosterone, cholesterol and phospholipid are present in a weight ratio of (native testosterone): ((cholesterol)+(phospholipid)) ranging from 1:0:1.0 and 1.0:2.5; and (c) removing the water miscible solvent by evaporation until a dry powder is obtained.