Patent ID: 6379707
Filing Date: 2002-04-30
Classification: A61K,A61P,C07D

Abstract:
A method of preparing a granular particle comprising:(a) a solid solution of an amorphous, pharmaceutically active agent and a pharmaceutically acceptable hydrophobic vehicle, wherein said pharmaceutically active agent is normally crystalline and sparingly water soluble at ambient pressure and temperature; (b) a stabilizer comprising a polyethylene glycol, sugars, sorbitol, mannitol, polyvinylpyrrolidone, or one or more cellulose ethers; and (c) a disintegrant comprising croscarmellose sodium, sodium starch glycolate, crospovidone, or a cross-linked polyacrylate; wherein said method comprises the steps of. (i) heating the hydrophobic vehicle to a temperature above the temperature at which said hydrophobic vehicle melts and to a temperature at which said active agent dissolves in the molten hydrophobic vehicle; (ii) dissolving said pharmaceutically active agent in the molten vehicle to form a molten solution of said active agent in said hydrophobic vehicle; then (iii) adding a stabilizing amount of said stabilizer to the molten solution of said pharmaceutically agent and hydrophobic vehicle; and (iv) granulating the molten mixture from step (iii) with a cooled disintegrant and optionally a binder at a temperature below about 30Â° C. to form the granular particle comprising the solid solution of pharmaceutically active agent stabilized in amorphous form in said hydrophobic vehicle.