Patent ID: 8067032
Filing Date: 2011-11-29
Classification: A61K,A61P

Abstract:
1. A method for preparing a pharmaceutical composition of submicron particles of precipitated paclitaxel or docetaxel, the solubility of which is greater in a water-miscible first solvent than in a second solvent that is aqueous, the method comprising the steps of: (i) mixing into the water-miscible first solvent or the second solvent or both the water-miscible first solvent and the second solvent, a first surface modifier comprising a phospholipid conjugated with a water-soluble or hydrophilic polymer; (ii) mixing into the water-miscible first solvent or the second solvent or both the water-miscible first solvent and the second solvent, a second surface modifier comprising a copolymer of oxyethylene and oxypropylene; (iii) dissolving an active agent consisting of paclitaxel or docetaxel in the water-miscible first solvent to form a solution; (iv) mixing the solution with the second solvent to define a pre-suspension of particles; and (v) homogenizing the pre-suspension to form a suspension of precipitated small particles of the active agent, a phospholipid conjugated with a water-soluble or hydrophilic polymer, and a copolymer of oxyethylene and oxypropylene, the precipitated small particles having an average effective particle size of less than 1000 nm, and the active agent consisting of paclitaxel or docetaxel.