Preparation of an oil-in-water emulsion for polymer stabilized pharmaceutical formulations

Abstract

An improved process for producing an oil-in-water emulsion to deliver a substantially water insoluble active pharmaceutical ingredient includes creating a microemulsion containing such ingredient in the oil phase of the emulsion by mixing an aqueous phase including non-ionic surfactant, polyol, and water, wherein the weight ratio of the surfactant to polyol to water is between 10:20:70 and 1:1:1, to generate a mixture, with an oil phase comprising a substantially water insoluble active pharmaceutical ingredient and a long-chain triglyceride; circulating the said mixture through a homogenizer at a temperature from 20° C. to 60° C. to generate a coarse emulsion; passing the coarse emulsion through a microfluidizer at a pressure of from 70 MPa to 150 MPa at least once to produce an oil-in-water microemulsion; and, optionally, filtering the microemulsion through a 0.2 μm filter and/or mixing the microemulsion with a polymeric stabilizer.

Dependencies are inferred from the claim text.