Patent ID: 8465778
Filing Date: 2013-06-18
Classification: A61K,A61P,Y10T

Abstract:
1. A process for making biodegradable microspheres encapsulating a tyrosine kinase inhibitor (TKI), the process comprising the steps of: (a) preparing an organic phase comprising a tyrosine kinase inhibitor, a biodegradable poly(lactide-co-glycolide) polymer, and an organic solvent for the tyrosine kinase inhibitor and the polymer; (b) preparing a first aqueous phase; (c) crystallizing the tyrosine kinase inhibitor in the organic phase; (d) combining the organic and the first aqueous phase with stirring to form an emulsion; (e) preparing a second aqueous phase; (f) adding the second aqueous phase to the emulsion to form a solution; (g) stirring the solution; and (h) evaporating the organic solvent, thereby making biodegradable microspheres encapsulating a tyrosine kinase inhibitor, wherein the tyrosine kinase inhibitor is 10-30 wt % of the microspheres.