PRODUCTION OF SUSTAINED RELEASE FORMULATION OF WATER SOLUBLE PEPTIDES CONTAINING POLYPEPTIDE, PREFERABLY SOMATOSTATIN OR OCTREOTIDE IN POLYMERIC MATRIX, PREFERABLY POLY(LACTIDE-CO-GLYCOLIDE) GLUCOSE

摘要

PURPOSE: A method of making a sustained release formulation of water soluble peptides containing a polypeptide, preferably somatostatin or an analog or derivative thereof, more preferably octreotide, in a polymeric matrix, preferably poly(lactide-co-glycolide) glucose is provided. The sustained release formulation can exhibit drug serum levels having therapeutic activity over a predetermined period. CONSTITUTION: The sustained release formulation of microparticles containing drugs in a biodegradable and biocompatible polymer is prepared by the steps of: (a) dissolving a polymeric carrier material in a suitable solvent by which a drug compound is not dissolved; (b) adding a drug compound solution of a solvent by which the polymer is not dissolved to the solution of the step(a); (c) inducing the formation of microparticles by addition of a phase inducing agent to the dispersion of the step(c); hardening the microparticles by addition of an oil-in-water emulsion to the mixture of the step(c); and recovering the microparticles. The drug is somatostatin or an analog or derivative thereof, more preferably octreotide, and the polymer is poly(lactide-co-glycolide) glucose.