Patent ID: 6346274
Filing Date: 2002-02-12
Classification: A61K

Abstract:
A pharmaceutical composition, comprising microparticles of a biodegradable polymer matrix in which an active substance having a nonzero degree of loading of up to about 3% is embedded, whereinthe polymer is an ABA triblock copolymer, wherein A represents a copolymer of lactic acid and glycolic acid and B represents a polyethylene glycol chain, the active substance is a physiologically active polypeptide, and wherein the microparticle contains an additive comprising at least one member selected from the group consisting of (1) a disaccharide, (2) dextran having a molecular weight of 20,000 to 60,000 Daltons, (3) an amino sugar, (4) an amino acid, (5) a detergent, (6) a mixture of dextran having a molecular weight of 20,000 to 60,000 Daltons and a cyclodextrin or derivative thereof, (7) a mixture of dextran having a molecular weight of 20,000 to 60,000 Daltons and a polyamino acid, and (8) a mixture of dextran having a molecular weight of 20,000 to 60,000 Daltons and an amino acid, wherein the additive is contained in the pharmaceutical composition in an amount of 1 to 20% by weight in relation to the total weight of the microparticles and the additive substantially prevents aggregation of the physiologically active polypeptide and provides a lower rate of release of the physiologically active polypeptide from the microparticle than a corresponding pharmaceutical composition without the additive.