MICROSPHERES FOR SUSTAINED RELEASE OF OCTREOTIDE ACETATE

摘要

The present invention provides Octreotide acetate-loaded microspheres comprised of a linear PLGA co-polymer having a ratio of Octreotide acetate to PLGA co polymer of between 0.03 and 0.07 (g/g). Microspheres of the invention, compositions and formulations thereof are free of chlorinated solvent and contain less than 5% residual solvent. The Octreotide-loaded microspheres of the invention can be injected intra-muscularly to provide sustained release of Octreotide acetate over a period of up to 6 weeks. Pharmaceutical formulations of the invention are useful for treatment of disorders including but not limited to acromegaly and diarrhoea and flushing associated with malignant carcinoid tumors and VIPomas.