Slow release pharmaceutical composition made of microparticles

A - Human Necessities – 61 – K

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A61K 9/16 (2006.01) A61K 38/09 (2006.01) A61K 47/34 (2006.01)

Patent

CA 2688478

Pharmaceutical composition made of microparticles for the slow release of an active substance at least during a period covering the 6th month after injection of said composition, said composition comprising a group of microparticles made of a copolymer of the PLGA type which incorporate an active substance in the form of a water insoluble peptide salt; said copolymer furthermore comprising at least 75 % of lactic acid and an inherent viscosity between 0.1 and 0.9 dl/g, as measured in chloroform at 25 °C and at a polymer concentration of 0.5 g/dL; said microparticles furthermore having a size distribution defined as follows : - D (v,0.1 ) is between 10 and 30 micrometers, - D (v,0.5) is between 30 and 70 micrometers, - D(v,0.9) is between 50 and 1 10 micrometers.

L'invention concerne une composition pharmaceutique faite de microparticules pour la libération lente d'une substance active au moins pendant une période couvrant les 6 mois après l'injection de ladite composition, ladite composition comprenant un groupe de microparticules faites d'un copolymère du type PLGA qui incorporent une substance active sous la forme d'un sel de peptide insoluble dans l'eau; ledit copolymère comprenant de plus au moins 75 % d'acide lactique et une viscosité inhérente entre 0,1 et 0,9 dl/g, telle que mesurée dans le chloroforme à 25°C et à une concentration en polymère de 0,5/dL; lesdites microparticules ayant de plus une distribution de dimension définie comme suit : - D (v, 0,1 ) se trouve entre 10 et 30 micromètres, - D (v, 0,5) se trouve entre 30 et 70 micromètres, - D(v, 0,9) se trouve entre 50 et 110 micromètres.

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