Sustained-release preparation of physiologically active...

A - Human Necessities – 61 – K

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Details

A61K 38/27 (2006.01) A61K 9/16 (2006.01) A61K 9/19 (2006.01) A61K 47/18 (2006.01)

Patent

CA 2324568

A method for producing a sustained-release preparation, which comprises dispersing a physiologically active polypeptide into an organic solvent solution of a biodegradable polymer and removing the organic solvent, wherein the polypeptide is a powder obtained by lyophilizing an aqueous solution of the polypeptide which solution has a water-miscible organic solvent and/or a volatile salt; which is improved the easiness of handling of the physiologically active polypeptide powder in the process for producing the preparation; which is possible to industrially produce the sustained-release preparation in large scale; which provides a sustained-release preparation showing high and stable concentration of the active component in blood in long term, low initial release ratio of the physiologically active polypeptide, and high entrapment ratio of the polypeptide into the sustained-release preparation.

Cette invention se rapporte à un procédé de production d'une préparation à libération prolongée, qui consiste à disperser un polypeptide physiologiquement actif dans une solution de solvant organique d'un polymère biodégradable et à retirer le solvant organique, le polypeptide étant constitué par une poudre obtenue par lyophilisation d'une solution aqueuse du polypeptide, cette solution renfermant un solvant organique hydromiscible et/ou un sel volatil. Grâce à cette invention, on facilite la manipulation de la poudre de polypeptide physiologiquement active lors du procédé de production de ladite préparation et il est possible de produire industriellement cette préparation à libération prolongée à grande à échelle. On obtient ainsi une préparation à libération prolongée entraînant une concentration élevée et stable du constituant actif dans le sang à long terme, un faible rapport de libération initiale du polypeptide physiologiquement actif et un rapport d'emprisonnement élevé du polypeptide dans la préparation à libération prolongée.

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