Sustained-release composition and method for producing the same

A - Human Necessities – 61 – K

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A61K 9/16 (2006.01) A61K 31/55 (2006.01)

Patent

CA 2671670

Sustained-release compositions wherein a water-soluble physiologically active peptide is substantially uniformly dispersed in a microcapsule comprised of a lactic acid polymer or a salt thereof, and the physiologically active substance is contained in an amount of 15 to 35 wt/wt% to the total microcapsules and weight-average molecular weight (Mw) of the lactic acid polymer is about 11,000 to about 27,000, which is characterized by having a high content of the physiologically active substance, and suppression of the initial excessive release within one day after the administration and a stable drug sustained-release over a long period of time, and method for producing the same.

La présente invention se rapporte à des compositions à libération prolongée comprenant un peptide physiologiquement actif hydrosoluble dispersé de manière sensiblement uniforme dans une microcapsule composée d'un polymère d'acide lactique ou d'un sel de celui-ci, la substance physiologiquement active étant présente en une quantité comprise entre 15 et 35% poids/poids par rapport au poids total des microcapsules, le poids moléculaire moyen en poids (Mw) du polymère d'acide lactique étant compris entre 11000 et 27000 environ. Ces compositions se caractérisent par une forte teneur en substance physiologiquement active, par la suppression de la libération excessive initiale dans le jour suivant l'administration et par une libération prolongée stable de médicament sur une longue période. Cette invention concerne également un procédé de production correspondant.

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