Preparation of peptide containing biodegradable microspheres...

A - Human Necessities – 61 – K

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A61K 9/16 (2006.01) A61J 3/00 (2006.01) A61K 38/23 (2006.01) A61K 38/28 (2006.01) A61K 38/38 (2006.01) A61K 47/30 (2006.01) B01J 13/02 (2006.01)

Patent

CA 2235602

Peptide/protein biodegradable drug delivery devices are prepared as microspheres without the use of solvents by a polymer melt process. A melt of thermostable polypeptides and an appropriate low melting block copolymer mixture is prepared and dispersed in an appropriate fluid medium such as air, water or an immiscible organic fluid without using any organic solvent to form microdroplets. The fluid medium is cooled to solidify the microdroplets into microspheres and then collected and purified or further processed as drug delivery devices. These biodegradable microspheres are suitable as implantable or injectable pharmaceutical formulations. Following administration as solid microspheres into the body of a warm blooded animal, the formulations absorb water from the body to form a hydrogel from which the polypeptide is released continuously over an extended period of time.

On prépare des articles d'apport de médicaments prenant la forme de microsphères biodégradables et contenant des peptides ou des protéines, sans utiliser de solvants, par un procédé de fusion de polymères. On prépare un mélange à base de polypeptides thermostables fondus et d'un copolymère en bloc approprié, à bas point de fusion, et on le met en dispersion dans un fluide approprié tel que l'air, l'eau ou un fluide organique non miscible, sans utiliser de solvant organique, afin de former des micro-gouttes. On refroidit ce fluide pour solidifier ces micro-gouttes en microsphères, puis on le récupère et on le purifie ou on le transforme en article de libération de médicaments. Ces microsphères biodégradables se prêtent à l'utilisation sous forme de formulations pharmaceutiques implantables ou injectables. Après leur administration sous forme de microsphères solides dans le corps d'un animal à sang chaud, ces formulations absorbent l'eau du corps pour former un hydrogel qui libère le polypeptide en continu sur une période prolongée.

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