Biodegradable microparticles for controlled release...

A - Human Necessities – 61 – K

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A61K 9/16 (2006.01) A61K 9/00 (2006.01) A61K 9/50 (2006.01) B01J 13/02 (2006.01) B01J 13/22 (2006.01)

Patent

CA 2424892

A process for producing parenterally administrable microparticles, in which an at least 20 % by weight aqueous solution of purified amylopectin-based starch of reduced molecular weight is prepared, the solution is combined with biologically active substance, an emulsion of starch droplets is formed in an outer phase of polymer solution, the starch droplets are made to gel, and the gelled starch particles are dried. A release-controlling shell is optionally also applied to the particles. Microparticles which essentially consist of said starch, have an amino acid content of less than 50 µg and have no covalent chemical cross-linking.

L'invention concerne un procédé destiné à la production de microparticules pouvant être administrées par voie parentérale, consistant à préparer au moins 20 % en masse d'une solution aqueuse d'amidon à base d'amylopectine purifié de faible poids moléculaire, à combiner ladite solution avec une substance bioactive, à former une émulsion de gouttelettes d'amidon dans une phase externe de la solution polymère, à transformer les gouttelettes d'amidon en gel, et à sécher les particules d'amidon gélifié. On peut éventuellement appliquer une enveloppe à libération contrôlée sur les particules. Ces microparticules sont formées essentiellement d'amidon, présentent une teneur en aminoacide inférieure à 50 µg et n'ayant pas de réticulation chimique covalente.

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