Method of producing submicron particles of a labile agent

A - Human Necessities – 61 – K

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A61K 9/51 (2006.01)

Patent

CA 2373635

The present invention relates to a sustained release composition comprising micron particles of labile agent and a method of preparing and using the sustained release composition. The invention further relates to micron particles of a labile agent and a method of preparing the micron particles. The method of the invention for preparing a composition for the sustained release of a labile agent, comprises forming a suspension comprising the labile agent dispersed in a polymer solution comprising at least one biocompatible polymer and at least one polymer solvent. The suspension is then wet milled to achieve micron particles of the labile agent. The polymer solvent is then removed resulting in a solid polymer/labile agent matrix. The composition for sustained release of a labile agent is likewise prepared according to the method of the invention. The sustained release composition of the present invention can be used in a method for providing a therapeutically effective blood level of a labile agent, in a subject in need of treatment with said agent, for a sustained period comprising administering to the subject the sustained release composition described herein. The method for preparing micron particles of a labile agent comprises forming a suspension comprising the labile agent, dispersed in a polymer solution comprising at least one biocompatible polymer and at least one polymer solvent, and wet milling of the suspension. The submicron particles of labile agent, as described herein, are prepared according to this method.

L'invention concerne une composition retard comprenant des particules microniques d'un agent labile, ainsi qu'un procédé de préparation et d'utilisation de cette composition retard. L'invention concerne en outre des particules microniques d'un agent labile ainsi qu'un procédé de préparation de ces particules. Le procédé de l'invention, destiné à la préparation d'une composition retard d'un agent labile, comprend les étapes suivantes consistant: à former une suspension comprenant l'agent labile dispersé dans une solution polymère contenant au moins un polymère biocompatible et au moins un solvant polymère, puis à broyer par voie humide la suspension, afin d'obtenir les particules microniques de l'agent labile, et à enlever ensuite le solvant polymère de manière à obtenir une matrice solide polymère/agent labile. On prépare ainsi la composition retard d'un agent labile, selon le procédé de l'invention. On peut utiliser cette composition pour apporter un taux sanguin de cet agent labile, qui soit efficace sur le plan thérapeutique, chez un sujet nécessitant un traitement à l'aide de cet agent, et ce pendant une durée prolongée, en administrant à ce sujet la composition retard ici décrite. Le procédé de préparation de particules microniques d'un agent labile consiste à former une suspension comprenant l'agent labile dispersé dans une solution polymère comportant au moins un polymère biocompatible et au moins un solvant polymère, et à broyer par voie humide la suspension. On prépare, selon ce procédé ci-dessus, les particules submicroniques de l'agent labile ici décrites.

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