Preparation of microparticles having a selected release profile

A - Human Necessities – 61 – K

Patent

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Details

A61K 9/16 (2006.01) A61K 9/50 (2006.01) B01J 13/02 (2006.01) B01J 13/04 (2006.01) B01J 13/20 (2006.01)

Patent

CA 2352818

An improved method for preparing microparticles that exhibit controlled release of an effective amount of an active agent over an extended period of time. More particularly, a method is provided for preparing microparticles having a selected release profile for release of active agent contained in the microparticles. By adjusting the degree of drying that is performed during the preparation of the microparticles, the release profile can be controlled. By performing no intermediate drying, an initial burst and a substantially linear release profile is achieved. By performing substantially complete intermediate drying, an initial lag phase and a substantially sigmoidal release profile is achieved.

L'invention concerne un procédé amélioré de préparation de microparticules dotées d'une propriété de libération retard d'une dose efficace d'un principe actif, sur une période étendue. Ce procédé consiste notamment à préparer des microparticules possédant un profil de libération retard d'un principe actif contenu dans les microparticules. En réglant le degré de séchage, que l'on exécute au cours de la préparation des microparticules, on peut réguler le profil de libération du principe actif. En ne procédant pas à un séchage intermédiaire, on obtient une rupture initiale de la microparticule puis un profil de libération sensiblement linéaire, et en procédant à un séchage intermédiaire sensiblement complet, on obtient une phase retard initiale ainsi qu'un profil de libération sensiblement sigmoïde.

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