Process for microencapsulation of water soluble substances

A - Human Necessities – 61 – K

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A61K 9/50 (2006.01) A61K 9/16 (2006.01) B01J 13/12 (2006.01)

Patent

CA 2369808

The present invention relates to a process for the preparation of microparticles, with an extremely high encapsulation rate, comprising a water- soluble substance in a biodegradable polymer, said water-soluble substance and said biodegradable polymer being first incorporated in an organic liquid phase comprising at least one organic non-water miscible solvent. The organic phase is poured into an aqueous liquid phase having a volume which is sufficient to dissolve said organic solvent, said aqueous phase containing a surfactant, the resulting organic-aqueous phase being homogenised in order to perform in one single step the microparticle formation and the organic solvent removal. The thus obtained microparticles show surprisingly good agent retention qualities.

La présente invention concerne un procédé de préparation de microparticules offrant une vitesse d'encapsulation très élevée. Ce procédé comprend une substance hydrosoluble dans un polymère biodégradable, ladite substance hydrosoluble et ledit polymère biodégradable étant d'abord incorporés dans une phase liquide organique comprenant au moins un solvant non miscible avec l'eau. La phase organique est introduite dans une phase liquide aqueuse présentant un volume suffisamment élevé pour dissoudre ledit solvant organique. Ladite phase aqueuse contient un agent tensio-actif, la phase aqueuse organique résultante étant homogénéisée de manière à réaliser en une seule étape la formation de microparticules et l'élimination du solvant organique. Les microparticules ainsi obtenues présentent une capacité de rétention d'agent étonnamment élevée.

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