Process for production of essentially solvent-free small...

A - Human Necessities – 61 – K

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A61K 9/16 (2006.01) A61K 9/14 (2006.01)

Patent

CA 2541493

The present invention is concerned with the formation of small particles of an organic compound by mixing a solution of the organic compound dissolved in a water-miscible organic solvent with an aqueous medium to form a mix and simultantously homogenizing the mix while continuously removing the organic solvent to form an aqueous suspension of small particles essentially free of the organic solvent. These processes are preferably used to prepare an aqueous suspension of small particles of a poorly water-soluble, pharmaceutically active compound suitable for in vivo delivery by an administrative route such as parenteral, oral pulmonary, nasal, buccal, topical, ophthalmic, rectal, vaginal, transdermal or the like.

L'invention concerne la formation de petites particules d'un composé organique par le mélange d'une solution du composé organique dissous dans un solvant organique miscible avec l'eau avec un milieu aqueux en vue de la formation d'un mélange et par l'homogénéisation du mélange tout en enlevant en continu le solvant organique de manière qu'une suspension aqueuse de petites particules sensiblement exemptes de solvant organique soit formée. Ces procédés sont de préférence utilisés pour la préparation d'une suspension aqueuse de petites particules d'un composé faiblement hydrosoluble, actif au plan pharmaceutique convenant à la libération in vivo par voie parentérale, orale, pulmonaire, nasale, buccale, locale, ophtalmique, rectale, vaginale, transdermique ou similaire.

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