Method for preparing small particles

A - Human Necessities – 61 – K

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A61K 9/10 (2006.01) A61K 9/14 (2006.01) A61K 31/496 (2006.01)

Patent

CA 2517589

The present invention is concerned with the formation of small particles or organic compounds by precipitating the organic compounds in an aqueous medium to form a pre-suspension followed by adding energy to stabilize a coating of the particle or to alter the lattice structure of the particle. The process includes the steps of: (i) dissolving the organic compound in the water- miscible first solvent to form a solution; (ii) mixing the solution with the second solvent to define a presuspension of particles; and (iii) adding energy to the presuspension to form a suspension of particles having an average effective particle size of less than about 100 µm. The process is preferably used to prepare a suspension of small particles of a poorly water- soluble, pharmaceutically active compound suitable for in vivo delivery by an administrate route such as parenteral, oral, pulmonary, nasal, buccal, topical ophthalmic, rectal, vaginal, transdermal or the like.

La présente invention concerne la formation de fines particules ou de composés organiques, par précipitation des composés organiques dans un milieu aqueux, afin de former une présuspension, suivie d'une adjonction d'énergie pour stabiliser un enrobage de la particule ou modifier la structure maillée de la particule. Le procédé consiste à: i) dissoudre le composé organique dans le premier solvant miscible dans l'eau pour former une solution; ii) mélanger la solution avec le second solvant pour former une présuspension de particules; et iii) ajouter de l'énergie à la présuspension pour former une suspension de particules présentant une taille moyenne effective de la particule inférieure à environ 100 ?m. De préférence, le procédé est utilisé pour préparer une suspension de fines particules d'un composé pharmaceutiquement active, faiblement soluble dans l'eau, qui convient pour une administrationin vivo par voie parentérale, orale, pulmonaire, nasale, buccale, topique, ophtalmique, rectale, vaginale, transdermique ou analogue.

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