Method for preparing submicron particles of paclitaxel

A - Human Necessities – 61 – K

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A61K 9/133 (2006.01) A61K 31/337 (2006.01) A61K 47/24 (2006.01)

Patent

CA 2540383

The present invention is concerned with the formation of submicron particles of an antineoplastic agent, particularly paclitaxel, by precipitating the antineoplastic agent in an aqueous medium to form a pre-suspension followed by homogenization. Surfacants with phospholipids conjugated with a water soluble or hydrophilic polymer such as PEGare used as coating for the particles. The particles produced generally have an average particle size of less than about 1000 nm and are not rapidly soluble.

La présente invention a pour objet la formation de particules sous-microniques d'un agent antinéoplasique, particulièrement de paclitaxel, par la précipitation d'un agent antinéoplasique dans un milieu aqueux afin de former une présuspension, puis une homogénéisation. Les tensioactifs avec phospholipides conjugués à un polymère hydrosoluble ou hydrophile, notamment PEG sont utilisés comme revêtement pour les particules. Les particules produites présentent généralement une granulométrie moyenne inférieure à environ 1 000 nm et ne sont pas rapidement solubles.

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