Submicron nanoparticle of poorly water soluble camptothecin...

A - Human Necessities – 61 – K

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A61K 9/16 (2006.01)

Patent

CA 2663558

The present invention relates to a nanoparticle composition comprising a camptothecin derivative, solid polyethyleneglycol and an anti-associative agent, and the process for preparing the same. Specifically, the present invention provides a composition comprising a nanoparticle of the camptothecin derivative, which is prepared by solid-dispersing the poorly water soluble camptothecin derivative in polyethyleneglycol and dissolving the solid dispersions in an aqueous solution containing an anti-associative agent. The composition of the present invention stabilizes the camptothecin derivative lactone form in body fluid for effective anticancer activity.

La présente invention concerne une composition nanoparticulaire comprenant un dérivé de camptothécine, du polyéthylèneglycol solide et un agent anti-associatif, ainsi que le procédé de préparation de ladite composition. Plus spécifiquement, la présente invention concerne une composition comprenant une nanoparticule du dérivé de camptothécine, qui est préparée par dispersion solide du dérivé de camptothécine faiblement soluble dans l'eau dans du polyéthylèneglycol et dissolution des dispersions solides dans une solution aqueuse contenant un agent anti-associatif. La composition de la présente invention stabilise la forme lactone du dérivé de camptothécine dans un liquide corporel pour assurer une activité anticancéreuse efficace.

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