Taxane formulations comprising phospholipids

A - Human Necessities – 61 – K

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A61K 31/335 (2006.01) A61K 9/127 (2006.01) A61K 31/70 (2006.01)

Patent

CA 2153326

The present invention relates to a pharmaceutical composition for use in treatment of cancer patients. The composition includes at least one taxane present in a pharmaceutical effective amount and a mixture of one or more negatively charged phospholipids and one or more zwitterion (i.e. uncharged) phospholipids. This mixture entraps the at least one taxane in what is believed to be a liposome. The mixture contains a ratio of negatively charged phospholipids to zwitterion phospholipids of 1:9 to 7:3. The taxol is present in an amount of 1.5-8.0 mole percent taxane. The composition is in the form of particles having a size of 0.025 to 10 microns with substantially no taxane crystals.

La présente invention concerne une composition pharmaceutique pour traiter le cancer. Cette composition comprend au moins un taxane, en une quantité pharmaceutiquement efficace, et un mélange de un ou plusieurs phospholipides à charge négative et un ou plusieurs phospholipides à ions hermaphrodites (c'est-à-dire, sans charge). Ce mélange englobe le taxane dans ce que l'on pense être un liposome. Dans ce mélange, le rapport de phospholipides à charge négative sur les phospholipides à ions hermaphrodites est compris entre 1:9 et 7:3. La quantité de taxol est de 1,5-8,0 mole pour cent de taxane. La composition se présente sous la forme de particules de 0,025 à 10 microns de taille, sensiblement dépourvue de cristaux de taxane.

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