Stable polymeric micelle-type drug composition and method...

A - Human Necessities – 61 – K

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A61K 47/30 (2006.01) A61K 9/107 (2006.01) A61K 9/51 (2006.01) A61K 31/337 (2006.01) A61K 47/34 (2006.01)

Patent

CA 2408716

The invention is directed to a biocompatible stable composition containing a hydrophobic drug, such as paclitaxel. The composition, which forms a syringeable polymeric micellar solution in aqueous or body fluids, is a freeze- dried product comprising a hydrophobic drug, i.e. paclitaxel, and an amphiphilic block copolymer wherein a hydrophobic group having affinity or attraction with the hydrophobic drug, such as paclitaxel, is incorporated on its end. The invention provides a shelf life of longer than three years in a sterilized container, stability of longer than three days in infusion fluid, has minimal side effects and shows improved bioavailability.

L'invention concerne une composition stable biocompatible contenant un médicament hydrophobe, tel que paclitaxel. Ladite composition, qui forme une solution micellaire polymère injectable par seringue dans des fluides aqueux ou biologiques, est un produit lyophilisé comprenant un médicament hydrophobe, c'est-à-dire du paclitaxel, et un copolymère bloc amphiphile, le groupe hydrophobe présentant une affinité ou une attraction vis-à-vis du médicament hydrophobe, tel que paclitaxel, étant intégré à son extrémité. La composition de l'invention possède une durée de conservation supérieure à trois ans dans un récipient stérilisé, une stabilité supérieure à trois jours dans un fluide de perfusion, a des effets secondaires minimum et une biodisponibilité améliorée.

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