Composition for solubilization of paclitaxel and preparation...

A - Human Necessities – 61 – K

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A61K 31/337 (2006.01) A61K 45/06 (2006.01) A61K 47/44 (2006.01)

Patent

CA 2493336

The present invention relates to a paclitaxel composition and the preparation methods thereof to solubilize paclitaxel wherein said composition comprises 4~90% by weight of at least one selected from the monoglycerides, 0.01~90% by weight of at least one oil and 0.01~20% by weight of paclitaxel. Also the present invention relates to a paclitaxel composition including emulsifiers and the preparation methods thereof to solubilize paclitaxel wherein said composition comprises 4~90% by weight of at least one selected from the monoglycerides, 0.01~90% by weight of at least one oil, 0.01~90% by weight of at least one emulsifier and 0.01~20% by weight of paclitaxel. The composition of the present invention is an effective paclitaxel delivery system since the composition solubilizes paclitaxel, does not form aggregates after being dispersed in water, adsorbs well on the intestinal wall, and therefore has high bioavailability.

Cette invention concerne une composition de paclitaxel et des procédés de préparation permettant de solubiliser le paclitaxel. En poids, ladite composition contient entre 4 et 90 % d'au moins un monoglycéride, entre 0,01 et 90 % d'au moins une huile et de 0,01 à 20 % de paclitaxel. L'invention concerne également une composition de paclitaxel renfermant des émulsionneurs et des procédés de préparation de cette composition. La dite composition contient, en poids, entre 4 et 90 % d'au moins un monoglycéride, entre 0,01 et 90 % d'au moins une huile, entre 0,01 et 90 % d'au moins un émulsionneur et de 0,01 à 20 % de paclitaxel. Cette composition constitue un système efficace d'administration de paclitaxel dans la mesure où elle solubilise ce dernier, ne forme pas d'agrégats après dispersion dans l'eau, adsorbe bien sur la paroi intestinale et offre donc une grande biodisponibilité.

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