Inclusion complex of paclitaxel with...

A - Human Necessities – 61 – K

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A61K 47/48 (2006.01) A61K 31/337 (2006.01)

Patent

CA 2467110

The present invention relates to a method for producing a 2-hydroxypropyl-beta- cyclodextrin inclusion complex of taxol, said 2-hydroxypropyl-beta- cyclodextrin having a degree of substitution of 0.4 to about 0.9, wherein the method comprises admixing the 2-hydroxypropyl-beta-cyclodextrin with taxol at a molar ratio of 1-1000 times with respect to taxol. A second aspect of the invention relates to a method for improving the solubility of taxol, said method comprising: (i) dissolving taxol in ethanol; (ii) dissolving 2- hydroxypropyl-beta-cyclodextrin, having a degree of substitution of 0.4 to about 0.9, in water; (iii) admixing the solution from step (i) with the solution from step (ii) and stirring, shaking or heating. A third aspect of the invention provides a 2-hydroxypropyl-beta-cyclodextrin inclusion complex of taxol, wherein said 2-hydroxypropyl-beta-cyclodextrine has a degree of substitution of 0.4 to about 0.9.

Cette invention concerne un procédé de production d'un complexe d'inclusion renfermant de la 2-hydroxypropyl-beta-cyclodextrine et du taxol, laquelle 2-hydroxypropyl-beta-cyclodextrine présente un degré de substitution compris entre 0,4 et 0,9. Ce procédé consiste à mélanger la 2-hydroxypropyl-beta-cyclodextrine avec du taxol selon un rapport molaire de 1/1000 par rapport au taxol. Un deuxième aspect de cette invention porte sur un procédé permettant d'améliorer la solubilité du taxol, lequel procédé consiste : (i) à dissoudre du taxol dans de l'éthanol ; (ii) à dissoudre de la 2-hydroxypropyl-beta-cyclodextrine présentant un degré de substitution compris entre 0,4 et 0,9 dans de l'eau ; (iii) à mélanger la solution obtenue à l'étape (i) avec la solution obtenue à l'étape (ii) puis à remuer, agiter ou chauffer. Un troisième aspect de cette invention concerne un complexe d'inclusion renfermant de la 2-hydroxypropyl-beta-cyclodextrine et du taxol, laquelle 2-hydroxypropyl-beta-cyclodextrine présente un degré de substitution compris entre 0,4 et 0,9.

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