Improved aqueous solubility pharmaceutical formulations

A - Human Necessities – 61 – K

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A61K 9/16 (2006.01) A61K 31/496 (2006.01) A61K 47/38 (2006.01)

Patent

CA 2362728

A formulation of a sparingly water-soluble, crystalline pharmaceutically active agent wherein the active agent is converted to and stabilized in its amorphous form as a solid solution of a normally hydrophobic vehicle is described. The amorphous state is stabilized by the composition of the formulation, providing long shelf life of the improved composition. This stabilized formulation also provides increased solubility and bioavailability of the active agent. Solutions of the active agent are stabilized by the composition, preventing recrystallization and precipitation of the less soluble, crystalline form of the active agent from aqueous solutions thereof.

L'invention concerne une formulation à base d'un agent actif du point de vue pharmaceutique, cristallin et modérément soluble dans l'eau, l'agent actif étant converti et stabilisé dans sa forme amorphe comme solution solide d'un excipient normalement hydrophobe. L'état amorphe est stabilisé par la composition de la formulation, ce qui rallonge la durée de vie de la composition améliorée. Cette formulation stabilisée augmente aussi la solubilité de l'agent actif et améliore sa biodisponibilité. Les solutions à base de l'agent actif sont stabilisées par la composition, ce qui empêche la recristallisation et la précipitation de la forme cristalline, moins soluble de l'agent actif à partir des solutions aqueuses de l'agent.

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