Oral solid pharmaceutical formulation of the tribulin...

A - Human Necessities – 61 – K

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A61K 9/16 (2006.01) A61K 31/4439 (2006.01)

Patent

CA 2612288

The present invention relates to a pharmaceutical formulation for oral administration of the poorly soluble and therefore hardly bioavailable tubulin inhibitor Indibulin and a process for its manufacture. In particular, there is provided a pharmaceutical formulation of lndibulin for oral administration comprising a granulate containing micronized lndibulin having a particle size of less than 20 ~m for at least 99 vol.-% of the particles, at least one hydrophilic surfactant, and one or more capsulation excipients.

L'invention concerne une formulation pharmaceutique pour l'administration par voie orale du composé indibuline, inhibiteur de la tubuline, qui est peu soluble et présente par conséquent une faible biodisponibilité, et un procédé de fabrication de cette formulation. Elle concerne en particulier une formulation pharmaceutique de l'indibuline s'administrant par voie orale, qui comprend un granulé renfermant de l'indibuline micronisée dont la taille des particules est inférieure à 20 ?m pour au moins 99 % en volume des particules, au moins un tensioactif hydrophile et un ou plusieurs excipients d'encapsulation.

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