Continuous fluorochemical microdispersions for the delivery...

A - Human Necessities – 61 – K

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A61K 9/10 (2006.01) A61K 9/00 (2006.01) A61K 47/06 (2006.01) A61K 49/00 (2006.01)

Patent

CA 2222081

A method for preparing a pharmaceutical microdispersion exhibiting enhanced bioavailability, including the steps of providing a thermodynamically stable pharmaceutical composition comprising at least one pharmaceutical agent incorporated in a physiologically acceptable liquid carrier, the liquid carrier comprising one or more lipophilic solvents such as fluorochemicals and preferably at least one nonfluorinated co-solvent, and combining the stable pharmaceutical composition with an amount of at least one miscible diluent sufficient to initiate phase separation of the pharmaceutical agent from the pharmaceutical composition wherein a microdispersion of the pharmaceutical composition is formed. Also disclosed are microdisperse pharmaceutical compositions and kits for forming such compositions.

L'invention concerne un procédé permettant de préparer une microdispersion pharmaceutique présentant une biodisponibilité accrue, comprenant les étapes suivantes: constitution d'une composition pharmaceutique stable sur le plan thermodynamique, comprenant au moins un agent pharmaceutique incorporé dans un excipient liquide physiologiquement acceptable, ledit excipient liquide contenant un ou plusieurs solvants lipophiles tels que des composés fluorés et, de préférence, au moins un co-solvant non fluoré; et combinaison de la composition pharmaceutique stable obtenue avec une quantité d'au moins un diluant miscible suffisante pour amorcer la séparation des phases c'est-à-dire la séparation de l'agent pharmaceutique de la composition pharmaceutique, ce qui entraîne la formation d'une microdispersion de cette composition pharmaceutique. L'invention concerne également des compositions pharmaceutiques microdispersées et des nécessaires permettant la production de telles compositions.

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