A - Human Necessities – 61 – K
Patent
A - Human Necessities
61
K
A61K 9/00 (2006.01) A61K 9/127 (2006.01) A61K 9/16 (2006.01) C09K 19/52 (2006.01)
Patent
CA 2488701
Compounds which are otherwise difficult to solubilize, such as, for example, pharmaceutical actives difficult for the body to absorb, are solubilized into a composition using a solvent system that is a structured fluid. The structured fluid is a reversed cubic phase or reversed hexagonal phase material, or a combination thereof, which includes a polar solvent, a surfactant and a non-paraffinic liquid with a high octanol-water partition coefficient which does not qualify as a surfactant. The compositions thus formed are able to enhance absorption of drugs by the induction of local, transient nanopores in biomembrane absorption barriers and particularly those in which efflux mechanisms, such as those associated with P-glycoprotein and/or cytochrome 3A4, are active. The compositions and methods that are used for solubilizing pharmaceutical actives in structured fluids can simultaneously accomplish solubilization of difficultly soluble drugs and enhancement of absorption.
L'invention concerne des composés difficiles à solubiliser, de type principes actifs pharmaceutiques difficiles à absorber pour le corps, qui sont solubilisés en une composition au moyen d'un système de solvants qui est un fluide structuré. Ce fluide structuré est un matériau à phase cubique inversée ou à phase hexagonale inversée, ou une combinaison de celles-ci, qui comprend un solvant polaire, un tensioactif et un liquide non paraffinique présentant un coefficient de répartition octanol/eau élevé non qualifié de tensioactif. Les compositions ainsi obtenues peuvent améliorer l'absorption de médicaments par l'induction de nanopores locaux, transitoires dans des barrières d'absorption biomembraneuses, et en particulier ceux dont les mécanismes de libération, de type ceux associés à la P-glycoprotéine et/ou au cytochrome 3A4, sont actifs. Les compositions et les procédés utilisés pour solubiliser des principes actifs pharmaceutiques dans des fluides structurés peuvent permettre de solubiliser des médicaments difficilement solubles et d'améliorer leur absorption simultanément.
Lyotropic Therapeutics Inc.
Macrae & Co.
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