Use of essential oils to increase bioavailability of oral...

A - Human Necessities – 61 – K

Patent

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A61K 47/44 (2006.01) A61K 31/337 (2006.01) A61K 38/13 (2006.01) A61K 45/00 (2006.01) A61K 47/10 (2006.01)

Patent

CA 2224227

A method for increasing bioavailability of an orally administered hydrophobic pharmaceutical compound, which comprises orally administering the pharmaceutical compound to a mammal in need of treatment with the compound concurrently with an essential oil or essential oil component in an amount sufficient to provide bioavailability of the compound in the presence of the essential oil or essential oil component greater than bioavailability of the compound in the absence of the essential oil or essential oil component, wherein the essential oil or essential oil component has an activity of at least 10% inhibition at a concentration 0.01 wt.% or less in an assay that measures reduced conversion of cyclosporine to hydroxylated products using an assay system containing 250 µg rat liver microsomes, 1 µM cyclosporine and 1 mM reduced nicotinamide adenine dinucleotide phosphate (NADPH) in 1 ml of 0.1 M sodium phosphate buffer, pH 7.4.

La présente invention concerne un procédé permettant d'accroître la biodisponibilité d'un composé pharmaceutique hydrophobe administré oralement. Ce procédé consiste en l'administration par voie orale du composé pharmaceutique au mammifère justifiant d'un tel traitement concurremment avec une huile essentielle ou un composé d'huiles essentielles en une quantité suffisante pour conférer au composé en présence de l'huile essentielle ou du composant d'huile essentielle une biodisponibilité supérieure à celle du composé en l'absence de l'huile essentielle ou d'un composant d'huiles essentielles. En l'occurrence, l'huile essentielle ou le composant d'huiles essentielles présente une activité inhibitrice d'au moins 10 % pour une concentration pondérale de 0,01 % ou moins dans un dosage destiné à mesurer la conversion réduite de la cyclosporine en produits hydroxylatés grâce à un système de dosage contenant 250 µg de microsomes de foie de rat, 1 µM de cyclosporine, et 1 mM de nicotinamide adénine dinucléotide phosphate (NADPH) dans 1 ml de tampon pH 7,4 de phosphate de sodium 0,1M.

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