Avmax, Inc.

Anmax, Inc.

Vincent J Wacher

Leslie Z Benet

Reed M Benet

A method is disclosed for increasing bioavailability of an orally administered pharmaceutical compound comprising orally coadministering the pharmaceutical compound to a mammal in need of treatment with the compound and a gallic acid ester. Preferred gallic acid esters of the invention include octyl gallate, propyl gallate, lauryl gallate, and methyl gallate. Improved formulations of pharmaceutical compounds include the gallic acid ester to enhance the bioavailability of the active ingredient of the pharmaceutical compound.

Use of gallic acid esters to increase bioavailability of orally administered pharmaceutical compounds

A method for increasing bioavailability and reducing inter- and intra-individual variability of an orally administered hydrophobic pharmaceutical compound, which comprises orally coadministering the pharmaceutical compound to a mammal in need of treatment with the compound 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 of 0.01 wt. % or less in an assay that measures conversion of cyclosporine to hydroxylated products using an assay system containing 250 .mu.g rat liver microsomes, 1 .mu.M cyclosporine, and 1 mM reduced nicotinamide adenine dinucleotide phosphate (NADPH) in 1 ml of 0.1 M sodium phosphate buffer, pH 7.4.

Use of essential oils to increase bioavailability of orally administered

A method for increasing bioavailability of an orally administered pharmaceutical compound comprises orally administering the pharmaceutical compound to a mammal in need of treatment with the compound concurrently with propyl gallate. Improved formulations of pharmaceutical compounds include propyl gallate to enhance the bioavailability of the active ingredient of the pharmaceutical compound.

Propyl gallate to increase bioavailability of orally administered

Use of benzoin gum to inhibit P-glycoprotein-mediated resistance of

A method for increasing bioavailability and reducing inter- and intra-individual variability 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 of 0.01 wt. % or less in an assay that measures conversion of cyclosporine to hydroxylated products using an assay system containing 250/.mu.g rat liver microsomes, 1.mu.M cyclosporine, and 1 mM reduced nicotinamide adenine dinucleotide phosphate (NADPH) in 1 ml of 0.1M sodium phosphate buffer, pH 7.4.

Use of essential oils to increase bioavailability of oral pharmaceutical

A method for increasing bioavailability and reducing inter- and intra-individual variability 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 of 0.01 wt. % or less in an assay that measures conversion of cyclosporine to hydroxylated products using an assay system containing 250 .mu.g rat liver microsomes, 1 .mu.M cyclosporine, and 1 mM reduced nicotinamide adenine dinucleotide phosphate (NADPH) in 1 ml of 0.1M sodium phosphate buffer, pH 7.4.

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San Francisco, CA, United States of America

Vincent J Wacher