United States Patent:  5,962,522

Assignee:  AvMax, Inc. (Berkeley, CA)

Filed:  September 5, 1997

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.

SUMMARY OF THE INVENTION

An object of this invention is to identify compositions with superior ability to increase drug bioavailability, particularly by increasing net drug absorption and/or decreasing drug biotransformation in the gut wall by inhibiting cytochrome P450 drug metabolism.

Another object of the invention is to provide compositions that strongly inhibit enzymes of the cytochrome P450 3A class (CYP3A) in the gut in preference to in other locations, such as the liver, which was previously thought to be the primary site of drug metabolism.

One specific object of the present invention is to reduce inter-individual variability of the systemic concentrations of the active pharmaceutical compound, as well as intra-individual variability of the systemic concentrations of the pharmaceutical compound being administered.

The invention is carried out by co-administering propyl gallate with an oral pharmaceutical compound (drug) or compounds to increase drug bioavailability. The compositions and methods of the invention can be used to increase drug efficacy in humans and in other mammals. Although veterinary use is specifically contemplated, the primary use will be in human treatment. Administration schemes include, but are not limited to, use of oral and topical formulations in humans and use of similar formulations for livestock.

Claim 1 of 23 Claims

1. A method for increasing bioavailability of an orally administered pharmaceutical compound, which comprises:

orally coadministering (1) the pharmaceutical compound to a mammal in need of treatment with the compound and (2) propyl gallate in an amount of the propyl gallate sufficient to provide bioavailability of the compound in the presence of the propyl gallate greater than bioavailability of the compound in the absence of the propyl gallate, the amount being at least 1% by weight relative to the total weight of a mixture including (1) and (2).

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