Method for increasing bioavailability of orally administered pharmaceutical compounds
First Claim
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1. A method for increasing bioavailability of an orally administered pharmaceutical compound, which comprises:
- orally coadministering to a mammal in need of treatment by said pharmaceutical compound (1) said pharmaceutical compound and (2) a bioenhancer, said bioenhancer comprising an inhibitor of a cytochrome P450 3A enzyme or an inhibitor of P-glycoprotein-mediated membrane transport in normal gut tissue, said bioenhancer being active only in the gut when administered orally and being present in sufficient amount to provide bioavailability of said compound in the presence of said bioenhancer greater than bioavailability of said compound in the absence of said bioenhancer.
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Abstract
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 a bioenhancer comprising an inhibitor of a cytochrome P450 3A enzyme or an inhibitor of P-glycoprotein-mediated membrane transport, the bioenhancer being present in sufficient amount to provide bioavailability of the compound in the presence of the bioenhancer greater than the bioavailability of the compound in the absence of the bioenhancer.
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18 Claims
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1. A method for increasing bioavailability of an orally administered pharmaceutical compound, which comprises:
orally coadministering to a mammal in need of treatment by said pharmaceutical compound (1) said pharmaceutical compound and (2) a bioenhancer, said bioenhancer comprising an inhibitor of a cytochrome P450 3A enzyme or an inhibitor of P-glycoprotein-mediated membrane transport in normal gut tissue, said bioenhancer being active only in the gut when administered orally and being present in sufficient amount to provide bioavailability of said compound in the presence of said bioenhancer greater than bioavailability of said compound in the absence of said bioenhancer. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10)
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11. The method of clam 1, wherein said bioenhancer comprises a single compound that inhibits both a cytochrome P450 3A enzyme and P-glycoprotein-mediated membrane transport.
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12. A method for increasing bioavailability of an orally administered pharmaceutical compound, which comprises:
orally coadministering to a mammal in need of treatment by said pharmaceutical compound (1) said pharmaceutical compound and (2) a bioenhancer, said bioenhancer comprising an inhibitor of a cytochrome P450 3A enzyme or an inhibitor of P-glycoprotein-mediated membrane transport in normal gut tissue, said bioenhancer being active only in the gut when administered orally and being present in sufficient amount to provide bioavailability of said compound in the presence of said bioenhancer greater than bioavailability of said compound in the absence of said bioenhancer, wherein whether a bioenhancer is active only in the gut is determined by measuring change in bioavailability of said compound when orally coadministered to said mammal with said bioenhancer, measuring change in integrated systemic concentration of said compound when said compound is intravenously administered and said bioenhancer is orally coadministered, and determining that said change in said bioavailability when said compound is orally administered is a statistically significant increase and said change in said integrated systemic concentration when said compound is intravenously administered is not statistically significant. - View Dependent Claims (13, 14, 15, 16, 17, 18)
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