Patent ID: 6028054
Filing Date: 2000-02-22
Classification: A61K,A61P,C12Q,G01N,Y10S

Abstract:
A method of formulating an oral pharmaceutical composition, which method comprises:admixing a pharmaceutical compound, a pharmaceutical carrier, and a bioenhancer comprising an inhibitor of P-glycoprotein-mediated membrane transport or an inhibitor of a cytochrome P450 3A enzyme 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 pharmaceutical compound in the presence of said bioenhancer greater than the bioavailability of said pharmaceutical compound in the absence of said bioenhancer when said pharmaceutical composition is administered orally to a mammal, and further wherein whether a bioenhancer is active only in the gut is determined by measuring change in bioavailability of said pharmaceutical compound when orally coadministered to said mammal with said bioenhancer, measuring change in integrated systemic concentration of said pharmaceutical compound when said pharmaceutical compound is intravenously administered and said bioenhancer is orally coadministered, and determining that said change in said bioavailability when said pharmaceutical compound is orally administered is a statistically significant increase and said change in said integrated systemic concentration when said pharmaceutical compound is intravenously administered is not statistically significant.