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Title: Pharmacokinetics of a new proton pump inhibitor, YJA-20379-8, in rats with 48-hour water deprivation. Author: Kim HJ, Han KS, Chung YK, Chang MS, Lee MG. Journal: Res Commun Mol Pathol Pharmacol; 1998 Aug; 101(2):137-46. PubMed ID: 9821210. Abstract: The pharmacokinetics of YJA-20379-8 after the intravenous, 20 mg/kg, and oral, 50 mg/kg, administration of the drug, and tissue distribution of YJA-20379-8 after intravenous administration of the drug, 20 mg/kg, to control and 48-h water-deprived rats were reported. After 15-min intravenous infusion of YJA-20379-8, the drug was not detected in urine and less than 0.5% of intravenous dose of the drug was excreted in bile, suggesting that YJA-20379-8 is essentially completely metabolized in rats. Therefore, the CL (clearance) of YJA-20379-8 represents the CLNR (metabolic clearance) of the drug in rats. After oral administration of YJA-20379-8, the F values were low; the values were 21.2 and 19.4% for control and water-deprived rats, respectively. The values were considerably low considering that 93.4 and 84.6% orally administrated YJA-20379-8 were absorbed from rat GI tract of control and water-deprived rats, respectively. This could be due to considerable first-pass (hepatic, gastric, and intestinal) effects. Recently, it was found that gastric and intestinal first-pass effects of YJA-20379-8 were considerable in rats. The amounts of YJA-20379-8 in small intestine, brain, lung, stomach, and kidney increased significantly in water-deprived rats. However, the T/P ratios were comparable (not significantly different) for both groups of rats, indicating that tissue distribution of the drug was not affected by water deprivation.[Abstract] [Full Text] [Related] [New Search]