Absorption, distribution and excretion of 14C-omeprazole.
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Absorption, distribution and excretion of omeprazole, a potent antiulcer agent, were investigated in rats after oral administration of <SUP>14</SUP>C labeled compound (<SUP>14</SUP>C-OPZ).<BR> Urinary and fecal recoveries of radioactivity (<SUP>14</SUP>C) within 4 days at a dose of 5 mg/kg were about 22% and 72% after po dose, about 32 % and 66 % after iv dose, respectively. In male rats, urinary excretion had a tendency to increase under the fasting condition and the higher dose levels.<BR> About 48 % of dose was excreted in the bile of male rats during 30 hours after oral dose of 5 mg/kg, and about 26 % of <SUP>14</SUP>C excreted in the bile was reabsorbed from the intestines due to enterohepatic circulation.<BR> Peak plasma levels of <SUP>14</SUP>C was reached within 0.5 hour, and the radioactivity was eliminated with the terminal half-lives (T<SUB>1/2</SUB>) of 23.1 ?? 30.9 hours after oral dose. A significant increase in Cmax and AUC's was found, exceeding the expected values proportional to administered dose.<BR> High levels of <SUP>14</SUP>C were observed in the liver, kidney, urinary bladder and gastrointestinal tracts, but there was no evidence of an accumulation of <SUP>14</SUP>C in any tissues after oral administration. Tissue distribution pattern of <SUP>14</SUP>C in female rats was similar to that in male rats. The level of <SUP>14</SUP>C in the milk of lactating rats was slightly higher than that in the plasma. The level of <SUP>14</SUP>C in the placenta and tissues in fetuses was lower than that in the maternal blood or plasma.<BR> No significant quantitative and qualitative differences in urinary metabolite pattern were observed among dose levels, but a slightly quantitative difference was observed between males and females.
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日本薬物動態学会 | 論文
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