Pharmacokinetic studies of terguride(1): Absorption, distribution and excretion in rats.
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The absorption, distribution and excretion of terguride, a new anti-hyperprolactinemia drug, were studied in rats.<BR> 1. After oral administration of <SUP>3</SUP>H- or <SUP>14</SUP>C-terguride (0.02mg/kg), the radioactivity in plasma reached the maximum(C<SUB>max</SUB>) at 0.5hr, and then disappeared with a half-life of 5hr. The absorption from gastrointestinal tract was complete.<BR> 2. Concentration of terguride in plasma reached C<SUB>max</SUB> at 2hr after oral dosing of unlabelled terguride (0.2mg/kg), and then disappeared with a half-life of 2hr. The bioavailability of terguride after oral administration was about 30%.<BR> 3. Binding to plasma protein <I>in vitro</I> was about 80%, and the binding to plasma proteins were 63 and 55% in the samples collected at 1 and 4hr, respectively.<BR> 4. The radioactivity in tissues after oral dosing of <SUP>3</SUP>H-terguride (0.02mg/kg) showed higher levels in liver, kidney, submaxillary gland and pituitary than in other tissues. No long-lasting retention and accumulation were observed after single and repeated oral dosing. In pregnant rats, foetus and amniotic fluid at 1hr showed similar radioactivity to that in maternal plasma, and then disappeared almost completely within 72hr.<BR> 5. Concentration of terguride in pituitary after oral dosing of unlabelled terguride(0.2mg/kg) was about 5 folds higher than that in plasma and brain.<BR> 6. Urinary and fecal excretion within 7days after oral dosing of <SUP>14</SUP>C-terguride (0.02mg/kg) was 20 and 76%, respectively. After multiple oral dosing for 16days, 25% of the total dose was excreted in urine and 72% in feces within 4days. Biliary excretion after intravenous dosing was 67%, and 15% of the excreted radioactivity was recirculated enterohepatically.<BR> 7. Radioactivity in the stomach milk of a neonate was below 0.04% of the dose given to dam. No radioactivity in neonatal plasma was detected.
- 日本薬物動態学会の論文
日本薬物動態学会 | 論文
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