PHARMACOLOGICAL PROPERTIES OF GALENICAL PREPARATION .16. PHARMACOKINETICS OF EVODIAMINE AND THE METABOLITE IN RATS

In an attempt to evaluate its pharmacokinetics, [H-3]evodiamine, which is one of the characteristic alkaloids of Evodia fruit was synthesized. The pharmacokinetics of [H-3]evodiamine were investigated in rats. In plasma, the main source of radioactivity was a metabolite of d-evodiamine (EM). One hour after oral administration of 200 mug/kg of [H-3]evodiamine, the radioactivity level in the plasma was maximal. The radioactivity declined in a biphasic manner with half-life times of 1.6 and 78.4 h. The distribution volume was 560 ml/kg. Radioactivity in tissues was higher in the liver, kidney, heart, lung, and adipose tissue than in plasma, but radioactivity in other tissues it was lower than that in plasma. In all tissues the radioactivity proportionally decreased to the level of that in plasma. At 24 h after administration, 19% and 63% of orally administered radioactivity was excreted in urine and bile, respectively.