THE ABSORPTION, DISTRIBUTION AND ELIMINATION OF NEVADENSIN IN THE RAT, AND THE RELATIONSHIP BETWEEN PLASMA CONCENTRATION OF THE DRUG AND ITS HYPOTENSIVE EFFECT

By means of polyamide TLC and UV spectrophotometry the following results were obtained:The absorption of suspension and aqueous solution of nevadensin from rat GI tract following intragastric administration was poor, being poorer than the former preparation.Five minutes after iv administration, highest levels were found in liver and plasma; moderate in lymphatic tissue, lungs, heart, brain, kidneys, and spleen; and lowest in adipose tissue, muscle, and testis. The drug-plasma protein binding rate was found to be 51.3±2.2% (X±SD) using equilibrium dialysis method. In rats, the drug was excreted in urine, bile and faeces.The drug was metabolized rapidly and extensively in rats and mice. In the urine, in addition to nevadensin glucuronide and sulfate, there was Still a more polar metabolite with flavonoid structure similar to nevadensin.The hypotensive effect of the drug in dogs after iv infusion at a constant rate was found to parallel with its plasma level. In addition, the maximal hypotensive effect of the drug for each dog closely correlated with the corresponding plasma level.