Phenotropyl, or 1-(4-phenyl-2-pyrrolidone)acetamide, is a new original domestic drug possessing high nootropic activity [1]. Previously, the pharmacokinetics of phenotropyl upon administration by various methods in rats was experimentally studied by monitoring the drug concentration dynamics in the blood plasma [2]. Another inseparable part of the characterization of drug pharmacokinetics is investigation of the excretion of parent compounds and their metabolites from the organism.The aim of this study was to monitor the excretion of phenotropyl upon single peroral administration in rats.
EXPERIMENTAL PARTThe excretion of phenotropyl was studied in a group of six male mongrel rats weighing 200 ± 20 g, to which the drug was introduced per os in a dose of 100 mg/kg in the form of an aqueous solution. Samples of urine for analyses were collected from test animals kept in metabolic boxes over 48 h after drug administration for time intervals 0 -2, 2 -4, 6 -8, 8 -24, and 24 -48 h. In a separate experiment, the urine was collected for 72 h after drug administration.The quantitative determination of phenotropyl in the urine samples was performed using gas chromatography as described in [3].
RESULTS AND DISCUSSIONThe results of investigation of the kinetics of phenotropyl excretion with urine from the rat organism are presented in Table 1. As can be seen from these data, about 7.74 mg of the drug (about 38.7 % of the administered dose) is excreted from the rat organism with urine. About 94 % of this amount is eliminated within the first 24 h, while about 6 % is eliminated during the second day after drug administration, and only trace amounts of phenotropyl are detected in the urine collected on the third day.The kinetics of phenotropyl excretion with urine from the rat organism was described in terms of the cumulative excretion equationwhere M is the amount of drug excreted for the time t after administration, M fin is the final amount of the drug excreted 587 0091-150X/04/3811-0587