[Evaluation of pharmacokinetic interaction of aphobazole with CYP1A2 drug-substrate in experiments].

The effect of aphobazole on CYP1A2 (drug-marker caffeine) was studied in rats. Aphobazole was administered orally at doses 5 and 25 mg/kg, caffeine 50 mg/kg. The metabolic ratios (MR) for the caffeine metabolites (theobromine and paraxanthine) were accounted.

[Pharmacokinetics of afobazole metabolite (M-11) in rats].

Pharmacokinetics of compound M-11 (main metabolite of afobazole) after administration via different routes was studied in rats. After oral and intravenous administration, M-11 exhibited weakly pronounced bioconversion with the formation of a few metabolites that could be detected in plasma samples for about 3 hours. The absolute bioavailability of M-11 after oral administration was 68.

[Model study of afobazole distribution in pregnant and lactating female rats and infant rat pups].

Afobazole and M-11, its major metabolite were detected in placental and embryonic rat tissues after single peroral administration to pregnant female rats at a dose of 100 mg/kg. The anxiolytic drug and its metabolite are also detected in rat milk and body of the breast-fed infant rat pups after 4 days of daily administration (200 mg/kg, per os) to lactating female rats.

[Comparative pharmacokinetics of dihydroquercetin in rats upon peroral administration of a parent compound and liposomal flamen D].

The pharmacokinetics of dihydroquercetin (DHQ) in the forms of parent substance and a new liposomal formulation (Flamena D) have been studied in rats upon single peroral administration in a dose of 50 mg/kg. DHQ concentration after enzymatic hydrolysis in the blood plasma was determined by HPLC with UV detection. The elimination half-life of DHQ introduced in the form of Flamena D was about T(1/2) = 1.

[Afobazole metabolism in rats].

Metabolism of afobazole in rats has been studied using mass-spectrometry and HPLC, which revealed 17 products of afobazole biotransformation along with the parent compound. The structures of six afobazole metabolites were established and confirmed by comparison of HPLC retention times with the synthetic reference compounds and HPLC/mass spectrometry. Other metabolites were characterized by the masses of molecular ions.