The pharmacokinetics of the new psychotropic agent tetramezine in rats has been studied with the aid of gas chromatography. The drug concentration profiles in the blood, excreta, and urine have been determined. Upon peroral administration, tetramezine is rapidly absorbed from the gastrointenstinal tract, and the maximum drug concentration in the blood plasma is observed within 5 min. The pharmacokinetics of tetramezine upon intravascular and intramuscular injections are dose-dependent and linear within the dose range studied. The average half-elimination times are 0.42 h (i.v.); 0.32 h (i.m.); and 0.42 h (p.o.). The obtained data are important for the subsequent investigation of the drug bioaccessibility and metabolism and for establishing relationships between the drug behavior in vitro, in experiments on animals, and in clinics. 3450091-150X/05/3907-0345

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The metabolism of a new antioxidant agent -phenozan acid -was studied in rabbits. The main directions of this process are (i) oxidation of benzene ring with the formation of 2,6-di-tert-butyl-p-benzoquinone and (ii) dehydration of the propionic acid fragment with the formation of 4-hydroxy-3,5-di-tert-butylphenylacrylic acid methyl ester. The structures of metabolites were established by computer-aided gas chromatography/mass spectrometry and confirmed by direct synthesis. 61 0091-150X/06/4002-0061

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The excretion of the novel antipsychotic agent tetramezine in rats was investigated using gas chromatography. Upon a single intramuscular administration in a dose of 200 mg/kg, only 5.2% of the introduced drug was recovered in the unchanged form, which implies that feces and urine are not the major routes of tetramezine excretion. The results suggest that tetramezine is well absorbed and the major proportion of it is subject to biotransformation, so that metabolism is the principal mechanism of clearance. The renal clearance (0.15 liter/(h × kg)) and half-elimination time (0. 37 h) for tetramezine in rats are determined using the experimental pharmacokinetic parameters (elimination constant and distribution volume).