Correlation betweenin vitro andin vivo drug metabolism rate: Oxidation of ethoxybenzamide in rat
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In vitroand in vivocorrelations of the microsomal oxidation of drugs were examined, using ethoxybenzamide as a model drug. Ethoxybenzamide disappearance time course from rat plasma in vivowas analyzed by a two-compartment model assuming a Michaelis-Menten type elimination process. Ethoxybenazmide oxidation in vitrowas measured by the appearance rate of salicylamide in rat liver microsomal suspension. Parameters obtained were Vmax=3.46 and 3.77 μmoles/min/kg body weight and Km=0.378 and 0.192mM, in vitroand in vivo,respectively.
Key wordsin vitro andin vivo correlation microsomal oxidation of drugs nonlinear pharmacokinetics physiological pharmacokinetics tissue distribution distribution volume ethoxybenzamide Michaelis-Menten parameters
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- 7.G. Levy and T. Matsuzawa. Pharmacokinetics of salicylamide elimination in man.Pharmacol. Exp. Ther. 156:285–293 (1967).Google Scholar
- 8.S. Awazu, M. Hanano, H. H. Moon, T. Fuwa, T. Iga, and H. Nogami. Pharmacokinetic analysis by digital computer [in Japanese]. In K. Kakemi (ed.),Absorption, Metabolism, and Excretion of Drugs. Hirokawa Publishing Co., Tokyo, 1971, pp. 301–332.Google Scholar
- 9.S. Awazu. Analogue and digital computer [in Japanese]. In K. Tsuda and H. Nogami (eds.),Biopharmacy, Chijin Shokan, Tokyo, 1971, pp. 448–489.Google Scholar