Correlation between in vitro and in vivo drug metabolism rate: oxidation of ethoxybenzamide in rat.

In vitro and in vivo correlations of the microsomal oxidation of drugs were examined, using ethoxybenzamide as a model drug. Ethoxybenzamide disappearance time course from rat plasma in vivo was analyzed by a two-compartment model assuming a Michaelis-Menten type elimination process. Ethoxybenazmide oxidation in vitro was measured by the appearance rate of salicylamide in rat liver microsomal suspension. Parameters obtained were Vmax = 3.46 and 3.77 mumoles/min/kg body weight and Km = 0.378 and 0.192 mM, in vitro and in vivo, respectively.