Studies on Absorption, Biotransformation and Excretion of Drug.(1). Metabolites of Clofexamide in Rat

Abstract

The metabolites of clofexamide (2-(p-chlorophenoxy)-N-(2-diethylaminoethyl)-acetamide)(I) have been investigated in rat urine and feces. When rats were given a single 200mg/kg dose of clofexamide (I), thirteen metabolites were found in the urine and only unchanged clofexamide in the feces. Twelve metabolites were identified by their spectrometric data (infrared (IR), mass spectrum, ultraviolet (UV) and nuclear magnetic resonance (NMR) spectra) and by thin-layer chromatography (TLC). The following compounds were found to be present in the urine: unchanged clofexamide (I), 2-(p-chlorophenoxy)-N-(2-diethylaminoethyl) acetarnide N-oxide (II), 2-(p-chlorophenoxy)-N-(2-ethylaminoethyl) acetamide (III), 2-(p-chlorophenoxy)-N-(2-aminoethyl) acetamide (IV), p-chlorophenoxyacetic acid (V), p-chlorophenoxyaceturic acid (VI), 2-(4-chloro-3-hydroxyphenoxy)-N-(2-diethylaminoethyl) acetamide (VII), its glucuronide (VIII), 2-(4-chloro-2-hydroxyphenoxy)-N-(2-diethylaminoethyl) acetamide (IX), 2-(4-chloro-3-hydroxyphenoxy)-N-(2-ethylaminoethyl) acetamide (X), its glucuronide (XI) and 2-(4-chloro-2-hydroxyphenoxy)-N-(2-ethylaminoethyl) acetamide (XII).