The absorption, excretion, and biotransformation of 3,4,4'-trichlorocarbanilide in humans.
The metabolism and disposition of 14C-TCC (3,4,4'-trichlorocarbanilide) have been evaluated in humans following oral exposure to 2.2 mumol/kg body wt. Fecal elimination (70% of dose) was complete 120 hr after dosing and the urinary excretion (27% of dose) was completed in 80 hr. The maximum plasma level occurred 2.8 hr after dosing and was 3.7 nmol-equivalents of TCC per g of plasma (approximately 1.2 ppm). Biotransformation of TCC was rapid but did not appear to involve splitting of the basic TCC structure. The major plasma metabolites were N- and N'-glucuronides of TCC which were eliminated with t1/2 approximately 2 hr to the urine and 2'-hydroxy-TCC sulfate and 6-hydroxy-TCC sulfate (the o-hydroxy-TCC sulfates) which were removed with t1/2 approximately 20 hr (presumably into the bile). It is concluded that a nonradioactive analytical method based on the urinary excretion of the N-glucuronides would be suitable for the determination of TCC absorption in humans.
D000328:Adult; D000891:Anti-Infective Agents, Local / Q000378:metabolism*; D001711:Biotransformation; D002224:Carbanilides / Q000378:metabolism*; D005243:Feces / Q000032:analysis; D006801:Humans; D006900:Hydroxylation; D007408:Intestinal Absorption; D007700:Kinetics; D008297:Male; D013997:Time Factors
D000891:Anti-Infective Agents, Local; D002224:Carbanilides