1990 Volume 5 Issue 6 Pages 871-881
The metabolism of emedastine difumarate(KG-2413) after oral administration in human was studied. In human urine, 5-hydroxy-and 6-hydroxyemedastine and their conjugated metabolites were found as major metabolites and emedastine corresponding to 3.6% of dose was also excreted. Moreover 5-hydroxy and 6-hydroxy-5'-oxoemedastine, and emedastine N-oxide were found as minor metabolites. The sum of urinary excretion ratio of emedastine and its metabolites was about 44% for 24h after dosing. Taking urinary excretion ratio and plasma concentration of emedastine into consideration, the extent of bioavailability of emedastine difumarate in human might be similar to that in guinea pigs. However, the metabolic pattern in human was similar to that in rats, in which 5-hydroxy and 6-hydroxyemedastine were urinary major metabolites and emedastine N-oxide was minor metabolites.
