Following a single oral dose of (+)-[14C]cyanidanol-3 in human volunteers, a mean of 55% of the dose was excreted in urine, with 90% of urinary excretion occurring within 24 hours.
What is the metabolism and excretion profile of (+)-[14C]cyanidanol-3 following oral administration in human volunteers?
Following oral administration, (+)-cyanidanol-3 is primarily excreted in the urine as glucuronide and sulphate conjugates within 24 hours, while metabolites persist in plasma for at least 120 hours.
Following administration of a single dose of U14Ccyanidanol-3 to human volunteers, a mean of 55% of the dose of 14C was excreted in urine; 90% of urine 14C was excreted within 24 h of drug administration. The major urinary metabolites were the glucuronides of (+)-catechin and 3'-O-methyl-(+)-catechin, and the sulphate of the latter. These three conjugates collectively accounted for three quarters of urine 14C. Urinary excretion of unchanged (+)-cyanidanol-3 was 0.1-1.4% dose. (+)-Cyanidanol-3 and metabolites containing the intact flavanol ring system accounted for 90% of urine 14C. Ring scission was, under these conditions, a minor metabolic pathway resulting in the excretion of small amounts of 3-hydroxybenzoic acid, 3-hydroxyhippuric acid and 3-hydroxyphenylpropionic acid. Unchanged (+)-cyanidanol-3 was detected in plasma between 30 min and 12 h after administration. Metabolites (as total 14C) persisted in plasma for at least 120 h after administration.
Hackett et al. (Sat,) reported a other. (+)-[14C]cyanidanol-3 was evaluated on Urinary excretion of 14C. Following a single oral dose of (+)-[14C]cyanidanol-3 in human volunteers, a mean of 55% of the dose was excreted in urine, with 90% of urinary excretion occurring within 24 hours.