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The metabolites of TA-510, a novel hepatic agent, were investigated by HPLC and LC/MS/MS after oral administration of 14C-TA-510 (30 mg/kg) to rats and dogs or TA-510 (200 mg) to human. The presence of conjugated metabolites was confirmed by enzymatic hydrolyses. 1. Major radioactive components in the urine of rats and dogs and in the bile of rats were the glucuronides of O-demethylated metabolites which consisted of M2 (3'-O-demethylated form), M3 (4'-Odemethylated form), and M4 (3',4'-di-O-demethylated form). The unchanged TA-510 was found in trace amount, accounting for 0.25% and 1.38% of the administered dose in the urine of rats and dogs, respective ly. 2. Within 24 hr after administration to rats, in urine 4.89% and 4.18% of the dose were excreted into the urine as M3-glucuronide and M4-glucuronide, and 29.15% and 4.82% of the dose were excreted into the bile as M3-glucuronide and M2-glucuronide, respectively. In dog urine, main metabolite was identified as M3-glucuronide, 18.22% of the dose, and the other metabolites accounted for less than 2% of the dose. 3. Within 24 hr after oral administration of TA-510 to human, the unchanged TA-510 was hardly detect ed in the urine (0.04% of the dose), and three kinds of glucuronides were found to be the main metabolites. The enzymatic hydrolyses of the human urine produced the aglucones M1 (4-ketone reduced form), M5 (4'-O-demethylated form of M1) and M3, which accounted for 7.73%, 11.11% and 17.02% of the dose, respectively. 4. The metabolites of TA-510 in human urine were analyzed using chiral column because TA-510 was administered as a racemate. There was a large difference in the enantiomer ratios [5S, 6R, 7S] / [5R, 6S, 7R] among the metabolites, 4.22-10.41 as M1, 0.99-2.31 as M3 and 0.18-0.34 as M5, suggesting that TA-510 racemate might be metabolized enantioselectively.

Studies on the Metabolic Fate of TA-510, a Hepatic Anti-inflammatory Agent. (II). Metabolism alter Oral Administration to Rats. Dogs and Human.