The metabolic fate of a new diuretic, tienilic acid, was investigated in Wistar rats, Swiss mice, Beagle dogs, and large white pigs using the 14C-labelled compound. Tienilic acid and its metabolites were determined in bile, urine, and plasma following intravenous and oral administration. In general, only a small amount of unmetabolized drug is excreted. Biotransformation consists of two major metabolic routes; one is reduction and the other is oxidative hydrolysis of the molecule at the level of the carbonyl group. These two routes co-exist in all species studied, but the reduction route is prominent in the dog. Mass spectrometry was used to elucidate the structure of two metabolites and confirm it for the third.
14C-Diclofurime, a new Ca antagonist, was administered orally to dogs and pigs, and metabolites detected in urine and plasma. Metabolites contained in pooled urine were concentrated by column chromatography (reverse phase, gel permeation and normal phase). Chemical structures were determined by i.r. mass and 1H n.m.r. spectroscopy. The main route of Diclofurime biotransformation involved cleavage of the furan ring. Subsequent biotransformation steps involved N-deethylation in the side-chain and O-demethylation in the aromatic moiety of the drug. The major pathway is unusual for molecules with a furan heterocycle.
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