The metabolic fate of tizoprolique acid in baboons.
1. After oral administration of the anti-lipolytic drug [14C]tizoprolique acid (2-propyl-5-carboxyl[4-14C]thiazole), to baboons (60 mg/kg), the radioactivity was well absorbed and rapidly excreted. During 6 and 24 h respectively, 60 +/- 25% (S.D.) and 90 +/- 2% were excreted in the urine. 2. Plasma concn. of 14C reached a max. (182 +/- 65, range 85-221 micrograms equiv./ml) at 1-1.5 h after an oral dose, and declined rapidly with an apparent half-life of about 0.5 h. A mean of 77 +/- 7% of the 14C in peak plasma samples was bound to plasma proteins, somewhat less than that of [14C]tizoprolique acid (84 +/- 5%). 3. Tissue concn. of 14 C were highest in an animal killed at 0.5 h after an oral dose, but were lower than those in plasma in all tissues examined except the kidneys. 4. The major metabolite of tizoprolique acid was its glycine conjugate, which accounted for about 80% dose excreted in the 24 h urine. About 2% dose was excreted as unchanged drug. About 70% and 20% respectively of plasma 14C were associated with the unchanged drug and its glycine conjugate during the period 15 min to 4 h after dosing.
D000042:Absorption; D000818:Animals; D001798:Blood Proteins / Q000378:metabolism; D005260:Female; D008297:Male; D013058:Mass Spectrometry; D010215:Papio; D013844:Thiazoles / Q000097:blood / Q000378:metabolism* / Q000652:urine; D014018:Tissue Distribution
D001798:Blood Proteins; D013844:Thiazoles; C016789:tizoprolic acid