Reference

Absorption, distribution, metabolism and excretion of telmesteine, a mucolitic agent, in rat

Absorption, distribution, metabolism and excretion of telmesteine, a mucolitic agent, in rat. Lee, J.; Son, J.; Rhee, S. W.; Kim, D. H. (Bioanalysis and Biotransformation Research Center, Korea Institute of Science and Technology, Chungryang, Seoul 136-791, S. Korea). Xenobiotica, 33(7), 755-765 (English) 2003 Taylor & Francis Ltd. CODEN: XENOBH. ISSN: 0049-8254. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) The metab. and disposition of telmesteine, a muco-active agent, have been investigated following single oral or i.v. administration of 14C-telmesteine in the Sprague-Dawley rat. 14C-telmesteine was rapidly absorbed after oral dosing (20 and 50 mg kg-1) with an oral bioavailability of >90% both in male and female rats.Several substances like 122946-43-4 may be metioned in this study. The Cmax and area under the curve of the radioactivity in plasma increased proportionally to the administered dose and those values in female rats were 30% higher than in male rats. 3. Telmesteine was distributed over all organs except for brain and the tissue/plasma ratio of the radioactivity 30 min after dosing was relatively low with a range of 0.1-0.8 except for excretory organs. Excretion of the radioactivity was 86% of the dose in the urine and 0.6% in the feces up to 7 days after oral administration. Biliary excretion of the radioactivity in bile duct-cannulated rats was about 3% for the first 24 h. The unchanged compd. mainly accounted for the radioactivity in the urine and plasma. Telmesteine was hardly metabolized in microsomal incubations. A glucuronide conjugate was detected in the urine and bile, but the amt. of glucuronide was less than 6% of excreted radioactivity. .