A. Ryrfeldt
Mar 13, 2009
Citations
0
Influential Citations
14
Citations
Quality indicators
Journal
Acta pharmacologica et toxicologica
Abstract
The tissue distribution of radioactivity in mice was studied by whole body autoradiography after oral and intravenous administration of 14C-cloforex. A high uptake and persistence of activity was noted in the lungs and brain. A distinct difference in the distribution of activity in adipose tissue was obtained after oral and intravenous administration. A high activity was found in the fat tissue of mice which had received the drug intravenously, but no activity was found following oral administration. This difference may be due to the fact that very little or no cloforex is present in the circulation after oral administration. The excretion of radioactivity was slow. Twenty-four hours after oral administration to rats about 50 % of the administered dose was eliminated, and after 1 week, about 90 %. Most of the activity was eliminated through the kidneys and only small amounts in the faeces and expired air. The tissue retention of activity is certainly of great importance in the slow elimination. The major metabolite in the rat, accounting for about 80 % of the total activity in 8–24 hours urine, was identified as chlorphentermine. The remaining activity was attributed to an unknown metabolite, which seemed to be some conjugate of chlorphentermine. No unchanged cloforex could be found in the urine.