Whole body autoradiographic and quantitative tissue distribution studies with 14C-cefotaxime in the rat

The absorption, distribution and elimination of radioactivity following intravenous (i.v.) or intramuscular (i.m.) administration of 14C-cefotaxime (14C-HR 756) to the rat has been examined by qualitative and quantitative techniques. After i.v. and i.m. doses to male albino animals radioactivity was extensively distributed throughout the body and rapidly eliminated with a predominant half-life of approximately 30 to 40 min. Maximum plasma levels for the i.m. dose were reached within 20 min and approximately 85% of the dose was recovered from the urine (74%) and faeces (11%) within 8 h after dosing. In all quantitative studies 100 +/- 5% of the dose was recovered within 24 h. Whole body autoradiography studies showed good distribution of radioactivity from the blood into the tissues including lung, liver, kidney, heart, bone marrow and the gastrointestinal tract. Lowest levels were seen in the eye and brain. There was limited placental transfer of radioactivity in 14-day pregnant animals although by day 18 of the gestation period radioactivity was detected in the foetus but distribution into individual organs and tissues could not be seen. There was no evidence to show that retention of radioactivity in pigmented tissues had occurred nor was there any suggestion of accumulation of radioactivity in any organ or tissue as a consequence of multiple dosing with 14C-cefotaxime.