Pharmacokinetic studies of Trimoprostil in Rats (I): Blood level profile, tissue distribution and excretion after a single oral administration of trimoprostil

Abstract

Trimoprostil [11 R, 16, 16-trimethyl-15 R-hydroxy-9-oxoprosta-cis-5-trans-13-dienoic acid] labeled with either ³H or ¹⁴C was orally administered to rats (100 μg/kg) to examine blood level profile, tissue distribution, excretion and reabsorption.
The blood peak level occurred within 45 min then the concentration followed a biphasic decline; t_1/2 from the peak time to 3 hr was 1.1-1.6 hr and t_1/2 from 3 to 24 hr was 5.2-5.9 hr. The intact drug comprised 30-40 % of total radioactivity during the first 4 hr. The liver, kidney and GIT wall were the organs containing a high radioactivity.
Approximately 90 % of the administered radioactivity was recovered from the urine and feces during 24 hr postdosing period. Biliary excretion was as high as 80-90 %.