The disposition of threo-alpha-(2-piperidyl)-2-trifluoromethyl-6-(4-trifluoromethylphenyl)-4-pyridinemethanol phosphate in mice

Abstract

Following oral administration of the 14C-labeled title compound to male mice, the drug was well absorbed and rapidly distributed throughout the body. At least 90% of the radioactivity in the tissues at 2 hr after dosing was identified as parent compound by thin-layer chromatography. The peak plasma level of radioactivity occurred at 4 hr, and the t1/2 of elimination of parent drug was about 26 hr from the plasma and about 27 hr from the red blood cells. The major route of elimination of total radioactivity was fecal (84%), with only 5.5% in the urine at 240 hr. Only a trace of radioactivity (0.32%) was found in the expired air over a 192-hr period.