Disposition of the diastereoisomer of mefloquine in mice

Abstract

The disposition of the diastereoisomer of mefloquine, WR 177,602 . HCl, was examined over a 168-hour period after 10 mg/kg of the 14C-labeled drug was administered orally to female albino ICR mice. This drug was absorbed readily. 2 h after dosing, the drug was distributed throughout the animal body with a large percent of the administered dose found in the eyes, submaxillary salivary glands, lungs, spleen, liver, gallbladder plus bile, kidney and carcasses. The elimination half-life of the unmetabolized WR 177,602 in plasma was estimated to be 16.1 h. The major route of excretion of the drug was via the feces (70%), with 23% in the urine 168 h. The elimination half-lives of the unmetabolized drug in urine and feces were 8.0 and 6.9 h, respectively. The disposition of WR 177,602 . HCl was similar to its erythrodiastereoisomer in female mice.