a preliminary study of stereoselectivity of mefloquine enantiomers in rat

stereoselectivity of mefloquine enantiomers were studied in rats after oral administration of a single 50mg/kg dose of the racemate. pharmacokinetic parameters of (+)-(rs)-mfq in blood and plasma showed no significant difference. the concentration, auc , clif and vdlf of (+)-(rs)-enantiomerin blood were significantly higher than those for the (-)-(sr)-enantiomer. tlie results obtained from this study showed a reverse stereoselectivity of mfq as compared with what reported for human. a very low amount of enantiomers excreted in urine and the excretion was not stereoselective. a preliminary study in different blood fractions showed that the accumulation of mfq enantiomers in blood cells is stereoselective with a tendency of ( + )-(rs)-enatiomer for leukocytes and (-)-(sr)-enantiomer for erythrocytes.