A PRELIMINARY STUDY OF STEREOSELECTIVITY OF MEFLOQUINE ENANTIOMERS IN RAT

Abstract

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.