Direct determination of the enantiomers of the antimalarial drug halofantrine and its active metabolite N-desbutylhalofantrine in human plasma.

The plasma concentrations vs. time profiles of the enantiomers of halofantrine and its main metabolite N-desbutylhalofantrine have been determined in two healthy volunteers after a single oral administration of 500 mg of racemic halofantrine hydrochloride (Halfan). A solid-phase extraction method was used for the purification of the samples. The enantiomers of halofantrine and N-desbutylhalofantrine were determined simultaneously using chiral high-performance liquid chromatography on chiral stationary phases with fluorescence detection.