Abstract: AimTo develop a rapid and sensitive LC/MS/MS method for the analysis of levodropropizine in plasma and study the pharmacokinetics of levodropropizine in healthy Chinese volunteers. MethodsLevodropropizine and zolmitriptan (internal standard, IS) were extracted from plasma samples and chromatographed on a C18 column and detected using a tandem mass spectrometer with a TurboIon Spray ionization interface. Quantitation was performed using multiple reaction monitoring (MRM) of the transitions of the m/z 237 → m/z 120 for levodropropizine and m/z 288 → m/z 58 for the IS. ResultsThe limit of quantification of the method for levodropropizine was 0.25 μg·L^-1.The assay was linear over the concentration range from 0.25 to 500.0 μg·L^-1 and intra- and inter-day precision over this range were <11.4% with good accuracy. ConclusionThe method is shown to be accurate, and suitable for clinical pharmacokinetic study of levodropropizine.