Abstract: OBJECTIVE To investigate the metabolite profile of schisantherin A in rat urine. METHODS Ultra high performance liquid chromatography combined with Triple TOF mass spectrometry(UPLC-TOF/MS/MS) was used for the separation and analysis of schisantherin A and its metabolites in rat urine. The metabolites were separated using a Phenomenex UPLC C₁₈ column with gradient elution program of acetonitrile and 0.1‰ formic acid aqueous as mobile phase. RESULTS MetabolitePilot software was employed to speculate the structures of the metabolites of schisantherin A and five metabolites were identified. CONCLUSION Oxidation and reduction reactions are the metabolic pathways of schisantherin A in rat.