Abstract: OBJECTIVE To explore the metabolism process of major chemical constituents in Coptidis Rhizome Dispensing Granule. METHODS UHPLC-TOF/MS technology was adopted. Based on accurate relative molecular mass and fragment ion analysis, combined with relevant literature search and mass spectrometry fragmentation rules, the chromatograms of serum and urine of rats were compared before and after administration of Coptidis Rhizome Dispensing Granule. RESULTS Fifteen parent components and 9 metabolites were found in containing drug serum. There were 18 parent components and 20 metabolites in containing drug urine. CONCLUSION This study comprehensively explains the in vivo process of the main chemical components of Coptidis Rhizome Dispensing Granule. The results can provide scientific reference for the study of pharmacokinetics, metabolite prediction, pharmacodynamic material basis and mechanism of action about Coptidis Rhizome Dispensing Granule.