Abstract: The technique of microdialysis combined with liquid chromatography-mass spectrometry not only can be used for real-time and continuous minimally invasive sampling in vivo, but also has the characteristics of high sensitivity, fast analysis speed and wide detection range, which has become a powerful means for the research of Chinese medicine. It has been widely used in many aspects such as the study of the in vivo process and action mechanism of traditional Chinese medicine. In this paper, the microdialysis technology was briefly introduced, then combined with relevant research examples, the research strategy and application of microdialysis-liquid chromatography-mass spectrometry technique in the screening of active components from Chinese medicine, in vivo and in vitro metabolism, pharmacokinetics, metabolomics were reviewed.