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Two kinds of liquid chromatography coupled with tandem mass spectrometry (LC–MS/MS) techniques with high resolution and good sensitivity characteristics respectively are used to analyze the chemicals and rat metabolites of Biqi capsule with different exposure level. On the one hand, 23 chemical compositions of Biqi capsule and 56 metabolites in rats were identified by high-performance liquid chromatography coupled with high-resolution hybrid mass spectrometry (HPLC-HRMS/MSⁿ). On the other hand, 15 prototype compounds and 22 metabolites at low level in plasma were detected by high-performance liquid chromatography coupled with triple-quadrupole tandem mass spectrometry (HPLC-QQQ-MS/MS) with high sensitivity and selectivity. Total 44 absorbed components in plasma were used to dock protein targets to reveal the probable active effects and mechanism of action of Biqi capsule, and …