Both qualitative and quantitative analyses combined with activity evaluation were used for the inte-grated quality control study of Pien-Tze-Huang (PZH), a precious lozenge used for 460 years in China. Inqualitative analysis, a high performance LC-quadrupole time-of-flight MS method was developed for theidentification of chemical profiling in PZH. 27 compounds were unambiguously identified by comparingwith reference substances, and 12 compounds were tentatively deduced based on their MS data and com-paring with literatures. Then the in vitro anti-inflammatory activity of 27 compounds were evaluated,and 9 saponins, 11 bile acids, taurine and muscone exhibited significant inhibitory activities on TNF- production with IC50values ranging from 12.34 to 147.24 M. In quantitative analysis, 21 active com-pounds, selected as quality control markers, were simultaneously detected in 15 batches of PZH samplesby ultra-performance LC-triple quadrupole MS. All the analytes were detected within 15 min. Satisfac-tory linearity was achieved with wide linear range and fine determination coefficient (r2> 0.9990). Therespective relative standard deviations of intra- and inter-day precisions, repeatability, stability, andrecovery were less than 4.32%, 4.94%, 4.78%, 4.87%, and 4.91%. This study ...