Quantitative analysis and pharmacokinetic comparison of multiple bioactive components in rat plasma after oral administration of Qi-Shen-Ke-Li formula and its single herb extracts by ultra-high performance liquid chromatography-tandem mass spectrometry.

Zhou, Hui; He, Yang; Zheng, Zhong; Liu, Zhiqiang; Song, Fengrui; Liu, Shu

Qi-Shen-Ke-Li (QSKL), a traditional Chinese formula prepared from six herbs, has long been used for the treatment of coronary heart disease and chronic heart failure. However, the herbal combination mechanism and underlying material basis of this multi-herbal formula are not clear. In this study, an ultra-high performance liquid chromatography-tandem mass spectrometry (UHPLC-MS/MS) method to simultaneously determine multiple bioactive compounds in QSKL was established and validated. Using the developed method, 18 bioactive components in rat plasma after oral administration of QSKL formula and its single herb extracts were quantified. Based on these results, PK parameters (T1/2 , Tmax , Cmax , AUC0-48h , and AUC0-∞ ) of the 18 bioactive components were analyzed and compared by using PKSlover 2.0 PK software. The experimental data suggested that significant changes in PK profiles were observed between the QSKL formula and its single herb extracts. The herbal combination in QSKL significantly influences the system exposure and the PK behaviors of the 18 bioactive components, indicating multicomponent interactions among the herbs. This study provides insight into the herbal combination mechanism and underlying material basis of the QSKL formula.