Direct analysis of blood concentration and pharmacokinetics of active constituents of Xuebijing injection in rats using miniature mass spectrometry

• A rapid method for a pharmacokinetic study was developed based on MESI-mini-MS/MS. • The analytical method is simple and has the features of green chemistry. • The method qualitatively and quantitatively analyzes multiple TCM constituents. • The method is reliable for blood concentration and pharmacokinetic investigation. The study of pharmacokinetics of traditional Chinese medicine (TCM) is closely related to its efficacy and safety. Mass spectrometry (MS)-based techniques play a crucial role in the research of TCM pharmacokinetics. However, there are few reports on the use of miniature mass spectrometry (mini-MS) for pharmacokinetic studies of TCM. In this study, we developed a rapid analytical method based on membrane electrospray ionization (MESI)-mini-MS/MS that enables direct pharmacokinetic studies of TCM. Xuebijing Injection (XBJ) is a representative drug in the combined treatment of severe diseases with TCM and Western medicine, and was selected as the model TCM in this study. Seven representative active constituents of XBJ in rat blood were directly identified and quantified after administration. In the qualitative analysis, information of the precursor-product ions in the MS/MS spectrum of each analyte must be consistent with that of the standard. In the qualitative analysis, the precursor-product ion information in the MS/MS spectrum of each analyte must be consistent with that of the standard. In the quantitative analysis, we selected appropriate quantification ions for each analyte and performed quantification based on their intensities in MS/MS analysis. Finally, we used the established MESI-mini-MS/MS method to study the pharmacokinetic parameters of seven representative constituents of XBJ in rats. The results indicate that the pharmacokinetic data obtained from direct analysis based on mini-MS are consistent with previous studies using commercial tandem mass spectrometry. This fully demonstrates that mini-MS is feasible and reliable for on-site blood concentration measurement and direct pharmacokinetic studies of TCM components. Mini-MS has the advantages and characteristics of low cost, low power consumption, and strong portability, embodying many benefits of “green analytical chemistry”. Direct determination of blood concentration and pharmacokinetic studies of TCM components based on mini-MS will have broad application prospects in the future.