Comparative pharmacokinetics of 11 major bioactive components between two dosage forms of Qixue Shuangbu Prescription in rats by ultra‐high‐performance liquid chromatography‐tandem mass spectrometry

Abstract

Although Qixue Shuangbu Prescription (QSP) is a classic Chinese medicine prescription for treating chronic heart failure. Low bioavailability due to the insolubility and poor biofilm permeability of the main bioactive ingredients of QSP is still a key factor limiting its efficacy. In this study, a novel self‐microemulsifying drug delivery system was proposed to effectively improve the bioavailability of QSP. The qualified ultra‐high‐performance liquid chromatography‐tandem mass spectrometry methodology was established to investigate the pharmacokinetics characteristics of the QSP self‐microemulsifying drug delivery system. Our results showed that 11 components in the self‐microemulsifying drug delivery system group had prolonged T1/2 and MRT0‐t values compared with QSP extract. The Cmax of calycosin‐7‐glucoside (CG), vanillic acid and paeoniflorin increased 2.5 times, 2.4 times and 2.3 times, respectively. The relative bioavailability values of CG, paeoniflorin and ononin were most significantly affected, increasing by 383.2%, 336.5% and 307.1%, respectively. This study promoted the development of new dosage forms of QSP and provided a useful reference for improving dosage forms to solve the problem of low bioavailability of traditional Chinese medicine.