Abstract
Guanjiekang (GJK) that is formed by five medicinal herbs including Astragali Radix, Aconiti Lateralis Radix Praeparaia, Glycyrrhizae Radix et Rhizoma, Corydalis Rhizoma and Paeoniae Radix Alba was used for the treatment of rheumatoid arthritis (RA). However, the pharmacokinetic (PK) profile of active components in GJK remains unclear. This study aims to evaluate the pharmacokinetic behavior of seven representative active constituents in GJK (i.e., benzoylhypaconine, benzoylmesaconine, paeoniflorin, tetrahydropalmatine, calycosin-7-glucoside, formononetin and isoliquiritigenin) after oral administration of GJK in rats. A rapid, sensitive and reliable ultra-performance liquid chromatography-tandem mass spectrometer (UPLC–MS/MS) method has been successfully developed for the simultaneous determination of these seven constituents in rat plasma. Chromatographic separation was achieved on a C18 column with a gradient elution program that consists of acetonitrile and water (containing 0.1% formic acid) at a flow rate of 0.35 mL/min. Detection was performed under the multiple reaction monitoring (MRM) in the positive electrospray ionization (ESI) mode. The calibration curves exhibited good linearity (R2 > 0.99) over a wide concentration range for all constituents. The accuracies ranged from 92.9% to 107.8%, and the intra-day and inter-day precisions at three different levels were below 15%. Our PK results showed that these seven compounds were quickly absorbed after the administration of the GJK product, and Tmax ranged from 30 min to 189 min. The in vivo concentrations of paeoniflorin and isoliquiritigenin were significantly higher than the reported in vitro effective doses, indicating that they could partly contribute to the therapeutic effect of GJK. Therefore, we conclude that pharmacokinetic studies of representative bioactive chemicals after administration of complex herbal products are not only necessary but also feasible. Moreover, these seven compounds that were absorbed in vivo can be used as indicator standards for quality control and for determining pharmacokinetic behavior of herbal medicines in clinical studies.
Highlights
The constituents in Chinese herbal medicine (CHM) are complex and diverse
Molecules 2016, 21, 1732 mediated via multi-target and multi-pathway actions of multiple components during the preparation of CHM [1,2]. These multiple components are believed to generate a synergistic effect for treating illnesses, rather than the pharmacological actions produced by a single compound [3,4,5,6]
The pharmacokinetic (PK) studies on multiple components are more valuable for elucidating the pharmacological mechanisms for treating relevant diseases as well as for ensuring the quality of CHM preparations [7,8,9,10]
Summary
The constituents in Chinese herbal medicine (CHM) are complex and diverse. Molecules 2016, 21, 1732 mediated via multi-target and multi-pathway actions of multiple components during the preparation of CHM [1,2]. These multiple components are believed to generate a synergistic effect for treating illnesses, rather than the pharmacological actions produced by a single compound [3,4,5,6]. The method of simultaneous determination of multiple constituents in rat plasma for the pharmacokinetic study of CHM preparations is significantly more difficult than the method for determining the PK behavior of a single chemical compound
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