Effect of compatible herbs on the pharmacokinetics of effective components of Panax notoginseng in Fufang Xueshuantong Capsule

Abstract

Fufang Xueshuantong (FXT) is a well-known Chinese herbal formula which has been used to treat cardiovascular and ophthalmic diseases, especially diabetic retinopathy. Panax notoginseng (Burkill) F.H. Chen (PN) is the main herb of FXT, whose major bioactive constituents are ginsenosides. However, the scientific basis of the compatibility of FXT is still ambiguous. The present study investigated the scientific basis of the compatibility of FXT by comparing the pharmacokinetics of marker compounds after oral administrations of PN and FXT. A high performance liquid chromatography-electrospray ionization tandem mass spectrometry (HPLC-ESI-MS/MS) method was developed for simultaneous detection of notoginsenoside R1 (NR1), ginsenoside Rg1 (GRg1), and ginsenoside Rb1 (GRb1) in rat plasma. The pharmacokinetic studies of FXT and PN were performed using the established method with the pharmacokinetic parameters being determined by non-compartmental analysis. The results showed that the pharmacokinetic parameters (maximum concentration, area under the curve (AUC_0–t ), clearance, and mean residence time) of NR1, GRg1, and GRb1 were significantly different after oral administration of FXT (P<0.05) compared with PN. The AUC_0–t values of GRg1 and GRb1 were 1.7- and 3.4-fold greater, respectively, in FXT than in PN. The compatible herbs of FXT could prolong the retention time and increase the systemic exposure of NR1, GRg1, and GRb1 compared with PN in vivo, providing some scientific basis for the compatibility and clinical use of FXT.

中文概要

题目

复方血栓通中多药配伍对君药三七有效成分药代动力学的影响

目的

通过比较君药三七和复方血栓通中有效成分的药 代动力学,为复方血栓通的配伍和组方寻找科学 依据。

创新点

首次为复方血栓通的组方合理性提供一定的科学依据。

方法

研究采用实验室前期建立的液相色谱-质联用方 法同时测定大鼠血浆中的三七皂苷R1(NR1)、 人参皂苷Rg1(GRg1)和人参皂苷Rb1(GRb1), 对灌胃给予三七和复方血栓通胶囊后大鼠血浆 中NR1、GRg1 和GRb1 的药代动力学参数进行 测定。

结论

复方血栓通胶囊中除三七外的其他三味药的成分 可以增加三七中NR1、GRg1 和GRb1 在大鼠体 内的暴露水平,一定程度上揭示了复方血栓通全 方配伍的合理性。