Comparative Study on the Pharmacokinetics of Paeoniflorin, White Peony Root Water Extract, and Taohong Siwu Decoction After Oral Administration in Rats
Comparative Study on the Pharmacokinetics of Paeoniflorin, White Peony Root Water Extract, and Taohong Siwu Decoction After Oral Administration in Rats
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DOI：
10.1007/s13318-023-00825-9
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发表时间：
2023-04-20
影响因子：
1.9
通讯作者：
Li，Wei-rong
中科院分区：
文献类型：
--
作者：
Chen，Wei-chun;Liang，Xiao-yi;Li，Wei-rong
背景与目的桃红四物汤（TSD）是具有舒张血管、降血脂等药理作用的经典中药复方。芍药苷（Paeoniflorin， PF）是芍药的有效成分之一。本研究的目的是评价中药提取物及其纯化形式中PF在大鼠体内的药代动力学。方法建立灵敏快速的高效液相色谱-串联质谱（HPLC-MS-MS）测定大鼠血浆中PF的方法。将大鼠分为3组，分别灌胃PF溶液、白芍水提物（WPR）和丹参皂苷（TSD）。在灌胃后预定的不同时间点，从眶静脉采血。测定三组大鼠血浆中PF的药动学参数。结果药代动力学研究表明，纯化型组的PF达到最大浓度（Tmax）的时间相对较高，而TSD和WPR组的PF半衰期（t1 / 2）较长。三组中，纯化形式组的浓度-时间曲线下面积最大（AUC0-t= 732.997µg/L·h），最大浓度最大（Cmax= 313.460µg/L），与TSD组比较差异有统计学意义（P< 0.05）。与纯化组相比，TSD组PF的清除率（CLz/F = 86.004 L/h/kg）和表观分布容积（Vz/F = 254.787 L/kg）均显著升高（P< 0.05）。结论建立了一种特异、灵敏、快速的HPLC-MS-MS测定大鼠血浆中PF的方法。结果表明，丹参、丹参均能延长芍药苷在体内的作用时间。
Background and ObjectiveTaohong Siwu Decoction (TSD) is a classic traditional Chinese medicine (TCM) compound with pharmacological effects such as vasodilation and hypolipidemia. Paeoniflorin (PF) is one of the active ingredients of TSD. The aim of this study was to evaluate the pharmacokinetics of PF in herbal extracts and their purified forms in rats.MethodA sensitive and rapid high-performance liquid chromatography–tandem mass spectrometry (HPLC–MS-MS) method for the determination of PF in rat plasma was developed. Rats were divided into three groups, and given PF solution, water extract of white peony root (WPR), or TSD by gavage. At different predetermined timepoints after gavage, blood was collected from the orbital vein. The pharmacokinetic parameters of PF in the plasma of rats in the three groups was determined.ResultsThe pharmacokinetic studies showed that the time to reach maximum concentration (Tmax) of PF in the purified forms group was relatively high, while the half-lives (T½) of PF in the TSD and WPR groups were longer. Among the three groups, PF in the purified forms group had the maximum area under the concentration–time curve (AUC0-t= 732.997 µg/L·h) and the largest maximum concentration (Cmax= 313.460 µg/L), which showed a significant difference compared with the TSD group (P< 0.05). Compared with the purified group, the clearance (CLz/F = 86.004 L/h/kg) and the apparent volume of distribution (Vz/F = 254.787 L/kg) of PF in the TSD group increased significantly (P< 0.05).ConclusionsA highly specific, sensitive, and rapid HPLC–MS-MS method was developed and applied for the determination of PF in rat plasma. It was found that TSD and WPR can prolong the action time of paeoniflorin in the body.