Li Peifan, Zhang Yunhui, Xiao Li, Jin Xinghua, Yang Kun
School of Pharmaceutical Science and Technology, Tianjin University, No. 92, Weijin Road, 300072, Tianjin, People's Republic of China.
Anal Bioanal Chem. 2007 Dec;389(7-8):2259-64. doi: 10.1007/s00216-007-1612-5. Epub 2007 Sep 27.
Radix Scrophulariae (xuanshen) is one of the famous Chinese herbal medicines widely used to treat rheumatism, tussis, pharyngalgia, arthritis, constipation, and conjunctival congestion. Harpagoside and cinnamic acid are the main bioactive components of xuanshen. The purpose of this study was to develop an HPLC-UV method for simultaneous determination of harpagoside and cinnamic acid in rat plasma and investigate pharmacokinetic parameters of harpagoside and cinnamic acid after oral administration of xuanshen extract (760 mg kg(-1)). After addition of syringin as internal standard, the analytes were isolated from plasma by liquid-liquid extraction. Separation was achieved on a Kromasil C18 column, and detection was by UV absorption at 272 nm. The described assay was validated in terms of linearity, accuracy, precision, recovery, and limit of quantification according to the FDA validation guidelines. Calibration curves for both analytes were linear with the coefficient of variation (r) for both was greater than 0.999. Accuracy for harpagoside and cinnamic acid ranged from 100.7-103.5% and 96.9-102.9%, respectively, and precision for both analytes were less than 8.5%. The main pharmacokinetic parameters found for harpagoside and cinnamic acid after oral infusion of xuanshen extract were as follows: Cmax 1488.7 +/- 205.9 and 556.8 +/- 94.2 ng mL(-1), Tmax 2.09 +/- 0.31 and (1.48 +/- 0.14 h, AUC(0-24) 10,336.4 +/- 1426.8 and 3653.1 +/- 456.4 ng h mL(-1), AUC(0-infinity) 11,276.8 +/- 1321.4 and 3704.5 +/- 398.8 ng h mL(-1), and t(1/2) 4.9 +/- 1.3 and 2.5 +/- 0.9 h, respectively. These results indicated that the proposed method is simple, selective, and feasible for pharmacokinetic study of radix Scrophulariae extract in rats.
玄参是一种著名的中药材，广泛用于治疗风湿病、咳嗽、咽痛、关节炎、便秘和结膜充血。哈巴苷和肉桂酸是玄参的主要生物活性成分。本研究的目的是建立一种高效液相色谱 - 紫外检测法（HPLC - UV），用于同时测定大鼠血浆中哈巴苷和肉桂酸，并研究口服玄参提取物（760 mg kg⁻¹）后哈巴苷和肉桂酸的药代动力学参数。加入紫丁香苷作为内标后，通过液 - 液萃取从血浆中分离出分析物。在Kromasil C18柱上实现分离，并通过272 nm处的紫外吸收进行检测。根据美国食品药品监督管理局（FDA）的验证指南，对所描述的测定方法进行了线性、准确度、精密度、回收率和定量限方面的验证。两种分析物的校准曲线均呈线性，两者的变异系数（r）均大于0.999。哈巴苷和肉桂酸的准确度分别为100.7 - 103.5%和96.9 - 102.9%，两种分析物的精密度均小于8.5%。口服玄参提取物后，哈巴苷和肉桂酸的主要药代动力学参数如下：Cmax分别为1488.7 ± 205.9和556.8 ± 94.2 ng mL⁻¹，Tmax分别为2.09 ± 0.31和1.48 ± 0.14 h，AUC(0 - 24)分别为10336.4 ± 1426.8和3653.1 ± 456.4 ng h mL⁻¹，AUC(0 - ∞)分别为11276.8 ± 1321.4和3704.5 ± 398.8 ng h mL⁻¹，t(1/2)分别为4.9 ± 1.3和2.5 ± 0.9 h。这些结果表明，所提出的方法对于玄参提取物在大鼠体内的药代动力学研究简单、具有选择性且可行。
