引经药对血府逐瘀汤中芍药苷在大鼠体内药代动力学的影响

EFFECT OF GUIDING-HERB AND ON PAEONIFLORIN PHARMACOKINETICS OF XUEFU ZHUYU TANG IN RATS.

作者信息

Tang Song-Qi, Chen Yun-Hui, Chen Xi-Ping, Zhang Xiao-Dan, Huang Wei

机构信息

College of Traditional Chinese Medicine, Hainan Medical University, Haikou 571199, China.

College of Basic Medicine, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China.

出版信息

Afr J Tradit Complement Altern Med. 2017 Jun 5;14(4):289-296. doi: 10.21010/ajtcam.v14i4.32. eCollection 2017.

DOI:10.21010/ajtcam.v14i4.32

PMID:28638892

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5471477/

Abstract

BACKGROUND

Xuefu Zhuyu Tang (XFZYT), first recorded in by Qing-ren Wang, has been proven reliable and effective for curing various diseases such as atherosclerosis, hypertension, hyperlipidemia, and angina pectoris. It consists of 11 herbs and two of them, and , have been traditionally considered as guiding herbs and deeply valued by tens of millions of Chinese medicine practitioners. Do and affect the pharmacokinetics of the effective constituent-paeoniflorin of XFZYT? If yes, in what way? This study aims to answer these questions.

MATERIALS AND METHODS

The medicinal solutions of XFZYT, XFZYT without (XFZYT-JG), XFZYT without (XFZYT-NX), and XFZYT without and (XFZYT-JG-NX) were prepared and administrated to rats in the normal group and the blood-stasis model group by gavage, respectively. The blood samples of rats in the normal group were obtained 5, 10, 15, 20, 30, 45, 60, 120, and 240 minutes after gavage; whereas the blood samples of rats in the blood-stasis model group were obtained 10, 15, 20, 30, 45, 90, 150, and 240 minutes after gavage. Biological samples were processed; the assays of specificity, precision, linearity, intra-day and inter-day precisions, recovery and stability were conducted; high performance liquid chromatography was performed to detect paeoniflorin content; and DAS software was adopted to generate pharmacokinetic parameters. Mobile phase was composed of acetonitrile and water (16:84), detection wavelength was 230 nm, and riboflavin was set as internal standard substance.

RESULTS

The pharmacokinetic parameters of the rats in the normal group after oral gavage of XFZYT, XFZYT-JG, XFZYT-NX, and XFZYT-JG-NX were C = (0.363±0.248, 0.065±0.020, 0.099±0.033, 0.099±0.020) mg/L, = (0.276±0.084, 0.583±0.342, 0.555±0.228, 0.317±0.033)h, t = (0.501±0.241, 1.021±0.522, 0.853±0.377, 1.227±0.402) h; and AUC = (0.381±0.415, 0.13±0.085, 0.166±0.066, 0.185±0.059) mg/L·h.; whereas the pharmacokinetic parameters for the rats in the blood-stasis model group after oral gavage of XFZYT, XFZYT-JG, XFZYT-NX, and XFZYT-JG-NX were C = (0.315±0.153, 0.215±0.044, 0.228±0.056, 0.248±0.09) mg/L, = (0.5±0, 0.667±0.129, 0.5±0, 0.542±0.102) h, t = (0.408±0.146, 0.813±0.135, 0.708±0.383, 0.741±0.173) h, and AUC = (0.306±0.157, 0.408±0.136, 0.368±0.159, 0.381±0.246) mg/L·h.

CONCLUSION

The guiding herbs, s and , significantly increased the absorption amount and rate of paeoniflorin in XFZYT, and accelerated its elimination from the blood.

摘要

背景

血府逐瘀汤（XFZYT）最早由王清任于[具体年份未给出]记载，已被证明对治疗多种疾病如动脉粥样硬化、高血压、高脂血症和心绞痛可靠且有效。它由11味草药组成，其中两味药，[草药名称1]和[草药名称2]，传统上被视为引经药，深受数以千万计的中医从业者重视。[草药名称1]和[草药名称2]会影响血府逐瘀汤有效成分芍药苷的药代动力学吗？如果会，以何种方式？本研究旨在回答这些问题。

材料与方法

制备血府逐瘀汤、不含[草药名称1]的血府逐瘀汤（XFZYT - JG）、不含[草药名称2]的血府逐瘀汤（XFZYT - NX）以及不含[草药名称1]和[草药名称2]的血府逐瘀汤（XFZYT - JG - NX）的药液，分别通过灌胃给予正常组和血瘀模型组大鼠。正常组大鼠在灌胃后5、10、15、20、30、45、60、120和240分钟采集血样；而血瘀模型组大鼠在灌胃后10、15、20、30、45、90、150和240分钟采集血样。对生物样品进行处理；进行特异性、精密度、线性、日内和日间精密度、回收率和稳定性测定；采用高效液相色谱法检测芍药苷含量；并采用DAS软件生成药代动力学参数。流动相由乙腈和水（16:84）组成，检测波长为230 nm，以核黄素为内标物。

结果

正常组大鼠灌胃血府逐瘀汤、XFZYT - JG、XFZYT - NX和XFZYT - JG - NX后的药代动力学参数为C =（0.363±0.248，0.065±0.020，0.099±0.033，0.099±0.020）mg/L，t₁/₂ =（0.276±0.084，0.583±0.342，0.555±0.228，0.317±0.033）h，tmax =（0.501±0.241，1.021±0.522，0.853±0.377，1.22(7)±0.402）h；AUC =（0.381±0.415，0.13±0.085，0.166±0.066，0.185±0.059）mg/L·h；而血瘀模型组大鼠灌胃血府逐瘀汤、XFZYT - JG、XFZYT - NX和XFZYT - JG - NX后的药代动力学参数为C =（0.315±0.153，0.215±0.044，0.228±0.056，0.248±0.09）mg/L，t₁/₂ =（0.5±0，0.667±0.129，0.5±0，0.542±0.102）h，tmax =（0.408±0.146，0.813±0.135，0.708±0.383，0.741±0.173）h，AUC =（0.306±0.157，0.408±0.136，0.368±0.159，0.381±0.246）mg/L·h。