IN VIVO EFFECT OF GUIDING-HERB RADIX PLATYCODONIS AND RADIX CYATHULAE ON PAEONIFLORIN PHARMACOKINETICS OF XUEFU ZHUYU TANG IN RATS.
IN VIVO EFFECT OF GUIDING-HERB RADIX PLATYCODONIS AND RADIX CYATHULAE ON PAEONIFLORIN PHARMACOKINETICS OF XUEFU ZHUYU TANG IN RATS.
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DOI：
10.21010/ajtcam.v14i4.32
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发表时间：
2017
期刊：
影响因子：
--
通讯作者：
Huang W
中科院分区：
文献类型：
--
作者：
Tang SQ;Chen YH;Chen XP;Zhang XD;Huang W
血府逐瘀汤最早见于王庆仁的《医案纠错》一书，对动脉粥样硬化、高血压、高脂血症、心绞痛等多种疾病疗效可靠。它由11种药材组成，其中桔梗和半夏是传统上被认为是指导性药材的两种药材，深受数千万中医的重视。桔梗、柴胡对血府逐瘀汤中有效成分--芍药苷的药代动力学有影响吗？若有，以何种方式进行？本研究旨在回答这些问题。分别以正常组和血瘀证模型组大鼠灌胃给药，制备血府逐瘀汤、无桔梗血府逐草汤(XFZYT-JG)、血瘀证血瘀证模型组(XFZYT-NX)、血瘀证血瘀证模型组(XFZYT-JG-NX)。正常组大鼠分别于灌胃后5、10、15、20、30、45、60、120、240min取血，血瘀组于灌胃后10min、15、20、30、45、90、150、240min取血。对生物样品进行处理，进行专属性、精密度、线性、日内和日间精密度、回收率和稳定性的测定，用高效液相色谱法测定芍药苷的含量，并用DAS软件生成药代动力学参数。流动相为乙腈-水(16：84)，检测波长230 nm，内标物为核黄素。正常组大鼠灌胃消肿养阴汤、消肿消炎片、消风消炎片、消风消炎片后的药动学参数分别为：Cmax=(0.363±0.248，0.065±0.020，0.099±0.033，0.099±0.020)mg/L，Tmax=(0.276±0.084，0.583±0.342，0.555±0.228，0.317±0.033)h，t1/2=(0.501±0.241，1.021±0.522，0.853±0.377，1.227±0.402)h；AUC0-∞=(0.381±0.415，0.13±0.085，0.166±0.066，0.185±0.059)mg/L·h；血瘀组大鼠灌胃血府逐瘀汤、血府逐瘀汤后的药动学参数分别为：Cmax=(0.315±0.153，0.215±0.044，0.228±0.056，0.248±0.09)mg/L，Tmax=(0.5±0，0.667±0.129，0.5±0，0.542±0.102)h，t1/2=(0.408±0.146，0.813±0.135，0.708±0.383，0.741±0.173)h，AUC0-∞=(0.306±0.157，0.408±0.136，0.368±0.159，0.381±0.246)mg/L·h。
Xuefu Zhuyu Tang (XFZYT), first recorded in Correction of Errors in Medical Works 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, Radix platycodonis and Radix cyathulae, have been traditionally considered as guiding herbs and deeply valued by tens of millions of Chinese medicine practitioners. Do Radix platycodonis and Radix cyathulae affect the pharmacokinetics of the effective constituent-paeoniflorin of XFZYT? If yes, in what way? This study aims to answer these questions. The medicinal solutions of XFZYT, XFZYT without Radix platycodonis (XFZYT-JG), XFZYT without Radix cyathulae (XFZYT-NX), and XFZYT without Radix platycodonis and Radix cyathulae (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. The pharmacokinetic parameters of the rats in the normal group after oral gavage of XFZYT, XFZYT-JG, XFZYT-NX, and XFZYT-JG-NX were Cmax = (0.363±0.248, 0.065±0.020, 0.099±0.033, 0.099±0.020) mg/L, Tmax = (0.276±0.084, 0.583±0.342, 0.555±0.228, 0.317±0.033)h, t1/2 = (0.501±0.241, 1.021±0.522, 0.853±0.377, 1.227±0.402) h; and AUC0-∞ = (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 Cmax = (0.315±0.153, 0.215±0.044, 0.228±0.056, 0.248±0.09) mg/L, Tmax = (0.5±0, 0.667±0.129, 0.5±0, 0.542±0.102) h, t1/2 = (0.408±0.146, 0.813±0.135, 0.708±0.383, 0.741±0.173) h, and AUC0-∞ = (0.306±0.157, 0.408±0.136, 0.368±0.159, 0.381±0.246) mg/L·h. The guiding herbs, Radix platycodonis and Radix cyathulae, significantly increased the absorption amount and rate of paeoniflorin in XFZYT, and accelerated its elimination from the blood.