引导中药桔梗、牛膝对血府助瘀汤芍药苷在大鼠体内药动学的影响。

Song-Qi Tang, Yun-Hui Chen, Xi-Ping Chen, Xiao-Dan Zhang, Wei Huang
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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. 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引用次数: 8

摘要

背景:血瘀瘀汤(XFZYT)最早记载于王清仁《医学著作纠错》中,已被证明对动脉粥样硬化、高血压、高脂血症、心绞痛等多种疾病具有可靠和有效的治疗作用。它由11种草药组成,其中两种,桔梗和牛膝,传统上被认为是指导草药,深受数千万中医的重视。桔梗、牛膝对中药复方丹参有效成分芍药苷的药动学影响吗?如果是,以何种方式?本研究旨在回答这些问题。材料与方法:制备XFZYT、XFZYT不含桔梗(XFZYT- jg)、XFZYT不含牛膝(XFZYT- nx)、XFZYT不含桔梗、牛膝(XFZYT- jg - nx)的药液,分别灌胃给正常组和血瘀模型组大鼠。正常组大鼠于灌胃后5、10、15、20、30、45、60、120、240分钟取血;血瘀模型组大鼠于灌胃后10、15、20、30、45、90、150、240分钟取血。对生物样品进行处理;进行特异性、精密度、线性、日内、日间精密度、回收率、稳定性分析;采用高效液相色谱法测定芍药苷含量;采用DAS软件生成药动学参数。流动相为乙腈-水(16:84),检测波长为230 nm,以核黄素为内标物。结果:正常组大鼠灌胃XFZYT、XFZYT- jg、XFZYT- nx、XFZYT- jg - nx后药动学参数为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;和AUC0 -∞=(0.381±0.415,0.13±0.085,0.166±0.066,0.185±0.059)mg / L·h。;血瘀模型组大鼠灌胃XFZYT、XFZYT- jg、XFZYT- nx、XFZYT- jg - nx后的药代动力学参数为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。结论:导药桔梗、牛膝能显著提高泻泻合剂中芍药苷的吸收量和吸收率,加速其在血液中的消除。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

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IN VIVO EFFECT OF GUIDING-HERB RADIX PLATYCODONIS AND RADIX CYATHULAE ON PAEONIFLORIN PHARMACOKINETICS OF XUEFU ZHUYU TANG IN RATS.

Background: 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.

Materials and methods: 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.

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 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.

Conclusion: 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.

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