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川芎-天麻配伍对川芎中2种成分在大鼠脑内药动学的影响

Effects of Chuanxiong Rhizoma-Gastrodiae Rhizoma compatibility on the pharmacokinetics of two constituents in Chuanxiong Rhizoma in rat brain

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【作者】 米雅慧郭思宇刘明平韦品清程欢柯国韩

【Author】 MI Ya-hui;GUO Si-yu;LIU Ming-ping;WEI Pin-qing;CHENG Huan;KE Guo-han;School of Pharmaceutical Sciences, Guangzhou University of Chinese Medicine;

【通讯作者】 刘明平;

【机构】 广州中医药大学中药学院

【摘要】 目的探讨川芎-天麻配伍对川芎中川芎嗪、阿魏酸在大鼠脑内药动学的影响。方法 18只大鼠随机分成川芎组、川芎-天麻(1∶0.25)组、川芎-天麻(1∶1)组,每组6只,建立血瘀型偏头痛模型。灌胃给药后,于大鼠脑内插入微透析探针,收集不同时间点脑透析液,UPLC-MS/MS法检测川芎嗪、阿魏酸含有量,绘制血药浓度-时间曲线,计算药动学参数。结果与单味药组比较,配伍组2种成分T1/2[川芎-天麻(1∶1)组阿魏酸除外]、MRT0~∞、Cmax、AUC0~∞升高(P<0.05,P<0.01);川芎-天麻(1∶0.25)组两者T1/2、MRT0~∞、AUC0~∞高于川芎-天麻(1∶1)组(P<0.05,P<0.01),川芎嗪Cmax降低(P<0.05)。结论天麻可提高川芎中川芎嗪、阿魏酸脑组织吸收程度,延长作用时间,减缓消除速率,增加蓄积,其作用强度与天麻剂量有关。

【Abstract】 AIM To explore the effects of Chuanxiong Rhizoma-Gastrodiae Rhizoma compatibility on pharmacokinetics of tetramethylpyrazine and ferulic acid in Chuanxiong Rhizoma in rat brain.METHODS Eighteen rats were randomly assigned into Chuanxiong Rhizoma group, Chuanxiong Rhizoma-Gastrodiae Rhizoma(1∶0.25) group and Chuanxiong Rhizoma-Gastrodiae Rhizoma(1∶1) group, six rats in each group, after which the models of migraine due to Blood Stasis were established. After intragastric administration, microdialysis probe was inserted into rat brain, cerebral dialysates at different time points were collected, UPLC-MS/MS was adopted in the content determination of tetramethylpyrazine and ferulic acid, blood concentration-time curve was drawn, and pharmacokinetic parameters were calculated.RESULTS Compared with the single drug group, the compatibility groups demonstrated increased these two constituents’ T1/2 [except for that of ferulic acid in the Chuanxiong Rhizoma-Gastrodiae Rhizoma(1∶1) group], MRT0-∞, Cmax and AUC0-∞(P<0.05, P<0.01). The T1/2, MRT0-∞ and AUC0-∞ of two constituents in the Chuanxiong Rhizoma-Gastrodiae Rhizoma(1∶0.25) group were higher than those in the Chuanxiong Rhizoma-Gastrodiae Rhizoma(1∶1) group(P<0.05, P<0.01), along with decreased Cmax of tetramethylpyrazine(P<0.05).CONCLUSION Gastrodiae Rhizoma can enhance the absorption degrees of tetramethylpyrazine and ferulic acid in Chuanxiong Rhizoma in brain tissue, prolong the duration of action, slow down elimination rate and increase accumulation, whose action intensity is related to Gastrodiae Rhizoma dose.

【基金】 国家自然科学基金资助项目(81274107)
  • 【文献出处】 中成药 ,Chinese Traditional Patent Medicine , 编辑部邮箱 ,2020年02期
  • 【分类号】R285.5
  • 【被引频次】8
  • 【下载频次】484
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