基于肠吸收特征探讨“苦参-白花蛇舌草”药对的相互作用

    Interaction of the Drug Pair of Sophorae Flavescentis Radix-Hedyotis Diffusa Based on Intestinal Absorption Characteristics

    • 摘要:
      目的 探讨“苦参-白花蛇舌草”单株及药对中有效成分在肠道中的吸收及相互作用特征。
      方法 通过构建大鼠肠外翻模型,采用HPLC检测肠吸收液中特征性成分苦参碱、氧化苦参碱和车叶草苷含量,计算其吸收参数,分析单味药与药对中成分在大鼠小肠不同部位、不同时间的吸收特征并对其肠吸收部位、时间、给药浓度进行研究。
      结果 通过对单味药、药对中的苦参碱、氧化苦参碱和车叶草苷吸收情况进行比较,发现相同吸收部位、相同浓度的样品溶液中,药对中苦参碱和车叶草苷的吸收量(Q)、吸收速率常数(Ka)较单药组显著增加(P<0.05)。同时,研究发现3种有效成分在十二指肠、空肠、回肠、结肠中均有一定的吸收,在回肠中得到累积Q最高。随时间与浓度的增加,3种有效成分在肠道中Q也随之增加。
      结论 “苦参-白花蛇舌草”药对配伍应用产生协同增效的治疗作用,这3种成分肠吸收特性可能为具有时间与浓度依赖性的被动运输模式且在回肠段中吸收最佳,该研究结果可以为进一步的临床用药设计提供参考。

       

      Abstract:
      OBJECTIVE To investigate the absorption characteristics and interaction of active ingredients of Sophorae Flavescentis Radix-Hedyotis diffusa Willd. individual herbs and drug pair in intestine.
      METHODS The location, time and concentration of the intestinal absorption were studied by everted intestinal sac models. The contents of matrine, oxymatrine and asperuloside in the intestinal sac absorption solution were detected by HPLC, and the absorption kinetic parameters were calculated to investigate the intestinal absorption characteristics of each component.
      RESULTS A comparison of the absorption characteristics of matrine, oxymatrine, and asperuloside in single herbs and herb pairs revealed that, at the same absorption site and concentration, the absorbed amount(Q) and absorption rate constant(Ka) of matrine and asperuloside were significantly higher in the herb pair group than in the single herb group(P<0.05). Additionally, the study found that all three active components were absorbed to some extent in the duodenum, jejunum, ileum, and colon, with the highest Q observed in the ileum. Furthermore, the intestinal absorption of these components increased with both time and concentration.
      CONCLUSION Sophorae Flavescentis Radix-Hedyotis diffusa herb pair has a synergistic therapeutic effect on the compatible application, and the intestinal absorption characteristics of these three components may be passive transport mode with time and concentration dependence and the best absorption in the ileum segment. These findings can provide a reference for further clinical drug design.

       

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