五味子木脂素16种成分的大鼠血浆药动学研究

    Pharmacokinetics Study of 16 Effective Components of Lignans from Schisandra Chinensis in Rat Plasma

    • 摘要:
      目的  利用超高效液相色谱-三重四级杆质谱(UHPLC-TQ-MS)研究五味子木脂素中五味子醇甲、戈米辛D、戈米辛J等16种成分在正常大鼠血浆中的体内药动学。
      方法 SD大鼠灌胃给予五味子木脂素纯化物的0.5%羧甲基纤维素钠混悬液(0.01 mL·g−1),连续给药5 d,并于最后一次给药后0.08、0.25、0.5、1、1.5、2、4、6、8、10、12、24、30、36、48、72 h眼静脉丛取血,利用UHPLC-TQ-MS测定血浆中各成分浓度,并计算主要药动学参数。
      结果 除戈米辛G在大鼠血浆中的响应低于定量下限外,其余15个五味子木脂素成分均能被吸收进入血液,且大部分木脂素药时曲线存在双峰现象,可部分延长其作用时间。
      结论 该研究进一步完善了木脂素成分在大鼠体内的药动学过程,对于开展木脂素有效成分的相关研究及临床应用提供了有益参考。

       

      Abstract:
      OBJECTIVE To study the in vivo pharmacokinetics of 16 components including schisandrol A, gomisin D, and gomisin J in the lignans from Schisandra chinensis in rat plasma using ultra-performance liquid chromatography-tandem quadrupole mass spectrometry(UHPLC-TQ-MS).
      METHODS SD rats given intragastric administration of the 0.5% carboxymethyl cellulose sodium(CMC-Na) suspension(0.01 mL·g−1) of purified lignans from Schisandra chinensis for five consecutive days. After the final administration, blood samples were collected from the retro-orbital plexus at 0.08, 0.25, 0.5, 0.75, 1, 1.5, 2, 4, 6, 8, 12, 24, 48 h, UHPLC-TQ-MS was adopted in the plasma concentration determination of various active constituents, and main pharmacokinetic parameters were calculated.
      RESULTS With the exception of gomisin G, whose response in rat plasma was below the lower limit of quantification, the other 15 lignan constituents from Schisandra chinensis were absorbed into systemic circulation. Furthermore, most of the lignans from Schisandra chinensis had a bimodal drug-time curves, which could partially prolong the duration of action of the lignans.
      CONCLUSION The present study further improved the pharmacokinetic process of lignans from Schisandra chinensis in rats, and provided a useful reference for carrying out the research related to the active ingredients of lignans and their clinical applications.

       

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