应用化学 ›› 2017, Vol. 34 ›› Issue (1): 118-122.DOI: 10.11944/j.issn.1000-0518.2017.01.160132

• 研究论文 • 上一篇    

刺五加叶黄酮脂质体和滴丸的药动学差异比较

简勇abc,丁茹c,刘舒a*(),刘忠英b,宋凤瑞a,刘志强a   

  1. a中国科学院长春应用化学研究所,长春质谱中心&吉林省中药化学与质谱重点实验室 长春 130022;
    b吉林大学药学院 长春 130021
    c贵州省中国科学院天然产物化学重点实验室 贵阳 550002
  • 收稿日期:2016-03-30 接受日期:2016-08-08 出版日期:2017-01-03 发布日期:2017-01-03
  • 通讯作者: 刘舒
  • 基金资助:
    国家自然基金面上资助项目(81573574);吉林省科技发展计划项目—吉林省医药产业发展专项基金资助项目(20130727002YY);吉林省科技发展计划自然科学基金项目(20150101078JC)

Comparison of the Pharmacokinetics Difference Between Acanthopanax Leaf Flavonoids Liposome and Acanthopanax Leaf Drop Pills

JIAN Yongabc,DING Ruc,LIU Shub*(),LIU Zhongyingb,SONG Fengruia,LIU Zhiqianga   

  1. aNational Center of Mass Spectrometry in Changchun & Jilin Province Key Laboratory of Chinese Medicine Chemistry and Mass Spectrometry, Changchun Institute of Applied Chemistry,Chinese Academy of Sciences,Changchun 130022,China;
    bCollege of Pharmacy,Jilin University,Changchun 130021,China
    cThe Key Laboratory of Chemistry for Natural Products of Guizhou Province and Chinese Academy of Sciences,Guiyang 550002,China
  • Received:2016-03-30 Accepted:2016-08-08 Published:2017-01-03 Online:2017-01-03
  • Contact: LIU Shu
  • Supported by:
    Supported by the National Natural Science Foundation of China(No.81573574), the Science and Technology Development Foundation of Jilin Province(No.20130727002YY, No.20150101078JC)

摘要:

采用液质联用(LC-MS/MS)方法,分析刺五加叶黄酮脂质体、刺五加叶滴丸和刺五加叶黄酮提取物经大鼠灌胃给药后其主要成分金丝桃苷的药代动力学和生物利用度,考察刺五加叶黄酮的适宜剂型。 用PKsolver软件进行药代动力学数据处理,大鼠灌胃刺五加叶黄酮提取物、刺五加叶滴丸和刺五加叶黄酮脂质体后测得金丝桃苷的最大血药浓度(Cmax)分别为(210.24±10.3)、(254.12±9.2)、(349.34±12.5) μg/L;0~t时间内药时曲线面积(AUC0-t)分别为(30.7±2.7)、(35.01±1.98)、(45.2±2.8) μg/(mL·min);平均驻留时间(MRT)分别为(334.42±75.36)、(394.56±90.26)和(640.35±84.26) min。 结果表明,刺五加叶黄酮脂质体血药达峰浓度增加,清除速率降低,药时曲线下面积加大,生物利用度显著提高,脂质体有望成为刺五加叶黄酮的适宜剂型。

关键词: 刺五加, 脂质体, 滴丸, 生物利用度, 药动学

Abstract:

Acanthopanax leaf flavonoids liposome, acanthopanax leaf drop pills, and acanthopanax leaf flavonoid extract were fed to rats by intragastric administration to study the bioavailability and pharmacokinetics of hyperoside, and appropriate dosage form of acanthopanax leaf flavonoid by liquid chromatography-tandem mass spectrometry(LC-MS/MS). Pharmacokinetic data were processed with PKsolver software. The main pharmacokinetic parameters maximum plasma concentrations(Cmax) are (210.24±10.3), (254.12±9.2), and (349.34±12.5) μg/L for acanthopanax leaf flavonoids liposome, acanthopanax leaf drop pills and acanthopanax leaf flavonoid extract, respectively; area under the curve from zero to t(AUC0-t) is (30.7±2.7), (35.01±1.98), and (45.2±2.8) μg/(mL·min), respectively; mean retention time(MRT) is (334.42±75.36), (394.56±90.26), and (640.35±84.26) min, respectively. The results show that compared with acanthopanax leaf flavonoids extracts and acanthopanax leaf drop pills, the Cmax and bioavailability of acanthopanax leaf flavonoids liposome are increased, the elimination rate of acanthopanax leaf flavonoids liposome is reduced. Liposome is expected to be the suitable dosage form of acanthopanax leaf flavonoids, and may become the new research direction in the field of chinese medicine chemistry.

Key words: acanthopanax, liposomes, dropping pills, bioavailability, pharmacokinetic