天然产物研究与开发 ›› 2018, Vol. 30 ›› Issue (增刊1): 198-206.doi: 10.16333/j.1001-6880.2018.S.036

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青蒿素及其衍生物制剂技术及新型给药系统研究进展

杨蓉1,吴卓娜1,王冰2*   

  1. 1上海中医药大学中药学院;2上海中医药大学教学实验中心,上海 201203
  • 出版日期:2018-07-31 发布日期:2018-07-31
  • 基金资助:

    上海市科委科研项目(17401902300)-

Advances on Preparations Technology and New Drug Delivery System of Artemisinin and Its Derivatives

YANG Rong1, WU Zhuo na1, WANG Bing2*   

  1. 1School of Pharmacy,Shanghai University of Traditional Chinese Medicine; 2Experiment Center for Teaching and Learning,Shanghai University of Traditional Chinese Medicine Shanghai 201203,China
  • Online:2018-07-31 Published:2018-07-31

摘要: 青蒿素及其衍生物抗疟活性已得到世界公认。其主要衍生物包括双氢青蒿素、蒿甲醚、蒿乙醚、青蒿琥酯等。现代药理研究表明,青蒿素及其衍生物除抗疟活性外,还具有抗肿瘤、抗炎、免疫调节及抗病毒等作用,具有潜在的临床应用价值。但青蒿素及其衍生物存在水溶性差、半衰期短,生物利用度低等缺点,阻碍了其临床应用。研究表明,运用现代新型给药系统及制剂技术,能够增加青蒿素及其衍生物的溶解度和稳定性,改善生物利用度,提高其作为临床用药的医疗应用前景。本文查阅了近二十年来国内外文献,对青蒿素及其衍生物制剂技术及新型给药系统相关文献进行归纳和总结,期望为该类药物的研究开发及未来的临床应用提供参考价值。

关键词: 青蒿素, 青蒿素衍生物, 制剂技术, 新型给药系统

Abstract: The antimalarial activity of artemisinin and its derivatives had been recognized worldwide.Its main derivatives include dihydroartemisinin,artemether,artemether,artesunate and so on.Modern pharmacological studies had shown that artemisinin and its derivatives,besides antimalarial activity,had antitumor,anti-inflammatory,immunomodulatory and antiviral effects,and had potential clinical value.However,artemisinin and its derivatives had disadvantages of poor water solubility,short half-life and low bioavailability,which hinder their clinical application.The research showed that the use of modern new drug delivery system and preparation technology can increase the solubility and stability of artemisinin and its derivatives,ameliorate the bioavailability,improve the clinical drug application in medical field.This article had consulted the domestic and foreign literature in recent twenty years.The related literature of artemisinin and its derivatives preparation technology and new drug delivery system were classified and summarized,hoping to provide some reference value for the research and development of drugs and future clinical application.

Key words: artemisinin, artemisinin derivatives, preparation technology, new drug delivery system

中图分类号: 

R28