神经药理学报 ›› 2020, Vol. 10 ›› Issue (4): 10-13.DOI: 10.3969/j.issn.2095-1396.2020.04.003

• 实验方法学 • 上一篇    下一篇

药物体外肝代谢研究方法

李兰,张丹参   

  1. 河北科技大学,石家庄,050018,中国
  • 出版日期:2020-08-26 发布日期:2020-08-26
  • 通讯作者: 张丹参,女,博士生导师;研究方向:神经药理学;Tel:+86-0311-81668016,E-mail:zhangds2011@126.com
  • 作者简介:李兰,女,硕士研究生;研究方向:神经药理学;E-mail:940383050@qq.com
  • 基金资助:
    河北省重点研发计划项目生物医药专项(No.20372509D);河北省自然科学基金(No.H2020208032);河北省高等学校科学
    技术研究项目(No.ZD2020117);河北省中医药管理局中医药科研计划项目(No.2020268);中央财政公共卫生专项“中药资
    源普查项目”(No.Z135080000022)

Research Methods of Drug in Vitro Liver Metabolism

LI Lan,ZHANG Dan-shen   

  1. Hebei University of Science and Technology,Shijiazhuang,050018,China
  • Online:2020-08-26 Published:2020-08-26
  • Contact: 张丹参,女,博士生导师;研究方向:神经药理学;Tel:+86-0311-81668016,E-mail:zhangds2011@126.com
  • About author:李兰,女,硕士研究生;研究方向:神经药理学;E-mail:940383050@qq.com
  • Supported by:
    河北省重点研发计划项目生物医药专项(No.20372509D);河北省自然科学基金(No.H2020208032);河北省高等学校科学
    技术研究项目(No.ZD2020117);河北省中医药管理局中医药科研计划项目(No.2020268);中央财政公共卫生专项“中药资
    源普查项目”(No.Z135080000022)

摘要:

体外代谢研究对阐明药效物质基础及作用机制有重要意义。常见的体外肝代谢研究方法有肝微粒体体外温孵法、肝细胞体外温孵法、肝灌流技术、肝组织切片技术、基因重组P450 酶系等。药物体外肝代谢不能全面反映体内药物的综合代谢情况,与体内的真实代谢情况存在差异,今后需结合体内实验等方法来完善药物在体内外的药物代谢转运的研究。目前肝灌流技术和基因重组P450 酶系等体外肝代谢研究方法对设备、实验操作成本、数据处理技术等要求较高,其运用和推广仍然受到一定的约束和限制,今后需建立简单、快速、经济、高效的科学技术方法和手段。由于药物体外肝代谢对新药研究与开发、正确指导临床合并用药有着巨大的推动作用,因此该文将对其进行重点论述。

关键词: 体外肝代谢, 肝微粒体体外温孵法, 基因重组P450 酶系法, 离体肝灌流法, 器官组织切片法, 肝细胞体外温孵法

Abstract:

In vitro metabolism research is of great significance to elucidate the substance basis and mechanism of action of drugs. Common in vitro liver metabolism research methods include liver microsome in vitro warming method,hepatocyte in vitro warming method,liver perfusion technology,liver tissue sectioning technology,gene recombinant P450 enzyme system,etc. The liver metabolism of drugs in vitro cannot fully reflect the comprehensive metabolism of drugs in the body,and there is a difference from the actual metabolism in the body. In the future,it is necessary to combine in vivo experiments and other methods to improve the study of drug metabolism and transport in and out of the body;In vitro liver metabolism research methods such as the P450 enzyme system have high requirements on equipment,experimental operation costs,and data processing technology. Their application and promotion are still subject to certain constraints and restrictions. In the future,simple,fast,economical,and efficient scientific and technical methods and means need to be established. Because the liver metabolism of drugs in vitro has a huge role in promoting the research and development of new drugs and correctly guiding clinical co-administration,this article will focus on them.

Key words: in vitro liver metabolism, in vitro incubation of liver microsomes, gene recombinant P450 enzyme system, in vitro liver perfusion, organ tissue section method, in vitro incubation of liver cells

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