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磷脂复合物: 一种能够提高中药活性成分口服生物利用度的有效方法

郝海军*, 贾幼智, 韩茹   

  1. 上海医药工业研究院 分析测试中心, 上海 200437
  • 收稿日期:2012-10-22 修回日期:2012-12-20 出版日期:2013-09-15 发布日期:2013-09-15
  • 通讯作者: 郝海军*

Phytosomes: an effective approach to enhance the oral bioavailability of active constituents extracted from plants

Haijun Hao*, Youzhi Jia, Ru Han   

  1. Instrumental Analysis & Research Center, Shanghai Institute of Pharmaceutical Industry, Shanghai 200437, China
  • Received:2012-10-22 Revised:2012-12-20 Online:2013-09-15 Published:2013-09-15
  • Contact: Haijun Hao*

摘要: 很多中药活性成分在体外具有确切的药效, 但是由于自身的各种缺陷导致药物在体内有很小甚至没有药效, 限制了在临床上的应用。中药活性成分与磷脂在非质子溶剂中形成磷脂复合物后, 显示出与原料药不同的理化性质, 尤其是由于药物磷脂复合物透膜能力的改善, 使活性成分很容易进入体循环, 其生物利用度得到很大的提高。因此, 近几年来药物磷脂复合物受到了越来越多的关注。本文根据文献报道, 分别从磷脂复合物的制备、表征、鉴定以及在药学方面的应用进行了综述。

关键词: 磷脂, 磷脂复合物, 活性成分, 生物利用度

Abstract:

Many active constituents from herbal plants have well-established pharmacological effects in vitro. But they demonstrate less or no activities in vivo due to various problems of themselves, which severely restricts their clinical applications. After forming phytosomes with phospholipids in aprotic solvent, the active constituents exhibit different physicochemical properties from the free form. In particular, the bioavailability of the active constituent-phytosomes is enhanced greatly due to the improved capacity to cross the biomembrane and reach circulation. Therefore, increasing attention has been attracted to the use of phytosomes in recent years. Based on the published reports, we reviewed the recent progress in the research of phytosomes including preparation, characterization, structure verification and clinical applications.

Key words: Phospholipids, Phytosomes, Active constituents, Bioavailability

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Supporting:

Foundation item: The National Science and Technology Major Projects "Major New Drugs Innovation and Development" (Grant No. 2009ZX09103-007).
*Corresponding author. Tel.: 86-21-55514600-222