人参皂苷类化合物水溶性提升方法的研究进展

Advances in studies on improvement of water solubility of ginsenoside

水溶性是人参皂苷类化合物关键的物理化学性质,也是其药物研发过程中极为重要的问题之一。人参皂苷类药物具有良好的水溶性会有助于药效的发挥和药动学性质的改善,所以其水溶性提升方法的研究引起了人们的关注。通过查阅整理近十年的国内外文献,对人参皂苷类化合物水溶性提升的方法进行了综述,包括成盐、引入极性基团、降低不饱和度、氨基酸酯化、糖基化、二元酸酯化等化学方法,以及制成微球以及自微乳释药系统等物理化学方法,为该类化合物的进一步研发利用提供参考。

Water solubility is an essential physical chemistry property of ginsenoside, and is also a very important issue in drug discovery. Good water solubility of ginsenoside drugs often contributes to a pleasant drug potency and nice pharmacokinetic profiles, so the research on improving water solubility has attracted people＇s attention. This article mainly summarizes the research advances of the improvement of water solubility ofginsenoside in 10 years, including salt formation, polar group introduction, saturation reduction, amino acid esterification, glycosylation, dibasic acid esterification, microsphere formation, and self microemulsion drug delivery system formation, which could be able to provide information for research and development of ginsenoside.