水溶性是人參皂苷類化合物關(guān)鍵的物理化學(xué)性質(zhì),也是其藥物研發(fā)過程中極為重要的問題之一。人參皂苷類藥物具有良好的水溶性會(huì)有助于藥效的發(fā)揮和藥動(dòng)學(xué)性質(zhì)的改善,所以其水溶性提升方法的研究引起了人們的關(guān)注。通過查閱整理近十年的國(guó)內(nèi)外文獻(xiàn),對(duì)人參皂苷類化合物水溶性提升的方法進(jìn)行了綜述,包括成鹽、引入極性基團(tuán)、降低不飽和度、氨基酸酯化、糖基化、二元酸酯化等化學(xué)方法,以及制成微球以及自微乳釋藥系統(tǒng)等物理化學(xué)方法,為該類化合物的進(jìn)一步研發(fā)利用提供參考。

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 of ginsenoside 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.

國(guó)家自然科學(xué)基金資助項(xiàng)目(81273389)