Zhong Hui, Zhu Yuan, Yu Jiang-nan, Xu Xi-ming
Zhongguo Zhong Yao Za Zhi. 2014 Sep;39(17):3226-31.
With the development of natural products, the research activities on the solubilization methods of water-insoluble natural products have been carried out worldwide. Big molecular weight and poor solubility of most natural active ingredients lead to a very poor oral absorption and low bioavailability, which has extremely limited their development in pharmaceutical fields and clinical application. As a result, it is necessary to find out a suitable technique to improve the solubility and enhance the oral bioavailability of insoluble natural drugs. Based on the related references published in these years, this review introduced some new techniques to improve the solubility and bioavailability of natural drugs, including prodrugs, inclusion complex, solid dispersion, cocrystals, osmotic pump, liquisolid compacts, micronization, self-microemulsifying, nanosuspensions, lipsomes, polymeric micelles and so on, and summarized the theory, characteristics, application range, application examples, problems and development direction of each technique.
随着天然产物的发展，全球范围内都在开展关于水不溶性天然产物增溶方法的研究活动。大多数天然活性成分分子量较大且溶解度差，导致口服吸收非常差且生物利用度低，这极大地限制了它们在制药领域的开发和临床应用。因此，有必要找到一种合适的技术来提高不溶性天然药物的溶解度并增强其口服生物利用度。基于这些年发表的相关参考文献，本综述介绍了一些提高天然药物溶解度和生物利用度的新技术，包括前体药物、包合物、固体分散体、共晶体、渗透泵、液固压缩物、微粉化、自微乳化、纳米混悬液、脂质体、聚合物胶束等，并总结了每种技术的原理、特点、应用范围、应用实例、存在的问题及发展方向。
