难溶性天然药物增溶方法的研究进展  

Advanced in solubilization methods of water-insoluble natural drugs

作　　者：钟慧[1] 朱源[1] 余江南[1] 徐希明[1] 

机构地区：[1]江苏大学药学院,江苏镇江212013

出　　处：《中国中药杂志》2014年第17期3226-3231,共6页China Journal of Chinese Materia Medica

基　　金：国家自然科学基金项目(30973677);教育部博士点基金项目(20113227110012);江苏省"六大人才高峰"项目(2011YY012)

摘　　要：近年来随着人们对天然药物应用的重视,难溶性天然药物的增溶研究受到广泛关注。天然活性成分大多数存在相对分子质量大、溶解性差等问题,导致口服吸收差,生物利用度低,阻碍了其在制剂研发和临床应用等方面的发展。因此,选择合适的增溶方法,增加难溶性天然药物的溶解度,提高药物的生物利用度十分重要。该文就近年来制剂开发领域研究的热点技术,如前体药物技术、包合物技术、固体分散体技术、共晶技术、渗透泵技术、液固压缩技术、微粉化技术、自微乳、纳米混悬剂、脂质体、聚合物胶束等制剂新技术在增加难溶性天然药物溶解度和提高其生物利用度等方面的应用进行综述,介绍和评述了每一种技术或方法的原理、特点、适用范围、应用实例、存在的问题及发展方向。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.

关 键 词：难溶性天然药物 增溶技术 溶解度 生物利用度 

分 类 号：R283.6[医药卫生—中药学]