口服药物纳米结晶的研究进展  

Research Progress of Drug Nanocrystals for Oral Delivery

作　　者：涂亮星[1] 胡凯莉[1] 奉建芳[1] 

机构地区：[1]上海中医药大学穆拉德中药现代化研究中心,上海201203

出　　处：《中国医药工业杂志》2015年第4期396-403,共8页Chinese Journal of Pharmaceuticals

基　　金：国家重点基础研究项目(973项目;2009CB930300);上海市优秀技术带头人计划项目(13XD1425300);上海市科委纳米专项项目(11nm0506700)

摘　　要：溶解度差已成为难溶性药物成功上市的主要壁垒。纳米结晶技术具有制备简便、载药量高和易放大等优势,可将药物破碎成纳米级,提高药物的饱和溶解度和溶出速率,从而提高药物口服生物利用度。如何获得粒径小、稳定性好的纳米结晶是目前该领域研究的重点与难点。本文将就这两方面的内容进行评述。Poor water-solubility is becoming a major hurdle for water-insoluble drug to reach the market. The preparation for nanocrystals has the advantages of simplicity of production, high drug loading and easy to scale-up, etc. The water-insoluble drug can be broken into samller particles easily with this technology, so that the saturation solubility and dissolution velocity as well as the oral bioavailability are improved. How to produce nanoscale particles and enhance stability of the nanocrystals are the key point and diffi culty in this fi eld at present. This paper will summarize and make comments on these two aspects.

关 键 词：纳米结晶 粒径 稳定性 口服生物利用度 综述 

分 类 号：R944.9[医药卫生—药剂学]