那格列奈壳聚糖微球的制备及其释放性能  

Preparations and Properties of Nateglinide-Chitosan Drug-Loading Microspheres

作　　者：程利霞[1] 李国明[1] 钱程根[1] 杨珍娥[1] 石光[1] 

机构地区：[1]华南师范大学化学与环境学院,广东广州510006

出　　处：《华南师范大学学报（自然科学版）》2013年第3期68-72,共5页Journal of South China Normal University(Natural Science Edition)

基　　金：国家自然科学基金项目(51203054);广东高校高分子新型材料产学研结合示范(暨研究生创新培养)基地项目(cgzhzd1007)

摘　　要：采用乳化分散-化学交联法,以那格列奈(nateglinide)为模型药物,戊二醛为交联剂,制备了那格列奈壳聚糖微球,考察各种条件对所制备微球的理化性质和药物释放性能的影响.结果表明,所得微球球形规整,粒度分布均匀,呈黄褐色,平均粒径2.054μm,载药量为9.12%,药物包封率达48.9%.微球内部药物主要以无定形聚集态存在.体外模拟释放结果表明,微球有良好的平稳缓释性能.其释药速率随着壳聚糖浓度增大而减慢,在酸性介质中略大于在弱碱性介质中.With a novel antidiabetic nateglinide as the model drug, nateglinide-chitosan microspheres were prepared by emulsion cross-linking techniques with glutaric dialdehyde （GD） as cross-linking agent and chitosan（CS） as polymeric carrier. The influence of various conditions on microspheres＇ physicochemical properties and the drugrelease performances were investigated. The results indicated that the microspheres were tawny and had a spherical shape with an average diameter of 2. 054 μm. The drug content was 9.12% （mass fraction） and the drug encapsulation efficiency reached 48.9%. XRD analysis indicates that nateglinide in microspheres is mainly amorphous. The results of drug release in vitro show that the microspheres have a satisfactory performance of slowly and steady releasing the nateglinide. The release rate of nateglinide decreased with the increase of chitosan concentration, and is faster in the acidic buffer than in the weak alkaline buffer.

关 键 词：那格列奈 壳聚糖 微球 缓释 乳化交联 

分 类 号：O636.1[理学—高分子化学]