正交试验优选羧甲基壳聚糖-醋甲唑胺纳米微球的制备方案  

Otimization on preparation technology of carboxymethyl chitosan-methazolamide nanoparticles by orthogonal design

作　　者：张桂贤[1] 陈斌[1] 王晓辉[1] 李楠[1] 刘佩莉[1] 李光远[1] 祝君梅[1] 

机构地区：[1]天津市医药科学研究所,天津300020

出　　处：《天津药学》2014年第2期10-13,共4页Tianjin Pharmacy

基　　金：天津市卫生局科技基金(青年)项目(No.2012KY34)

摘　　要：目的:制备羧甲基壳聚糖载药纳米微球,醋甲唑胺为模型药物,测量药物的包封率和纳米微球形态。方法:采用乳化交联法,在微乳液的基础上制备载药纳米微球,对可能影响药物包封率的处方因素进行优化设计,筛选出最优配方。结果:羧甲基壳聚糖溶液的浓度对包封率有显著性影响,三聚磷酸钠溶液浓度和醋甲唑胺药量对包封率未见影响。优化方案的载药纳米微球包封率为49.36%,其电镜下为较规整的球型纳米微球,平均粒径386.0 nm。结论:采用乳化交联法,可形成较高包封率的羧甲基壳聚糖-醋甲唑胺纳米微球。Objective： To prepare carboxymethyl chitosan （CMC） drug - loaded nanoparticles, with methazolamide as model drug. The drug encapsulation efficiency and morphology should be measured. Methods ： Drug - loaded nanoparticles were preparated in microemulsion by emulsion crosslinking method. The design of formulation factors that may affect the drug entrapment efficiency was optimized to select optimal formulation. Results ： The concentration of carboxymethyl chitosan solution has a significant effect on the entrapment efficiency, when sodium tripolyphosphate （TPP） solution concentration and weight of methazolamide don＇ t effect on the entrapment efficiency. Entrapment efficiency of optimization of drug - Loaded nanoparticles was 49.36%. The nanoparticles is regular and baLL - type, with average particle size in 386.0 nm on electron microscope. Conclusion： Nanoparticles can be formated with hydrophilic carboxymethyl - chitosan coating lipophilic methazolamide by emulsion crosslinking method, and high encapsulation efficiency can be achieved.

关 键 词：羧甲基壳聚糖 纳米微球 醋甲唑胺 乳化交联 

分 类 号：TQ460.6[化学工程—制药化工]