恩替卡韦微球的制备与质量评价  

Preparation and quality evaluation of entecavir microspheres

作　　者：李艳敏 周梦莹 魏开芳[1] 张春燕[1] LI Yanmin;ZHOU Mengying;WEI Kaifang;ZHANG Chunyan(School of Pharmacy,Jining Medical University,Rizhao 276826,China)

机构地区：[1]济宁医学院药学院,日照276826

出　　处：《济宁医学院学报》2024年第6期461-465,共5页Journal of Jining Medical University

基　　金：山东省2019-2020年度中医药科技发展计划项目(2019-0452);2022年济宁医学院大学生创新训练计划项目(cx2022169)。

摘　　要：目的制备恩替卡韦微球,并进行质量评价。方法采用喷雾干燥法制备恩替卡韦微球,利用扫描电镜观察形态,Masterzier 3000粒度仪测试粒径分布,高效液相色谱法测定包封率、载药量、体外释药曲线。结果所得微球呈圆球形,平均粒径9.58μm,载药量为11.5%,包封率为92.0%,体外释药可达24d。喷雾干燥器进口温度、PLGA浓度、PLGA黏度对微球形态具有一定影响,PLGA浓度和乳酸/羟基乙酸(LA/GA)比例影响微球体外释药过程。结论本实验制备得到的恩替卡韦微球体外具有良好的缓释作用,有望为抗乙肝病毒药物新剂型的开发提供依据和参考。Objective To prepare entecavir microspheres and evaluate the quality.Methods The entecavir microspheres were prepared by spray drying method.The morphology and particle size distribution were observed by scanning electron microscope and a Masterzier 3000 Particle Size Analyzer respectively.The entrapment efficiency,drug loading rate and in vitro release rate were determined by HPLC.Results The microspheres were spherical,with an average particle size of 9.58μm,drug loading rate of 11.5%,entrapment efficiency of 92.0%,and it could release for 24 days in vitro.The morphology of microspheres was influenced by the inlet temperature,PLGA concentration,and PLGA viscosity.The in vitro drug release process was affected by the concentration of PLGA and the ratio of LA/GA.Conclusion The entecavir microspheres showed good sustained release effect in vitro,and it is expected to provide reference for the development of anti HBV drugs.

关 键 词：恩替卡韦 聚乳酸-羟基乙酸共聚物 微球 

分 类 号：R969.1[医药卫生—药理学]