恩替卡韦微球的制备与质量评价
Preparation and quality evaluation of entecavir microspheres
李艳敏 1周梦莹 1魏开芳 1张春燕1
作者信息
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.
Abstract
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Key words
Entecavir/PLGA/Microspheres引用本文复制引用
出版年
2024
NETL
NSTL
万方数据