可注射奥沙利铂缓释微粒制备及其理化性质研究  

Preparation and physicochemical properties of injectable oxaliplatin sustained⁃release microparticles

作　　者：张俊伟 焦斌琪 曹坤 张彦志 陈铭哲 黄克祥 梁月祥 李井泉 ZHANG Junwei;JIAO Binqi;CAO Kun;ZHANG Yanzhi;CHEN Mingzhe;HUANG Kexiang;LIANG Yuexiang;LI Jingquan(Department of Gastrointestinal Oncology Surgery,the First Affiliated Hospital of Hainan Medical University,Haikou 570100,China)

机构地区：[1]海南医学院第一附属医院胃肠肿瘤外科,海南海口570100

出　　处：《海南医学院学报》2024年第10期779-783,共5页Journal of Hainan Medical University

基　　金：海南省科学技术厅重点研发项目(ZDYF2020137)。

摘　　要：目的:开发可注射奥沙利铂缓释微粒,并对其制备工艺和理化性质进行研究。方法:采用热熔挤出-冷冻研磨工艺制备可注射奥沙利铂缓释微粒,使用扫描电镜、粒度分析仪了解微粒形貌及粒径分布,采用液相色谱系统测量缓释微粒中奥沙利铂含量和微粒体外释放度。结果:可注射奥沙利铂缓释微粒粒度分布曲线稳定,微粒中奥沙利铂包封率为46.8%,包封率高;体外释放结果显示,奥沙利铂缓释微粒释放周期为144 h,最终释放度在80.0%以上,具有缓释性能;缓释微粒注射剂pH值在6.18~6.45的范围内,不会对注射部位造成损伤。结论:通过热熔挤出-冷冻研磨工艺制备的可注射奥沙利铂缓释微粒粒径分布均匀、药物包封率高,并且具有优异的缓控释特性以及稳定的理化性质。Objective:Injectable oxaliplatin sustained-release microparticles were developed,and their preparation process and physical and chemical properties were studied.Methods:Injectable oxaliplatin sustained-release microparticles were prepared by hot melt extrusion freeze grinding process.The morphology and particle size distribution of the sustained-release microparticles were studied by scanning electron microscope and particle size analyzer.The content of oxaliplatin in the sustained-release microparticles and the release of microsome were measured by liquid chromatography system.Results:The particle size distribution curve of injectable oxaliplatin sustained-release microparticles was stable,and the encapsulation efficiency of oxaliplatin in the microparticles was 46.8%,which was high.The results of in vitro release showed that the release period of oxaliplatin sustained-release microparticles was 144 hours,and the final release degree was above 80.0%,with sustained release performance.The pH value of the sustained-release microparticles injection is within the range of 6.18-6.45,and it will not cause damage to the injection site.Conclusion:Injectable oxaliplatin sustained-release microparticles prepared by hot melt extrusion freeze grinding process have uniform particle size distribution,high drug encapsulation efficiency,excellent slow and controlled release characteristics and stable physical and chemical properties.

关 键 词：可注射奥沙利铂缓释微粒 制备工艺 理化性质 

分 类 号：TQ460.6[化学工程—制药化工]