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.
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)
出处
《海南医学院学报》
CAS
北大核心
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)。
关键词
可注射奥沙利铂缓释微粒
制备工艺
理化性质
Injectable oxaliplatin sustained-release microparticles
Preparation process
Physical and chemical properties
