注射用依匹哌唑缓释微球的体外释放度研究  

In vitro release study of brexpiprazole sustained release microspheres for injection

作　　者：孙金梅 余飞 徐志红 张连庆 周凤梅 刘万卉[1,2,3] SUN Jin-mei;YU Fei;XU Zhi-hong;ZHANG Lian-qing;ZHOU Feng-mei;LIU Wan-hui(College of Pharmacy,Yantai University,Yantai 264005,China;Key Laboratory of Molecular Pharmacology and Drug Evaluation of Ministry of Education,Yantai University,Yantai 264005,China;State Key Laboratory of Long-acting and Targeting Drug Delivery System,Shandong Luye Pharmaceutical Co.,Ltd.,Yantai 264670,China)

机构地区：[1]烟台大学药学院,烟台264005 [2]烟台大学分子药理和药物评价教育部重点实验室,烟台264005 [3]山东绿叶制药有限公司长效和靶向制剂国家重点实验室,烟台264670

出　　处：《中国新药杂志》2023年第16期1684-1689,共6页Chinese Journal of New Drugs

摘　　要：目的:建立注射用依匹哌唑缓释微球的体外加速释放度方法,并探讨与体内释放的相互关系,为该制剂处方筛选和质量控制提供参考。方法:考察了释放介质中表面活性剂的种类和浓度、盐种类、温度等对释放行为的影响,通过区分能力和体内外关系(in vivo and in vitro relationship,IVIVR)分析最终确定了体外加速释放方法。结果:建立了45℃、pH 7.4的羟乙基哌秦乙硫磺酸(HEPES,含0.2%十六烷基三甲基溴化铵)的体外加速释放度方法,与体内释放具有良好的相互关系(r^(2)>0.99)。结论:本研究建立的体外加速释放度方法可以在药物开发的各阶段指导处方筛选以及工艺变更,对产品的质量控制具有重大意义。Objective:To establish a method of accelerated release of brexpiprazole sustained release microspheres for injection in vitro and discuss the in vivo and in vitro relationship,so as to provide reference for prescription screening and quality control of this preparation.Methods:The effects of surfactant type,salt type and temperature on the release behavior were investigated by the method of constant temperature water bath.The in vitro accelerated release method was finally determined by the analysis of distinguishing ability and in vivo and in vitro relationship(IVIVR).Results:A method for accelerated release of pH 7.4 HEPES(containing 0.2%cetyltrimethylammonium bromide)at 45℃in vitro was established,which showed a good correlation with in vivo release(r^(2)>0.99).Conclusion:The method of accelerated release in vitro established in this paper can guide prescription screening and process modification in all stages of drug development,and it is of great significance for product quality control.

关 键 词：依匹哌唑 缓释微球 体内外关系 十六烷基三甲基溴化铵 体外加速释放实验 

分 类 号：R943[医药卫生—药剂学]