尼索地平纳米混悬液的制备及其体外溶出度  

Preparation and in vitro dissolution of nisoldipine nanosuspension

作　　者：房明明[1] 杨文倩[1] 邵靖博 付强[1] 何仲贵[1] 王永军[1] 

机构地区：[1]沈阳药科大学药学院,辽宁沈阳110016

出　　处：《沈阳药科大学学报》2016年第2期93-97,共5页Journal of Shenyang Pharmaceutical University

基　　金：国家自然科学基金资助项目(81173008);辽宁省博士科研启动基金资助项目(20141066);辽宁省教育厅一般资助项目(L2014379);沈阳药科大学中青年教师事业发展支持计划

摘　　要：目的制备、优化尼索地平纳米混悬液,检测研磨介质残留,评价尼索地平纳米混悬液的体外溶出度。方法采用介质研磨法制备尼索地平纳米混悬液,以粒径为指标筛选、优化处方,利用电感耦合等离子体质谱仪测定研磨介质的残留,采用浆法评价尼索地平纳米混悬液的体外溶出。结果最优处方为尼索地平与PVP-K30质量比4∶1,其平均粒径为(445.5±2.8)nm,zeta电位为(0.294±1.00)m V,20 min时纳米混悬液累积溶出(87.0±4.5)%,在4℃和20℃条件下,该纳米混悬液30 d内物理稳定性良好。结论采用介质研磨法制备的纳米混悬液可以提高尼索地平的体外溶出度。Objective To prepare nisoldipine nanosuspension, detect quantity of zirconium and optimize its formulation, and then to evaluate its in vitro dissolution. Methods Nisoldipine nanosuspension was prepared by bead milling, and its formulation was optimizedbased on particle size. The zirconium residuewas determined by inductively coupled plasma mass spectrometry, and the in vitro dissolution was evaluated by oar method. Results The optimal ratio of nisoldipine and PVP- K30 was 4：1 ,the mean particle size and zeta potential of nisoldipine nanosuspension was （445.5 ±2. 8 ） nm and （0. 294 ±1.00） mV, respectively. In vitro release study revealed that the 20 min accumulative release percentage reached （ 87.0 ±4. 5 ） %. Conclusions Nisoldipine nanosuspension is successfully prepared by bead milling method. It can increase the in vitro dissolution of nisolidpine.

关 键 词：尼索地平 纳米混悬液 介质研磨 处方筛选 溶出度 

分 类 号：R94[医药卫生—药剂学]