硝苯地平中空控释微球的处方研究及质量评价  

Formulation Study and Quality Evaluation of Nifedipine Hollow Controlled-release Microspheres

作　　者：蔚坤妍 黄绍秋 魏郁梦 冯婷 郑文武 赵领 

机构地区：[1]西南医科大学附属医院研究生部,四川泸州646099 [2]西南医科大学药学院药剂学教研室,四川泸州646099 [3]西南医科大学附属医院心血管内科,四川泸州646099

出　　处：《中国药房》2017年第13期1820-1823,共4页China Pharmacy

基　　金：国家自然科学基金资助项目(No.81341124);四川省科技计划项目(No.2014FZ0105;14ZC0066)

摘　　要：目的:制备硝苯地平(NF)中空控释微球并评价其质量。方法:采用溶剂扩散挥发法制备微球。以2、12、24 h的累积释放度(Q_(2h)、Q_(12h)、Q_(24h))的综合评分为指标,设计正交试验筛选处方中载体材料乙基纤维素(EC)、聚乙烯吡咯烷酮(PVP)和主药NF用量;评价最优处方所制微球的外观形态、粒径分布、载药量、漂浮性及累积释放度,并与进口制剂NF控释片(Adalat~?)比较体外释放行为。结果:最优处方为NF 3.00 g、PVP 1.60 g、EC 15.65 g。所制NF中空控释微球外观呈球形,粒径主要分布于20~40目,载药量为8.66%;在释放介质中24 h的漂浮率为97.93%;(Q_(2h)、Q_(12h)、Q_(24h))分别为20.49%、52.90%、91.00%(RSD<10%,n=3),与进口制剂比较,累积释放度的相似因子(f_2)均大于50;体外释药符合零级动力学方程(r=0.999 3),其Ritger-Peppas方程(r=0.980 7)的n为0.478。结论:所制NF中空控释微球与进口制剂具有相似的释药行为,其释药机制为扩散和骨架溶蚀共同作用。OBJECTIVE：To prepare nifedipine （NF） hollow controlled-release microspheres and evaluate the quality. METH-ODS：Solvent diffusion volatilization method was used to prepare microspheres,using comprehensive scores of cumulative release in 2,12,24 h（Q2 h,Q12 h,Q24 h）as indexes,orthogonal test was designed to screen the carrier material ethyl cellulose（EC）,poly-vinyl pyrrolidone（PVP）and main drug NF amounts;appearance,particle size distribution,drug loading,floating and cumulative release of the microspheres prepared by optimal formulation were evaluated and compared of in vitro release behavior with imported preparation of Nifedipine controlled-release tablets （Adalat？）. RESULTS：The optimal formulation was as follow as NF 3.00 g, PVP 1.60 g,EC 15.65 g. Prepared NF hollow controlled-release microspheres were spherical in shape with particle size distribution of 24-40 mesh and drug loading of 8.66%;24 h floating rate in release medium was 97.93%,Q2 h,Q12 h,Q24 h were 20.49%, 52.90%,91.00%（RSD〈10%,n=3）. Compared with the imported preparation,similarity factor f2 values of cumulative release were higher than 50,showing in vitro drug-release was consistent with the zero-order kinetic equation （r=0.9993）;n of Rit-ger-Peppas equation （r=0.9807） was 0.478. CONCLUSIONS：Prepare NF hollow controlled-release microspheres show similar drug-release behavior with the imported preparation,the drug is released by the combination of diffusion and erosion.

关 键 词：硝苯地平 中空控释微球 处方筛选 制备 正交试验 质量评价 

分 类 号：R943[医药卫生—药剂学]