硝苯地平中空控释微球的处方研究及质量评价

发布时间：2018-05-15 12:22

本文选题：硝苯地平 + 中空控释微球　；参考：《中国药房》2017年13期

【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%(RSD10%,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。
[Abstract]:Objective: to prepare nifedipine NFN hollow controlled-release microspheres and evaluate their quality. Methods: the solvent diffusion volatilization method was used to prepare microspheres. Based on the cumulative release rate of 2h / 2h / s / 24h / h, the orthogonal test was designed to screen the dosage of ethyl cellulose, polyvinylpyrrolidone (PVP) and main drug NF in the formulation, and to evaluate the appearance and particle size distribution of the microspheres prepared by the optimal formulation, and to evaluate the distribution of the appearance and particle size of the microspheres prepared by the best prescription. Drug loading, floatability and cumulative release, with imported NF controlled-release tablets. To compare the release behavior in vitro. Results: the best prescription was NF 3.00 g PVP 1.60 g EC 15.65 g. The NF hollow controlled-release microspheres were spherical in appearance, the diameter of which was mainly distributed at 20 ~ 40 mesh, and the drug content was 8.66. The floatation rate was 97.93% in the release medium for 24 h. The floatation rate of the NF hollow controlled-release microspheres was 20.499,52.90,91.00% RSD10nc3H, respectively, compared with the imported preparations. The similar factor of cumulative release was more than 50 (n = 0.478), and the drug release in vitro was in accordance with the zero order kinetic equation (r = 0.999 3) and its Ritger-Peppas equation (r = 0.980 7). Conclusion: NF hollow controlled-release microspheres have similar drug release behavior to imported preparations, and the drug release mechanism is the joint action of diffusion and skeleton dissolution.
【作者单位】：西南医科大学附属医院研究生部;西南医科大学药学院药剂学教研室;西南医科大学附属医院心血管内科;
【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)
【分类号】：R943

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