尼莫地平壳聚糖微球的制备及其体外释药特性的研究

The Preparation of Nimodipine Chitosan Microspheres and Their Sustained Release Characteristics in Vitro

关键词:  尼莫地平  壳聚糖  微球  缓释

Key words:  nimodipine  chitosan  microsphere  sustained release

摘要:

目的 以壳聚糖为载体材料制备尼莫地平微球，并考察其体外释药特性。方法 以壳聚糖为载体，液体石蜡为油相，戊二醛为交联剂，span80为乳化剂，采用正交设计优化壳聚糖微球的制备工艺，用乳化交联法制备尼莫地平壳聚糖微球。模拟人体肠液的环境进行体外释药研究。结果 通过单因素考察和正交实验，筛选出尼莫地平壳聚糖微球的优化制备工艺和处方，所得微球形态圆整，大小均匀，表面光滑，平均粒径为9.56 μm，载药量为17.82%，包封率为52%。体外释药结果表明，一级动力学方程能较好的对其进行拟合。结论 尼莫地平壳聚糖微球的制备工艺稳定可行，所得壳聚糖微球有良好的缓释效果。

Abstract:

OBJECTIVE To prepare nimodipine chitosan microsperes, and investigate their release characteristics in vitro. METHODS Chitosan was used as a carrier, liquid paraffin as oil phase, glutaradehyde as the cross-linker, and Span-80 as emulsifier. Nimodipine chitosan microspheres was prepared using emulsion-linking technique, in which orthogonal experimental design was introduced to optimize the preparation conditions. The release characteristics of the microspheres was investigated in artificial gut fluid in vitro. RESULTS After optimizing, the microspheres with good shape, smooth surface and narrow size distribution were prepared. The average particle size was 9.56 μm, the drug loading rate was 17.82% and the entrapment rate was 52%. The release rate of the microsperes could be appropriately simulated by first order kinetics equation. CONCLUSION The preparation procedure established was stable and practical, and the microspheres obtained showed good sustained release characteristics.