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液相中制备尼群地平的固体分散体缓释微球
Preparation of sustained-release nitrendipine microspheres with a solid dispersed structure in liquid system
【摘要】 目的 在液相中制备尼群地平的固体分散体缓释微球并研究其影响因素。方法 采用球晶造粒技术与溶剂沉积法相结合的方法 ,以滑石粉为固体分散体载体 ,EudragitRSPO为阻滞剂 ,在液相中一步制备尼群地平的固体分散体微球 .考察了微球的收率、粉体性质及影响微球成形和释放速度的因素。结果 采用该方法制备的尼群地平缓释微球圆整、均匀 ,粒径在 2 80~ 90 0 μm的微球收率可达 70 %以上 ,堆密度在 0 7kg·L- 1 左右 ,药物的包封率可达95 %以上 ,微球的成形主要受溶剂系统中液体架桥剂量和不良溶剂中乳化剂的影响 ,药物从微球中的释放速度可通过调节处方中阻滞剂和分散剂的量的比例控制。结论 本方法适用于难溶性药物制备缓释微球
【Abstract】 Aim To prepare the sustained release nitrendipine microspheres with a solid dispersed structure in liquid system. Methods The sustained release nitrendipine microspheres with a solid dispersed structure was prepared in liquid system by combining spherical crystallization technique and solvent deposition method in one step. The resultant microspheres were evaluated for the recovery, micromeritc properties, incorporation efficiency. The factors of effect on the formation and the release rate of microspheres were also investigated. Results The recovery of microspheres (280-900 μm) was more than 70% and the bulk density was around 0 7 kg·L -1 . The incorporation efficiency always exceeded 95%. The formation of microspheres was mainly affected by the amount of bridging liquid and the emulsifying agents in poor solvent. The release rate of nitrendipine from the microspheres could be controlled as desired by adjusting the ratio of talc to Eudragit RS PO in the formulation. Conclusion The presented method was suitable for preparing sustained release microspheres of a water insoluble drug.
【Key words】 spherical crystallization technique; solvent deposition method; nitrendipine; sustained release microspheres;
- 【文献出处】 药学学报 ,Acta Pharmaceutica Sinica , 编辑部邮箱 ,2003年08期
- 【分类号】R943
- 【被引频次】4
- 【下载频次】455