挤出滚圆法制备间尼索地平-磺丁醚--环糊精微丸及其质量评价.PDFVIP

·药 剂· 挤出滚圆法制备间尼索地平-磺丁醚-?-环糊精微丸及其质量评价 齐晓丹，王伟，田珊(河北医科大学药学院药剂学教研室，石家庄 050017) 摘要：目的 制备具有较高水溶性的间尼索地平微丸。方法 以磺丁醚-?-环糊精(SBE-?-CD)为成丸辅料，羟丙基纤维素 乙醇溶液为黏合剂，采用挤出滚圆法制备间尼索地平微丸，对影响成球的关键参数挤出速度、滚圆转速进行筛选优化， 对微丸体外释放进行评价，并对微丸进行粉体学性质的考察。结果 制得的间尼索地平微丸水中溶出度高，圆整度好， 收率可达 70%，各项粉体学性质较为理想。结论 以 SBE-?-CD 为成丸辅料，采用挤出滚圆法制备高水溶性的间尼索地 平微丸在工艺上是可行的，对难溶性药物微丸的制备具有一定借鉴作用。 关键词：挤出滚圆；间尼索地平；磺丁醚-?-环糊精；微丸；体外溶出；粉体学 中图分类号：R943.4 文献标志码：A 文章编号：1007-7693(2011)01-0060-04 Preparation and Quality Evaluation of m-Nisoldipine-Sulfobutyl Ether-?-Cyclodextrins Pellets by Extrusion-Spheronization Method QI Xiaodan，WANG Wei，TIAN Shan(Department of Pharmaceutics, College of Pharmacy, Hebei Medical University, Shijiazhuang 050017, China) ABSTRACT: OBJECTIVE To prepare high solubility m-nisoldipine pellets. METHODS The m-nisoldipine-sulfobutyl ether (SBE)-β-cyclodextrins (CD) pellets were prepared by extrusion-spheronization, ethanol solvent with hydroxypropyl cellulose as a binder. The effects of key parameters on spheronization process were the proportion of extrusion speed and spheronisation speed, which were investigated to obtain optimal formulation. In vitro release of pellets and micromeritics of pellets were evaluated. RESULTS m-Nisoldipine pellets have good water soluble property, presented perfect sphericity and yield over 70%. CONCLUSION The m-nisoldipine-SBE-β-CD pellets are successfully prepared by extrusion-spheronization. It presents a method for poor water soluble drugs pellets. KEY WORDS: extrusion-spheronization; m-nisoldipine; sulfobutyl ether-?-cyclodextrins; pellets; in vitro release; micromeritics 间尼索地平(m-Nis)化学名称：1,4-二氢-2,6- 低及溶血性小等优点，是性能优良的药用辅料。 二甲基-4-(3-硝基苯基)-3,5-吡啶二羧酸甲酯异丁 作为最适合药剂应用的环糊精[6] ，国内外对 酯，为尼索地平的同分异构体，系河北医科大学 SBE-?-CD 研究非常活跃[7]。 药学院合成的新分子实体药物。通过结构