超细琥珀酸舒马普坦的制备及其性能评价  

Preparation and Properties of Ultra-Fined Sumatriptan Succinate

作　　者：刘淼[1] 乐园[1] 赵宏[1] 杨宗阳[1] 陈建峰[1] 

机构地区：[1]北京化工大学纳米材料先进制备技术与应用科学教育部重点实验室,北京100029

出　　处：《化学反应工程与工艺》2008年第5期405-410,共6页Chemical Reaction Engineering and Technology

基　　金：国家自然科学基金(20806004);北京市科技新星计划(Z0078022)

摘　　要：利用反溶剂重结晶法进行琥珀酸舒马普坦微粉化研制,考察了溶液和反溶剂的体积比、结晶温度、搅拌速率和干燥方式等因素对产品粒径、形貌及性能的影响。采用扫描电镜(SEM)、红外光谱(FT-IR)和 X 射线衍射(XRD)对产品进行了表征。得到适宜的微粉化条件为溶液与反溶剂的体积比1:20,结晶温度4℃,搅拌速率2 000 r/min。利用体外模拟肺部沉积实验考察了不同干燥方式(真空干燥和喷雾干燥)对产品性能的影响。实验结果表明,真空干燥可以得到平均粒径约为1 μm的琥珀酸舒马普坦超微粉,喷雾干燥得到流动性好的薄片状产品,且喷雾干燥的产品体外肺部沉积效果明显优于经真空干燥制备的产品,有效部位沉积量高达(66.52±5.2)%,真空干燥产品仅有(16.54±6.4)%。The micronized sumatriptan succinate was prepared by antisolvent recrystallization method. The effects of the volume ratio of solution to antisolvent, temperature, stirring speed and drying methods on the particle size, morphology and property of sumatriptan succinate were investigated. The optimal conditions were volume ratio of solution to antisolvent 1 ： 20, temperature 4 ℃, stirring speed 2 000r/min. The as-prepared sumatriptan suecinate was characterized by scanning electron microscopy （SEM）, Fourier transformed infrared spectroscopy （FT-IR） and X-ray diffraction （XRD）. The aerosol performance of the products prepared by different drying methods （vacuum drying and spray drying） was evaluated using vitro lung deposition test. The mean particle size of the micronized sumatriptan succinate obtained under optimum conditions was 1μm, and the spray-dried product was thin slice shape with good flow ability. The aerosol performance of the spray-dried product with vitro lung deposition（66.52±5.2）^ was better than that of the vacuum-dried one with vitro lung deposition（16.54±6.4）%.

关 键 词：微粉化 琥珀酸舒马普坦 反溶剂重结晶 干粉吸入剂 

分 类 号：TQ460.6[化学工程—制药化工]