摘要
在四氢呋喃体系中以舒马普坦(碱)和丁二酸为反应物,采用反应结晶法制备琥珀酸舒马普坦干粉吸入剂。对影响产物粒径和形貌的因素,如反应物的配比、反应温度、搅拌速度等进行了考察,并对最优条件下所得的干粉进行了相关的物化性质表征。结果表明,当反应物的配比nST∶n丁二酸为1∶2、反应温度范围为0～15℃、搅拌速度为10000 r/min时,可以得到平均粒径大约为1μm、且粒度分布窄的琥珀酸舒马普坦颗粒,其体外沉积实验结果明显优于现有市售琥珀酸舒马普坦产品,肺部沉积值大约提高了5倍。
The purpose of this study was to produce ultrafine sumatriptan succinate （SS） for dry powder inhalation formulation via reactive crystallization, The effects of mole ratio of sumatriptan to succinic acid, reaction temperature and mixing intensity on particle size and morphology were investigated. Fourier transform infrared spectroscopy, scanning electron microscopy and X-ray diffraction were used to characterize the physicochemical properties of as-prepared SS dry powder. The results showed that ultrafine particles of SS with an average size of about 1μm could be produced and well controlled under the following conditions, mole ratio （nST ：nsuccinic acid） 1 ： 2, at 0-15 ℃ mixing intensity 10000r/min. Furthermore, after foundational aerosol performance evaluation, the fine particle fraction （FPF） （〈5μm） was increased up to 25.35%, which was approximate 5 times of the FPF value for the milled commercial SS.
出处
《化工进展》
EI
CAS
CSCD
北大核心
2008年第9期1412-1416,共5页
Chemical Industry and Engineering Progress
基金
国家高技术研究发展计划(863计划)项目(2006AA030202)
关键词
琥珀酸舒马普坦
超细颗粒
反应结晶
干粉吸入剂
sumatriptan succinate
ultrafine particles
reactive crystallization
dry powder inhalation
