超临界CO_2抗溶剂法制备苯扎贝特药物微粒  

Formation of Bezafibrate Particles via Gas Antisolvent Process with Supercritical CO_2

作　　者：陈琪[1] 陈鹏丽 谭柳杨 胡国勤[2] CHEN Qi;CHEN Pengli;TAN Liuyang;HU Guoqin(Dept. of Pharmacy, Henan Provincial People ＇s Hospital, Zhengzhou 450003;School of Chemical Engineering and Energy, Zhengzhou University, Zhengzhou 450001)

机构地区：[1]河南省人民医院药学部,河南郑州450003 [2]郑州大学化工与能源学院,河南郑州450001

出　　处：《中国医药工业杂志》2018年第6期789-795,共7页Chinese Journal of Pharmaceuticals

基　　金：河南省科技攻关重点项目(152102310148)

摘　　要：采用超临界CO_2流体抗溶剂技术制备了苯扎贝特药物微粒。结果表明微粒大小随重结晶压力的升高而增大,随重结晶温度的升高而降低;苯扎贝特浓度越大,微粒越大;CO_2流速变化对微粒大小几乎无影响;使用不同溶剂重结晶生成的微粒大小不同。采用红外光谱、X射线衍射、热重和差示扫描量热分析法对制得微粒进行表征,结果表明采用超临界CO_2流体抗溶剂技术制备的苯扎贝特微粒尺寸小、粒度分布均匀,且物理化学性质没有发生变化。Bezafibrate（BZ） was micronized by gas antisolvent（GAS） process with supercritical CO_2（SCCO_2） as an antisolvent, and the needle-like crystallines with ordered structure were obtained. The results showed that smaller microparticles were obtained at higher crystallizing temperature and lower pressure, and meanwhile the length of crystalline decreased as the concentration of BZ decreased. The length of crystalline altered with the kind of solvents, and it did not show significant change with the flow rate of SC-CO_2. The crystallines of BZ were analyzed by microscopic imaging system, scanning electron microscopy（SEM）, Fourier transform infared spectroscopy（FT-IR）, X-ray diffraction（XRD）, thermogravimetric analysis（TGA） and differential scanning calorimetry（DSC）. The recrystallization of BZ was successfully performed by GAS and needle-like crystallitns with smaller particle size and a narrow distribution were obtained. The results of FT-IR, XRD, TGA and DSC indicated that there was no significant differences in physicochemical properties between the raw material and particles of BZ micronized by GAS.

关 键 词：苯扎贝特 超临界流体 抗溶剂技术 超细微粒 形貌 粒径 表征 

分 类 号：R944.9[医药卫生—药剂学]