达沙替尼固体分散体的制备、表征及溶出特性  

Preparation,Characterization and Dissolution Characteristics of Dasatinib Solid Dispersion

作　　者：刘祺 冯菊红[1,2] 张朵朵[1,2] 陈雅婷 汪涛 盛余豪 胡学雷[1,2] LIU Qi;FENG Juhong;ZHANG Duoduo;CHEN Yating;WANG Tao;SHENG Yuhao;HU Xuelei(School of Chemical Engineering and Pharmacy,Wuhan Institute of Technology,Wuhan 430074,China;Key Laboratory for Green Chemical Process of Ministry of Education,Wuhan 430074,China)

机构地区：[1]武汉工程大学化工与制药学院,湖北武汉430074 [2]绿色化工过程教育部重点实验室,湖北武汉430074

出　　处：《化学与生物工程》2022年第4期40-44,共5页Chemistry & Bioengineering

基　　金：湖北省自然科学基金重点项目(2011CDA048)。

摘　　要：为了改善达沙替尼在中性环境中的溶解性,采用溶剂法制备达沙替尼固体分散体(SD),通过考察载体种类、药载比(达沙替尼与载体的质量比)、反应温度和反应时间对累积体外溶出度的影响优化制备工艺,并通过傅立叶变换红外光谱仪(FTIR)、X-射线衍射仪(XRD)、扫描电镜(SEM)对达沙替尼固体分散体进行表征。结果表明,当达沙替尼与载体HP-β-CD的质量比为1∶9、反应温度为60℃、反应时间为30 min时,达沙替尼固体分散体的溶出效果最佳,60 min时累积体外溶出度可达到71.55%,远高于达沙替尼原料药(11.66%)及达沙替尼与HP-β-CD的物理混合物(18.92%);FTIR、XRD和SEM分析表明,达沙替尼以无定形态高度分散于载体HP-β-CD中。In order to improve the solubility of Dasatinib in neutral environment,we prepared its solid dispersions(SD)by a solvent method.Moreover,we optimized the preparation process by investigating the effects of carrier type,drug-carrier ratio(mass ratio of Dasatinib to carrier),reaction temperature,and reaction time on the cumulative in vitro dissolution.Furthermore,we characterized the Dasatinib SD by Fourier transform infrared spectroscopy(FTIR),X-ray diffraction(XRD),and scanning electron microscopy(SEM).The results show that,when the mass ratio of Dasatinib to HP-β-CD is 1∶9,the reaction temperature is 60℃,and the reaction time is 30 min,the dissolution effect of Dasatinib SD is the best,and the cumulative in vitro dissolution can reach 71.55%at 60 min,which is much higher than that of Dasatinib(11.66%)and the physical mixture of Dasatinib and HP-β-CD(18.92%).FTIR,XRD,and SEM analyses show that Dasatinib is highly dispersed in carrier HP-β-CD with amorphous form.

关 键 词：达沙替尼 固体分散体 累积体外溶出度 溶剂法 

分 类 号：TQ460[化学工程—制药化工] R979.1[医药卫生—药品]