The preparation and characteristics of febuxostat SiO2 solid dispersions  

非布索坦二氧化硅固体分散体的制备及表征(英文)

作　　者：宋文丁 杜若[1] 宋平[1] 钟婷[1] 张卫强[1] 赵阳[1] 王超[1] 张烜[1,2] 张强[1,2] 

机构地区：[1]北京大学医学部药学院药剂学系,北京100191 [2]北京大学医学部药学院天然药物及仿生药物国家重点实验室,北京100191

出　　处：《Journal of Chinese Pharmaceutical Sciences》2014年第7期463-470,共8页中国药学（英文版）

基　　金：National Natural Science Foundation of China(Grant No.81172992);the National Basic Research Program of China(Grant No.973 Program 2009CB930300);Innovation Team of Ministry of Education(Grant No.BMU20110263)

摘　　要：In the present research, we selected Sylysia as a porous material and febuxostat（FBT） as model drug to prepare the FBT SiO2 solid dispersions using a solvent evaporation method. We firstly established an HPLC method for determining FBT in our prepared FBT SiO2 solid dispersions. And then, the characteristics of FBT SiO2 solid dispersions were investigated, including differential scanning calorimetry（DSC）, powder X-ray diffraction（PXRD）, scanning electron microscope（SEM）, particle size and distribution. The solubility and dissolution of FBT SiO2 solid dispersion were also evaluated. The results of DSC and PXRD showed that the FBT existed in an amorphous state in FBT SiO2 solid dispersions. The SEM and particle size results indicated that the shape and average particle size of FBT SiO2 solid dispersions was similar to the Sylysia. The solubility and dissolution of FBT in FBT SiO2 solid dispersions were significantly enhanced compared with the pure FBT. In conclusion, we successfully prepared FBT SiO2 solid dispersions to increase the solubility and dissolution rate of the poorly water-soluble FBT.本文选择Sylysia(SiO2)为多孔载体材料,以非布索坦(febuxostat,FBT)为模型药物,制备非布索坦二氧化硅固体分散体并进行表征。首先我们建立了非布索坦的HPLC测定方法,对非布索坦固体分散体的DSC、PXRD、SEM和粒径进行表征,对非布索坦固体分散体的溶解度和溶出度进行测定。DSC和PXRD数据结果表明,非布索坦在固体分散体中以无定型存在。SEM和粒径结果表明,非布索坦固体分散体的粒径和Sylysia相近。溶解度和溶出度结果显示,非布索坦固体分散体的溶解度和溶出度相对于非布索坦而言显著提高。上述结果表明,所制备的非布索坦固体分散体可增加难溶性药物非布索坦的溶解度和溶出度。

关 键 词：FEBUXOSTAT Sylysia Solid dispersion Solubility and dissolution 

分 类 号：R943[医药卫生—药剂学]