中文摘要：

目的为提高水难溶性药物的分散性及溶出度,制备介孔二氧化硅纳米粒作为水难溶性药物的载体。方法探索得到简单有效地制备球状介孔二氧化硅纳米粒的工艺条件,采用扫描电镜及氮气吸附-脱附等手段分析表征载体的外观形貌,比表面积及孔径分布,并选取水难溶性药物西洛他唑作为模型药物,以溶剂浸渍挥干法载药制得药物固体分散体,采用热分析、氮气吸附-脱附曲线以及溶出度实验研究药物固体分散体的基本性质。结果制得的二氧化硅载体的形貌近球状,粒径大小分布在200～250 nm,载体的比表面积最高可达1 101.54 m2.g-1,孔径分布主要集中在3.0～4.0 nm。载药过程对西洛他唑在载体中的存在形式没有影响,固体分散体中西洛他唑的溶出度得到显著提高,当药物与载体的质量比为1∶3时,药物60 min累计溶出达85%。结论介孔二氧化硅纳米粒有望成为水难溶性药物的优良载体。

英文摘要：

Objective To enhance the dispersibility and dissolution of poorly water-soluble drug taking synthesized mesoporous silica nanoparticle as poorly water-soluble drug solid dispersion carrier.Methods Simple and effective synthesis process conditions of spherical mesoporous silica nanoparticle were explored and then obtained.Shape appearances specific surface areas and pore size distributions were systematically studied using scanning electron microscopy（SEM）,nitrogen adsorption.Cilostazol（CLT）was chosen as model drug and the solid dispersion was developed though solvent-dipping method.Investigations were carried out using nitrogen adsorption,differential scanning calorimetry（DSC）and the dissolution experiment,which demonstrated the basic properties of CLT solid dispersion.Results The spherical shape of silica carrier was displayed in SEM images and the size of the particle was between 200-250 nm.The consequences of nitrogen adsorption suggested a high specific surface areas reaching up to 1 101.54 m2 · g-1and a concentrating pore size distribution between 3.0-4.0 nm.The existence form of CLT did not change during the drug loading process.The dissolution results indicated that the best drug to carrier ratio were 1∶ 3（m∶ m）for CLT and the accumulated dissolution of CLT solid dispersions could reach about 85% within 60 min.Conclusions It is believed that MSN has a promising application value as a good carrier for poor water-soluble drug.