扎鲁司特介孔二氧化硅固体分散体的制备及其体外释放考察

Preparation and in Vitro Release of Zafirlukast Mesoporous Silica Solid Dispersion

目的制备扎鲁司特(zafirlukast,ZLST)介孔二氧化硅固体分散体,提高体外溶出速度。方法通过溶胶凝胶法制得介孔二氧化硅(MCM-41),将其甲基化改性(MCM-41CH_3);采用浸渍挥干法将ZLST载入,测定体外溶解速度;并采用X射线衍射、差示扫描量热、傅立叶变换红外光谱、扫描电镜、透射电镜等手段对固体分散体进行表征。结果药物介孔二氧化硅固体分散体可以显著地加快药物的溶出速度,ZLST-MCM-41的释放率略高于ZLST-MCM-41CH_3;物相鉴定表明,ZLST以无定型或微晶形式分散于介孔载体中。结论介孔二氧化硅可以作为ZLST优良的载体材料。

OBJECTIVE To prepare zafirlukast-mesoporous silica solid dispersion in order to improve the dissolution rate of zafirlukast. METHODS Mesoporous silica(MCM-41) was synthesized via sol-gel method, the samples were also modified by silylation using trimethylchlorosilane(denoted as: MCM-41CH3);zafirlukast was loaded into mesoporous silica by impregnation method. The dissolution rate of solid dispersions were tested, and the samples were also characterized by means of X-ray diffraction, differential scanning calorimeter, scanning electron microscope, Fourier Transform infrared spectroscopy, transmission electron microscopy. RESULTS The dissolution rate of solid dispersions were significant increased, the accumulated dissolution of ZLST-MCM-41 was slight higher than that of ZLST-MCM-41CH3. According to the characterization results, the drug in samples was amorphous or fine crystals. CONCLUSION It is believed that mesoporous silica is a good carriers for zafirlukast .