| 引用本文: | 纪嘉宾,葛海燕,王子淳,赵在臻,王仁亮.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[J].中国现代应用药学,2019,36(9):1071-1074. |
| JI Jiabin,GE Haiyan,WANG Zichun,ZHAO Zaizhen,WANG Renliang.Preparation and in Vitro Release of Zafirlukast Mesoporous Silica Solid Dispersion[J].Chin J Mod Appl Pharm(中国现代应用药学),2019,36(9):1071-1074. |
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| 摘要: |
| 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-41CH3）；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-41CH3；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。 |
| 关键词: 介孔二氧化硅 扎鲁司特 固体分散体 溶出度 |
| DOI：10.13748/j.cnki.issn1007-7693.2019.09.008 |
| 分类号:R944 |
| 基金项目:教育部高等教育司国家级大学生创新创业训练计划项目（201710439184） |
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| Preparation and in Vitro Release of Zafirlukast Mesoporous Silica Solid Dispersion |
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JI Jiabin, GE Haiyan, WANG Zichun, ZHAO Zaizhen, WANG Renliang
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School of Chemistry and Pharmaceutical Engineering, Taishan Medical University, Tai'an 271016, China
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| Abstract: |
| 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. |
| Key words: mesoporous silica zafirlukast solid dispersion dissolution |
