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目的制备介孔二氧化硅微球,以期提高吲哚美辛的溶出速率。方法以表面活性剂十六烷基三甲基溴化铵和普兰尼克三嵌段共聚物P123作为双模板,用软膜板法制备具有介孔孔道的介孔二氧化硅微球药物载体,采用扫描电镜及氮气吸附-脱附手段表征载体形貌、比表面积及孔径分布。用吸附平衡挥干法载药制得吲哚美辛固体分散体,并对该固体分散体的溶出性质进行研究。结果制得的介孔二氧化硅载体由粒径相对均一的球形粒子组成。其粒径主要集中在2～5μm,载体的比表面积为502.87 m~2·g~(-1),孔容为2.23 cm~3·g~(-1),孔径为23.75 nm。吲哚美辛/介孔二氧化硅固体分散体的药物溶出速率与累积溶出度与吲哚美辛原料药相比均有了显著提高。结论吲哚美辛已高度分散于微球载体中,药物的溶出速率明显加快,为提高吲哚美辛生物利用度的研究打下了基础。
Objective To prepare mesoporous silica microspheres in order to improve the dissolution rate of indomethacin. Methods Mesoporous silica microspheres drug carrier with mesopores was prepared by soft membrane method using surfactant cetyltrimethylammonium bromide and pramonic acid triblock copolymer P123 as double template. Scanning electron microscopy and nitrogen adsorption - desorption means characterization of the carrier morphology, specific surface area and pore size distribution. The indomethacin solid dispersion was prepared by adsorption equilibrium dry-swinging method and the dissolution properties of the solid dispersion were studied. The resulting mesoporous silica support consisted of spherical particles with a relatively uniform particle size. The particle size was mainly in the range of 2 ~ 5μm. The specific surface area of the carrier was 502.87 m 2 · g -1, the pore volume was 2.23 cm -3 · g -1, and the pore size was 23.75 nm. The drug dissolution rate and cumulative dissolution of indometacin / mesoporous silica solid dispersions were significantly increased compared with that of indomethacin. Conclusion Indomethacin has been highly dispersed in the microspheres carrier, the dissolution rate of the drug significantly accelerated, and laid the foundation for the study of improving the bioavailability of indomethacin.