介孔二氧化硅微球的制备及用于吲哚美辛载药与溶出性质

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 m²·g2·g^(-1),孔容为2.23 cm(-1),孔容为2.23 cm³·g3·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。

Mesoporous silica microspheres preparation and used for indomethacin in medicine and dissolution of nature

Objective To prepare mesoporous silica microspheres and improve indomethacin dissolue rate. Methods Mesoporous silica microspheres was synthesized using Pluronic123 triblock polymer (P123) as a surfactant coupled with cetyltrimethyl ammonium bromide (CTAB)as a co-surfactant by the soft template. The mesoporous silica microspheres drug carrier which has mesoporous channels, the morphology, specific surface area and pore size distribution were studied by the scanning electron microscopy and the nitrogen adsorption /desorption. The indomethacin/mesoporous silica solid dispersion was prepared by evaporating solvent and filtering solvent, and the dissolution properties of IMCsolid dispersion were researched. Results The mesoporous silica carrier by particle size relatively homogeneous spherical particle composition. The particle size mainly concentrated in the 2-5 μm, with the carrier specific surface area of 502.87 cm². g^-1, volume of 2.23 cm³.g^-1 and pore diameter of 23.75 nm. The dissolution rate and cumulative dissolution degrees of indomethacin /mesoporous silica solid dispersion was dramatically improved compared with the pure drug. Conclusions Indomethacin is highly dispersed in silica microspheres drug carrier and its dissolution rate is accelerated significantly, which lay the foundation for the study of indomethacin bioavailability.