西洛他唑/介孔碳固体分散体的制备及体外溶出性质的考察

目的为了提高难溶性药物西洛他唑的溶出度,制备西洛他唑/介孔碳固体分散体。方法以表面活性剂F127为胶束模板,以酚醛树脂的乙醇溶液为碳源制备介孔碳,选用西洛他唑作为模型药,采用吸附平衡挥干法和溶液吸附法载药制得西洛他唑固体分散体,采用扫描电镜、氮气吸附-脱附和热分析手段表征介孔碳及西洛他唑/介孔碳固体分散体的性质。结果制得的介孔碳孔径均一,其孔径主要集中在6.3 nm,载体的比表面积为1 255.4 m2.g-1,孔容为1.441 cm3.g-1,载体的载药质量可高达33.1%,溶出数据表明西洛他唑/介孔碳固体分散体的溶出速率与累积溶出度与药物西洛他唑相比均有了显著提高。结论介孔碳有望成为能提高难溶性药物溶出度的优良载体。

Preparation of cliostazol-mesoporous carbon solid dispersion and the preliminary study in vitro release

Objective To improve the water-insoluble drug cilostazol(CLT) dissolution via the preparation of the cilostazol-mesoporous carbon solid dispersion.Methods The mesoporous carbon was obtained using Pluronic block co-polymer F127 as template and ethanol solution of resols as the carbon souse by the soft template.The morphology,specific surface area and pore size distribution were studied by the scanning electron microscopy and the nitrogen adsorption/desorption.The cilostazol/mesoporous carbon solid dispersion was prepared by evaporating solvent and filtering solvent,respectively.Though differential scanning calorimetry and the dissolution experiment,the basic properties of cilostazol solid dispersion were researched.Results The mesoporous carbon was showed on SEM images.The pore size was focused on 6.7 nm.The specific surface area was reaching up to 1 255.4 m2 · g-1 and the volume of 1.441 cm3 · g-1.The dissolution of cilostazol was dramatically improved compared with the pure drug.Conclusions Mesoporous carbon is expected to become the prospect of water-insoluble drug carrier.