尼美舒利固体分散体的制备及其性质考察

Preparation and evaluation of nimesulide solid dispersion

目的提高尼美舒利释放速率及生物利用度。方法分别以聚乙二醇(PEG)、聚乙烯吡咯烷酮(PVP k30)及泊洛沙姆188为载体,采用熔融法、溶剂法及溶剂-熔融法等制备尼美舒利固体分散体;考察载体类别及载体-药物质量比对释放的影响;配合差示扫描量热(DSC)分析与电子扫描电镜(SEM)观察考察药物在载体中的存在状态。结果尼美舒利以无定型状态存在于固体分散体中,载体类别不同、载体-药物质量比不同,药物的释放度不同。结论将尼美舒利制成固体分散体能显著增加尼美舒利的体外释放度。

Objective To prepare and identify nimesulide solid dispersion, and determine its dissolution property. Methods The hot melt, solvent and solvent-hot melt methods, with several different cartier materials （PEG, PVP k30 and Poloxamer 188 ）, were used for preparation and differential scanning calorimetry （DSC） and scanning electron microscopy （SEM） for identification of nimesulide solid dispersion. The dissolution of the dispersion was determined with paddle method. Results The study showed that nimesulide in solid dispersion could be dispersed in carriers materials with amorphous stabilities. Conclusions The dissolution of nimesulide is increased by solid dispersion method.