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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 increase the release rate and bioavailability of nimesulide. Methods Polyethylene glycol (PEG), polyvinylpyrrolidone (PVP k30) and poloxamer 188 were used as carriers to prepare nimesulide solid dispersions by melt method, solvent method and solvent-melting method, respectively. The effect of drug-drug mass ratio on drug release was evaluated by differential scanning calorimetry (DSC) and scanning electron microscopy (SEM). Results Nimesulide exists in amorphous state in the solid dispersion, with different carrier types, different carrier-drug mass ratios, and different degrees of drug release. Conclusion The solid dispersion of nimesulide can significantly increase the in vitro release of nimesulide.