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目的制备螺内酯固体分散体,提高其体外溶出。方法分别以亲水性高分子材料聚乙烯己内酰胺-聚醋酸乙烯酯-聚乙二醇接枝共聚物和乙烯吡咯烷酮-醋酸乙烯酯共聚物为载体,采用热熔挤出技术制备螺内酯固体分散体,以有关物质、体外溶出为指标,筛选、优化处方及工艺,并应用差示扫描量热法、X射线衍射法、红外光谱法、偏振光显微镜表征最优固体分散体。结果采用热熔挤出技术可以制备螺内酯固体分散体;最优处方中,螺内酯以分子或无定型状态分散于载体中;固体分散体显著提高了螺内酯在水中的溶出。结论热熔挤出技术制备的固体分散体显著地提高了螺内酯的体外溶出。
Objective To prepare spironolactone solid dispersion and improve its dissolution in vitro. Methods Polyethylene caprolactam - polyvinyl acetate - polyethylene glycol graft copolymer and vinylpyrrolidone - vinyl acetate copolymer were used as carriers respectively, and the solid dispersion of spironolactone was prepared by hot melt extrusion. The relevant substances and in vitro dissolution as an indicator, screening, optimization of prescription and process, and the application of differential scanning calorimetry, X-ray diffraction, infrared spectroscopy, polarization microscopy characterization of the optimal solid dispersion. Results The spironolactone solid dispersion was prepared by hot melt extrusion. In the optimal formulation, the spironolactone was dispersed in the carrier in molecular or amorphous state. The solid dispersion significantly increased the dissolution of spironolactone in water. Conclusion The solid dispersions prepared by hot melt extrusion significantly improve the dissolution of spironolactone in vitro.