尼群地平固体分散体的制备与评价

Preparation and Evaluation of the Nitrendipine Solid Dispersion

目的:制备固体分散体以提高尼群地平的溶出度。方法:采用单因素法,以溶出度为评价指标优化固体分散体制备工艺。以气相二氧化硅为载体,采用超临界CO2浸渍方法制备尼群地平固体分散体。采用差示扫描量热法(DSC)对制备的固体分散体进行表征,同时采用900 mL的0.1 mol·L^-1盐酸溶液-乙醇(70∶30)为溶出介质,测定固体分散体的溶出度。结果:DSC的测定结果表明,在尼群地平固体分散体中,尼群地平以无定形状态存在。体外溶出试验结果表明,尼群地平固体分散体的溶出度明显高于尼群地平原料药。结论:超临界CO2浸渍方法制备固体分散体操作简单方便,能明显提高尼群地平的溶出度。

Objective:A solid dispersion was prepared to increase the dissolution of nitrendipine.Methods:The processing parameters were optimized by using single factor method.The supercritical CO 2 technology was used to prepare the nitrendipine solid dispersion;and the silica was selected as the carrier.Differential scanning calorimetry(DSC)was used to characterize the prepared solid dispersion.At the same time,900 mL of 0.1 mol·L^-1 hydrochloric acid solution-ethanol(70∶30)was used as the dissolution medium to determine the dissolution of the solid dispersion.Results:DSC measurement results showed that in the solid dispersion of nitrendipine,nitrendipine existed in an amorphous state.The results of in vitro dissolution tests showed that the dissolution rate of the solid dispersion of nitrendipine was significantly higher than that of nitrendipine API.Conclusion:The supercritical CO 2 impregnation method is simple and convenient to prepare solid dispersions,and can significantly improve the dissolution of nitrendipine.