穿心莲内酯固体分散体的制备及体外溶出实验

Preparation of Andrographolide Solid Dispersion Systems and Their Dissolution Test in Vitro

目的应用固体分散体技术,以提高穿心莲内酯的体外溶出速率。方法采用溶剂法制备了含有不同比例表面活性剂吐温-80的穿心莲内酯-聚乙烯吡咯烷酮(PVPk30)固体分散体,采用正交实验优化固体分散体组成,并进行体外溶出;采用X射线衍射(XRD)与扫描电镜(SEM)分析了固体分散体中药物的分散状态。结果穿心莲内酯从固体分散体中溶出的速率明显增加,增加表明活性剂含量有利于药物的溶出;XRD与SEM结果表明,固体分散体中药物以无定形形式存在于载体中。结论以PVPk30为载体,并加入表面活性剂吐温-80制备穿心莲内酯固体分散体能有效地提高穿心莲内酯的溶出速率。

OBJECTIVE Solid dispersion technique was used for enhancing the dissolution rate of Andrographolide （Andro）. METHODS Andro PVP solid dispersions which contain different proportion Tween-80 were prepared by solvent method. The composing of solid dispersion was optimized using orthogonal design. The dissolution rate in vitro was studied in artificial gastric juice. Powder X-ray diffraction （XRD） and Scanning electron micrograph （SEM） were used to analyze the characteristics of Andrographolide in solid dispersions. RESULTS Andro release from solid dispersions was significantly increased and its dissolution rate was raised when the higher content of Tween-80 was used. It was demonstrated that drug in Andro solid dispersion was an amorphous form by XRD and SEM. CONCLUSION Andro solid dispersion and surfactant Tween-80 can obviously increase Andro dissolution rate.