基于共聚维酮的丹参酮ⅡA固体分散体的研究

目的:将共聚维酮(PVP-S630)应用于丹参酮ⅡA(TSⅡA)固体分散体的制备,以提高药物的体外溶出度降低固体分散体的吸湿性.方法:采用喷雾干燥法制备丹参酮ⅡA固体分散体,运用差示扫描量热法(DSC)、扫描电镜法(SEM)、X-射线粉末衍射法(XRD)等分析方法对其物相进行表征,考察其溶出行为、吸湿特性、稳定性.结果:丹参酮ⅡA和共聚维酮按1:10比例所制备的固体分散体,丹参酮ⅡA以非晶型分散于载体表面,0.5h体外溶出度可达100％,吸湿性低于同比例制备的聚维酮(PVP-K30)固体分散体,经过3个月稳定性加速试验后,其药物溶出度和含最未发生显著性变化.结论:共聚维酮作为载体制备的固体分散体能显著改善丹参酮ⅡA的溶出,引湿性相对较低,稳定性好,具有应用前景.

Study on solid dispersion of copovidone-based tanshinone IIA

Objective: To apply PVP-S630 in the preparation of tanshinone II_A (TS II_A) solid dispersion, in order to improve its dissolution in vitro and reduce the moisture absorption of the solid dispersion. Method: Tanshinone II_A solid dispersion was prepared by spray drying method.Such analytical methods as SEM, DSC, XRD were used to characterize their phases and detect their dissolution, moisture absorption and stability. Result: In the solid dispersion prepared with tanshinone II_A and copovidone with proportion of 1:10, tanshinone II_A was scattered on the surface of the carrier in the amorphous form, with a dissolution in vitro up to 100% at 0.5 h and a lower moisture absorption than PVP-K30 solid dispersion prepared with the same proportion.After a three-month accelerated stability test, it showed no significant change in drug dissolution and content. Conclusion: The solid dispersion prepared with copovidone as the carrier can significantly improve the dissolution of tanshinone II_A, with a relatively low moisture absorption and high stability, thereby having a good prospect of application.