[关键词]
[摘要]
目的 探索丹参酮ⅡA喷雾干燥粉体的药剂学性质。方法 采用喷雾干燥法处理丹参酮ⅡA,并运用比表面积测定法(BET)、扫描电镜法(SEM)、差示扫描量热法(DSC)和X射线粉末衍射法(XRD)等方法对丹参酮ⅡA粉体进行分析,考察其体外溶出度和稳定性。结果 BET结果显示经喷雾干燥处理后的丹参酮ⅡA具有较窄的粒径分布范围及较大的比表面积;XRD和DSC分析结果显示部分丹参酮ⅡA已转变为非晶形式;在8 h丹参酮ⅡA的累积溶出度为85.2%。结论 喷雾干燥方法处理丹参酮ⅡA有利于提高药物体外溶出度,为难溶性药物口服给药制剂的设计提供参考。
[Key word]
[Abstract]
Objective To explore a method to improving the in vitro dissolution of tanshinone ⅡA spray drying powder and to study its pharmceutical properties. Methods Tanshinone ⅡA was processed with spray drying method and analyzed by determination of the specific surface area (BET), scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and X-ray powder diffraction (XRPD). And in vitro dissolution and drug stability were also investigated. Results The BET results showed that tanshinone ⅡA powder after spray drying had narrow particle size distribution range and large specific surface area; XRD and DSC analyses showed that most drug was transformed into amorphous form. The in vitro dissolution achieved 85.2% within 8 h. Accelerating experiment showed that the in vitro dissolution of tanshinone ⅡA decreased by approximately 21% stored for 6 months. Conclusion The drug dissolution is improved by spray-drying method. It provides a reference for the research and development of poorly soluble pharmaceutical preparations for oral administration.
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[基金项目]
国家自然科学基金资助项目(81274088)