[关键词]
[摘要]
目的 采用热熔挤出技术制备虎杖提取物(PCE)速释固体分散体(SD),以提高其有效成分的体外溶出度,并探索热熔挤出技术在中药提取物SD的制备适用性。方法 以丙烯酸树脂Eudragit EPO为载体,热熔挤出技术制备PCE-SD,以PCE中有效成分白藜芦醇和大黄素的体外溶出为评价指标,采用单因素试验对其制备工艺进行优化,并采用差示扫描量热法(DSC)、X射线衍射法(XRD)、傅里叶变换红外光谱法(FTIR)和扫描电子显微镜(SEM)法对最佳SD进行表征。结果 最佳制备工艺:螺杆转速为120 r/min,机筒温度为160℃,冷却方法为液氮冷却。在优化条件下制备的PCE-SD,白藜芦醇和大黄素的溶出度均有显著提高,PCE以无定形态分散在载体中。结论 热熔挤出技术可制备PCE速释SD,提高其有效成分白藜芦醇和大黄素的溶出度,为采用热熔挤出技术制备中药复方SD的研究提供了一定的数据支持和实验参考。
[Key word]
[Abstract]
Objective To prepare solid dispersions (SD) of Polygonum cuspidatum extract (PCE) with the intention of improving the dissolution rate of its active ingredients in vitro and exploring the applicability of hot melt extrusion in SD of traditional Chinese medicine extract. Methods The SD of PCE were prepared via hot melt extrusion based on Eudragit EPO. The cumulative dissolution of resveratrol and emodin in the extract of PCE was used as an evaluation index, and the single factor experiment was optimized. Then physicochemical properties of the SD prepared by optimized process were investigated by differential scanning calorimetry (DSC), powder X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FTIR), and scanning electron microscope (SEM). Results The optimized process was 120 r/min for screw speed, 160℃ for barrel temperature and liquid nitrogen cooling. Under the optimized conditions, the dissolution rate of resveratrol and emodin in the extract was significantly improved, and the drug was present in the amorphous state in the carrier. Conclusion Hot melt extrusion can prepare SD of PCE to improve the dissolution rate of resveratrol and emodin, which provided experimental reference and data support for the study of preparation of SD of traditional Chinese medicine by hot melt extrusion.
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[基金项目]
国家自然科学基金资助项目(30801552,81274095);江苏省中药资源产业化过程协同创新中心第三批立项资助重点项目(012092002006-10);第55批博士后课题(021062001001)