目的:制备并表征丹皮酚固体分散体,绘制体外多条溶出曲线并分析体外溶出特性。方法:采用熔融法制备固体分散体,以溶出度为评价指标优化丹皮酚固体分散体制备工艺;采用电镜扫描分析(SEM)、差示扫描量热分析(DSC)、X-射线衍射分析(XRD)与傅里叶红外扫描分析(FTIR),对其理化性质进行制剂学表征;绘制体外多条溶出曲线,进行溶出动力学方程拟合。结果:最优处方工艺为以PEG4000∶PEG6000(2∶1)为基质,丹皮酚与基质比例为1∶9;SEM、DSC及XRD分析显示丹皮酚由晶型态转变为无定型态或分子态存在,FTIR分析显示丹皮酚化学结构未发生改变;体外多条溶出曲线基本重合且均具有较好的溶出行为,20 min时各组溶出均超95%,接近溶出完全,且各组累积溶出度RSD为1.89%,溶出行为符合一级动力学方程,拟合相关性系数r均高于0.99。结论:丹皮酚固体分散体可明显改善丹皮酚在水系环境的溶出度,且具有很好的溶出适应性,为提高生物利用度奠定了制剂基础。

Objective:To prepare and characterize a solid dispersion of paeonol,to map multiple dissolution curves in vitro and to analyze the dissolution characteristics in vitro. Methods:Solid dispersions were prepared by melt method,and the preparation process of paeonol solid dispersion was optimized with dissolution rate as the evaluation index. Scanning electronic microscopy(SEM),differential scanning calorimetry(DSC),X-ray diffraction(XRD) analysis and Fourier transform infrared spectroscopy(FTIR) were applied to characterize the physicochemical properties. Multiple dissolution curves in vitro were drawn to fit the dissolution kinetic equation. Results:The optimal formulation process was PEG4000∶PEG6000(2∶1). The ratio of paeonol to matrix was 1∶9. SEM,DSC and XRD analysis showed that paeonol changed from crystalline to amorphous or molecular state. FTIR analysis showed that there was no change of the chemical structure of paeonol.The multiple dissolution curves in vitro were basically coincident with good dissolution behavior. After 20 minutes,the dissolution of each group was over95%,close to complete dissolution. Besides,the cumulative dissolution RSD of each group was1.89%,the dissolution behavior was in accordance with the first-order kinetic equation,and the fitting correlation coefficient r was higher than 0.99. Conclusion:The solid dispersion of paeonol can significantly improve the dissolution of paeonol in the aqueous environment,and has a good dissolution adaptability. This study has laid a foundation for the improvement of bioavailability.