[关键词]
[摘要]
目的 制备白藜芦醇苷(PD)固体分散体(SD),以期提高PD的生物利用度。方法 以溶出度为指标,采用溶剂蒸发法制备PD-SD,利用傅里叶变换红外光谱(FT-IR)、差示扫描量热分析(DSC)、粉末X衍射(XRD)和扫描电子显微镜(SEM)对PD-SD进行表征。采用HPLC法测定大鼠ig给药后的血药浓度。结果 PD-SD的体外溶出度较PD明显提高,FT-IR显示药物与载体间没有形成新的化学键,DSC和XRD结果显示PD在载体中以无定型的形式存在,SEM结果表明制备成的PD-SD外观形态为不规则球形。ig给药后,PD-SD和PD的药时曲线下面积(AUC0-∞)分别为328.79、139.70 μg·min/mL。结论 溶剂蒸发法制备PD-SD工艺简单可行,PD-SD能显著提高PD的生物利用度。
[Key word]
[Abstract]
Objective Polydatin solid dispersion (PD-SD) was prepared for improving bioavailability. Methods In this study, PD-SD was prepared by solvent evaporation method with dissolution as index for improving bioavailability. The physicochemical properties of PD-SD were evaluated by Fourier transform infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC), X-ray power diffraction (XRD), and scanning electron microscope (SEM). HPLC was employed to determine the plasma concentration of PD-SD with PD crude drug as reference group in rats after oral administration. Results FT-IR revealed that there was no new chemical bond between drug and carrier. DSC and XRD results indicated that PD in PD-SD was amorphous. SEM results showed that the morphology of PD-SD was close to irregular globular. The AUCs of PD-SD and PD were 328.79 and 139.70 μg·min/mL after oral administration, respectively. Conclusion PD-SD is prepared by simple technology. PD-SD significantly improved the in vitro dissolution and oral bioavailability of PD in rats.
[中图分类号]
[基金项目]
国家自然科学基金项目(51303006);安徽省自然科学基金项目(1408085MH196,KJ2012ZD09);安徽中医药大学教学研究项目(2014xjjy025,2013xjzc014)