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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、139.70μg·min/m L。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。
Objective To prepare polydatin (PD) solid dispersion (SD) in order to improve the bioavailability of PD. Methods PD-SD was prepared by solvent evaporation method using dissolution as an index. The structure of PD-SD was studied by Fourier transform infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC), powder X-ray diffraction (XRD) and scanning electron microscopy SEM) to characterize PD-SD. The plasma concentration of rat after ig administration was determined by HPLC. Results The in vitro dissolution of PD-SD was significantly higher than that of PD. FT-IR showed no new chemical bond between the drug and the carrier. The DSC and XRD results showed that the PD existed in amorphous form in the carrier. SEM results showed that the prepared PD -SD appearance of irregular spherical shape. After ig administration, the area under the curve (AUC0-∞) of PD-SD and PD were 328.79 and 139.70 μg · min / m L, respectively. Conclusion PD-SD by solvent evaporation is simple and feasible. PD-SD can significantly improve the bioavailability of PD.