目的 制备白头翁皂苷D(PSD)固体分散体(PSD-SD),并评价其体内外释药行为.方法 采用溶剂法考察了不同载体材料对PSD溶解度的影响,采用红外光谱法(IR)、差示扫描量热法(DSC)以及X射线衍射法(XRD)表征了PSD-SD,采用溶出度和大鼠血药浓度变化评价了固体分散体体内外释药行为.结果 以PEG 6000为载体材料可使PSD在水中溶解度由2.39 mg/mL增大至7.06 mg/mL,制备的PSD-PEG 6000(1:6)PSD-SD 60 min药物累积释放率达到了90%,大鼠给药PSD-SD后其AUC_0～∞是原料药的2.24倍.结论 以PEG 6000为载体材料制备的PSD-SD可以增加PSD溶解度,有效地提高PSD溶出速率,有利于提高PSD生物利用度.

Objective To prepare the solid dispersion of Pulsatilla saponin D (PSD-SD) and evalution its in vivo and in vitro drug release behavior. Methods The PSD-SD was prepared by solvent method. Three carriers were used in the PSD-SD. Infrared spectroscopy (IR), differential thermal analysis (DSC), and X-ray diffraction (XRD) were used to determine the PSD-SD. Dissolution rates and pharmacokinetic parameters were evaluated in vitro and in vivo characteristics of the PSD-SD. Results When the PEG 6000 was used as carrier, the solubility of PSD was increased from 2.39 to 7.06 mg/mL, and the cumulative release rate of PSD reached 90% in 60 min, and the bioavailability of PSD was increased to 2.24 times. Conclusion The solid dispersion prepared PSD can increase the solubility, dissolution rate, and bioavailability.

江西省自然科学基金资助项目(20142BAB205082,20132BAB215031);江西省战略新型产业重点开发项目(2013AFC30031);江西中医药大学重点学科青年教师培养计划(2013jzzdxk045)