蒙花苷磷脂复合物的制备及其药动学评价

Buddleoside-phospholipids Complex: Preparation and Pharmacokinetic Evaluation

目的制备蒙花苷磷脂复合物,研究其药动学性质。方法溶剂挥发法制备蒙花苷磷脂复合物,以复合率为评价指标,通过正交试验优化制备工艺。SD大鼠灌胃给予蒙花苷磷脂复合物,HPLC测定蒙花苷的血药浓度。结果采用优化后的磷脂复合物制备工艺,复合率接近100%。X射线衍射结果表明蒙花苷以无定型状态存在于磷脂复合物中,在水和正辛醇中的表观溶解度显著增大。药动学结果显示,蒙花苷磷脂复合物的tmax,Cmax,AUC0-t等参数与蒙花苷原料药相比具有显著性差异,口服吸收生物利用度提高1.11倍。结论磷脂复合物改善了蒙花苷的溶解性质,口服吸收生物利用度得到明显提高。

OBJECTIVE To prepare buddleoside-phospholipids complex,and then investigate its pharmacokinetic properties.METHODS The buddleoside-phospholipids complex was prepared by solvent evaporation method,and the compounding rate was used as the evaluation index.The preparation process was optimized by orthogonal experiment.After SD rats were administrated with drugs,the blood concentration of buddleoside was detected by HPLC.RESULTS The recombination ratio of buddleoside-phospholipids complex was near to 100%under the optimized preparations.The results of X-ray diffraction indicated that buddleoside showed an amorphous state in the complex.The solubility in water and octanol was enhanced greatly.Pharmacokinetic results in SD rats showed that the tmax,Cmax,AUC0-t and other parameters of the complex has significant difference compared to buddleoside suspension.The bioavailability of buddleoside was enhanced to 1.11 times by the complex.CONCLUSION The phospholipids complex improved the solubility property of buddleoside,and the oral bioavailability of buddleoside was improved significantly.