姜黄素磷脂复合物壳聚糖微球在大鼠体内药动学研究

In vivo pharmacokinetics of curcumin-phospholipid complex-chitosan microspheres in rats

目的比较姜黄素磷脂复合物壳聚糖微球、姜黄素磷脂复合物、姜黄素壳聚糖微球、姜黄素原料药的药动学特征,探讨磷脂复合物壳聚糖微球药物载体的优势。方法 SD大鼠ig给予4种姜黄素制剂100 mg/kg(以姜黄素计)后,定时取血,以大黄素为内标,乙腈-2%醋酸水溶液(55∶45)为流动相,HPLC法检测姜黄素血药浓度,绘制药-时曲线,DAS程序计算药动学参数。结果姜黄素脂复合物壳聚糖微球的tmax、t1/2分别为2.0、3.2 h,较原料药(0.6、1.2 h)、壳聚糖微球(1.4、2.3 h)、磷脂复合物(1.2、1.7 h)均有所延长;曲线下面积(AUC)分别为原料药、壳聚糖微球、磷脂复合物的7.49、2.07、2.67倍。结论磷脂复合物壳聚糖微球较单一的磷脂复合物或壳聚糖微球更能延缓药物释放,促进药物吸收,是半衰期短、溶解度低药物的优良口服给药载体。

Objective To compare the in vivo pharmacokinetics of curcumin-phospholipid complex-chitosan microspheres（Cur-PLC-CM）,Cur-PLC,Cur-CM,and crude drug of Cur,and to discuss the advantage of PLC-CM as carrier.Methods SD rats were ig administered with the above four preparations 100 mg/kg（corresponding to Cur）,respectively.Then blood samples were obtained at certain time points.The concentration of Cur in blood was analyzed by HPLC method using emodin as internal standard.The mobile phase was acetonitrile-2% acetic acid（55∶45）.Concentration-time curve was drawn and the data were analyzed by DAS program.Results The tmaxand t1/2of Cur-PLC-CM were 2.0 and 3.2 h,respectively,which were much longer than those of crude drug（0.6 and 1.2 h）,Cur-CM（1.4 and 2.3 h）,and Cur-PLC（1.2 and 1.7 h）.The AUC of Cur-PLC-CM was 7.49,2.07,and 2.67 times as those of crude drug,Cur-CM,and Cur-PLC.Conclusion The PLC-CM have better sustained-releasing and absorption property than CM and PLC,which may have a great potential to be used as oral delivery system for the low solubility and short half-life drug.