姜黄素磷脂复合物的药代动力学评价

Pharmacokinetics evaluation of curcumin-phospholipid complex

目的通过对大鼠口服灌胃给药,评价姜黄素磷脂复合物在SD大鼠体内的药物代谢动力学性质。方法制备姜黄素磷脂复合物,以姜黄素作为对照,检测两者在水中的溶解度和体外累计溶出率;取SD大鼠12只,经口服灌胃给予姜黄素磷脂复合物或姜黄素混悬液后,不同时间点于大鼠眼底静脉丛取血,采用高效液相色谱法(HPLC)测定血浆中姜黄素的浓度。结果姜黄素磷脂复合物的溶解度、累计溶出率分别为0.150g/L、68.04%,较姜黄素(0.057g/L、50.68%)均有所增加。姜黄素磷脂复合物和姜黄素的药代动力学参数分别如下:Cmax为(74.34±5.57)μg/L和(61.64±4.29)μg/L,Tmax为(0.17±0)h和(0.25±0)h,AUC0-t为(637.38±30.04)μg·h·L-1和(172.41±31.66)μg·h·L-1,AUC0-∞为(857.80±223.69)μg·h·L-1和(191.08±43.27)μg·h·L-1。日内及日间精密度、回收率符合测定要求。结论姜黄素磷脂复合物混悬液与姜黄素相比吸收速度快,消除速率慢。

Objective To evaluate the pharmacokinetics of curcumin phospholipid complex（CCPC）in rats following oral administration.Methods Blood samples were collected from the retinal venous plexus of SD rats after oral administration of CCPC or curcumin（CC）,and the blood concentration of curcumin was determined by high-performance liquid chromatography（HPLC）.Results The solubility and cumulative dissolution of CCPC（0.150g/L and 68.04%,respectively）were higher than those of CC（0.057g/L and 50.68 %,respectively）.The pharmacokinetic parameter of CCPC and CC were calculated as follows：Cmax（74.34±5.57）μg/L and（61.64±4.29）μg/L,Tmax（0.17±0）h and（0.25±0）h,AUC0-t（637.38±30.04）μg·h·L-1 and（172.41±31.66）μg·h·L-1,and AUC0-∞（857.80±223.69）μg·h·L-1 and（191.08±43.27）μg·h·L-1,respectively.The intra-day,inter-day precision,and recovery rate met the criteria for content determination.Conclusion Compared with curcumin,CCPC can be absorbed more rapidly and eliminated more slowly.