石榴皮提取物中鞣花酸和没食子酸在大鼠体内的药代动力学研究

Pharmacokinetic study of ellagic acid and gallic acid of Punica granatum L.husk extract in rats

目的研究石榴皮提取物中鞣花酸和没食子酸在大鼠体内的药代动力学特征。方法健康大鼠灌胃给予石榴皮提取物,收集不同时间的含药血浆,采用高效液相色谱法检测大鼠血浆中鞣花酸和没食子酸两种成分的血药浓度,运用Win Nonlin 5.2药动学软件拟合房室模型,计算其药动学参数。结果鞣花酸和没食子酸在大鼠体内均呈二室模型分布,鞣花酸和没食子酸的主要药动学参数分别为:半衰期速率常数T1/2(ka)=0.150、0.779 h,分布半衰期T1/2α=0.570、0.856 h,消除半衰期T1/2β=6.73、5.59 h,达峰时间Tmax=0.50、1.38 h,最大血药浓度Cmax=7.29、7.15μg/m L,分布相速率常数α=1.21、0.81 h-1,消除相速率常数β=0.103、0.124 h-1,吸收速率常数Ka=0.462、0.889 h-1。结论鞣花酸和没食子酸药动学特征为口服吸收、分布快、达峰时间短,石榴皮中没食子酸的吸收大于鞣花酸的吸收。

Objective To study the pharmacokinetic character of ellagic acid and gallic acid of pomegranate peel extract in rats. Methods After the rats were administered by pomegranate peel extract through ig, HPLC was used to determine the concentration of ellagic acid and gallic acid in blood plasma at different times, pharmacokinetic software Win Nonlin 5.2 was used to process concentration-time date. Results Ellagic acid and gallic acid were shown to be two room distribution model in rats, the main pharmacokinetic parameters of ellagic acid and gallic acid： T1/2（ka）=0.150, 0.779 h,T1/2α=0.570, 0.856 h, T1/2β=6.73, 5.59 h, Tmax=0.50, 1.38 h, Cmax=7.29, 7.15 μg/m L, α=1.21, 0.81 h-1, β=0.103, 0.124 h-1,Ka= 0.462, 0.889 h-1. Conclusion It indicates that the pharmacokinetic profile of ellagic acid and gallic acid are rapid absorption and distribution after oral administration pomegranate peel extraction, peak time is short, the absorption of gallic acid is greater than ellagic acid in pomegranate peel.