橙皮素在大鼠体内的吸收机制

Study on the absorption mechanism of hesperetin in rat

目的探讨维拉帕米对橙皮素血浆浓度与肝脏分布的影响,揭示橙皮素的吸收机理。方法将大鼠随机分为3组,第1组灌胃橙皮素的0. 5%羧甲基纤维素钠溶液,第2组灌胃橙皮素和维拉帕米的0. 5%羧甲基纤维素钠溶液,第3组作为对照组,给药后于1、2、4 h三个时间点,取血浆及肝脏,经处理后,用HPLC测定药物的含量。结果维拉帕米+橙皮素组与橙皮素组的血药浓度与肝脏含药量存在显著性差异。结论橙皮素以缀合物被吸收,且以原型在肝脏分布,维拉帕米可显著提高橙皮素的吸收及肝脏分布量。维拉帕米抑制p-糖蛋白从而抑制橙皮素外排是其促进吸收的原因之一。

OBJECTIVE To investigate the effect of Verapamil on the plasma concentration and liver distribution of hesperetin and to reveal its absorption mechanism.METHODS The rats were randomly divided into 3 groups.Group 1 was given 0.5%sodium carboxymethylcellulose solution containing hesperidin,and group 2 was given 0.5%of sodium carboxymethylcellulose solution containing hesperidin and Verapamil.The third group served as a control group was given 0.5%of sodium carboxymethylcellulose solution.Plasma and liver samples were taken 1,2,4 h after administration,and the drug content of samples were determined by HPLC after a series of treatment.RESULTS There was a significant difference in plasma concentration and liver content between Verapamil plus hesperetin group and hesperetin group.CONCLUSION Hesperetin is absorbed by mean of its conjugates and distribute in the liver in free-types.Verapamil promotes the absorption of hesperetin and the distribution of it in liver.Inhibition of p-glycoprotein by Verapamil hence the inhibition of the efflux of hesperetin is one of the explanation.