葛根7,4′-二氧代醋酸黄豆苷元在大鼠体内的药物动力学研究

Pharmacokinetic study on 7,4'-oxo-acetic acid daidzein in rats

目的研究葛根 7,4′ 二氧代醋酸黄豆苷元 (DZC)大鼠体内药物动力学特征。方法采用不同途径给大鼠注射 3种剂量 (1 5、2 5、3 5mg·kg-1)药物 ;大鼠灌胃给药 (1 2 0mg·kg-1) ,分别测定大鼠体内药动学参数。结果大鼠注射DZC ,其药时过程符合二室开放模型特征 ,其t1/2 ( β) 分别为(4 2 65± 9 3 4)、(4 6 96± 5 5 9)、(82 1 8± 2 8 1 7)min,大鼠静脉注射 1 5、2 5mg·kg-1后 ,其药时过程符合线性动力学 ,但静注 3 5mg·kg-1后为非线性动力学。大鼠灌胃给药后 ,其药时过程符合单室开放 -吸收模型特征。大鼠经灌胃、颈静脉交叉给药后 ,绝对生物利用度为 3 8 66%。结论DZC口服生物利用度提高不显著 ,适于静脉给药。

Objective To study the pharmacokinetic characteristic of 7,4′-oxo-acetic acid daidzein (DZC) in rats. Method The drug was administrated to the rats crossly by the jugular vein injection of 3 doses (15,25 and 35 mg·kg -1 )and intragastic administration ( 120 mg·kg -1 ).Result The experimental results showed that the concentration-time of DZC in rats after iv of 15,25 and 35 mg·kg -1 were shown to fit a two-compartment open model with half-lives of (42.65±9.34),(46.96±5.59) and (82.18±28.17)min,respectively.At the doses of 15 and 25 mg·kg -1 the elimination of the DZC from plasma was found to be in accord with linear kinetics but when the dosage was 35 mg·kg -1 ,a non-linear kinetics was observed.The concentration-time curve of DZC in rats fit one-compartment open model with first-order absorption after oral administration.The absolute availability by intragastric administration was 38.66%.Conclusion There is no significant elevation of oral administration,DZC fits the vein injection.