茶儿茶素的口服吸收与生物利用度。

Oral absorption and bioavailability of tea catechins.

作者信息

Zhu M, Chen Y, Li R C

机构信息

Department of Pharmacy, Chinese University of Hong Kong, Shatin, N.T., Hong Kong.

出版信息

Planta Med. 2000 Jun;66(5):444-7. doi: 10.1055/s-2000-8599.

Abstract

The absorption characteristics and oral bioavailability of three tea catechins, namely (-)-epicatechin (EC), (-)-epicatechin gallate (ECG), and (-)-epigallocatechin gallate (EGCG), were assessed in this study. Male Sprague Dawley rats (210-230 g) received either an intravenous (i.v. 50 mg/kg) or oral (5000 mg/kg) dose of decaffeinated catechin-fraction containing EC (5%), EGCG (50%), and ECG (13%). Concentrations of the compounds in plasma, urine, and feces were measured using HPLC. A non-compartmental approach was employed for pharmacokinetic analysis. Results indicated that maximum plasma concentrations for the catechins (15-112 micrograms/ml) were achieved at 2 h post-oral dosing and the apparent volume of distribution (Vd/F) ranged from 30 to 63 l/kg. Absolute bioavailability (F) of EC, EGCG, and ECG was assessed to be 0.39, 0.14, and 0.06, respectively. Estimates of terminal elimination half-life (t1/2, lambda z) of the catechins after oral dosing were 451-479 min and were 1.4-10 fold longer than those observed for the i.v. dosing. The discrepancy in terminal elimination and low rate and extent of absorption indicated the possibility of flip-flop kinetics. Respective urinary recoveries were 0.17-4.72% and 2.11-14.2% after oral and i.v. dosing. In conclusion, the low systemic availability of tea catechins observed could be a result of slow absorption, high first pass effect, and wide tissue distribution.

摘要

本研究评估了三种茶儿茶素,即(-)-表儿茶素(EC)、(-)-表儿茶素没食子酸酯(ECG)和(-)-表没食子儿茶素没食子酸酯(EGCG)的吸收特性和口服生物利用度。雄性Sprague Dawley大鼠(210 - 230 g)接受静脉注射(i.v. 50 mg/kg)或口服(5000 mg/kg)含EC(5%)、EGCG(50%)和ECG(13%)的脱咖啡因儿茶素组分剂量。使用高效液相色谱法(HPLC)测量血浆、尿液和粪便中化合物的浓度。采用非房室方法进行药代动力学分析。结果表明,口服给药后2小时达到儿茶素的最大血浆浓度(15 - 112微克/毫升),表观分布容积(Vd/F)范围为30至63升/千克。EC、EGCG和ECG的绝对生物利用度(F)分别评估为0.39、0.14和0.06。口服给药后儿茶素的末端消除半衰期(t1/2,lambda z)估计为451 - 479分钟,比静脉注射给药时观察到的长1.4 - 10倍。末端消除的差异以及低吸收速率和程度表明存在反翻转动力学的可能性。口服和静脉注射给药后各自的尿回收率分别为0.17 - 4.72%和2.11 - 14.2%。总之,观察到的茶儿茶素全身利用率低可能是吸收缓慢、首过效应高和组织分布广泛的结果。

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