Effect of Food on Pharmacokinetics of Catechin in Chinese Healthy Volunteers

目的 研究饮食对中国健康受试者口服儿茶素代谢动力学的影响.方法 采用单次摄取、随机、开放标签、交叉分组设计法,洗脱期为7 d.20名中国健康受试者在空腹或伴餐条件下摄取1瓶绿茶饮料(含儿茶素600 mg),24 h内分别在受试前和受试后不同时间点采集静脉血样,采用高效液相色谱结合电化学检测器(HPLC-ECD)测定血浆中的游离态和总儿茶素浓度,计算代谢动力学参数并进行比较.结果 伴餐状态下,游离态和总EGCG、ECG的AUC、Cmax均显著降低(P<0.01).总EC、EGC的AUC、Cmax有一定程度上升(P<0.05).结论 食物会显著降低没食子酸酯型儿茶素的吸收,对非没食子酸酯型儿茶素的吸收和代谢有一定促进作用.Objective To investigate the influence of food on the pharmacokinetics of catechin in healthy Chinese volunteers.Methods In a single dose, randomized, open-label, two-way crossover study with 7 days of washout, 20 volunteers consumed a bottle of green tea beverage containing 600 mg catechin with or without a standard food. Venous blood samples were collected at different time points during 24 hours before and after drinking. Plasma free and total catechin levels were analyzed by HPLC with electrochemical detection (HPLC-ECD). The pharmacokinetic parameters were calculated and compared.Results AUC and Cmax of free and total EGCG, ECG were significantly reduced (P<0.01) when catechin was taken with food. In contrast,AUC and Cmax of total EC and EGC increased to some extent (P<0.05).Conclusion Simultaneous ingestion of food significantly reduced the absorption of galloylated catechin and played a role in promoting the absorption and metabolism of non-galloylated catechin.国家自然科学基金资助项目11-71