Ottawa Hospital Research Institute, Ottawa, Ontario K1H 8L6, Canada.
Clin Pharmacokinet. 2010 Jul;49(7):449-54. doi: 10.2165/11531820-000000000-00000.
Trans-resveratrol is a polyphenol, which is found in red wine and has cancer chemo-preventive properties and disease-preventive properties. The pharmacokinetics of trans-resveratrol have been investigated in single-dose studies and in studies with relatively low dosages. The present study aimed to investigate the steady-state pharmacokinetics and tolerability of trans-resveratrol 2000 mg twice daily with food, quercetin and alcohol (ethanol).
This was a two-period, open-label, single-arm, within-subject control study in eight healthy subjects. The steady-state 12-hour pharmacokinetics of trans-resveratrol 2000 mg twice daily were studied with a standard breakfast, a high-fat breakfast, quercetin 500 mg twice daily and 5% alcohol 100 mL. Trans-resveratrol plasma concentrations were determined using liquid chromatography with tandem mass spectrometry.
The mean (SD) area under the plasma concentration-time curve from 0 to 12 hours (AUC(12)) and maximum plasma concentration (C(max)) of trans-resveratrol were 3558 (2195) ng * h/mL and 1274 (790) ng/mL, respectively, after the standard breakfast. The high-fat breakfast significantly decreased the AUC(12) and C(max) by 45% and 46%, respectively, when compared with the standard breakfast. Quercetin 500 mg twice daily or 5% alcohol 100 mL did not influence trans-resveratrol pharmacokinetics. Diarrhoea was reported in six of the eight subjects. Significant but not clinically relevant changes from baseline were observed in serum potassium and total bilirubin levels.
Trans-resveratrol 2000 mg twice daily resulted in adequate exposure and was well tolerated by healthy subjects, although diarrhoea was frequently observed. In order to maximize trans-resveratrol exposure, it should be taken with a standard breakfast and not with a high-fat meal. Furthermore, combined intake with quercetin or alcohol did not influence trans-resveratrol exposure.
白藜芦醇是一种多酚，存在于红酒中，具有抗癌化学预防和疾病预防特性。白藜芦醇的药代动力学已在单剂量研究和相对低剂量的研究中进行了研究。本研究旨在研究每日两次与食物、槲皮素和酒精（乙醇）一起服用白藜芦醇 2000mg 的稳态药代动力学和耐受性。
这是一项在 8 名健康受试者中进行的两期、开放标签、单臂、自身对照研究。研究了每日两次标准早餐、高脂肪早餐、每日两次 500mg 槲皮素和 5%乙醇 100ml 时白藜芦醇 2000mg 的 12 小时稳态药代动力学。使用液相色谱-串联质谱法测定白藜芦醇的血浆浓度。
标准早餐后，白藜芦醇的平均（SD）0 至 12 小时血浆浓度-时间曲线下面积（AUC（12））和最大血浆浓度（C（max））分别为 3558（2195）ng*h/ml 和 1274（790）ng/ml。高脂肪早餐分别使 AUC（12）和 C（max）降低 45%和 46%。每日两次 500mg 槲皮素或 5%乙醇 100ml 不影响白藜芦醇的药代动力学。8 名受试者中有 6 名报告腹泻。与基线相比，血清钾和总胆红素水平有显著但无临床意义的变化。
每日两次 2000mg 白藜芦醇在健康受试者中具有足够的暴露量，且耐受性良好，尽管腹泻频繁发生。为了最大限度地提高白藜芦醇的暴露量，应在标准早餐时服用，而不是高脂肪餐时服用。此外，与槲皮素或酒精联合摄入不影响白藜芦醇的暴露量。
