The flavanol epigallocatechin gallate (EGCG) is being tested for the treatment of several diseases in humans. However, its bioavailability and pharmacokinetic profile needs a better understanding to enable its use in clinical trials. There is no consensus on the most appropriate concentration of EGCG in the body to obtain the maximum therapeutic effects. Therefore, the aim of this study is to analyze the bioavailability of EGCG orally administered alone or with different food supplements after overnight fasting in order to determine its optimal conditions (high concentrations in blood and the lowest interindividual variations) to be used as a pharmacological tool in human trials. Ten healthy volunteers (5 men and 5 women) aged 25 to 35 years were recruited prospectively. Three series of clinical experiments with a washout period of seven days among each were performed: 1) Teavigo® (EGCG extract) alone, 2) Teavigo® with a standard breakfast, and 3) FontUp® (Teavigo® commercially prepared with fats, carbohydrates, proteins, vitamins, and minerals). Blood samples were collected at 0, 30, 60, 90, 120, 180, 240, and 360 min after EGCG intake. Free EGCG in plasma was measured using a liquid chromatography and mass spectrometry UPLC-ESI-MS/MS analytical method. The pharmacokinetic variables analyzed statistically were area under the curve (AUC0-360), Cmax, Cav, Cmin, T1/2, and Tmax,. EGCG (Teavigo®) alone was the group with higher AUC0-360, Cmax, and Cav both in men (3.86 ± 4.11 µg/mL/kg/6 h; 5.95 ng/mL/kg; 2.96 ng/mL/kg) and women (3.33 ± 1.08 µg/mL/kg/6 h; 6.66 ng/mL/kg; 3.66 ng/mL). Moreover, FontUp® was the group with the highest value of T1/2 both in men (192 ± 66 min) and women (133 ± 28 min). Teavigo® intake after fasting overnight revealed the highest concentration of EGCG in plasma according to its pharmacokinetic profile, indicating that this is an excellent alternative of administration if the experimental design requires good absorption in the gastrointestinal tract. Moreover, EGCG taken along with food supplements (FontUp®) improved the stability of the molecule in the body, being the best choice if the experimental design wants to reduce interindividual variation.

中文翻译：

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表没食子儿茶素没食子酸酯在健康志愿者中采用不同营养策略的生物利用度。

黄烷醇表没食子儿茶素没食子酸酯 (EGCG) 正在测试用于治疗人类多种疾病。然而，需要更好地了解其生物利用度和药代动力学特征，以使其能够在临床试验中使用。对于EGCG在体内最合适的浓度以获得最大的治疗效果，目前还没有达成共识。因此，本研究的目的是分析隔夜禁食后单独口服或与不同食品补充剂一起口服 EGCG 的生物利用度，以确定其作为药理学工具的最佳条件（血液中的高浓度和最低的个体差异）在人体试验中。前瞻性招募 10 名年龄 25 至 35 岁的健康志愿者（5 男 5 女）。进行了三个系列的临床实验，每个系列的洗脱期为 7 天：1) Teavigo®（EGCG 提取物）单独使用，2) Teavigo® 与标准早餐一起使用，以及 3) FontUp®（商业上用脂肪、碳水化合物制备的 Teavigo®） 、蛋白质、维生素和矿物质）。摄入 EGCG 后 0、30、60、90、120、180、240 和 360 分钟收集血样。采用液相色谱和质谱UPLC-ESI-MS/MS分析方法测定血浆中的游离EGCG。统计分析的药代动力学变量为曲线下面积(AUC0-360)、Cmax、Cav、Cmin、T1/2和Tmax。单独使用 EGCG (Teavigo®) 的 AUC0-360、Cmax 和 Cav 组在男性中均较高（3.86 ± 4.11 µg/mL/kg/6 h；5.95 ng/mL/kg；2.96 ng/mL/kg），女性（3.33 ± 1.08 µg/mL/kg/6 小时；6.66 ng/mL/kg；3.66 ng/mL）。此外，FontUp® 是男性（192 ± 66 分钟）和女性（133 ± 28 分钟）T1/2 值最高的组。根据其药代动力学特征，禁食过夜后摄入的 Teavigo® 揭示了血浆中 EGCG 的最高浓度，这表明如果实验设计需要在胃肠道中良好吸收，那么这是一种极好的给药替代方案。此外，EGCG与食品补充剂（FontUp®）一起服用可以提高分子在体内的稳定性，如果实验设计想要减少个体差异，是最佳选择。