一种新型食品级辅酶 Q10 配方可提高生物利用度：健康志愿者单次和重复给药的药代动力学研究。

A New Food-grade Coenzyme Q10 Formulation Improves Bioavailability: Single and Repeated Pharmacokinetic Studies in Healthy Volunteers.

机构信息

Research and Development Department, Indena SpA, 20139 Milan, Italy.

出版信息

Curr Drug Deliv. 2019;16(8):759-767. doi: 10.2174/1567201816666190902123147.

DOI:10.2174/1567201816666190902123147

PMID:31475897

Abstract

BACKGROUND

Coenzyme Q10 is a fundamental endogenous factor involved in cell energy production that shows protective properties in oxidative stress, mainly in skeletal and heart muscle. Coenzyme Q10 supplementation appears to benefit athletes in strenuous training and in the elderly, demonstrating ant-inflammatory properties by reducing inflammatory cytokines. Improved absorption of coenzyme Q10 via a new delivery system would represent an important step forward in the use of coenzyme Q10 as a dietary supplement.

OBJECTIVE

The aim of the study was to evaluate the solubility and oral absorption in human healthy volunteers of a new food grade coenzyme Q10 phytosome formulation.

METHODS

Solubility studies were performed in vitro in simulated gastrointestinal fluids; human studies were conducted in healthy volunteers to evaluate oral absorption in a Single dose study, in comparison with the coenzyme Q10 capsules, and in a repeated study at two increasing doses.

RESULTS

The highest solubility shown by coenzyme Q10 phytosome in simulated intestinal fluids results in an improvement in oral absorption of coenzyme Q10 in healthy volunteers, three times more than the coenzyme Q10 according to AUC (area under the time/concentration curve) values. When two increasing doses (one and two capsules) were administered to healthy volunteers within a two-week schedule, the plasmatic levels of coenzyme Q10 resulted in 0.864±0.200 μg/ml (Mean±S.D.+41%) and 1.321±0.400 μg/ml (+116%), respectively versus baseline (0.614±0.120 μg/ml one capsule, 0.614±0.160 μg/ml two capsules). This detected dose-related bioavailability of coenzyme Q10 phytosome was even observed with no alterations in vital signs, neither in the physical examination nor in ECG, and no changes of clinical and biochemical parameters were observed.

CONCLUSION

These findings, taken together, support the safety profile and significantly improved coenzyme Q10 oral absorption in humans with this new phytosome delivery formulation.

摘要

背景

辅酶 Q10 是一种基本的内源性因子，参与细胞能量产生，在氧化应激中具有保护作用，主要在骨骼肌和心肌中。辅酶 Q10 补充剂似乎对剧烈训练的运动员和老年人有益，通过减少炎症细胞因子显示出抗炎特性。通过新的输送系统提高辅酶 Q10 的吸收将代表将辅酶 Q10 作为膳食补充剂使用的重要一步。

目的

本研究旨在评估新型食品级辅酶 Q10 复合体制剂在健康志愿者中的溶解度和口服吸收情况。

方法

在模拟胃肠道液中进行体外溶解度研究；在健康志愿者中进行人体研究，以评估单次剂量研究中的口服吸收情况，与辅酶 Q10 胶囊进行比较，并在两个递增剂量的重复研究中进行评估。

结果

在模拟肠液中显示出的辅酶 Q10 复合体制剂的最高溶解度导致辅酶 Q10 在健康志愿者中的口服吸收得到改善，根据 AUC（时间/浓度曲线下面积）值，比辅酶 Q10 高三倍。当在两周的方案内给予健康志愿者递增的两个剂量（一个和两个胶囊）时，辅酶 Q10 的血浆水平分别为 0.864±0.200 μg/ml（平均值±S.D.+41%）和 1.321±0.400 μg/ml（+116%），与基线相比（一个胶囊 0.614±0.120 μg/ml，两个胶囊 0.614±0.160 μg/ml）。即使在没有改变生命体征、体检或心电图的情况下，也观察到了辅酶 Q10 复合体制剂的这种剂量相关的生物利用度，并且没有观察到临床和生化参数的变化。