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The Plasma Bioavailability of Coenzyme Q10 Absorbed from the Gut and the Oral Mucosa

机译:凝固和口腔粘膜吸收的辅酶Q10的血浆生物利用度

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摘要

Coenzyme Q10 (CoQ10) has a central role in the generation of cellular bioenergy and its regulation. The hydrophobicity exhibited by the CoQ10 molecule leads to reports of poor absorption profiles, therefore, the optimization of formulations and modes of delivery is an ever-evolving therapeutic goal. The aim of this study was to investigate different CoQ10 formulations. The article summarizes the findings from an Australian comparative study involving adults administered CoQ10 through different oral delivery platforms. A total of 11 participants (six males and five females) voluntarily participated in a comparative clinical study of three different CoQ10 formulations across a six-week period, completing 198 person-hours of cumulative contribution equivalent to n = 33 participation. All of the eligible participants (n = 11) administered the three formulations blinded from who the commercial supplier of the formulation was and from what the chemical form of the CoQ10 was that was being administered. The dosing between the CoQ10 preparations were dispensed sequentially and were administered following three-week washouts. Three commercial preparations were tested, which included the following: formulations with capsules each containing ubiquinol and ubiquinone (150 mg/capsule), and a liposome ubiquinone formulation (40 mg/mL at 2 actuations of the pump). A significant inter-subject variation in the plasma level of CoQ10 at baseline that was observed to increase with an increase in age. This trend persisted in the post administration of the different formulations. Furthermore, it was observed that the intestinal absorption and bioavailability of CoQ10 varied significantly in the plasma between subjects, irrespective of whether the ubiquinol or ubiquinone forms were administered. The administration of CoQ10 as a liposome for preparation showed the poorest response in bioavailability. Although the ubiquinol capsule form of CoQ10 was observed to have increased in the plasma versus the ubiquinone capsules and the ubiquinol liposome at the two-hour interval, the inter-subject variation was such that the difference was not significant (p > 0.05). All of the CoQ10 formulations showed no further increases in their plasma levels over the remaining study period (i.e., four hours). This study further concluded that the intestinal absorption of CoQ10 is highly variable and is independent of the molecular form administered. Furthermore, it also concludes that liposomes are not an effective vehicle for the oral administration of CoQ10, and as such, did not improve the oral mucosal/sublingual absorption and bioavailability of the molecule. Of interest was the observation that with the increasing subject age, there was an observed increase in the baseline plasma CoQ10 levels in the participants prior to dosing. It was posited that the increase in the baseline plasma levels of CoQ10 with an increase in age could be due to the loss of skeletal muscle mass, a result that still needs to be verified.
机译:辅酶Q10(COQ10)在细胞生物能量及其调节中具有核心作用。 CoQ10分子表现出的疏水性导致吸收曲线不良的报告,因此,优化配方和交付方式是一项不断发展的治疗目标。本研究的目的是调查不同的COQ10配方。本文总结了涉及通过不同口头交付平台管理Co Q10的成年人的澳大利亚比较研究的调查结果。共有11名参与者(六名男性和五名女性)自愿参加了在六周期间的三种不同COQ10配方的比较临床研究中,完成了198人的累积贡献,相当于N = 33参与。所有符合条件的参与者(n = 11)管理的三种配方由世卫组织蒙蔽了制剂的商业供应商是且来自CoQ10的化学形式被施用的。依次分配CoQ10制剂之间的给药,并在三周的休养后施用。测试了三种商业制剂,其中包括以下内容:具有胶囊的配方,其各种含有ubiquinol和泛醌(150mg /胶囊),以及脂质体泛醌制剂(40mg / ml,在泵的2个致动下施加40mg / ml)。在基线上观察到增加的基线等血浆水平的显着间变异,随着年龄的增加而增加。这种趋势持续在不同配方的授权中。此外,观察到,无论是否施用了泛醇或泛醌形式,辅酶Q10的肠道吸收和生物利用度在受试者之间的血浆中显着变化。作为脂质体的辅助施用CoQ10,表明生物利用度最糟糕的反应。虽然观察到核苷酸胶囊的钙蛋白胶囊形式在血浆与泛醌胶囊中增加,但在两小时的间隔中含有泛醇胶囊和ubiquinol脂质体,但差异差异不显着(p> 0.05)。所有CoQ10制剂在其余的研究期间没有进一步增加其血浆水平(即4小时)。该研究进一步得出结论,CoQ10的肠道吸收是高度可变的,并且与施用的分子形式无关。此外,它还得出结论,脂质体不是用于口服施用CoQ10的有效载体,因此,未改善分子的口腔粘膜/舌下吸收和生物利用度。感兴趣的是观察到,随着主体年龄的增加,在给药之前,参与者的基线血浆COQ10水平的增加的增加。它被定位在于,CoQ10的基线血浆水平的增加随着骨骼肌损失的损失,仍然需要验证。

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