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不同辅酶Q10制剂与新型递送系统的相对生物利用度比较

Relative bioavailability comparison of different coenzyme Q10 formulations with a novel delivery system.

作者信息

Liu Zheng-Xian, Artmann Carl

机构信息

GeroNutra, Hayward, California, USA.

出版信息

Altern Ther Health Med. 2009 Mar-Apr;15(2):42-6.

Abstract

Commercial coenzyme Q10 (CoQ10, ubiquinone) formulations are often of poor intestinal absorption. The relative bioavailability of CoQ10 has been shown in National Institutes of Health-funded clinical trials to be increased by its delivery system. We investigated the bioavailability of a new CoQ10 formulation based on a new and patented technology, VESIsorb, with 3 other commercially available CoQ10 products, an oil-based formulation and 2 solubilizates. This new CoQ10 formulation (commercially branded CoQsource) is a lipid-based formulation that naturally self-assembles on contact with an aqueous phase into an association colloid delivery system (hereafter "colloidal-Q10"). Twenty healthy male and female subjects participated in a double-blind, comparative (parallel design), controlled, single-dose (120 mg) bioavailability study. Plasma concentration of CoQ10 was determined at baseline and at various intervals after administration over a 24-hour period. To compare bioavailability, maximum concentration (Cmax) and area under curve from 0 to 10 hours (AUC(0-10h)) were assessed. The kinetic profiles of all CoQ10 preparations revealed a 1-peak plasma concentration-time course. Highest Cmax values were seen after colloidal-Q10 administration. Colloidal-Q10 not only had the highest plasma concentration levels after 1 hour, but it continued to increase before reaching Cmax at about 4 hours. The plasma concentration of colloidal-Q10 remained well above the levels of the 3 other products throughout the 24-hour period. The relative bioavailability calculated using the AUC(0-10h) values was also the highest for colloidal-Q10; the AUC(0-10h) values were 30.6, 6.1, 4.9, and 10.7 microg/mL*h for colloidal-Q10, solubilizate 1, the oil-based formulation, and solubilizate 2, respectively. Differences in Cmax and AUC between colloidal-Q10 and the 3 other formulations were statistically significant. In summary, the data presented suggests that colloidal-Q10 improves the enteral absorption and the bioavailability of CoQ10 in humans.

摘要

市售辅酶Q10(CoQ10,泛醌)制剂的肠道吸收往往较差。美国国立卫生研究院资助的临床试验表明,CoQ10的相对生物利用度可通过其递送系统得到提高。我们研究了基于一种新的专利技术VESIsorb的新型CoQ10制剂与其他3种市售CoQ10产品(一种油基制剂和2种增溶剂)的生物利用度。这种新型CoQ10制剂(商品名为CoQsource)是一种脂质基制剂,与水相接触时会自然自组装成缔合胶体递送系统(以下简称“胶体Q10”)。20名健康男性和女性受试者参与了一项双盲、比较性(平行设计)、对照、单剂量(120毫克)生物利用度研究。在基线以及给药后24小时内的不同时间间隔测定CoQ10的血浆浓度。为比较生物利用度,评估了最大浓度(Cmax)和0至10小时的曲线下面积(AUC(0-10h))。所有CoQ10制剂的动力学曲线均显示为单峰血浆浓度-时间过程。胶体Q10给药后观察到最高的Cmax值。胶体Q10不仅在1小时后血浆浓度水平最高,而且在约4小时达到Cmax之前持续升高。在整个24小时期间,胶体Q10的血浆浓度一直远高于其他3种产品的水平。使用AUC(0-10h)值计算的相对生物利用度也是胶体Q10最高;胶体Q10、增溶剂1、油基制剂和增溶剂2的AUC(0-10h)值分别为30.6、6.1、4.9和10.7微克/毫升·小时。胶体Q10与其他3种制剂之间的Cmax和AUC差异具有统计学意义。总之,所呈现的数据表明胶体Q10可改善人体中CoQ10的肠道吸收和生物利用度。

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