Department of Movement and Sports Sciences, Ghent University, 9000 Ghent, Belgium.
Laboratory of Pharmaceutical Technology, Ghent University, 9000 Ghent, Belgium.
Nutrients. 2019 Jul 20;11(7):1663. doi: 10.3390/nu11071663.
Despite the presumption of the beneficial effects of magnesium supplementation, little is known about the pharmacokinetics of different magnesium formulations. We aimed to investigate the value of two in vitro approaches to predict bioavailability of magnesium and to validate this in subsequent in vivo testing. In vitro assessment of 15 commercially available magnesium formulations was performed by means of a Simulator of the Human Intestinal Microbial Ecosystem (SHIME) and by dissolution tests. Two magnesium formulations with contrasting bioavailability prediction from both in vitro tests (best vs. worst) were selected for in vivo testing in 30 subjects. In vivo bioavailability was compared following one acute ingestion by monitoring blood magnesium concentrations up to 6 h following intake. The in vitro tests showed a very wide variation in absorption and dissolution of the 15 magnesium products. In the in vivo testing, a significant different serum magnesium absorption profile was found up to 4 h following supplement ingestion for the two supplements with opposing in vitro test results. Moreover, maximal serum magnesium increase and total area under the curve were significantly different for both supplements (+6.2% vs. +4.6% and 6.87 vs. 0.31 mM.min, respectively). Collectively, poor bioaccessibility and bioavailability in the SHIME model clearly translated into poor dissolution and poor bioavailability in vivo. This provides a valid methodology for the prediction of in vivo bioavailability and effectiveness of micronutrients by specific in vitro approaches.
尽管人们普遍认为镁补充剂有益,但对于不同镁制剂的药代动力学知之甚少。我们旨在研究两种体外方法预测镁生物利用度的价值,并在随后的体内试验中验证这一点。通过模拟人体肠道微生物生态系统(SHIME)和溶解试验对 15 种市售镁制剂进行了体外评估。选择两种体外试验预测生物利用度差异最大的(最佳和最差)镁制剂进行 30 名受试者的体内试验。通过监测摄入后 6 小时内的血液镁浓度,比较单次急性摄入后的体内生物利用度。体外试验显示 15 种镁产品的吸收和溶解差异很大。在体内试验中,两种补充剂的吸收曲线在补充后 4 小时内存在显著差异,而这两种补充剂的体外试验结果相反。此外,两种补充剂的最大血清镁增加量和曲线下总面积均存在显著差异(分别为+6.2%比+4.6%和 6.87 比 0.31 mM.min)。总的来说,SHIME 模型中较差的生物可及性和生物利用度明显转化为较差的溶解和体内生物利用度。这为通过特定的体外方法预测体内生物利用度和微量营养素的有效性提供了有效的方法。