Dolberg Mette Konow Bøgebjerg, Nielsen Lars Peter, Dahl Ronald
Department of Respiratory Diseases and Allergy & Department of Clinical Pharmacology, Aarhus University Hospital, Aarhus, Denmark.
Basic Clin Pharmacol Toxicol. 2017 Mar;120(3):264-269. doi: 10.1111/bcpt.12642. Epub 2017 Jan 11.
Despite the presumption of a beneficial effect of magnesium (Mg) supplementation on various diseases, little is known concerning the pharmacokinetics of Mg hydroxide. This study was designed to provide a pharmacokinetic profile of Mg hydroxide after a single oral dose. Ten healthy male adults participated in this cross-over study with three 24-hr study days. Interventions were (i) none (baseline), (ii) oral intake of three (3 × 360 mg) tablets of Mg hydroxide (Mablet ) and (iii) IV bolus infusion of 2 g Mg sulphate (index drug). Blood samples were collected before the single dose, after (i.e. after treatment administration) 15, 30, 60, 90 and 120 min. and after 3, 4, 6, 8, 12 and 24 hr. Urine was collected in four 6-hr periods per study day. Blood (N = 10) and urine (N = 6) Mg were analysed by descriptive statistics. Bioavailability was 14.9% (CI: 8.3; 26.8), blood clearance was 5.1 L/hr (CI: 2.1; 17.0), apparent volume of distribution was 60.2 L (CI: 35.6; 102.0), elimination constant was 0.08 per hour (CI: 0.05; 0.14), half-life was 8.3 hr (CI: 4.8; 14.1), C was 0.11 mmol/L (CI: 0.07; 0.14), and AUC was 92.3 mmol/L × min. (CI: 45.5; 139.1). Urine Mg excretion augmented by 17.7% (CI: 8.9; 35.0) from baseline. No severe side effects were observed. The bioavailability of Mg hydroxide was 15%, and it constitutes a clinically relevant option for oral Mg supplementation. No severe side effects were seen.
尽管人们推测补充镁（Mg）对多种疾病有有益作用，但关于氢氧化镁的药代动力学却知之甚少。本研究旨在提供单次口服剂量后氢氧化镁的药代动力学概况。十名健康成年男性参与了这项交叉研究，研究为期三天，每天24小时。干预措施包括：（i）无干预（基线）；（ii）口服三片（3×360毫克）氢氧化镁片（镁片）；（iii）静脉推注2克硫酸镁（对照药物）。在单次给药前、给药后15、30、60、90和120分钟以及3、4、6、8、12和24小时采集血样。每天分四个6小时时间段收集尿液。采用描述性统计分析血液（N = 10）和尿液（N = 6）中的镁含量。生物利用度为14.9%（置信区间：8.3；26.8），血液清除率为5.1升/小时（置信区间：2.1；17.0），表观分布容积为60.2升（置信区间：35.6；102.0），消除常数为每小时0.08（置信区间：0.05；0.14），半衰期为8.3小时（置信区间：4.8；14.1），Cmax为0.11毫摩尔/升（置信区间：0.07；0.14），曲线下面积为92.3毫摩尔/升·分钟（置信区间：45.5；139.1）。尿镁排泄量较基线增加了17.7%（置信区间：8.9；35.0）。未观察到严重副作用。氢氧化镁的生物利用度为15%，是口服补充镁的一种具有临床相关性的选择。未观察到严重副作用。
