健康受试者中大剂量口服盐酸硫胺的药代动力学
Pharmacokinetics of high-dose oral thiamine hydrochloride in healthy subjects.
作者信息
Smithline Howard A, Donnino Michael, Greenblatt David J
机构信息
Department of Emergency Medicine, Tufts University School of Medicine and Baystate Medical Center, Springfield, MA, USA.
出版信息
BMC Clin Pharmacol. 2012 Feb 4;12:4. doi: 10.1186/1472-6904-12-4.
BACKGROUND
High dose oral thiamine may have a role in treating diabetes, heart failure, and hypermetabolic states. The purpose of this study was to determine the pharmacokinetic profile of oral thiamine hydrochloride at 100 mg, 500 mg and 1500 mg doses in healthy subjects.
METHODS
This was a randomized, double-blind, single-dose, 4-way crossover study. Pharmacokinetic measures were calculated.
RESULTS
The AUC₀₋₁₀ hr and C(max) values increased nonlinearly between 100 mg and 1500 mg. The slope of the AUC₀₋₁₀ hr vs dose, as well as the C(max) vs dose, plots are steepest at the lowest thiamine doses.
CONCLUSION
Our study demonstrates that high blood levels of thiamine can be achieved rapidly with oral thiamine hydrochloride. Thiamine is absorbed by both an active and nonsaturable passive process.
TRIAL REGISTRATION
ClinicalTrials.gov: NCT00981877.
背景
高剂量口服硫胺素可能在治疗糖尿病、心力衰竭和高代谢状态中发挥作用。本研究的目的是确定健康受试者口服100毫克、500毫克和1500毫克剂量盐酸硫胺素的药代动力学特征。
方法
这是一项随机、双盲、单剂量、四路交叉研究。计算药代动力学指标。
结果
在100毫克至1500毫克之间，AUC₀₋₁₀小时和C(max)值呈非线性增加。AUC₀₋₁₀小时与剂量以及C(max)与剂量的曲线斜率在最低硫胺素剂量时最陡。
结论
我们的研究表明，口服盐酸硫胺素可迅速达到高血硫胺素水平。硫胺素通过主动和非饱和被动过程吸收。
试验注册
ClinicalTrials.gov：NCT00981877。
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