Pharmacokinetics and dose proportionality of extended-release metformin following administration of 1000, 1500, 2000 and 2500 mg in healthy volunteers

被引:21
|
作者
Cullen, E [1 ]
Liao, J [1 ]
Lukacsko, P [1 ]
Niecestro, R [1 ]
Friedhoff, L [1 ]
机构
[1] Andrx Corp, Andrx Labs, Hackensack, NJ 07601 USA
关键词
metformin; extended-release formulation; tolerability; pharmacokinetics; dose proportionality;
D O I
10.1002/bdd.407
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The pharmacokinetics and dose-exposure relationship of an extended-release formulation of metformin (ER-metformin) was investigated in a randomized, single-dose, four-period crossover study in 24 healthy male volunteers. During each study period, subjects received a randomly assigned dose containing 1000, 1500, 2000 or 2500 mg metformin. Blood samples were drawn 0-72h after dosing for pharmacokinetic and dose-proportionality assessment. Although several pairwise comparisons between dose groups were significant (p < 0.05) with respect to dose-normalized C-max, AUC(0-72h), and AUC(infinity), the magnitude of the difference across the dose range was <20% for AUC(0-72h) and AUC(infinity), and was less than or equal to30% for C-max. The results indicate a consistent and predictable increase in metformin exposure with an extended-release formulation of metformin over 1000 to 2500 mg. Copyright (C) 2004 John Wiley Sons, Ltd.
引用
收藏
页码:261 / 263
页数:3
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