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Pharmacokinetics and dose proportionality of extended‐release metformin following administration of 1000, 1500, 2000 and 2500 mg in healthy volunteers
Author(s) -
Cullen Edward,
Liao James,
Lukacsko Peter,
Niecestro Robert,
Friedhoff Lawrence
Publication year - 2004
Publication title -
biopharmaceutics and drug disposition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.419
H-Index - 58
eISSN - 1099-081X
pISSN - 0142-2782
DOI - 10.1002/bdd.407
Subject(s) - metformin , pharmacokinetics , crossover study , dosing , medicine , pharmacology , dose–response relationship , bioequivalence , urology , placebo , insulin , alternative medicine , pathology
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 0–72 h 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 0–72 h , and AUC ∞ , the magnitude of the difference across the dose range was <20% for AUC 0–72 h and AUC ∞ , and was ⩽30% 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 © 2004 John Wiley & Sons, Ltd.