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Single- and multiple-dose pharmacokinetics of pioglitazone in adolescents with type 2 diabetes

By October 10, 2005September 24th, 2020No Comments

LINK TO RESEARCH
https://pubmed.ncbi.nlm.nih.gov/16172178/

PUBLICATION
The Journal of Clinical Pharmacology

AUTHORS
Michael L Christensen 1 ,
Bernd Meibohm,
Edmund V Capparelli,
Pedro Velasquez-Mieyer,
George A Burghen,
William V Tamborlane

ABSTRACT
This study assessed the single- and multiple-dose pharmacokinetics of 3
doses (15 mg, 30 mg, and 45 mg) of pioglitazone in 36 adolescents with type
2 diabetes. Blood samples were obtained over a 48-hour interval after the
first dose (day 1) and over a 72-hour interval after the last dose (day 15)
of pioglitazone and were assayed for pioglitazone and active metabolites
(M-III and M-IV). Pioglitazone systemic exposure increased dose dependently
but was less than dose proportional during multiple dosing. The median peak
pioglitazone concentration occurred at 2 hours. The mean half-life was 8 to
9 hours for pioglitazone and 24 to 32 hours for M-III and M-IV, with
similar values at each dose level. During multiple dosing, accumulation for
pioglitazone was negligible, but it reached 2.5- to 3.0-fold for M-III and
M-IV. The sustained total serum concentration of active compounds during
multiple dosing provides the basis for once-daily dose administration of
pioglitazone in adolescents.

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