In this open-label, single-center, pharmacokinetic study of repaglinide, 12
healthy volunteers (6 men, 6 women) were enrolled in each of 2 groups (tot
al, 24 volunteers). One group consisted of young adult subjects (18 to 40 y
ears), and the other group consisted of elderly subjects (greater than or e
qual to 65 years). On day 1, after a 10-hour fast, all 24 subjects received
a single 2-mg dose of repaglinide. Starting on day 2 and continuing for 7
days, subjects received a 2-mg dose of repaglinide 15 minutes before each o
f 3 meals. On day 9, subjects received a single 2-mg dose of repaglinide. P
harmacokinetic profiles, including area under the curve, maximum concentrat
ion (C-max), time to C-max, and half-life, were determined at completion of
the single-dose and multiple-dose regimens (days 1 and 9,respectively). Tr
ough repaglinide values were collected on days 2 through 7 to assess steady
state. The single-dose and multiple-dose pharmacokinetic variables of seru
m repaglinide were not significantly different between young adult and elde
rly subjects. Repaglinide was well tolerated in both groups. Hypoglycemic e
vents occurred in 5 young adult and 5 elderly subjects. This study demonstr
ates that the pharmacokinetics of repaglinide are similar in healthy young
adult and elderly subjects.