Pharmacokinetic profiles of single- and multiple-dose regimens of repaglini
de were evaluated in 12 elderly subjects with type 2 diabetes. On day 1, fo
llowing a 10-hour fast, subjects received a single 2-mg dose of repaglinide
. Starting on day 2 and continuing for 7 days, each subject received a 2-mg
dose of repaglinide 15 minutes before each of the three main meals. On day
9, subjects received a single 2-mg dose of repaglinide. Pharmacokinetic pr
ofiles, including area under the curve (AUC), log(AUC), maximal concentrati
on (C-max), log(C-max), time to maximal concentration (T-max), and half-lif
e (T-1/2), were determined at completion of the single- and multiple-dose r
egimens (days 1 and 9, respectively). Trough repaglinide values were collec
ted on days 2 through 7. The mean log(AUC) values after multiple dosing wer
e significantly higher than the values obtained after a single dose. The me
an values for log(C-max), and T-max were comparable after each dosing regim
en. The T-1/2 of repaglinide after multiple dosing was 1.7 hours. The troug
h values for repaglinide were low. No hypoglycemic events were reported. Th
e pharmacokinetic profiles of repaglinide after single- and multiple-dose r
egimens were similar, and repaglinide was well tolerated by elderly subject
s with type 2 diabetes.