TABLE 1

Pharmacokinetic parameters of repaglinide and urinary excretion of repaglinide metabolites M1 and M4 relating to the CYP2C8*3 genotype

Data, obtained by noncompartmental analysis, are shown as mean (95% confidence interval).

Genotype/ParameterAUC0–∞CmaxOral Clearance/b.wt.t1/2TmaxAe0–24 h
M1M4
ng · ml1 · hng · ml1l · h1 · kg1hhAU
All subjects (n = 29)97.4 (71.1–123.7)52.8 (40.1–65.4)0.46 (0.34–0.57)1.3 (1.0–1.5)0.8 (0.7–1.0)48.3 (30.3–66.3)217.8 (172.0–263.6)
CYP2C8*1/*1 (n = 12)105.9 (52.4–159.3)60.3 (31.5–89.1)0.45 (0.23–0.67)1.2 (1.0–1.4)0.8 (0.6–1.0)52.8 (8.4–97.2)184.2 (125.8–242.6)
CYP2C8*1/*3 (n = 13)97.2 (59.2–135.2)50.3 (37.5–63.0)0.46 (0.28–0.64)1.3 (0.8–1.8)0.8 (0.6–1.0)42.6 (28.2–57.1)212.4 (152.4–271.9)
CYP2C8*3/*3 (n = 4)72.4 (6.7–138.0)38.5 (3.8–73.2)0.48 (0.02–0.95)1.3 (−0.5–3.1)0.9 (0.5–1.2)53.3 (21.5–85.0)336.7 (11.6–661.7)
p, one-way ANOVA0.7170.5050.9790.8910.9000.6410.457
p, one-way ANOVA trend test (linear contrast)0.4200.2710.8400.7050.6780.3530.221
  • AUC0–∞, area under the plasma concentration time curve up to infinity; Cmax, maximal concentration; t1/2, terminal half-life; Tmax, time to reach maximal plasma concentration; Ae0–24 h, amount excreted in urine up to 24 h postdose; AU, arbitrary units.