Table 1.

Pharmacokinetic variables of 0.875 mg glibenclamide in 12 healthy volunteers after 3 days of pretreatment with clarithromycin (250 mg twice daily), placebo (control), or grapefruit juice (200 ml thrice daily)

Variable	Placebo (control) phase	Clarithromycin phase	Grapefruit juice phase
Cmax (ng ml−1)	43.6 ± 9.24	54.0 ± 8.21*	46.6 ± 9.81
Geometric mean ratio (95% CI)	1	1.25 (1.12, 1.40)	1.07 (0.93, 1.23)
tmax (h)	1.25 (1–1.5)	1.5 (1–2)	1.5 (1–1.5)
t1/2 (h)	2.4 ± 0.32	2.3 ± 0.31	2.3 ± 0.32
Geometric mean ratio (95% CI)	1	0.96 (0.91, 1.02)	0.98 (0.90, 1.07)
AUC(0,∞) (ng ml−1 h)	133 ± 40.4	177 ± 46.4*	139 ± 33.7
Geometric mean ratio (95% CI)	1	1.35 (1.21, 1.50)	1.07 (0.99, 1.15)
Metabolite excreted (0–12 h) (U)	6230 ± 2210	7690 ± 1850	7160 ± 1640
Geometric mean ratio (95% CI)	1	1.26 (0.88, 1.82)	1.19 (0.84, 1.67)

Data are mean values ± SD unless otherwise shown; t_max data are given as median with range. Geometric ratio is clarithromycin or grapefruit juice phase compared with placebo phase. C_max, peak plasma concentration; t_max, time to reach C_max; t_1/2, half-life; AUC(0,∞), area under the plasma concentration-time curve from time 0 to infinity.

^*P < 0.01 vs. placebo and grapefruit juice phases.