Table 2.

Pharmacokinetic (PK) parameters (mean±s.d.) of (−)-cisapride and (+)-cisapride after a single oral dose of 10 mg rac-cisapride (CIS) in water (W) (control) and 200 ml double-strength grapefruit juice (GFJ) treated healthy volunteers (n = 10).

PK parameters	W phase	GFJ phase	Ratio GFJ/W phase	Mean differences (95% CI)	P values
(–)-Cisapride
tmax (h)	1.35 ± 0.4	2.8 ± 1	2.33 ± 1.19	−1.45 (−2.33, −0.57)	0.0048
Cmax (ng ml−1)	30 ± 13.6	55.5 ± 18.2	1.96 ± 0.52	−25 (−33, −17)	< 0.0001
AUC(0, ∞) (ng ml−1 h)	201.2 ± 161	522 ± 303	2.79 ± 0.54	−320 (−439, −202)	0.0002
t1/2 (h)	4.7 ± 2.7	6.3 ± 2.4	1.48 ± 0.42	−1.5 (−2.8, −0.23)	0.026
(+/–)-Cisapride
tmax (h)	1.75 ± 0.5	2.9 ± 1.6	1.71 ± 0.86	−1.15 (−2.12, −0.18)	0.025
Cmax (ng ml−1)	10.5 ± 3.4	18.4 ± 6.2	1.89 ± 0.75	−7.9 (−11.8, −3.9)	0.0015
AUC(0, ∞) (ng ml−1 h)	70 ± 51.5	170 ± 91	2.75 ± 1.04	−100 (−143, −53)	0.0005
t1/2 (h)	4.8 ± 3.1	6.5 ± 2.8	1.8 ± 1.21	−1.75 (−4.6, −1.14)	0.205

Peak plasma concentration (C_max), time to C_max (t_max), area under the plasma concentration-time curve (AUC(0, ∞)) and elimination half-life (t_½).