Table 2.
Pharmacokinetic parameters of loperamide by period
| Period | Co-administered drug | Dose, mg | n | tmax (h) | Cmax (μg l−1) | t1/2 (h) | AUC(0,tlast) (μg l−1 h) | Ratio* (90% confidence interval) |
|---|---|---|---|---|---|---|---|---|
| 1 | None | 18 | 2.0 [1.0, 6.0] | 4.3 ± 2.1 | 18.4 ± 4.4 | 63.8 ± 27.4 | 1 (reference) | |
| 2 | Quinidine | 600 | 18 | 3.0 [2.0, 3.0] | 11.4 ± 5.1 | 14.6 ± 1.9 | 139.2 ± 56.0 | 2.20 (1.53, 3.18) |
| 3 | HM30181 | 15 | 6 | 2.5 [2.0, 5.0] | 6.7 ± 2.6 | 15.5 ± 1.7 | 98.7 ± 37.9 | 1.46 (0.96, 2.22) |
| 60 | 6 | 4.5 [3.0, 6.0] | 4.7 ± 1.5 | 18.5 ± 1.7 | 100.7 ± 37.6 | 1.63 (0.92, 2.91) | ||
| 180 | 6 | 2.5 [2.0, 5.0] | 4.8 ± 2.2 | 15.8 ± 1.6 | 79.7 ± 38.4 | 1.35 (0.68, 2.71) | ||
| All | 18 | 3.0 [2.0, 6.0] | 5.4 ± 2.3 | 16.6 ± 2.1 | 93.0 ± 37.0 | 1.48 (1.08, 2.02) |
Data are mean ± SD except for tmax, for which median [min, max] is shown.
*
Geometric mean ratios of the area under the concentration–time curve from time 0 to the last measurable time (AUC(0,tlast)) of loperamide for HM30181 or quinidine co-administration vs. loperamide alone.