Table 1.
Summary of ruboxistaurin and N-desmethyl ruboxistaurin pharmacokinetic parameters before and after induction with rifampicin
| Ruboxistaurin | N-desmethyl ruboxistaurin | |||||
|---|---|---|---|---|---|---|
| Parameter | Without rifampicin | With rifampicin | Ratio† of geometric means (90% CI) | Without rifampicin | With rifampicin | Ratio† of geometric means (90% CI) |
| n | 17 | 16 | – | 17 | 16 | – |
| Cmax | 200 | 10.7 | 0.049 | 128 | 42.1 | 0.316 |
| (nmol l−1)b | (63.3) | (5.68) | (0.041, 0.059)* | (37.6) | (16.4) | (0.271, 0.368)* |
| AUC(0,tlast) | 1216 | 53.4 | 0.041 | 1640 | 373 | 0.222 |
| (nmol l−1 h)b | (420) | (28.0) | (0.034, 0.050)* | (551) | (121) | (0.193, 0.256)* |
| AUC(0,∞) | 1364 | 60.4 | 0.042 | 1831 | 406 | 0.219 |
| (nmol l−1 h)b | (429) | (28.0) | (0.035–0.051)* | (600) | (122) | (0.189, 0.253)* |
| t1/2b | 13.8 | 2.28 | 0.186 | 20.6 | 13.7 | 0.658 |
| (h) | (10.1) | (0.82) | (0.141, 0.244)* | (7.09) | (3.87) | (0.562, 0.769)* |
| tmaxa | 2.00 | 2.00 | 0.417c | 2.50 | 2.00 | 0.374c |
| (h) | (1.00–4.00) | (0.500, 6.00) | (1.50, 4.00) | (0.500, 6.00) | ||
| CL/Fb | 109 | 2639 | 23.5 | NC | NC | NC |
| (l h−1) | (29.8) | (996) | (20.0, 28.5)* | |||
| VZ/Fb | 2107 | 8718 | 4.35 | NC | NC | NC |
| (l) | (1819) | (4548) | (3.23, 5.88)* | |||
tmax data are given as the median values with ranges
values are shown as the arithmetic mean (+ SD.)
P values based on Wilcoxon Signed Rank test
ratio of geometric means after: before rifampicin induction; P value ≤ 0.001; CI = confidence interval; NC = not calculated.