Table 4.
Pharmacokinetic parameters of unchanged drug after oral multiple administration of JTE-522.
C4 h (ng ml−1) | C24 h (ng ml−1) | t1/2 (h) | AUC(µg ml−1 h) | |
---|---|---|---|---|
Plasma | ||||
Day 1 | 334.2 ± 83.1 | 93.0 ± 10.9 | 11.09 ± 3.17# | 4.5 ± 0.8* |
(247.0, 421.4) | (81.6, 104.5) | (7.76, 14.42) | (3.7, 5.3) | |
Day 2 | 947.0 ± 261.3 | 78.4 ± 18.4 | ||
(672.7, 1221.2) | (59.1, 97.7) | |||
Day 3 | 787.1 ± 260.0 | 67.4 ± 20.5 | ||
(514.3, 1060.0) | (45.9, 88.9) | |||
Day 4 | 903.8 ± 131.5 | 65.8 ±16.8 | 5.43 ± 0.64# | 8.0 ± 1.6* |
(765.9, 1041.8) | (48.2, 83.4) | (4.75, 6.10) | (6.3, 9.7) | |
Day 5 | 675.8 ± 314.8 | 71.6 ± 16.6 | ||
(345.4, 1006.2) | (54.2, 89.0) | |||
Day 6 | 793.0 ± 237.1 | 69.7 ± 12.4 | ||
(544.2, 1041.8) | (56.7, 82.7) | |||
Day 7 | 1045.9 ± 193.9 | 60.9 ± 16.4 | 5.08 ± 0.73# | 8.5 ± 1.4* |
(842.4, 1249.3) | (43.6, 78.1) | (4.31, 5.84) | (7.1, 9.9) | |
9.4 ± 1.5** | ||||
(7.9, 10.9) |
C4 h (mg ml−1) | C24 h (mg ml−1) | t1/2 (h) | AUC(µg ml−1 h) | |
---|---|---|---|---|
Blood | ||||
Day 1 | 20.0 ± 2.2 | 8.2 ± 1.7 | 16.14 ± 3.20# | 305.6 ± 34.2* |
(17.6, 22.3) | (6.4, 9.9) | (12.78, 19.50) | (269.7, 341.5) | |
Day 2 | 12.2 ± 2.0 | 3.9 ± 1.0 | ||
(10.1, 14.3) | (2.8, 4.9) | |||
Day 3 | 9.4 ± 1.4 | 3.1 ± 0.9 | ||
(7.9, 10.8) | (2.1, 4.1) | |||
Day 4 | 9.3 ± 1.2 | 3.0 ± 0.9 | 12.48 ± 2.27# | 132.6 ± 25.5* |
(8.0, 10.6) | (2.0, 4.0) | (10.10, 14.86) | (105.8, 159.4) | |
Day 5 | 8.7 ± 1.5 | 3.2 ± 1.0 | ||
(7.2, 10.3) | (2.2, 4.3) | |||
Day 6 | 9.4 ± 2.1 | 3.2 ±1.0 | ||
(7.2, 11.5) | (2.2, 4.2) | |||
Day 7 | 9.3 ± 2.0 | 2.9 ± 1.0 | 12.62 ± 2.93# | 130.6 ± 26.3* |
(7.2, 11.4) | (1.9, 3.9) | (9.55, 15.70) | (103.0, 158.2) | |
42.42 ± 8.49## | 282.9 ± 97.6** | |||
(33.51, 51.34) | (180.4, 385.3) |
Data represent as mean ± s.d., n = 6 Figures in the parentheses represent the 95% confidence interval.
AUC(0,24 h)
AUC (0,•)
calculated from tmax −24 h
calculated from 48 h to last measured point.