Pharmacokinetic parameter | BI 187004 | ||||||||
---|---|---|---|---|---|---|---|---|---|
2.5 mg gMean (%gCV) | 5 mg gMean (%gCV) | 10 mg gMean (%gCV) | 20 mg gMean (%gCV) | 40 mg gMean (%gCV) | 80 mg gMean (%gCV) | 160 mg gMean (%gCV) | 240 mg gMean (%gCV) | 360 mg gMean (%gCV) | |
AUC0-∞ [nmol*h/L] | – (–) | 2,500 (23.0) | 5,910 (29.2) | 12,400 (41.2) | 25,900 (36.1) | 51,100 (40.2) | 111,000 (19.5) | 109,000 (53.4) | 191,000 (25.4) |
AUC0-24 [nmol*h/L] | 212 (35.2) | 1,490 (21.5) | 4,380 (23.2) | 9,450 (32.1) | 19,900 (26.6) | 43,100 (36.9) | 82,100 (12.6) | 71,700 (74.1) | 135,000 (22.0) |
Cmax [nmol/L] | 11.8 (75.0) | 150 (19.7) | 502 (14.0) | 1,030 (14.4) | 2,210 (27.8) | 2,460 (56.2) | 8,310 (11.0) | 7,120 (64.9) | 13,400 (34.1) |
C24 [nmol/L] | 4.54 (25.2) | 30.0 (28.0) | 71.3 (46.1) | 161 (66.3) | 321 (50.8) | 878 (36.0) | 1,630 (25.9) | 2,130 (22.5) | 2,690 (36.0) |
tmax [h]* | 1.0 (1.0—1.5) | 1.0 (1.0—1.5) | 1.0 (0.5—2.5) | 1.38 (0.5—1.5) | 1.0 (0.5—3.0) | 2.25 (1.0—2.5) | 1.0 (0.5—2.0) | 1.0 (1.0—24.0) | 1.0 (0.5—1.0) |
t1/2 [h] | – | 33.5 (14.4) | 23.7 (18.0) | 21.2 (17.8) | 18.9 (19.7) | 17.1 (35.6) | 14.5 (8.92) | 13.4 (28.9) | 13.9 (16.0) |
VZ/F [L] | – | 281 (27.7) | 169 (44.3) | 144 (52.2) | 123 (49.8) | 113 (53.3) | 87.9 (14.6) | 124 (48.2) | 110 (16.1) |
CL/F [L/h] | – | 5.82 (23.0) | 4.93 (29.2) | 4.70 (41.2) | 4.50 (36.1) | 4.56 (40.2) | 4.21 (19.5) | 6.44 (53.4) | 5.48 (25.4) |
fe0-72 h [%] | – | 3.00 | 4.03 | 4.93 | 4.21 | 4.55 | 4.75 | 4.88 | 4.25 |