Parameter | Riociguat 1 mg | Riociguat 2.5 mg | ||||
Geometric mean | CV % | Range | Geometric mean | CV % | Range | |
AUC μg·h·L−1 | 602.3 | 14.9 | 456.5–749.6 | 1411 | 39.2 | 597.5–3121 |
Cmax μg·L−1 | 59.43 | 5.9 | 53.49–65.05 | 119.4 | 16.1 | 74.69–172.4 |
tmax h | 0.750# | 0.500–1.500 | 0.500# | 0.250–1.500 | ||
t1/2 h | 9.953 | 8.6 | 8.737–12.14 | 11.65 | 38.6 | 4.680–28.58 |
Vz/f L·kg−1 | 0.354 | 7.3 | 0.307–0.393 | 0.378 | 20.7 | 0.005–0.609 |
CL/f L·h−1 | 1.660 | 14.9 | 1.334–2.191 | 1.771 | 39.2 | 0.801–4.184 |
Subjects valid for pharmacokinetic and pharmacodynamic analysis; n = 15 (n = 5 in 1 mg dose group and n = 10 in 2.5 mg dose group). CV: coefficient of variance (geometric); AUC: area under plasma concentration/time curve from zero to infinity after single dose; Cmax: maximum drug concentration in plasma after single-dose administration; tmax: time to reach maximum drug concentration in plasma; t1/2: terminal elimination half-life; Vz/f: apparent volume of distribution during terminal phase after oral administration; CL/f: total body clearance of drug from plasma calculated after oral administration. #: median.