Table 4.
Parameter | Cohort 1 q4 h |
Cohort 2 q2 h |
Cohort 3 q1 h |
Cohort 4 q0.5 h |
||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|
n | Mean | CV% | n | Mean | CV% | n | Mean | CV% | n | Mean | CV% | |
Cmax1 (ng/ml) | 6 | 0.337 | 62.84 | 6 | 0.549 | 40.59 | 6 | 0.477 | 35.25 | 6 | 0.369 | 54.09 |
Cmax1/D (ng/ml/µg) | 6 | 0.00673 | 62.84 | 6 | 0.0110 | 40.59 | 6 | 0.00955 | 35.25 | 6 | 0.00738 | 54.09 |
Tmax1 (h) | 6 | 0.16 | 101.80 | 6 | 0.08 | 0.00 | 6 | 0.08 | 0.00 | 6 | 0.13 | 50.02 |
Cmaxn (ng/ml) | 6 | 0.633 | 14.36 | 6 | 0.731 | 26.84 | 5 | 0.893 | 26.94 | 6 | 0.815 | 18.78 |
Cmaxn/D (ng/ml/µg) | 6 | 0.0127 | 14.36 | 6 | 0.0146 | 26.84 | 5 | 0.0179 | 26.94 | 6 | 0.0163 | 18.78 |
Tmaxn (h) | 6 | 0.08 | 0.00 | 6 | 0.09 | 7.92 | 5 | 0.09 | 8.62 | 6 | 0.09 | 18.26 |
AUC0–tau1 (h·ng/ml) | 6 | 0.3298 | 25.40 | 6 | 0.3020 | 11.27 | 6 | 0.2182 | 25.41 | 6 | 0.1093 | 34.27 |
AUC0–tau1/D (h·ng/ml/µg) | 6 | 0.00660 | 25.40 | 6 | 0.00604 | 11.27 | 6 | 0.00436 | 25.41 | 6 | 0.00219 | 34.27 |
AUC0–taun (h·ng/ml) | 6 | 0.6133 | 21.55 | 6 | 0.6106 | 18.59 | 5 | 0.3964 | 21.95 | 6 | 0.2578 | 10.19 |
AUC0–taun/D (h·ng/ml/µg) | 6 | 0.0123 | 21.55 | 6 | 0.0122 | 18.59 | 5 | 0.00793 | 21.95 | 6 | 0.00516 | 10.19 |
AUC0–t (h·ng/ml) | 6 | 2.139 | 26.38 | 6 | 2.400 | 24.23 | 5 | 2.211 | 34.50 | 6 | 2.286 | 17.34 |
AUC0–t/D (h·ng/ml/µg) | 6 | 0.0143 | 26.38 | 6 | 0.0160 | 24.23 | 6 | 0.0146 | 31.32 | 6 | 0.0152 | 17.34 |
AUC0–inf (h·ng/ml) | 1 | 2.882 | 0.00 | 5 | 2.628 | 28.25 | 4 | 2.358 | 40.07 | 6 | 2.517 | 17.65 |
AUC0–inf/D (h·ng/ml/µg) | 1 | 0.0192 | 0.00 | 5 | 0.0175 | 28.25 | 4 | 0.0157 | 40.07 | 6 | 0.0168 | 17.65 |
t1/2 (h) | 1 | 6.90 | 0.00 | 5 | 5.13 | 43.75 | 4 | 4.69 | 34.84 | 6 | 5.42 | 17.33 |
CL (L/h) | 1 | 52.05 | 0.00 | 5 | 61.48 | 32.25 | 4 | 72.29 | 40.05 | 6 | 61.22 | 18.02 |
Vz (L) | 1 | 518.2 | 0.00 | 5 | 413.3 | 28.35 | 4 | 439.7 | 10.99 | 6 | 468.4 | 11.08 |
6 | 3.08 | 79.40 | 6 | 1.57 | 49.04 | 5 | 2.19 | 57.13 | 6 | 2.72 | 50.85 | |
6 | 1.90 | 18.15 | 6 | 2.04 | 18.10 | 5 | 1.89 | 17.72 | 6 | 2.57 | 33.14 |
IV intravenous, q every, CV coefficient of variation, Cmax1 maximum plasma concentrations after first dose, D dose, Tmax1 time of the maximum plasma concentration after first dose, Cmaxn maximum plasma concentrations after last dose, Tmaxn time of the maximum plasma concentration after last dose, AUC0–tau1 area under the plasma concentration time curve during the first dosing interval, calculated using the linear-log trapezoidal rule, AUC0–taun area under the plasma concentration time curve during the last dosing interval, calculated using the linear-log trapezoidal rule, AUC0–t area under the plasma concentration–time curve from time–zero to the time of the last quantifiable concentration, calculated using the linear-log trapezoidal rule, AUC0–inf area under the plasma concentration–time curve from time–zero extrapolated to infinity, t1/2 apparent elimination half-life in the terminal phase by noncompartmental analysis, accumulation ratio of Cmax, accumulation ratio of AUCtau