Table 6. FBZ pharmacokinetic parameters following 5 days of dosing.
Group | Day | Treatment | Cmax| (μg/mL) |
tmax^ (h) |
terminal t1/2ℵ (h) | AUClast # (μg.h/mL) | H-FBZ /FBZ AUC ratio | R-FBZ/FBZ AUC ratio |
---|---|---|---|---|---|---|---|---|
A2 | 5 | 10mg/kg QD 5x SC | 0.04 | 3 | 648 | 9.9 | 0.6 | 0.2 |
A3 | 1 | 10mg/kg QD 1x SC | 0.07 | 1 | 332 | 5.3 | 0.3 | 0.1 |
A4 | 5 | 0.2mg/kg QD 5x OR | 0.03 | 0.5 | 4 | 0.12 | 0.4 | 0.2 |
A5 | 5 | 1.5mg/kg QD 5x OR | 0.3 | 0.5 | 0.5 | 0.72 | 0.7 | 0.4 |
B2 | 5 | 15mg/kg QD 5x OR | 2.91 | 1.0 | 2 | 10.3 | 0.55 | 0.40 |
C3 | 1 | 2mg/kg 1x OR |
0.4 | 0.5 | 2 | 1.4 | 0.5 | 0.4 |
C4 | 1 | 40mg/kg 1x OR |
3.7 | 0.5 | 3.5 | 14 | 0.4 | 0.6 |
*A = O. ochengi adult implant experiment A, B = O. ochengi adult implant experiment B, C = B. malayi mf infusion experiment
|Cmax: highest observed plasma concentration
^tmax: time point when Cmax is observed
#AUClast: Area Under the plasma concentration vs. time curve (last: last time point where plasma concentration is measured); H-FBZ: hydrolysed FBZ; R-FBZ: reduced FBZ
ℵ terminal t1/2: Apparent terminal elimination half-life (estimated graphically from simulated PK profiles)