Table 6.
Pharmacokinetics of doxycycline and MAL5166 in monkeysa
| Compound | i.v. dose (mg/kg) | Cmax (μg/ml) | Tmax (h) | AUC(0-∞) (h · μg/ml) | t1/2 (h) | Vss (ml/kg) | CL (ml/min/kg) | %Fb |
|---|---|---|---|---|---|---|---|---|
| Doxycyclinec | 5 | 11.1 | 0.25 | 19.9 | 2.86 | 780 | 4.2 | 101 |
| MAL5166 | 5 | 42.5 (5.00) | 0.0 (0.00) | 51.5 (5.72) | 11.8 (0.785) | 1,309 (190) | 1.6 (0.173) | 35.5 |
a
Pharmacokinetic studies were performed as described in Materials and Methods. All pharmacokinetic values, except %F, were calculated using data from the i.v. dose. The i.v. dose was administered as a 15-min infusion. Data are means (standard deviations).
b
%F (oral bioavailability) was calculated based on ratio between the i.v. and oral AUC exposure values.
c
Insufficient animal numbers did not allow for meaningful statistical analysis of the doxycycline data.