Parametera
Intravenous 2.5 mg/kg of Etravirine
Oral 200 mg/kg of Intelence
®
Oral 25 mg/kg of Formulation #59
Oral 50 mg/kg of Formulation #59
Number of Animals
6
5
8
8
C
max
(ng/mL)
2364 ± 1122
27.97 ± 11.9
222.3 ± 150
228.2 ± 169
AUC(ng h/mL)
1918±193
194.1 ± 74.2
1047 ± 654
1664 ± 1107
T
1/2
(h)
5.69± 0.75
5.65 ± 2.81
3.15 ±1.76
4.08 ± 1.43
V
ss
/F (mL/kg)
8.70 ± 1.4
8.0 ± 5.7
127 ± 79
207 ± 107
CL/F (mL/hr/kg)
1.05± 0.1
0.92 ± 0.17
29.0 ±10.4
36.3 ± 16.1
F
absolute
-
0.126%
5.45%
4.33%
F
relative
-
-
4,315%
3,429%
Table 4:
Pharmacokinetics of etravirine following intravenous administration of pure etravirine solution or oral administration of formulation #59 versus the commercial Intelence
®
product to male SD rats.
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