TABLE 1

Pharmacokinetic parameters obtained for ketoconazole in the monkey after either intravenous or intraduodenal administration All data are expressed as mean ± standard deviation for n = 3 monkeys per dose.


Parameter

Intravenous

Intraduodenal
Portal

Systemic
Dose (mg/kg) 0.98 ± 0.07 10.2 ± 0.1
Cmax (ng/ml) 961 ± 20 13,853 ± 2828 1259 ± 628
Tmax (min) -a 8.33 ± 5.77 30 ± 0
AUC (min · μg/ml) 78.4 ± 9.8 407 ± 106 116 ± 45
DNAUC (min · kg/l) 80.1 ± 7.1 28.5 ± 5.8 11.4 ± 4.4
CL (ml/min/kg) 12.5 ± 1.2 -
Vdss (l/kg) 0.661 ± 0.119 -
Half-life (min) 50.6 ± 6.5 -
MRT (min) 53.3 ± 12.0 -
Absorption (%)b - 55.2 ± 11.2
Hepatic extraction (%)b - 61.1 ± 6.9
Bioavailability (%)
-

22.0 ± 8.5

  • a -, not calculated for this route of administration

  • b Estimated based on portal and systemic data using the method of Ward et al. (2001)