Abstract:
To study the pharmacokinetics and biavailibility of terbinafine hydrochloride capsules in beagle dogs, a single intravenous (i.v.) and oral(p.o.) administration of terbinafine at a dosage of 10 mg·kg
-1 was performed in eight healthy beagles according to a two-period crossover design. Plasma concentrations of terbinafine were determined by a reverse phase high performance liquid chromatographic method. The pharmacokinetic parameters were calculated by noncompartmental analysis with WinNonlin 5.2.1 software. After intravenous administration, the main pharmacokinetic parameters were as follows: AUC
0-∞ =(5.47±1.03) μg·mL
-1·h,
Vss =(2.55±0.89) L·kg
-1, CL=(1.88±0.33) L·h
-1·kg
-1,
t1/2 =(3.02±1.70) h; whereas after oral dosing, the main pharmacokinetic parameters were as follows:
tmax =(1.09±0.37) h,
Cmax =(0.39±0.04)μg·mL
-1, AUC
0-∞ =(0.67±0.18) μg·mL
-1·h,
Vd/F =(35.17±6.58) L·kg
-1,
t1/2 =(1.69±0.74) h. The absolute bioavailibilty(
/F) of terbinafine hydrochloride capsules after oral administrtion was (12.54±3.43)%.Terbinafine was absorbed and eliminated rapidly in beagles and the absolute bioavailability was very low.