Pharmacokinetics and Bioavailability of Terbinafine Hydrochloride Capsules in Beagle Dogs
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    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: AUC0-∞ =(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, AUC0-∞ =(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.

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WANG Ang, DING Huan-zhong, GAO Yan,GAO Guo-feng, ZENG Zhen-ling. Pharmacokinetics and Bioavailability of Terbinafine Hydrochloride Capsules in Beagle Dogs[J]. Journal of South China Agricultural University,2012,33(4):556-560

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  • Received:February 20,2012
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  • Online: November 16,2012
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