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Pharmacokinetic Disposition of Triclabendazole in Cattle and Sheep; Discrimination of the Order and the Rate of the Absorption Process of Its Active Metabolite Triclabendazole Sulfoxide

Pharmacokinetic Disposition of Triclabendazole in Cattle and Sheep; Discrimination of the Order and the Rate of the Absorption Process of Its Active Metabolite Triclabendazole Sulfoxide

N Mestorino, E A Formentini, M F Lucas, C Fernandez, P Modamio, E Mariño Hernández, J O Errecalde

Vet Res Commun. 2008 Jan;32(1):21-33.

PMID: 17457687

Abstract:

A comparative pharmacokinetic study was conducted to determine the order and the rate of absorption of triclabendazole (TCBZ) in cattle and sheep. A commercial suspension of TCBZ (Biofasiolex, Biogénesis S.A., Argentina) was administered at a dose rate of 10 mg/kg by the oral route to six Holstein female calves and six Corriedale female sheep. The plasma concentration profiles of the metabolites triclabendazole sulfoxide (TCBZ-SO) and triclabendazole sulfone (TCBZ-SO(2)) were analysed by means of the non-compartmental method. The order of the absorption process of the active metabolite, TCBZ-SO, was determined by construction of curves of cumulative absorbed fraction of the drug by means of the Wagner-Nelson method. The appearance of TCBZ-SO in plasma of cattle and sheep resembles the entry of a constant quantity of drug into the organism per unit time. This is explained by the reservoir effect of the rumen, which acts as a biological slow-release system for TCBZ-SO and its precursor TCBZ to the posterior digestive tract where they are absorbed. The plasma concentration profiles of TCBZ-SO in both species were well described by a one-compartment open model with zero-order process of absorption and first-order process of elimination. The values of AUC(0-infinity) and C(max) of TCBZ-SO did not differ between species, while other kinetic parameters except for lambda(z) had higher values in calves than in sheep. In the case of TCBZ-SO(2), t(max) was the only parameter that did not differ between species, while other kinetic parameters except for lambda(z) had higher values in calves than in sheep.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP100648133	Triclabendazole sulfoxide		100648-13-3	Price

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