title: A high oxfendazole dose to control porcine cysticercosis: pharmacokinetics and tissue residue profiles.
abstract: Oxfendazole (OFZ) is efficacious for porcine cysticercosis at 30 mg/kg. OFZ is not registered to be used at this dose. The assessment of the OFZ and metabolites [(fenbendazole sulphone (FBZSO2), fenbendazole (FBZ)] plasma pharmacokinetic and tissue residue profiles after its oral administration to pigs and the withdrawal period for human consumption were reported. Forty-eight pigs allocated into two groups received OFZ (30 mg/kg) orally as a commercial (CF) or as experimental formulation (SMF). Samples (blood, muscle, liver, kidney and fat) were collected over 30 days post-treatment and analyzed by HPLC. OFZ was the main compound recovered in plasma, followed by FBZSO2 and low FBZ concentrations. OFZ AUC0-LOQ (209.9±33.9 μg·h/ml) and Cmax (5.40±0.65 μg/ml) parameters for the CF tended to be higher than those for the SMF (AUC0-LOQ: 159.4±18.3 μg h/ml, Cmax: 3.80±0.35 μg/ml). The highest total residue (OFZ+FBZSO2+FBZ) concentrations were quantified in liver, followed by kidney, muscle and fat tissue. FBZSO2 residue levels were the highest found in muscle (0.68±0.39 μg/g) and fat (0.69±0.39 μg/g). In liver and kidney the highest residues corresponded to FBZ (5.29±4.36 μg/g) and OFZ (2.86±0.75 μg/g), respectively. A withdrawal time of 17 days post-treatment was established before tissues are delivered for human consumption.
authors: Laboratorio de Farmacología, Facultad de Ciencias Veterinarias, Universidad Nacional del Cent de la Provincia de Buenos Aires y Centro de Investigación Veterinaria de Tandil (CIVETAN), CONICET, Tandil, Argentina. lmoreno@vet.unicen.edu.ar
authors: L
authors: L
authors: Moreno
authors: M T
authors: MT
authors: Lopez-Urbina
authors: C
authors: C
authors: Farias
authors: G
authors: G
authors: Domingue
authors: M
authors: M
authors: Donadeu
authors: B
authors: B
authors: Dungu
authors: H H
authors: HH
authors: García
authors: L A
authors: LA
authors: Gomez-Puerta
authors: C
authors: C
authors: Lanusse
authors: A E
authors: AE
authors: González
mesh_terms: D000273:Adipose Tissue / Q000737:chemistry; D000818:Animals; D000871:Anthelmintics / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000627:therapeutic use*; D019540:Area Under Curve; D001562:Benzimidazoles / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000627:therapeutic use*; D003551:Cysticercosis / Q000188:drug therapy / Q000473:pathology / Q000662:veterinary*; D004305:Dose-Response Relationship, Drug; D004350:Drug Residues / Q000032:analysis*; D005260:Female; D006207:Half-Life; D007668:Kidney / Q000737:chemistry; D008297:Male; D018482:Muscle, Skeletal / Q000737:chemistry; D013552:Swine; D013553:Swine Diseases / Q000188:drug therapy* / Q000469:parasitology
chemical_list: D000871:Anthelmintics; D001562:Benzimidazoles; C011030:oxfendazole