Lakritz Jeffrey, Linden Daniel, Anderson David E, Specht Terri A
Department of Veterinary Clinical Sciences, College of Veterinary Medicine, The Ohio State University, Columbus, OH, USA,
Department of Agriculture and Engineering Technologies, College of Food, Agriculture and Environmental Sciences, The Ohio State University, Wooster, OH, USA.
Vet Med (Auckl). 2015 Feb 19;6:71-81. doi: 10.2147/VMRR.S77255. eCollection 2015.
The objective of this study was to determine plasma pharmacokinetics and bioavailability of fenbendazole (FBZ) and oxfendazole (OFZ) after intravenous (iv) and oral administrations of FBZ (5 mg/kg) to alpacas. Plasma concentrations of FBZ and OFZ after administration of FBZ iv and orally (5 mg/kg) were determined by high-performance liquid chromatography with ultraviolet detection. Total clearance (CL) of FBZ was 16.5±4 mL/kg/min (range: 4-31 mL/kg/min), and steady-state volume of distribution (d) was 3.3±1 L/kg (range: 1.7-7.4 L/kg). The terminal phase half-life of FBZ after iv administration was 5.9±3.8 hours (range: 0.8-20 hours). After oral administration, the FBZ terminal phase half-life was 23±5 hours (range: 9-37 hours) and the systemic bioavailability of FBZ was 16%±6% (range: 1%-41%). Peak FBZ concentrations after oral administration were 0.13±0.05 µg/mL (range: 0.05-0.28 µg/mL) at 10 hours (range: 8-12 hours). Peak plasma OFZ concentrations after oral dosing with FBZ (5 mg/kg) were 0.14±0.05 µg/mL (0.05-0.3 µg/mL) at 24±7 hours (range: 12-48 hours). FBZ clearance is lower in comparison to that of other species. Systemic availability of FBZ after oral administration is low after oral dosing. Metabolites of FBZ produced by alpacas are similar to those observed in other species.
本研究的目的是确定给羊驼静脉注射（iv）和口服芬苯达唑（FBZ）（5mg/kg）后，芬苯达唑（FBZ）和奥芬达唑（OFZ）的血浆药代动力学及生物利用度。通过高效液相色谱-紫外检测法测定静脉注射和口服（5mg/kg）FBZ后FBZ和OFZ的血浆浓度。FBZ的总清除率（CL）为16.5±4mL/kg/min（范围：4-31mL/kg/min），稳态分布容积（d）为3.3±1L/kg（范围：1.7-7.4L/kg）。静脉注射后FBZ的终末相半衰期为5.9±3.8小时（范围：0.8-20小时）。口服给药后，FBZ的终末相半衰期为23±5小时（范围：9-37小时），FBZ的全身生物利用度为16%±6%（范围：1%-41%）。口服给药后FBZ的峰值浓度在10小时（范围：8-12小时）时为0.13±0.05μg/mL（范围：0.05-0.28μg/mL）。口服FBZ（5mg/kg）后，OFZ的血浆峰值浓度在24±7小时（范围：12-48小时）时为0.14±0.05μg/mL（0.05-0.3μg/mL）。与其他物种相比，FBZ在羊驼体内的清除率较低。口服给药后FBZ的全身利用率较低。羊驼产生的FBZ代谢物与其他物种中观察到的代谢物相似。
