Shen Jianzhong, Li Xiubo, Jiang Haiyang, Hsu Walter H
Department of Pharmacology and Toxicology, College of Veterinary Medicine, China Agriculture University, Beijing, China.
J Vet Pharmacol Ther. 2004 Jun;27(3):163-8. doi: 10.1111/j.1365-2885.2004.00574.x.
A study on bioavailability and pharmacokinetics of florfenicol was conducted in 20 crossbred healthy sheep following a single intravenous (i.v.) and intramuscular (i.m.) doses of 20 and 30 mg/kg body weight (b.w.). Florfenicol concentrations in serum were determined by a validated high-performance liquid chromatography method with UV detection at a wavelength of 223 nm in which serum samples were spiked with chloramphenicol as internal standard. Serum concentration-time data after i.v. administration were best described by a three-compartment open model with values for the distribution half-lives (T(1/2alpha)) 1.51 +/- 0.06 and 1.59 +/- 0.10 h, elimination half-lives (T(1/2beta)) 18.83 +/- 6.76 and 18.71 +/- 1.85 h, total body clearance (Cl(B)) 0.26 +/- 0.03 and 0.25 +/- 0.01 L/kg/h, volume of distribution at steady-state (V(d(ss))) 1.86 +/- 0.11 and 1.71 +/- 0.20 L/kg, area under curve (AUC) 76.31 +/- 9.17 and 119.21 +/- 2.05 microg.h/mL after i.v. injections of 20 and 30 mg/kg b.w. respectively. Serum concentration-time data after i.m. administration were adequately described by a one-compartment open model. The pharmacokinetic parameters were distribution half-lives (T(1/2k(a) )) 0.27 +/- 0.03 and 0.25 +/- 0.09 h, elimination half-lives (T(1/2k(e) )) 10.34 +/- 1.11 and 9.57 +/- 2.84 h, maximum concentrations (C(max)) 4.13 +/- 0.29 and 7.04 +/- 1.61 microg/mL, area under curve (AUC) 67.95 +/- 9.61 and 101.95 +/- 8.92 microg.h/mL, bioavailability (F) 89.04% and 85.52% after i.m. injections of 20 and 30 mg/kg b.w. respectively.
在20只健康杂交绵羊身上进行了一项关于氟苯尼考生物利用度和药代动力学的研究,分别静脉注射(i.v.)和肌肉注射(i.m.)20和30mg/kg体重(b.w.)的氟苯尼考。采用经过验证的高效液相色谱法,在波长223nm处进行紫外检测,以氯霉素为内标物,测定血清中氟苯尼考的浓度。静脉注射给药后的血清浓度 - 时间数据最适合用三室开放模型描述,分布半衰期(T(1/2α))的值分别为1.51±0.06和1.59±0.10小时,消除半衰期(T(1/2β))分别为18.83±6.76和18.71±1.85小时,全身清除率(Cl(B))分别为0.26±0.03和0.25±0.01L/kg/h,稳态分布容积(V(d(ss)))分别为1.86±0.11和1.71±0.20L/kg,静脉注射20和30mg/kg b.w.后曲线下面积(AUC)分别为76.31±9.17和119.21±2.05μg.h/mL。肌肉注射给药后的血清浓度 - 时间数据可用一室开放模型充分描述。药代动力学参数为分布半衰期(T(1/2k(a)))分别为0.27±0.03和0.25±0.09小时,消除半衰期(T(1/2k(e)))分别为10.34±1.11和9.57±2.84小时,最大浓度(C(max))分别为4.13±0.29和7.04±1.61μg/mL,曲线下面积(AUC)分别为67.95±9.61和101.95±8.92μg.h/mL,肌肉注射20和30mg/kg b.w.后的生物利用度(F)分别为89.04%和85.52%。