氟苯尼考3种不同给药方式在中国明对虾体内的药代动力学研究

Single dose pharmacokinetics of florfenicol in Fenneropenaeus chinensis

用高效液相色谱法研究静注、肌注和口服氟苯尼考在中国明对虾(Fenneropenaeuschinensis)体内的药代动力学特征,所得数据用MCP-KP程序分析。结果表明,3种给药方式的血药经时过程均符合二室开放模型,符合一级吸收二项指数方程,血窦注射、肌肉注射、口服药饵的时间对药物质量浓度的理论方程分别是:C血注=16.38e-2.58t+0.32e-0.1t,C肌注=18.7e-2.57t+0.26e-0.12t,C药饵=15.08e–1.49t+0.65e-0.09t–15.74e–10.38t。主要药物代谢动力学参数分别是:吸收半衰期(t(1/2)α)为0.269,0.270和0.465h,消除半衰期(t(1/2)β)为6.921,6.494和7.903h,表观分布容积(Vβ)为1.287,1.293和2.421L/kg,总体清除率(Cs)为0.129,0.138和0.213L/(h·kg),药时曲线下总面积(Au,c)为0.755,0.681和0.666L/(h·kg)。肌肉注射和口服给药的生物利用度(F)分别是90.20%和97.58%。

The pharmacokinetics of intravenously, intramuscularly and orally administered florfenicol were determined in Fenneropenaeus chinensis.The study was performed at 19-22 ℃ .A dose of 15mg/kg body mass was administered either intravenously or intramuscularly. The oral dose wasl 3.56 mg/kg body mass. At 8-10 time points, from 0.083 h to 24 h after administration, blood was sampled from 8 individual shrimps in each group. The plasma was assayed for florfenicol using an HPLC method. The pharmacokinetic modling of the results was performed using the computer program MCP-KP. Following the three administrations, the plasma concentration -time data of florfenicol were all best described by two-compartment open model. The important parameters of intravenous, intramuscular and oral administrations were listed. The volumes of distribution（ Vβ）were 1.287,1.293,2.421 L/kg, the total body clearance（Cs）was 0.129,0.138,0.213 L/（h·kg）, the elimination halflives （t（1/2）β） were 5.91,7.57,8.01 h, the peak plasma concentrations（Cmax） were 6.970,6.396,2.772 mg/L,and were estimated to occur at 0.206,0.239,0.605 h （Tmax） following dosing. The bioavailabilities （F） of intramuscular and oral administrations were 90.20% and 97.58%.