给药剂量对氟苯尼考在中华绒鳌蟹体内的药物代谢动力学影响

Pharmacokinetics of Florfenicol in the Chinese Mitten-handed Crab (Eriocheir sinensis):Dose Effect

在17℃水温下,单次肌肉注射给药,高效液相色谱法-荧光法测定中华绒螯蟹(Eriocheir sinensis)血淋巴、肌肉和肝中药物残留浓度,利用3P97药代动力学软件分析数据,研究不同剂量氟苯尼考在中华绒螯蟹血淋巴、肌肉和肝组织中的代谢规律及组织分布。结果表明,在3种(5.0、10.0、20.0mg/kg)给药剂量下,血淋巴和肌肉组织中氟苯尼考含量瞬时达到峰值,而肝中氟苯尼考含量则随给药时间,先上升后下降,各组织含量从大到小依次为:肌肉、血淋巴、肝。应用药代动力学计算软件3P97分析结果表明,血淋巴、肌肉、肝组织中氟苯尼考的代谢规律均符合二室开放模型,以3个浓度给药后,血淋巴中氟苯尼考的吸收半衰期(T1/2α)及消除半衰期(T1/2β)分别为0.04、0.21、0.87h和0.60、1.48、3.29h,整体清除率(CLs)分别是2.17、1.99和2.12ml/(kg·h),肌肉中氟苯尼考的T1/2α及T1/2β分别是1.38、0.93、0.47h和10.39、31.78、23.91h,CLs分别是0.07、0.03、0.03ml/(kg·h),肝中氟苯尼考的T1/2α及T1/2β分别是0.69、0.07、0.12h和0.73、4.90、4.49h,CLs分别是1.79、2.55、3.89ml/(kg·h)。

The pharmacokinetics of florfenicol （FF） after intramuscular injection was investigated in the Chinese Mitten-handed Crab （ Eriocheir sinensis） at 17℃ . Hemolymph,muscle and liver samples were obtained and analyzed by a high-performance liquid chromatography with fluorescence detection method, and the corresponding pharmacokinetic parameters were calculated with the 3P97 software. The florfenicol level in hemolymph and muscle reached maximum momentarily,while that in liver reached a maximum then declined at three administration doses （5. 0,10. 0,20. 0 mg /kg）. The kinetic profile of florfenicol in hemolymph,muscle and liver was conformed to a two-compartment model. The important parameters were listed. When three doses were injected,the absorption half-lives （ T1/2α ） and the elimination half-lives （ T1/2β ） in hemolymph were 0. 04,0. 21,0. 87 and 0. 60,1. 48,3. 29 h,respectively,and the total body clearance （ CLs） were 2. 17, 1. 99 and 2. 12 ml /（kg·h）,respectively; the T1/2α and T1/2β in muscle were 1. 38,0. 93,0. 47 h and 10. 39, 31. 78,23. 91 h,respectively,and the CLs were 0. 07,0. 03 and 0. 03 ml /（ kg·h）,respectively; the T1/2α and T1/2β in liver were 0. 69,0. 07,0. 12 h and 0. 73,4. 90,4. 49 h,respectively,and the CLs were 1. 79, 2. 55,and 3. 89 ml /（kg·h）,respectively.