摘要
采用反相高效液相色谱法(RP-HLPC),研究了(25±1)℃水温条件下单次经口灌注20mg.kg-1双氟沙星(DIF)后,DIF在异育银鲫体内的药代动力学特征及其代谢产物沙拉沙星(SAR)的残留规律。结果表明:DIF在血液及各组织中的药时数据均符合二室开放模型。血液和各组织中均出现重吸收峰现象,肝脏组织达峰浓度最大。其中DIF在血液、肝脏、肾脏、肌肉中吸收半衰期(T1/2α)分别为0.144、0.274、0.137和8.636h;消除半衰期(T1/2β)分别为18.322、26.013、33.066和52.504h;总体清除率(CL)分别为0.082、0.068、0.077和0.058L.h.kg-2;药时曲线下面积(AUC)分别为243.244μg.mL.h-2和294.857、258.587、344.630μg.g.h-2;表观分布容积(Vd)分别为0.676、0.220、0.226和1.258L.kg-1,血浆蛋白结合率为52.39%～64.10%。组织中均可检测到DIF的代谢产物SAR,其中血液中检测到的时间迟于其它组织;根据肌肉组织的DIF和SAR最大残留限量为100和30μg.kg-1,建议DIF休药期为18d以上。
Pharmacokinetics of difloxacin （DIF） and tissue distribution of its metaboiite were estimated with a single dose of 20 mg kg-1 body weight after oral administration in Carassais auratus gibebio at （25.0± 1. 0） ℃ by reversed phase high performance liquid chromatography（RP-HPLC）. The results showed that the kinetic profiles o{ DIF and SAR could described by a two-compartment open model. DIF had reuptake phenomena in plasma and tissues, and the largest concentration appeared in liver. The dis- tribution half-time （T1/2o）, elimination half-time （T1/2β）, body clearance （CL/F）, area under the concen- tration-time curve（AUC） and apparent volume of distribution （Vd/F） of DIF were 0. 144 h. 18. 322 h. O. 082 L. h kg2 .243. 244 μg mL h-2 and O. 676 1 kg1 in plasma, O. 2741 h,26. 0131 h.O. 068 L h kg-2 . 294. 857 μg g h-2 and 0. 2199 1 kg 1 in liver,0. 137 h.33. 066 h.0. 077 L h kg-2 .258. 587 μg g h-1and 0. 226 1 kg-1 in kidney, 8. 636 h.52. 504 h.0. 058 L h kg 2.344. 63μg g h-2 and 1. 258 1 kg-1 in muscle. DIF was 52. 39%-64. 10% bound to plasma protein. SAR, the metabolite of DIF, can be de- tected in the tissues mentioned above, but the time of SAR appeared in plasma lagged behind those of oth- er tissuesrs. According to the maximum residue limit of DIF and SAR in edible tissues, which were 100 and 30μg kg-1 in E. sinensis, the commended withdrawal time of DIF in Carassais auratus gibebio was 18 days at least.
出处
《中国海洋大学学报（自然科学版）》
CAS
CSCD
北大核心
2012年第11期81-86,共6页
Periodical of Ocean University of China
基金
淡水鱼类出血性疾病综合防治技术集成示范项目(200803013)
国家自然科学基金项目(31172430)
鱼虾用疫苗与药物研究开发项目(2011AA10A216)资助
