诺氟沙星在大黄鱼体内的药代动力学及残留研究  

Pharmacokinetics and residues of norfloxacin in Pseudosciaena polyactis

作　　者：刘玉林[1] 王翔凌[2] 杨先乐[2] 杨勇[2] 

机构地区：[1]长江大学动物科学学院,湖北荆州434025 [2]上海水产大学上海高校水产养殖学E-研究院农业部渔业动植物病原库,上海200090

出　　处：《水产学报》2007年第5期655-660,共6页Journal of Fisheries of China

基　　金：国家"十五"渔业科技攻关计划项目(2004BA526B0504);上海市教育委员会E-研究院建设资助项目(E03009);上海市重点学科建设资助项目(Y1101)

摘　　要：在试验水温（22±2）℃时，按10mg·kg^-1的剂量给大黄鱼单次口服诺氟沙星后，用高效液相色谱法测定血浆和组织中的药物浓度，研究了诺氟沙星在大黄鱼体内的代谢及消除。结果表明血药时间数据符合一级吸收二室开放模型，吸收分布迅速，但消除缓慢，半衰期（T1/2Ka、T1／2α、T1／2β）分别为0．7030、2．0926、154．3265h，最大血药浓度为0．8864μg·mL^-1，达峰时间为2．0914h，药时曲线下面积（AUC）为97．8038μg·h·mL^-1。组织中肝脏的药物浓度最高，在测定的时间里各组织的药物浓度高于血浆。药物消除速度依次为：肾脏、肝脏、肌肉，消除半衰期分别为135．88、173．25、223．55h，肌肉作为可食性组织，且消除最慢，因此选取肌肉组织作为残留检测的靶组织，以50μg·kg^-1为最高残留限量，因此在本试验条件下，建议休药期不低于23d；在治疗大黄鱼细菌性疾病时，以诺氟沙星10mg·kg^-1剂量给药，一般1d 1次，连用2～3d。In order to study the metabolism and elimination of norfloxacin （NFLX） in Pseudosciaena polyactis, single oral administration （10 mg· kg^-1 b. w ） of NFLX has been investigated in healthy Pseudosciaena polyactis at （22 ±2 ） ℃. The medicine was extracted by methanol from plasma and perchloric acid （6%） from tissues. NFLX was determined by high performance liquid chromatography（HPLC）. The mobile phase was methanol, 0.05 mol · L^-1 phosphate buffer and 0.05 mol · L^-1 terabutyl ammonium bromide （24.5/73.5/2, V/V/V） adjusted to pH 2.0 with phosphoric acid. The ZORAX SB-C18 column was used and ultraviolet detector was 280 nm. The mean recoveries were all higher than 88. 73% for samples and inter-day CV for plasma and tissues were all under 9.75 %. The sensitivity was 0.01 μg·mL^-1. The result demonstrated： Plasma concentration-time data of NFLX were best fitted using a two- compartmental open model, absorption and distribution were fast but elimination was slow, with absorption, distribution and elimination half-life of 0. 703 0, 2. 092 6 and 154. 326 5 h, respectively. The maximal plasma concentration was 0. 886 4 μg·mL^-1, peaking at 2. 091 4 h after dosing. Area under the plasma drug concentration-time curve from 0 to ∞ was 97. 803 8 μg·h· mL^-1. The concentration of NFLX was higher than other tisssues and all tissues＇ concentration is higher than plasma at the same time. The speed from fast to slow is kidney, liver, muscle with elimination half-life of 135. 88,173. 25,223. 55 h, respectively. As an edible tissue, muscle had a slowest depletion, so muscle was selected as target tissue in this experiment. According to the maximum residue limit（MRL） of 50 μg· kg^-1 in muscle, the withdrawl period should not be less than 23 d under this experiment condition; then the scheme of NFLX is established to fish bacterial disease, that is,the dose orally is 10 mg·kg^-1, at the intervals of 24 h for 2 ～3 times. This study had theory value to application of norfloxacin （NFLX

关 键 词：大黄鱼 药代动力学 诺氟沙星 残留 

分 类 号：S948[农业科学—水产养殖] R969.1[农业科学—水产科学]