Pharmacokinetics of oxolinic acid and Oxytetracycline in kuruma shrimp, Penaeus japonicus
Pharmacokinetics of oxolinic acid and Oxytetracycline in kuruma shrimp, Penaeus japonicus
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DOI：
10.1016/j.aquaculture.2003.10.007
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发表时间：
2004-02
期刊：
影响因子：
4.5
通讯作者：
K. Uno
中科院分区：
文献类型：
--
作者：
K. Uno
研究了恶喹酸（oxolinic acid）和土霉素（oxytetracycline）经鼻内（10和25 mg/kg）和口服（50 mg/kg）给药后在日本对虾（Penaeuscirca）体内的药代动力学。这些虾被保存在装有盐度为22 - 23 ppt的再循环人工海水的水槽中。水温保持在25 ± 0.6 °C。窦内给药后两种药物的血淋巴浓度最好用二室开放模型描述。恶喹酸的分布和消除半衰期（t1/2α和t1/2β）分别为0.59和33.2 h，土霉素的分布和消除半衰期分别为0.45和24.7 h。稳态表观分布容积（Vss）和全身清除率（CLb）估计分别为1309 ml/kg和28.8 ml/kg/h（恶喹酸）和748 ml/kg和22.7 ml/kg/h。经口给药后的血淋巴浓度-时间曲线未通过非线性最小二乘法拟合，该方法使用一室和二室模型，两种药物均为一级吸收。恶喹酸的血淋巴峰浓度（Cmax）、血淋巴浓度达峰时间（tmax）和消除半衰期分别为17.8 µg/ml、7 h和34.3 h，土霉素为24.3 µg/ml、10 h和33.6 h。口服给药后，恶喹酸的生物利用度（F）为32.9%，土霉素为43.2%。恶喹酸和土霉素的体内血淋巴蛋白结合率分别为36.7 ± 8.5%和22.9 ± 4.8%。
The pharmacokinetics of oxolinic acid and oxytetracycline were examined in kuruma shrimp(Penaeus japonicus)after intra-sinus (10 and 25 mg/kg, respectively) and oral (50 mg/kg) administration. The shrimp were kept in tanks with recirculated artificial seawater at a salinity of 22−23 ppt. The water temperature was maintained at 25 ± 0.6 °C. The hemolymph concentrations of both drugs after intra-sinus dosing were best described by a two-compartment open model. The distribution and elimination half-lives (t1/2αand t1/2β) were found to be 0.59 and 33.2 h for oxolinic acid and 0.45 and 24.7 h for oxytetracycline, respectively. The apparent volume of distribution at a steady state (Vss) and total body clearance (CLb) were estimated to be 1309 ml/kg and 28.8 ml/kg/h for oxolinic acid and 748 ml/kg and 22.7 ml/kg/h, respectively. The hemolymph concentration–time curves after oral administration did not fit by the nonlinear least squares method using one- and two compartment model with first-order absorption in either of the drugs. The peak hemolymph concentration(Cmax),the time to peak hemolymph concentration(tmax)and the elimination half-life were found to be 17.8 µg/ml, 7 h and 34.3 h for oxolinic acid and 24.3 µg/ml, 10 h and 33.6 h for oxytetracycline, respectively. The bioavailability (F) after oral administration was 32.9% for oxolinic acid and 43.2% for oxytetracycline. The hemolymph protein binding in vivo was determined to be 36.7 ± 8.5% for oxolinic acid and 22.9 ± 4.8% for oxytetracycline.