马波沙星在罗非鱼体内的药物代谢动力学研究

摘要

Objective] To study the pharmacokinetics characteristics of marbofloxacin in tilapia ( Oreo-chromis niloticus) , and provide references for rational clinical drug usage.[Method]The tilapia were di-vided into two groups for intramuscular ( i. m. ) and oral administrations, and each fish received marbo-floxacin at a dosage of 10 mg·kg-1 body mass. Water temperature was maintained at 30 ℃. The con-centration of marbofloxacin in plasma was measured using high performance liquid chromatography ( HPLC) combined with fluorescence detection. The plasma drug concentration-time data were analyzed by the non-compartment model of WinNonlin 6. 1 software.[Result]After i. m. administration, marbo-floxacin absorption and elimination were relatively faster, and it was widely distributed throughout the body. Peak time of plasma concentration ( tmax ) was 0. 25 h, the maximum plasma concentration (ρmax ) was 4. 31 μg·mL-1 , the elimination half-life ( t1/2λz ) was 19. 21 h, the volume of distribution was 3. 94 L·kg-1 and the area under the plasma concentration-time curve ( AUC) was 70. 36 μg·mL-1·h-1 . Fol-lowing oral administration, marbofloxacin absorption and elimination were relatively slower, and it was widely distributed throughout the body. tmax was 4. 00 h, ρmax was 2. 45 μg·mL-1 , t1/2λz was 22. 67 h, the volume of distribution was 4. 27 L·kg-1 and AUC was 76. 66 μg·mL-1 ·h-1 .[Conclusion]Using 10 mg·kg-1 marbofloxacin could effectively control susceptible micro-organisms involved in most com-mon infections in tilapia.%【目的】研究马波沙星在罗非鱼Oreochromis niloticus体内的药物代谢动力学(简称药动学)特征,为临床合理用药提供参考。【方法】将罗非鱼随机分成2组,水温维持在30℃,以10 mg · kg-1分别单剂量肌内注射和口服给药,高效液相色谱( HPLC)-荧光检测法测定血浆中马波沙星的质量浓度,用WinNonlin 6．1药动学软件的“非房室模型”分析药动学参数。【结果】肌内注射马波沙星后,药物吸收和消除均较口服快,体内分布广泛。达峰时间( tmax )为0．25 h,峰质量浓度(ρmax )为4．31μg · mL-1,消除半衰期( t1/2λz )为19．21 h,表观分布容积为3．94 L·kg-1,药-时曲线下面积( AUC)为70．36μg·mL-1·h-1。口服马波沙星后,药物吸收和消除均较慢,体内分布广泛。 tmax为4．00 h,ρmax为2．45μg · mL-1, t1/2λz为22．67 h,表观分布容积为4．27 L · kg-1, AUC 为76．66μg·mL-1·h-1。【结论】10 mg·kg-1马波沙星能够有效治疗大多数敏感菌引起的罗非鱼感染。