采用液相色谱串联质谱法,研究通过单剂量口灌给药,对甲砜霉素在鲫(Carassius auratus)体内的药代动力学进行研究,为甲砜霉素在鲫疾病预防和治疗方面提供理论基础。给药剂量为30 mg/kg体重,实验水温(20±0.2)℃,鲫平均体重(40.70±7.87)g。取给药后0.25、0.5、1、1.5、2、4、6、8、12、24、36、48、72 h鲫的肌肉、血浆、肝脏、肾脏,测定各组织中甲砜霉素的浓度,用药动学3p97软件进行数据的处理和分析。结果表明:甲砜霉素在鲫体内吸收分布迅速,符合一级吸收二室开放模型,但消除缓慢。甲砜霉素在鲫血浆、肝脏、肾脏和肌肉中的主要药代动力学参数如下:分布半衰期(T1/2α)分别为1.446 h、1.958 h、7.410 h和1.376 h;消除半衰期(T1/2β)分别为16.712 h、21.267 h、79.970 h和25.600 h;药时曲线下总面积(AUC)分别为669.073μg/(mL.h)、271.260μg/(g.h)、3616.060μg/(g.h)和158.634μg/(g.h)。甲砜霉素在水产动物体内吸收快,肌肉和肾脏消除半衰期长,消除缓慢,因此,在该类药物使用时,应相对延长给药间隔时间,避免耐药性的产生。
The pharmacokinetics of thiamphenicol was studied by oral administration of thiamphenicol at 30 mg/kg body weight in Carassius auratus by the means of LC-MS to provide theoretical basis of C.auratus in disease prevention and treatment.The average body weight of C.auratus was(40.70±7.87) g,and the water temperature was(20±0.2) ℃.The drug concentration in muscle,plasma,liver,kidney in 0.25,0.5,1,1.5,2,4,6,8,12,24,36,48,72 hours after administration.And the data were processed and analyzed by 3p97 software.The results showed that thiamphenicol.concentrations were shown as a two-compartent open model with 1st order absorption in the plasma,liver,kidney and muscle.The T1/2α was 1.446 h,1.958 h,7.410 h and 1.376 h respectively in the plasma,liver,kidney and muscle,and the T1/2β was 16.712 h,21.267 h,79.970 h and 25.60 h respectively in the plasma,liver,kidney and muscle.The AUC was 669.073 μg/mL·h in plasma,271.260 μg/g·h in liver,3 616.060 μg/g·h in kidney and 158.634 μg/g·h in muscle.Thiamphenicol was absorded fast by aquatic animal,and eliminated slowly by muscle and kidney.So we should extend dosing intervals to avoid drug resistant.