采用液相色谱与质谱连用技术(LC-MS),研究了以30mg/kg(体质量)的药量在单次口灌给药条件下,甲砜霉素在松浦镜鲤Cynipus carpio L体内的药物代谢动力学。试验水温为(20±O.2)℃,试验鲤(1^+龄)体质量为(84.84±17.45)g。在给药后0.25、0.50、0.75、1.00、1.50、2.00、4.00、6.00、8.00、12.00、24.00、36.00、48.00、72.00h采集鲤的肌肉、血浆、肝胰脏和肾脏,测定各组织中甲砜霉素的浓度,用药动学3P97软件进行数据分析和处理。结果表明,甲砜霉素在鲤体内吸收分布迅速,符合一级吸收二室开放模型,但消除缓慢。甲砜霉素在鲤血浆、肝胰脏、肾脏和肌肉中的主要药代动力学参数如下:消除半衰期(T1/2β)分别为77.292、24.625、79.966、25.600h;分布半衰期(T1/2a)分别为7.317、0.454、7.409、1.376h;药时曲线下总面积(AUC)分别为782.641μg/(mL·h)、544.756μg/(g·h)、3616.060μg/(g·h)和158.634μg/(g·h))。鉴于甲砜霉素在鲤血浆和肾脏中的消除半衰期长,消除缓慢,建议使用该类药物时应相对延长给药间隔时间。
The pharmacokinetics of thiamphenicol (TAP) was studied in 1^+ year old Songpu common carp Cypr/nus carpio L. administrated orally, with body weight of (84.84±17.45)g, by liquid chromatography-mass spectro- graphy (LC-MS) at 30 rag/ kg(body weight) at water temperature of(20+0.2)℃. The drug concentrations in plasma,hepatopancreas, kidney and muscle were monitored 0.25,0.50,0. 75, 1.00, 1.50,2. 00,4.00,6.00, 8.00,12. 00,24. 00,36. 00,48. 00, and 72.00 h after drug administration, and analyzed by 3P97 software. The thi- amphenicol absorption was found as a two-compartment open model with 1 st order absorption in plasma, hepato- pancreas, kidney and muscle, with T1/2,~ of 7. 317 h in plasma, 0. 454 h in hepatopancreas, 7. 409 h in kidney and 1. 376 h in muscle, and Tilde of 77. 292 h in plasma, 24,625 h in hepatopancreas, 79. 966 h in kidney and 25. 600 h in muscle. The AUC was found to be 782. 641 μg/(g · h) in plasma, 544.756 μg/(g · h) in hepatopancreas, 3 616. 060 μg/(g · h) in kidney and 158. 634 μg/(g · h) in muscle. The findings reveal that the drug is suggested to be administrated at a long interval every delivery time due to long period of TAP toxin and slow elimination in plasma and kidney.