甲砜霉素在红笛鲷体内的组织分布和药代动力学研究

The Distribution and Pharmacokinetics of Thiamphenicol in Tissues of Luthjanus sanguineus

关键词:  甲砜霉素  红笛鲷  药代动力学  组织分布

Key words:  Thiamphenicol  Lutjanus sanguineus  pharmacokinetics  tissue distribution

摘要:

研究腹腔注射和口灌给药方式下甲砜霉素在红笛鲷体内的组织分布和药代动力学特征。甲砜霉素单剂量10 mg/（kg.bw）分别腹注和口灌红笛鲷，给药后取血浆、肌肉、肝脏和肾脏，各组织中药物浓度用HPLC-MS/MS测定，所得药时数据用DAS3.0软件分析。结果显示：两种给药方式下红笛鲷血浆药时数据均符合一级吸收二室模型；血药达峰时间（tp）分别为2.39和4.51 h，血药浓度峰值（Cmax）分别为5.80和5.06 μg/mL，消除半衰期（t1/2β）分别为7.25和50.09 h。腹注和口灌给药肌肉、肝脏和肾脏的Cmax分别为2.504和2.678 μg/g、4.612和4.393 μg/g、12.464和7.509 μg/g，tp分别为6.0和4.0 h、2.0和4.0 h、1.5和4.0 h；甲砜霉素在红笛鲷体内消除速度较慢，肌肉、肝脏和肾脏的t1/2β分别为37.168和33.519 h、22.499和33.649 h、19.672和8.673 h。结果表明：腹注给药方式下甲砜霉素在红笛鲷体内的吸收快于口灌给药，在血浆和肝脏中的消除快于口灌给药，在肌肉和肾脏中的消除则慢于口灌给药。

Abstract:

To investigate tissues distribution and pharmacokinetics of thiamphenicol with a single dose of 10 mg/kg body weight after enterocoelia injection and oral administration in Lutjanus sanguineus at the water temperature of （20±2）℃ and salinity of 28，the drug concentration in blood, muscle, liver and kidney were samlped after administration and assayed by HPLC-MS-MS method. Pharmacokinetics parameters were calculated by DAS30 software. Present datas showed that TAP concentration-time data in plasma following the two different forms were best described by a two-compartment model with first-order absorption. And tP were 239 and 4.51 h, Cmax were 5.80 and 5.06 μg/mL, and t1/2β were 7.25 and 50.09 h, respectively. Cmax of muscle, liver and kidney were 2.504 and 2.678 μg/g, 4.612 and 4.393 μg/g, 12.464 and 7.509 μg/g，and tp were 6.0 and 4.0 h, 2.0 and 4.0 h,1.5 and 4.0 h, respectively. And the TAP eliminated slowly in muscle,liver and kidney, t1/2β were 37.168 and 33.519 h, 22.499 and 33.649 h,19.672 and 8.673 h, respectively. Results indicated that TAP was absorded more quickly, eliminated faster in plasma and liver but eliminated slower in muscle and kidney after enterocoelia injection than after oral administration.