| In this paper,the pharmacokinetics and residue elimination rules of sarafloxacin?SAR?,thiamphenicol?TAP?and florfenicol?FFL?in Scophthalmus maximus were studied respectively.Liquid chromatography-tandem mass spectrometry?HPLC-MS?was used to detect respectively the time-concentration data of three antibacterials in plasma,muscle,liver and kidney of Scophthalmus maximus after oral administration by gavage.Following the dose of 30 mg/kg body weight in 48 h,the pharmacokinetic parameters were computed by non-compartmental model using DAS3.0 software,whose results were time to peak(Tmax)of 2.600,21.968 and26.503 mg/L respectively,time to concentration(Cmax)of 4,9 and 9 h.SAR had an obvious difference of Cmaxax and Tmax with TAP and FFL,both of them which had the same time to peak(Tmax)and the nearly time to maximum concentration(Cmax)because of them belonging to amides.The result of area under the curve[AUC?0-??]was 540.133,319.754 and 992.256 mg/L·h in turbot,and the apparent volume of distribution?Vz/F?of 27.954,6.206 and 1.130 L/kg respectively.Three antibacterials'mean residence time[MRT?0-??]were 495.053,33.984 and38.763 h respectively,and the half-life(T1/2z)were 348.788,45.841 and 25.521 h respectively.The maximum concentration(Cmax)of SAR in muscle,liver and kidney tissues of Scophthalmus maximus were 3.500,10.155 and 3.867?g/g respectively.After the drug given,liver quickly reached the time to Tmax after 2 hours.And the time to Tmax of muscle and kidney were 4 and 3 h respectively.The maximum concentration(Cmax=10.155?g/g)in liver and the under the curve[AUC?0-??=363.718 mg/L·h]were the largest,and also the mean residence time in liver[MRT?0-??=36.565 h]was the longest.Combining with the elimination half-time(T1/2z=129.514 h),we discovred that liver had the highest absorption capacity of the drug,but the weakest elimination of it.The apparent volume of distribution was least(Vz/F=10.211 L·kg-1)and the total clearance was largest in muscle,which mean SAR had the least distribution and the fastest clearance in muscle.The maximum concentration(Cmax)of TAP in muscle,liver and kidney tissues of Scophthalmus maximus were 22.346,27.127 and 47.178?g/g respectively.The time to Tmax of Liver?4 h?was faster than muscle?9 h?and kidney's?9 h?.The maximum concentration(Cmax=47.718?g/g)in kidney and the under the curve[AUC?0-??=517.768 mg/L·h]were the largest,indicating that kidney had the highest absorption capacity of the antibacterial.The mean residence time in liver[MRT?0-??=36.565 h]was the longest and eliminating the half-life(T1/2z)was 42.370?g/g.It means liver cleared slowly the drug in 48 h after treatment.The maximum concentration(Cmax)of FFL in muscle,liver and kidney tissues of Scophthalmus maximus were 22.215,30.756 and 32.455?g/g respectively.The time to Tmax of muscle was relatively slow?9 h?,however the tissues of liver and kidney had quickly reached the Tmax?both of them were 4 h?.The maximum concentration(Cmax=32.455?g/g)in kidney and the under the curve[AUC?0-??=860.410 mg/L·h]were the largest,and also the mean residence time in kidney[MRT?0-??=36.565 h]was the longest.Combining with the elimination half-time(T1/2z=32.466 h),we discovered that kidney had the highest absorption capacity of the drug,but the weakest elimination of it.The apparent volume of distribution was least(Vz/F=1.203 L·kg-1)and the total clearance was largest in muscle,which mean FFL had the least distribution and the fastest clearance in muscle.Following the dose of 60 mg/kg in 30 d,the rules of residue elimination were regressed by WT1.4 program.They were showed that the calculated withdrawal time of thiamphenicol in plasma were 19.64?8.90 and 10.90 d,and there are 24.09,10.64 and 19.02 d in muscle;The withdrawal time of liver and kidney were 25.69,18.19,18.64 d and 25.32,23.95,25.51 d respectively.The presented study will provide scientific basis for sarafloxacin hydrochloride,thiamphenicol and florfenicol applied to Scophthalmus maximus. |
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