不同温度下氟苯尼考在大菱鲆体内的药代动力学研究

Pharmacokinetics of Florfenicol in Turbot(Scophthalmus maximus) at Two Water Temperatures

研究了14和17℃2种不同养殖温度下,氟苯尼考在健康大菱鲆(Scophthalmus maximus)体内的药代动力学特征。以15mg/kg BW的剂量经静注和口灌2种方式给药后,于0.25、0.5、1、2、4、6、8、12、16、24、48和96h采集血液样品,采用Agilent1200型高效液相色谱仪测定样品中药物的含量,药时数据采用DAS2.0自动药动学软件进行分析。研究显示,14和17℃下,静注给药后的消除相半衰期(t1/2β)分别为18.20和12.46h,表观分布容积(Vd)分别为0.03和0.11L/kg,清除率(CL)均为0.02L/(h·kg)。口灌给药后血药浓度均在12h达到峰值,分布相半衰期(t1/2α)分别为2.84和4.08h,消除相半衰期分别为14.48和12.45h,生物利用度(F)分别为17.02%和18.24%。研究结果表明,温度升高会加快大菱鲆对氟苯尼考的吸收、体内分布和消除,提高口灌方式氟苯尼考利用效率。结合氟苯尼考药效学研究结果,提出给药方案:14℃时,大菱鲆口灌给药剂量25mg/kg BW,每日一次;17℃时,大菱鲆口灌给药剂量22mg/kg BW,每日一次。

The pharmacokinetic profiles of florfenicol in turbot Scophthalmus maximus were investigated at two different water temperatures,14℃and 17℃,in the present study.After intravenous and oral administrations of florfenicol at a dose of 15 mg/kg BW,blood was sampled at 0.25,0.5,1,2,4,6,8,12,16,24,48 and 96 h post drug administration,respectively,with florfenicol concentration in blood determined using high performance liquid chromatography(HPLC).The concentration-time data were analyzed using the pharmacokinetic program DAS2.0.After intravenous administration,the elimination half life(t 1/2β)was 18.20 and 12.46 h,the apparent volume of distribution(Vd)was 0.03 and 0.11 L/kg,and the clearance(CL)was 0.02 and 0.02 L/(h·kg),respectively,for 14℃and 17℃;After intravenous administration,the peak concentration(C max)was found at 12 h,t 1/2αwas 2.84 and 4.08 h,t 1/2βwas 14.48 and 12.45 h,and the bioavailability(F)was 17.02 and 18.24%,respectively,for 14℃and 17℃.The results obtained in this study indicated that the increase of temperature could promote the absorption,distribution and elimination of florfenicol in turbot,and improve the efficiency of oral administration.According to the pharmacodynamics of florfenicol reported previously,the optimal dosage regimen was proposed for oral route as follows:1 time per day;25 mg/kg BW each time for fish cultured at 14℃and 22 mg/kg BW for those cultured at 17℃.