氟苯尼考混悬注射液与普通注射液在猪体内的药代动力学比较

Comparative pharmacokinetics of suspension injection and common injection of florfenicol in pigs

按20 mg/kg剂量分别给猪注射氟苯尼考混悬注射液与普通注射液后,用HPLC-UV法测定了血浆中氟苯尼考的浓度,所得药-时数据用3P97药代动力学软件进行了处理。静脉注射氟苯尼考普通注射液后的药-时数据符合无吸收二室开放模型,动力学参数为:t1/2β=(8.74±1.92)h,V/F(c)=(0.88±0.11)L/kg,AUC=(85.39±5.70)μg/(mL.h),Cl(s)=(0.24±0.02)L/(kg.h)。肌肉注射氟苯尼考混悬注射液及普通注射液后的药-时数据分别符合一室、二室开放模型,动力学参数分别为:t1/2ka=(0.60±0.11)h和(0.19±0.05)h,t1/2ke=(23.13±4.06)h和(22.77±2.58)h,Tamax=(9.00±1.00)h和(1.42±1.00)h,Camax=(2.10±0.27)μg/mL和(2.99±0.12)μg/mL,F=76.20%±5.54%和72.50%±7.89%。表明,氟苯尼考混悬注射液具有吸收慢、消除慢、生物利用度高、有效血药浓度时间长及缓释的特点。

The comparative pharmacokinetics of florfenicol suspension injection and florfenicol common injection was studied in pigs after intravenous （i. v. ） and intramuscular （i. m. ） administration with a dose of 20 mg/kg, respectively. Florfenicol concentrations in plasma were determined by the high performance liquid chromatography with ultraviolet detector （HPLC-UV）. Plasma concentration profiles were analyzed by the 3P97 software. The time data of florfenicol concentration were best fitted with the two-compartment open model after single i. v. injection. The main pharmacokinetic parameters were as follows：t1/2β = （8.74± 1.92） h,V/F（c） =（0.88±0.11） L/kg,AUC=（85. 39±5. 70） μg/（mL · h）,Cl（s） =（0.24±0.02） L/（kg · h）. The time data of drug concentration-fitted with the one- and two-compartment models after single i. m. administration of suspension injection and common injection, respectively. The main pharmacokinetic pa- rameters were as follows,respectively：t1/2ks= （0.60±0.11） h, and （0. 19±0.05） h,t1/2kc = （23.13±4.06） h,and （22.77±2.58） h, Tmax =-（9.00± 1.00） h, and （1.42±1.00） h, Cmax = （2. 10± 0.27） tμg/mL,and （2.99±0.12） μg/mL,F= 76. 20%±5. 54%, and 72.50%± 7.89%. The results showed that florfenicol suspension injection had slow absorption and elimination, high bioavailability,therapeutic plasma level.