新型硫酸头孢喹肟乳液猪体内药物浓度测定  

Determination of drug concentrations of new cefquinome sulfate emulsion in swine

作　　者：唐达[1] 陈诚[1] Tang Da;Chen Cheng(Chongqing Academy of Animal Sciences,Chongqing 40246)

机构地区：[1]重庆市畜牧科学院,重庆402460

出　　处：《中国抗生素杂志》2018年第11期1431-1435,共5页Chinese Journal of Antibiotics

基　　金：重庆市基本科研业务费资助项目(No.16420);重庆市农发资金项目(No.17413)

摘　　要：目的测定硫酸头孢喹肟乳液在猪体内的血药浓度。方法以吐温80、斯盘85为乳化剂,通过表面活性剂复配方法制备了新型硫酸头孢喹肟乳液制剂。与市售硫酸头孢喹肟混悬液对比研究硫酸头孢喹肟乳液生物等效性,将实验猪随机分组,并分别肌注硫酸头孢喹肟乳液及混悬液,采用高效液相色谱的方法测定其血药浓度,采用DAS 2.0药动学程序计算药动学参数。试验优化了硫酸头孢喹肟血液样品的处理方法,并考察了方法专属性。结果硫酸头孢喹肟分析方法在0.10～10.00μg/mL之间呈良好的线性关系,回归方程:y=157.06x+18.347,r2=0.9996 (n=5),日内变异系数低于5.76%,日间变异系数低于8.35%;样品的平均回收率为93.4%～97.7%,完全符合生物样品分析要求;两组药动学行为均符合一级吸收二室模型,其主要药动学参数为:吸收半衰期(T1/2a)分别为(0.842±0.015)h和(0.825±0.021)h;达峰时间(Tmax)分别为(1.357±0.043)h和(1.345±0.051)h;峰浓度(Cmax)分别为(3.386±0.083)μg/m L和(3.526±0.091)μg/m L;消除半衰期(T1/2β)分别为(1.054±0.059)h和(1.025±0.087)h;药时曲线下面积(AUC0～t)达(12.706±0.553)mg·h/L和(12.787±0.394)mg·h/L。对两实验组AUC0～t、Cmax、Tmax进行差异性分析,3种药代参数组间差异均不显著(P>0.05)。结论自制硫酸头孢喹肟乳液与市售硫酸头孢喹肟混悬液具有生物等效性。Objective To determine the blood concentrations of cefquimeoxime sulfate emulsion in pigs. Method Tween 80 and Span 85 were used as the emulsifier to prepare a novel cephalosporin cefquinome sulphate formulation of the emulsion by a surfactant method of preparing compound. The bioequivalence of cefquinoxime sulfate was compared with commercially available cefacrine suspension. Pigs were randomly divided into two experimental groups, and were given intramuscular injection of cefquinoxime sulfate emulsion and suspension, respectively. The plasma concentrations were determined by HPLC, and the pharmacokinetic parameters were calculated by the DAS2.0 pharmacokinetic program. The method of treating the blood samples of cefacrine hydrochloride was optimized and the specificity of the method was investigated. Results The cephalosporin sulfate analysis method had a good linear relationship in the range of 0.10-10.00μg/mL, and the regression equation was： y=157.06x＋18.347, r=0.9996 （n=5）. The daytime coefficient of variation was less than 8.35%. The average recovery of the sample was 93.4%-97.7%, which was in accordance with the requirements of biological sample analysis. The pharmacokinetic parameters of the two groups were （0.842±0.015）h and （0.825±0.021）h respectively. The peak time （Tmax） and （T1/2β） were （1.054±0.059）h, （1.025±0.087）11, respectively, and the peak concentrations （Cmax） were （3.386±0.083）μg/mL and （3.526±0.091）μg/mL respectively. AUC0.t reached （12.706±0.553）mg·h/L and （12.787±0.394）mg·h/L. The differences of AUC0-t, Cmax, and Tmax between the two experimental groups were not significant （P〉0.05）. Conclusion The self-made cefquinoxime emulsion had a bioequivalence with commercially available cefacizime suspensions.

关 键 词：硫酸头孢喹肟 乳液 药动学 生物等效性 

分 类 号：R917[医药卫生—药物分析学]