盐酸头孢噻呋混悬注射液在猪体内的药动学及相对生物利用度研究  

Pharmacokinetics and relative bioavailability of injectable ceftiofur hydrochloride suspension in pigs

作　　者：张卫元 陈翠兰 黄文辉 张翠平 徐永磊 张世硕 李在建[2] 

机构地区：[1]武汉回盛生物科技有限公司,湖北武汉430042 [2]华中农业大学,湖北武汉430070

出　　处：《中国兽医杂志》2013年第10期79-82,共4页Chinese Journal of Veterinary Medicine

摘　　要：研究并比较盐酸头孢混悬噻呋注射液(7.5%)和盐酸头孢噻呋注射液(5%)在猪体内的药物动力学特征及生物利用度。7头健康猪,按交叉试验设计,进行单次给药剂量(5mg/kg体重),肌肉注射盐酸头孢噻呋混悬液(7.5%)和盐酸头孢噻呋注射液(5%),高效液相色谱法测定血药浓度,3P97药动学计算软件处理血浆药物浓度-时间数据。猪肌肉注射盐酸头孢噻呋混悬液(7.5%)的药时数据符合一级吸收二室开放模型,主要的药物动力学参数分别为:吸收半衰期(t1/2Ka)(0.30±0.13)h,消除半衰期(t1/2β)(21.87±3.35)h,达峰时间(Tp)(1.92±0.19)h,达峰浓度(Cmax)(15.26±0.31)μg/mL,AUC(410.71±17.68)μg/mL·h。猪肌肉注射盐酸头孢噻注射液(5%)的药时数据则符合一级吸收二室开放模型,主要的药物动力学参数为:t1/2Ka为(0.52±0.05)h,t1/2β为(13.79±0.48)h,Tp为(1.51±0.05)h,Cmax为(35.78±1.16)μg/mL,AUC(390.90±5.56)μg/mL·h。平均相对生物利用度为(105.06±5.56)%。表明7.5%盐酸头孢噻呋混悬注射液,肌肉注射后在猪体内具有吸收快、体内分布广泛、消除缓慢、消除半衰期延长、生物利用度高的药动学特征。The pharmacokinetics and relative bioavailability of ceftiofur hydrochloride were investigated and compared in 7 healthy pigs in a Latin square design following single intramuscular （5 mg · kg^-1 b. w） administra-ion of injectable ceftiofur hydrochloride suspension （7.5 %） and single intramuscular （5 mg · kg^-1 b. w） adminis-tration of ceftiofur hydrochloride injection（5%）. The ceftiofur hydrochloride concentrations in plasma samples were determined by high performance liquid chromateography （ HPLC ） with UV detection. Pharmacokinetic a-nalysis of plasma drug concentration-time data for ceftiofur hydrochloride was carried out with a computer program 3P97. The ceftiofur hydrochloride concentration-time data were fitted to a two-compartment open model after single intravenous administration of injectable ceftiofur hydrochloride suspension（7.5%）. The main pharmacokinetic pa-rameters were as follows： tl/2Ka （0. 30±0. 13）h,t1/2β （21. 87±3.35）h,Tp （1.92±0.19）h,Cmax （15. 26±0. 31） μg/mL,AUC（410.71±17.68）μg/mLoh. The ceftiofur hydrochloride concentration-time data were described by a two-compartment open model with first-order absorption after single intramuscular administration of the ceftiofur hydrochloride injection（5%）. The main pharmacokinetic parameters were as follows： t1/2Ka （0. 52 ±0. 05）h, t1/2β （13.79±0.48）h,t1/2β（1. 51±0.05）h,Cmax （35. 78±1.16）μg/mL, AUC（390. 90±5.56）μg/mLoh, and The aver-age relative bioavailability was （105.06±5.56）%. The results of present studies showed that the pharmacokinetic characteristics of the injectable ceftiofur hydrochloride suspension（7.5 %） demonstrated rapid absorption, extensive distribution, slow elimination and high bioavailability.

关 键 词：盐酸头孢噻呋 混悬注射液 相对生物利用度 药物动力学 猪 

分 类 号：S858.28[农业科学—临床兽医学]