摘要
选用２１头健康杂种猪，随机分为３组，对静注、肌注及内服恩诺沙星（２．５ｍｇ／ｋｇ）的生物利用度和药物动力学进行了研究。用乙腈提取血浆中的药物，反相高效液相色谱法测定血浆中恩诺沙星及其主要代谢产物环丙沙星的浓度。所得血药浓药－时间数据用ＭＣＰＫＰ计算机程序处理。静注给药的药时数据适合二室开放模型，主要药物动力学参数：ｔ１／２α０．４８±０．２４ｈ；ｔ１／２β３．４５±０．８５ｈ；ｔ１／２Ｋ１０２．０１±０．３９ｈ；Ｖ１１．２２±０．２１Ｌ／ｋｇ；Ｖｄ（ａｒｅａ）３．３４±０．６９Ｌ／ｋｇ；Ｖｄ（ｓｓ）１．８５±０．３３Ｌ／ｋｇ；ＣｌＢ０．４２３±０．０４４Ｌ·ｋｇ－１·ｈ－１；ＡＵＣ５．９６７±０．６５５ｍｇ·Ｌ－１·ｈ－１。肌注给药的药时数据适合一级吸收一室模型，主要药物动力学参数：ｔ１／２ｋａ０．２６±０．０９ｈ；ｔ１／２ｋｅ４．０６±０．４８ｈ；ｔｍａｘ１．１２±０．２７ｈ；Ｃｍａｘ０．７９±０．１７ｍｇ／Ｌ；ＡＵＣ５．４８３±１．０９８ｍｇ·Ｌ－１·ｈ－１；Ｆ９１．９％±１８．４％。内服给药的药时数据适合一级吸收二室模型，主要药物动力学参数：ｔ１／２ｋａ０．２３±０．０８ｈ；ｔ１／２α１．５３±０．７?
Pharmacokinetics and bioavailability of enrofloxacin were investigated in crossbred (Duroc× Landrace×Yorkshire) pigs following single intravenous (2.5 mg/kg), intramuscular (2.5 mg/kg) and oral (2.5 mg/kg) administration of the drug. Blood samples were collected at different intervals after administration of enrofloxacin. Concentrations of enrofloxacin and its metabolite ciprofloxacin were determined by high performance liquid chromatography (HPLC). Traces of ciprofloxacin (<0.10 mg/L) were found only in 3 of 21 animals. The enrofloxacin concentration time data were fitted to a two compartment open model after single iv dosing in pigs. The main pharmacokinetic parameters of enrofloxacin in pigs were as follows: t 1/2α 0 48±0 24 h;t 1/2β 3 45±0 85 h;t 1/2K10 2 01±0 39 h;V 1 1 22±0 21 L/kg; Vd (area) 3 34±0 69 L/kg;Vd (ss) 1 85±0 33 L/kg; Cl B 0 423±0 044 L·kg -1 ·h -1 ;AUC 5 967±0 655 mg·L -1 ·h -1 . The drug concentration time data were fitted to a one compartment open model with first order absorption after single im administration in pigs. The main pharmacokinetic parameters of enrofloxacin in pigs were as follows: t 1/2ka 0 26±0 09 h;t 1/2ke 4 06±0 48 h;t max 1 12±0 27 h;C max 0 79±0 17 mg/L;AUC 5 483±1 098 mg·L -1 ·h -1 ;F 91 9%±18 4%. The drug concentration time data were fitted to a two compartment open model with first order absorption after single po administration in pigs. The main pharmacokinetic parameters of enrofloxacin in pigs were as follows:t 1/2ka 0 23±0 08 h;t 1/2α 1 53±0 73 h;t 1/2β 6 93±1 15 h;t max 0 97±0 17 h;C max 1 17±0 12 mg/L;AUC 8 937±1 393 mg·L -1 ·h -1 ;F 149 8%±23 4%.
出处
《中国兽医学报》
CAS
CSCD
1996年第6期606-612,共7页
Chinese Journal of Veterinary Science
基金
国家自然科学基金
高校博士学科点科研基金
关键词
恩诺沙星
生物利用度
药物动力学
猪
enrofloxacin
HPLC
bioavailability
pharmacokinetics
pigs
