›› 2013, Vol. 40 ›› Issue (12): 95-98.

• 生理生化 • 上一篇    下一篇

硫酸头孢喹肟在鸭体内的药动学及生物利用度研究

何祥来1,2, 陈晓兰2,3   

  1. 1. 扬州大学兽医学院, 江苏扬州 225009;
    2. 江苏农牧科技职业学院药物检测中心, 江苏泰州 225300;
    3. 南京农业大学动物医学院, 江苏南京 210095
  • 收稿日期:2013-05-20 出版日期:2013-12-20 发布日期:2014-02-11
  • 作者简介:何祥来（1979- ），男，安徽人，博士生，讲师，从事临床兽医学教学与科研。
  • 基金资助:
    江苏省自然科学基金（SBK201123283）。

Study on Pharmacokinetics and Bioavailabilities of Cefquinome Sulfate in Ducks

HE Xiang-lai1,2, CHEN Xiao-lan2,3   

  1. 1. College of Veterinary, Yangzhou University, Yangzhou 225009, China;
    2. Drug Analysis Center, Jiangsu Agri-animal Husbandry Vocational College, Taizhou 225300, China;
    3. College of Veterinary Medicine, Nanjing Agricultural University, Nanjing 210095, China
  • Received:2013-05-20 Online:2013-12-20 Published:2014-02-11

摘要： 试验将20只2月龄健康番鸭，随机分为2组，每组10只，雌雄各半，分别进行静脉注射和口服硫酸头孢喹肟给药的药动学研究。静脉注射和口服的给药剂量分别为10和20 mg/kg。以反相HPLC测定血浆中硫酸头孢喹肟的浓度，血药浓度—时间数据用3P97药动学程序软件处理。鸭单剂量静脉注射给药后，血药浓度—时间数据符合无吸收二室开放模型，其主要动力学参数分别为:V（c），（1.146±0.02） L/kg；t1/2α，（0.290±0.02）h；t1/2β，（1.691±0.15）h；AUC （6.635±0.18）（mg·h）/L；CL（s），（1.508±0.04）L/（kg·h）。鸭口服硫酸头孢喹肟的血药浓度—时间数据符合一级吸收一室开放模型，主要动力学参数分别为:t1/2（ka），（0.45±0.05）h；t1/2（ke），（0.96±0.29）h；T（peak），（0.91±0.09）h；C（max），（3.14±0.64）mg/L；AUC，（8.29±1.26）（mg·h）/L；F，（62.55±0.10）%。硫酸头孢喹肟在体内的药动学特征表现为吸收迅速、分布广泛、消除迅速。但口服给药在鸭体内生物利用度低，可能由于硫酸头孢喹肟的脂溶性低，其在消化道吸收率低所致。但8 h内能保持有效血药浓度范围（（0.14±0.03）~（3.14±0.64）μg/mL），可抑制鸭疫里默氏杆菌及其他细菌感染。

关键词: 硫酸头孢喹肟; 药物动力学; HPLC; 鸭

Abstract: The pharmacokinetics of cefquinome sulfate were investigated following single intravenous (IV) and oral administration at a dosage of 10 and 20 mg/kg, respectively, in healthy duck. 20 ducks were randomly divided into two groups for the experiments. The cefquinome sulfate in plasma was determined by reverse phase high performance liquid chromatography (PR-HPLC).The concentration-time data of cefquinome sulfate was analyzed with pharmacokinetic-compartment analysis soft (3P97). The concentration-time data of cefquinome sulfate after IV admistration was fitted to a two-compartment open model. The main pharmacokinetic parameters were as follows, V(c),(1.146±0.02)L/kg; t1/2α,(0.290±0.02)h; t1/2β,(1.691±0.15)h; AUC,(6.635±0.18)(mg·h)/L,CL(s),(1.508±0.04)L/(kg·h). The concentration-time data of cefquinome sulfate after oral admistration was fitted to a one-compartment open model with first-order absorbtion. The main pharmacokinetic parameters were as follows,t1/2(ka),(0.45±0.05)h; t1/2(ke),(0.96±0.29)h; T(peak),(0.91±0.09)h; C(max),(3.14±0.64)mg/L; AUC,(8.29±1.26)(mg·h)/L; F,(62.55±0.10)%. The results showed that the pharmacokinetic characteristics of cefquinome sulfate in healthy duck manifested the rapid absorbtion, wide distribution, rapid elimination but low bioavailability, probably due to its low lipsoluble characteristic. However cefquinome sulfate in blood could keep efficient concentration ((0.14±0.03) to (3.14±0.64)μg/mL) in 8 h, which could inhibit infections of Riemerella anatipestifer (RA) and other bacteria.

Key words: cefquinome sulfate; pharmacokinetics; HPLC; duck

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