恩诺沙星在健康猪肌肉注射后在鼻分泌物中的渗透情况以及鼻分泌物与血浆中恩诺沙星浓度之间的关系。
Penetration of enrofloxacin into the nasal secretions and relationship between nasal secretions and plasma enrofloxacin concentrations after intramuscular administration in healthy pigs.
作者信息
Bimazubute M, Cambier C, Baert K, Vanbelle S, Chiap P, Albert A, Delporte J P, Gustin P
机构信息
Department of Pharmacology, Pharmacotherapy and Toxicology, Faculty of Veterinary Medicine, University of Liège, Liège, Belgium.
出版信息
J Vet Pharmacol Ther. 2010 Apr;33(2):183-8. doi: 10.1111/j.1365-2885.2009.01123.x.
The pharmacokinetic behaviour of enrofloxacin (ENRO) in plasma and nasal secretions of healthy pigs was investigated, after a single-dose intramuscular administration of 2.5 mg/kg body weight of the drug. Blood samples and nasal secretions were collected at predetermined times after drug administration. Concentrations of ENRO and its active metabolite ciprofloxacin (CIPRO) were determined in plasma and nasal secretions by high-performance liquid chromatography (HPLC). CIPRO was not detected probably because we investigated young weaned pigs. The data collected in 12 pigs for ENRO were subjected to noncompartmental analysis. In plasma, the maximum concentration of drug (C(max)), the time at which this maximum concentration of drug (T(max)) was reached, the elimination half-life (t(1/2)(beta)) and the area under the concentration vs. time curve (AUC) were, respectively, 694.7 ng/mL, 1.0 h, 9.3 h and 8903.2 ngxh/mL. In nasal secretions, C(max), T(max), t(1/2)(beta) and AUC were, respectively, 871.4 ng/mL, 2.0 h, 12.5 h and 11 198.5 ngxh/mL. In a second experiment conducted in 10 piglets, the relationship between concentrations of ENRO measured in the plasma and the nasal secretions has been determined following single-dose intramuscular administration of 2.5, 10 or 20 mg/kg body weight of the drug. It has been demonstrated that, among several variables, i.e., (1) the dose administered, (2) the time between intramuscular injection and blood sampling, (3) the age, (4) the sex, (5) the animal body weight and (6) the plasma concentration of the drug, only the latter influenced significantly the ENRO concentration in nasal secretions. Practically, using a generalized linear mixed model, ENRO concentrations in the nasal secretions (microg/mL) can be predicted taking into account the ENRO concentrations in plasma (microg/mL), according to the following equation:
在对健康猪单次肌内注射2.5 mg/kg体重的恩诺沙星（ENRO）后，研究了其在血浆和鼻分泌物中的药代动力学行为。给药后在预定时间采集血样和鼻分泌物。通过高效液相色谱法（HPLC）测定血浆和鼻分泌物中ENRO及其活性代谢物环丙沙星（CIPRO）的浓度。未检测到CIPRO，可能是因为我们研究的是断奶仔猪。对12头猪采集的ENRO数据进行了非房室分析。在血浆中，药物的最大浓度（C(max)）、达到该最大浓度的时间（T(max)）、消除半衰期（t(1/2)(β)）和浓度-时间曲线下面积（AUC）分别为694.7 ng/mL、1.0小时、9.3小时和8903.2 ngxh/mL。在鼻分泌物中，C(max)、T(max)、t(1/2)(β)和AUC分别为871.4 ng/mL、2.0小时、12.5小时和11198.5 ngxh/mL。在对10头仔猪进行的第二项实验中，在单次肌内注射2.5、10或20 mg/kg体重的药物后，确定了血浆和鼻分泌物中测得的ENRO浓度之间的关系。结果表明，在几个变量中，即（1）给药剂量、（2）肌内注射与采血之间的时间、（3）年龄、（4）性别、（5）动物体重和（6）药物的血浆浓度中，只有后者对鼻分泌物中ENRO的浓度有显著影响（P<0.05）。实际上，使用广义线性混合模型，考虑到血浆中ENRO的浓度（μg/mL），可以根据以下方程预测鼻分泌物中ENRO的浓度（μg/mL）：
Zotero 插件