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Penetration of enrofloxacin into the nasal secretions and relationship between nasal secretions and plasma enrofloxacin concentrations after intramuscular administration in healthy pigs

机译:肌肉注射后恩诺沙星渗透入鼻腔分泌物以及鼻分泌物与血浆中恩诺沙星浓度的关系

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Bimazubute, M., Cambier, C., Baert, K., Vanbelle, S., Chiap, P., Albert, A., Delporte, J. P., Gustin, P. Penetration of enrofloxacin into the nasal secretions and relationship between nasal secretions and plasma enrofloxacin concentrations after intramuscular administration in healthy pigs. J. vet. Pharmacol. Therap.33, 183-188. 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 (Cmax), the time at which this maximum concentration of drug (Tmax) was reached, the elimination half-life (t[fraction one-half]o) 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 ngp"h/mL. In nasal secretions, Cmax, Tmax, t[fraction one-half]o and AUC were, respectively, 871.4 ng/mL, 2.0 h, 12.5 h and 11 198.5 ngp"h/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 (og/mL) can be predicted taking into account the ENRO concentrations in plasma (og/mL), according to the following equation: [graphic removed]
机译:Bimazubute,M.,Cambier,C.,Baert,K.,Vanbelle,S.,Chiap,P.,Albert,A.,Delporte,JP,Gustin,P.恩诺沙星渗透入鼻腔分泌物与鼻腔分泌物之间的关系肌肉注射后,健康猪的血浆和血浆恩诺沙星浓度。 J.兽医Pharmacol。 Therap.33,183-188。单剂量肌内注射2.5 mg / kg体重的药物后,研究了恩诺沙星(ENRO)在健康猪的血浆和鼻腔分泌物中的药代动力学行为。给药后的预定时间采集血样和鼻分泌物。通过高效液相色谱(HPLC)测定血浆和鼻腔分泌物中ENRO及其活性代谢产物环丙沙星(CIPRO)的浓度。未检测到CIPRO,可能是因为我们调查了断奶仔猪。对12头猪进行ENRO收集的数据进行了非房室分析。在血浆中,最大药物浓度(Cmax),达到该最大药物浓度的时间(Tmax),消除半衰期(t%一半)和浓度下的面积vs.时间曲线(AUC)分别为694.7 ng / mL,1.0 h,9.3 h和8903.2 ngp·h / mL。在鼻分泌物中,Cmax,Tmax,二分之一半和AUC分别为871.4 ng / mL,2.0 h,12.5 h和11 198.5 ngp.h / mL。在10头仔猪中进行的第二项实验中,在肌注2.5、10或20 mg / kg体重的单剂量肌肉后,测定了血浆中ENRO浓度与鼻腔分泌物之间的关系。已经证明,在几个变量中,即(1)给药剂量,(2)肌肉注射和采血之间的时间,(3)年龄,(4)性别,(5)动物体重(6)药物的血浆浓度,只有后者显着影响鼻分泌物中的ENRO浓度。实际上,使用广义线性混合模型,可以根据以下方程式,考虑到血浆中的ENRO浓度(og / mL),来预测鼻分泌物的ENRO浓度(og / mL):

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