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单剂量静脉注射后磷霉素在鸡体内的药代动力学及长期口服给药后的组织水平

Pharmacokinetics of fosfomycin in chickens after a single intravenous dose and tissue levels following chronic oral administration.

作者信息

Aramayona J J, Bregante M A, Solans C, Rueda S, Fraile L J, Garcia M A

机构信息

Department of Pharmacology and Physiology, Veterinary Faculty, University of Zaragoza, Spain.

出版信息

Vet Res. 1997 Nov-Dec;28(6):581-8.

PMID:9428152
Abstract

This paper describes the pharmacokinetics of fosfomycin following a single i.v. bolus dose (10 mg/kg of body weight) in broiler chickens. Serial blood samples were collected up to 5 h post-administration. Fosfomycin serum concentrations were determined by a microbiological method, using Proteus mirabilis as the test microorganism. The serum concentration versus time curves after i.v. administration followed a biexponential decline. The main pharmacokinetic variables were t1/2 lambda l = 23 min, t1/2 lambda n = 112 min, VDarea = 575 +/- 190 mL/kg and CLb = 3.12 +/- 0.44 mL.min-1.kg-1. Tissue levels of fosfomycin in kidney, liver, lung, muscle, heart, fat, gizzard and serum were also determined after oral chronic administration of the drug in drinking water (150 micrograms/mL). During the oral chronic administration period, high FOS concentrations in serum were maintained (mean 6.1 +/- 1.1 micrograms/mL), but a significant decline over time could be observed (P < 0.05). Fosfomycin was detected in all tissues except muscle, with mean concentrations ranging from 0.63 microgram/g in fat to 13.48 micrograms/g in kidney. Twenty-four hours after the treatment was finished, fosfomycin levels were below the assay detection limit in all tissues tested.

摘要

本文描述了在肉鸡中单次静脉推注剂量(10毫克/千克体重)磷霉素后的药代动力学。给药后长达5小时采集系列血样。磷霉素血清浓度通过微生物学方法测定,使用奇异变形杆菌作为测试微生物。静脉给药后的血清浓度-时间曲线呈双指数下降。主要药代动力学变量为t1/2λl = 23分钟,t1/2λn = 112分钟,VDarea = 575±190毫升/千克,CLb = 3.12±0.44毫升·分钟-1·千克-1。在饮用水中口服慢性给药(150微克/毫升)该药物后,还测定了肾脏、肝脏、肺、肌肉、心脏、脂肪、砂囊和血清中的磷霉素组织水平。在口服慢性给药期间,血清中维持了高磷霉素浓度(平均6.1±1.1微克/毫升),但随时间可观察到显著下降(P<0.05)。除肌肉外,在所有组织中均检测到磷霉素,平均浓度范围从脂肪中的0.63微克/克到肾脏中的13.48微克/克。治疗结束24小时后,在所有测试组织中磷霉素水平均低于检测限。

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