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头孢噻呋在健康肉用犊牛血清、组织腔液和支气管分泌物中的药代动力学评价。

Pharmacokinetic evaluation of ceftiofur in serum, tissue chamber fluid and bronchial secretions from healthy beef-bred calves.

作者信息

Halstead S L, Walker R D, Baker J C, Holland R E, Stein G E, Hauptman J G

机构信息

Department of Large Animal Clinical Sciences, College of Veterinary Medicine, Michigan State University, East Lansing 48823.

出版信息

Can J Vet Res. 1992 Oct;56(4):269-74.

Abstract

Ceftiofur is a new broad spectrum cephalosporin marketed for the treatment of acute bovine respiratory disease. In this investigation ceftiofur was administered by intramuscular injection, at 24 h intervals, to healthy beef-bred calves for four days at dosages of 2.2 and 4.4 mg/kg of body weight, with 4 wk intervals between dosing regimens. Serum, tissue chamber fluid (TCF), and bronchial secretion (BS) concentrations of ceftiofur were measured by microbiological assay after the first and fourth dose of each dosing regimen. Peak serum concentrations (Cmax) of 8.8 micrograms/mL and 17.3 micrograms/mL were obtained approximately 2 h (Tmax), the time of mean peak concentration) after single injections of 2.2 mg/kg and 4.4 mg/kg, respectively. The Cmax was increased approximately twofold following multiple doses of 2.2 mg/kg (Cmax = 13.1 micrograms/mL) and 4.4 mg/kg (Cmax = 24.1 micrograms/mL). Ceftiofur accumulated slowly into TCF and peak concentrations were found to be approximately 14% of those observed in serum after the first dose and approximately 24% after multiple dosing. Concentrations of ceftiofur in BS were obtained rapidly with peak concentrations reaching 45% of the serum Cmax after the first dose. After multiple dosing the Cmax for BS was approximately 25% of the serum Cmax. This study found that both the 2.2 mg/kg and 4.4 mg/kg dosing regimens resulted in continuous serum, TCF and BS concentrations of ceftiofur that exceeded the minimal concentration required to inhibit the bacteria most frequently isolated from calves with acute bovine respiratory disease.

摘要

头孢噻呋是一种新的广谱头孢菌素,用于治疗牛急性呼吸道疾病。在本研究中,对健康肉用犊牛每隔24小时进行一次肌肉注射头孢噻呋,连续四天,剂量分别为2.2毫克/千克和4.4毫克/千克体重,两次给药方案之间间隔4周。在每个给药方案的第一剂和第四剂后,通过微生物测定法测量血清、组织腔液(TCF)和支气管分泌物(BS)中头孢噻呋的浓度。单次注射2.2毫克/千克和4.4毫克/千克后,分别在约2小时(Tmax,平均峰值浓度时间)达到8.8微克/毫升和17.3微克/毫升的血清峰值浓度(Cmax)。多次注射2.2毫克/千克(Cmax = 13.1微克/毫升)和4.4毫克/千克(Cmax = 24.1微克/毫升)后,Cmax增加了约两倍。头孢噻呋缓慢蓄积到TCF中,发现第一剂后峰值浓度约为血清中观察到的浓度的14%,多次给药后约为24%。头孢噻呋在BS中的浓度迅速达到峰值,第一剂后峰值浓度达到血清Cmax的45%。多次给药后,BS的Cmax约为血清Cmax的25%。本研究发现,2.2毫克/千克和4.4毫克/千克的给药方案均导致血清、TCF和BS中头孢噻呋的浓度持续超过抑制从患有牛急性呼吸道疾病的犊牛中最常分离出的细菌所需的最低浓度。

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