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氟苯尼考在犊牛脑脊液和血浆中的药代动力学。

Pharmacokinetics of florfenicol in cerebrospinal fluid and plasma of calves.

作者信息

de Craene B A, Deprez P, D'Haese E, Nelis H J, Van den Bossche W, De Leenheer P

机构信息

Laboratorium voor Farmaceutische Microbiologie, Universiteit, Gent, Ghent, Belgium.

出版信息

Antimicrob Agents Chemother. 1997 Sep;41(9):1991-5. doi: 10.1128/AAC.41.9.1991.

Abstract

Florfenicol, a fluorinated analog of thiamphenicol, is of great value in veterinary infectious diseases that formerly responded favorably to chloramphenicol. In view of the treatment of meningitis in calves, we studied its pharmacokinetics in the cerebrospinal fluid (CSF) and plasma of six animals. To this end, a new high-performance liquid chromatography method was developed which, unlike previous ones, uses solid-phase instead of double-phase extraction to isolate the drug. After a single intravenous dose of 20 mg/kg of body weight, a maximum concentration in CSF of 4.67 +/- 1.51 microg/ml (n = 6) was reached, with a mean residence time of 8.7 h. The decline of florfenicol in both CSF and plasma fitted a biexponential model with elimination half-lives of 13.4 and 3.2 h, respectively. Florfenicol penetrated well into CSF, as evidenced from an availability of 46% +/- 3% relative to plasma. The levels remained above the MIC for Haemophilus somnus over a 20-h period. Our results provide evidence indicating the effectiveness of florfenicol in the treatment of bacterial meningitis of calves.

摘要

氟苯尼考是甲砜霉素的一种氟化类似物,在以前对氯霉素反应良好的兽医传染病中具有重要价值。鉴于犊牛脑膜炎的治疗,我们研究了其在六只动物的脑脊液(CSF)和血浆中的药代动力学。为此,开发了一种新的高效液相色谱法,与以前的方法不同,该方法使用固相而非双相萃取来分离药物。静脉注射单次剂量20mg/kg体重后,脑脊液中的最大浓度达到4.67±1.51μg/ml(n = 6),平均驻留时间为8.7小时。氟苯尼考在脑脊液和血浆中的下降符合双指数模型,消除半衰期分别为13.4小时和3.2小时。氟苯尼考能很好地渗透到脑脊液中,相对于血浆的可用性为46%±3%即可证明。在20小时内,其水平保持在高于睡眠嗜血杆菌的最低抑菌浓度之上。我们的结果提供了证据,表明氟苯尼考在治疗犊牛细菌性脑膜炎方面是有效的。

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