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头孢噻呋在亚洲象(印度象)体内的药代动力学及肌肉注射生物利用度

Pharmacokinetics and i.m. bioavailability of ceftiofur in Asian elephants (Elephas maximus).

作者信息

Dumonceaux G, Isaza R, Koch D E, Hunter R P

机构信息

Busch Gardens Tampa Bay, Tampa, FL, USA.

出版信息

J Vet Pharmacol Ther. 2005 Oct;28(5):441-6. doi: 10.1111/j.1365-2885.2005.00686.x.

DOI:10.1111/j.1365-2885.2005.00686.x
PMID:16207306
Abstract

Captive elephants are prone to infections of the feet, lungs, and skin. Often treatment regimens are established with no pharmacokinetic data on the agents being used for treatment in these species. A pharmacokinetic study using ceftiofur (1.1 mg/kg) was conducted in four adult female captive Asian elephants (Elephas maximus) at Busch Gardens in Tampa, Florida. Elephants were given both i.v. and i.m. administrations in a complete crossover design with a 3-week washout period between treatments. Blood samples were collected prior to drug administration and at 0.33, 0.67, 1, 1.5, 2, 4, 8, 12, 24, 48 and 72 h postadministration. Ceftiofur analysis was performed using a validated liquid chromatography/mass spectrophotometric (LC/MS) assay. Plasma concentrations for the i.m. samples were lower than expected. The mean C(max) following i.m. administration was 1.63 microg/mL with a corresponding T(max) of 0.55 h. Following i.v. administration, the median V(d(ss)) was 0.51 L/kg and a median Cl(p) of 0.069 L/kg/h. Mean i.m. bioavailability was 19%. The results indicate that ceftiofur used at 1.1 mg/kg i.m. could be useful in elephants when given two to three times a day or alternatively, 1.1 mg/kg i.v. once daily, depending upon the MIC of the pathogen.

摘要

圈养大象容易出现足部、肺部和皮肤感染。通常在制定治疗方案时,并未掌握用于这些物种治疗的药物的药代动力学数据。在佛罗里达州坦帕市布希花园对4头成年雌性圈养亚洲象(印度象)进行了一项使用头孢噻呋(1.1毫克/千克)的药代动力学研究。大象采用完全交叉设计接受静脉注射和肌肉注射给药,两次治疗之间有3周的洗脱期。在给药前以及给药后0.33、0.67、1、1.5、2、4、8、12、24、48和72小时采集血样。使用经过验证的液相色谱/质谱(LC/MS)分析法进行头孢噻呋分析。肌肉注射样本的血浆浓度低于预期。肌肉注射后的平均C(max)为1.63微克/毫升,相应的T(max)为0.55小时。静脉注射后,中位稳态分布容积(V(d(ss)))为0.51升/千克,中位清除率(Cl(p))为0.069升/千克/小时。平均肌肉注射生物利用度为19%。结果表明,根据病原体的最低抑菌浓度(MIC),每天肌肉注射2至3次1.1毫克/千克的头孢噻呋对大象可能有效,或者每天静脉注射1次1.1毫克/千克也可能有效。

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