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恩诺沙星及其主要代谢物环丙沙星在泰国沼泽水牛体内的处置情况。

Dispositions of enrofloxacin and its major metabolite ciprofloxacin in Thai swamp buffaloes.

作者信息

Ruennarong Nitwarat, Wongpanit Kannika, Sakulthaew Chainarong, Giorgi Mario, Kumagai Susumu, Poapolathep Amnart, Poapolathep Saranya

机构信息

Department of Pharmacology, Faculty of Veterinary Medicine, Kasetsart University, Bangkok 10900, Thailand.

出版信息

J Vet Med Sci. 2016 Mar;78(3):397-403. doi: 10.1292/jvms.15-0464. Epub 2015 Nov 20.

Abstract

Given the limited information available in this species, the aim of this study was to investigate the pharmacokinetic characteristics of enrofloxacin (ER) and its major metabolite ciprofloxacin (CP) in buffaloes, Bubalus bubalis. ER was administered intravenously (i.v.) or subcutaneously (s.c.) to buffaloes at doses of 5.0 and 7.5 mg/kg BW, and plasma, urine and fecal samples were collected until 48 hr post-administration. The concentrations of ER and CP in the plasma, urine and feces were analyzed using high-performance liquid chromatography equipped with a fluorescence detector. The plasma concentrations of ER and CP could be determined up to 24 hr and 32 hr after i.v. and s.c. administrations at doses of 5.0 and 7.5 mg/kg BW, respectively. CP concentrations were always lower than those of parental drug. The s.c. bioavailability of ER was 52.36 ± 4.24% and 72.12 ± 5.39% at doses of 5.0 and 7.5 mg/kg BW, respectively. Both ER and CP were detectable in urine and feces up to 24 hr. ER and CP were mainly excreted via the urine. Based on the pharmacokinetic data and PK-PD indices, s.c. administration of ER at doses of 5.0 and 7.5 mg/kg BW might be appropriate for the treatment of susceptible bacterial diseases in Thai swamp buffaloes.

摘要

鉴于该物种可用信息有限,本研究旨在调查恩诺沙星(ER)及其主要代谢物环丙沙星(CP)在水牛(Bubalus bubalis)体内的药代动力学特征。以5.0和7.5 mg/kg体重的剂量对水牛静脉注射(i.v.)或皮下注射(s.c.)恩诺沙星,并在给药后48小时内收集血浆、尿液和粪便样本。使用配备荧光检测器的高效液相色谱法分析血浆、尿液和粪便中恩诺沙星和环丙沙星的浓度。在5.0和7.5 mg/kg体重剂量下静脉注射和皮下注射后,恩诺沙星和环丙沙星的血浆浓度分别可在24小时和32小时内测定出来。环丙沙星浓度始终低于母体药物浓度。在5.0和7.5 mg/kg体重剂量下,恩诺沙星的皮下生物利用度分别为52.36±4.24%和72.12±5.39%。在尿液和粪便中,恩诺沙星和环丙沙星在24小时内均可检测到。恩诺沙星和环丙沙星主要通过尿液排泄。根据药代动力学数据和PK-PD指数,以5.0和7.5 mg/kg体重的剂量对泰国沼泽水牛皮下注射恩诺沙星可能适合治疗易感细菌性疾病。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/36da/4829506/13354d50c9bf/jvms-78-397-g001.jpg

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