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进食对健康成年马口服米诺环素药代动力学的影响。

Effect of feeding on the pharmacokinetics of oral minocycline in healthy adult horses.

作者信息

Echeverria K O, Lascola K M, Giguère S, Foreman J H

机构信息

Department of Veterinary Clinical Medicine, College of Veterinary Medicine, University of Illinois, Urbana, IL, USA.

Department of Large Animal Medicine, College of Veterinary Medicine, University of Georgia, Athens, GA, USA.

出版信息

J Vet Pharmacol Ther. 2018 Feb;41(1):e53-e56. doi: 10.1111/jvp.12456. Epub 2017 Sep 11.

DOI:10.1111/jvp.12456
PMID:28891075
Abstract

Minocycline is commonly used to treat bacterial and rickettsial infections in adult horses but limited information exists regarding the impact of feeding on its oral bioavailability. This study's objective was to compare the pharmacokinetics of minocycline after administration of a single oral dose in horses with feed withheld and with feed provided at the time of drug administration. Six healthy adult horses were administered intravenous (2.2 mg/kg) and oral minocycline (4 mg/kg) with access to hay at the time of oral drug administration (fed) and with access to hay delayed for 2 hr after oral drug administration (fasted), with a 7-day washout between treatments. Plasma concentration versus time data was analyzed based on noncompartmental pharmacokinetics. Mean ± SD bioavailability (fasted: 38.6% ± 4.6; fed: 15.7% ± 2.3) and C (fasted: 1.343 ± 0.418 μg/ml; fed: 0.281 ± 0.157 μg/ml) were greater in fasted horses compared to fed horses (p < .05 both). Median (range) T (hr) in fasted horses was 2.0 (1.5-3.5) and in fed horses was 5.0 (1.0-8.0) and was not significantly different between groups. Overnight fasting and delaying feeding hay 2 hr after oral minocycline administration improve drug bioavailability and thus plasma concentrations.

摘要

米诺环素常用于治疗成年马的细菌感染和立克次氏体感染,但关于进食对其口服生物利用度影响的信息有限。本研究的目的是比较在禁食和给药时同时提供饲料的马匹中单次口服米诺环素后的药代动力学。六匹健康成年马分别接受静脉注射(2.2毫克/千克)和口服米诺环素(4毫克/千克),口服给药时可获取干草(进食组),口服给药后延迟2小时获取干草(禁食组),两次治疗之间有7天的洗脱期。基于非房室药代动力学分析血浆浓度与时间的数据。与进食组马匹相比,禁食组马匹的平均±标准差生物利用度(禁食组:38.6%±4.6;进食组:15.7%±2.3)和Cmax(禁食组:1.343±0.418微克/毫升;进食组:0.281±0.157微克/毫升)更高(两者p均<0.05)。禁食组马匹的中位(范围)Tmax(小时)为2.0(1.5 - 3.5),进食组马匹为5.0(1.0 - 8.0),两组之间无显著差异。口服米诺环素后过夜禁食并延迟2小时提供干草可提高药物生物利用度,从而提高血浆浓度。

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