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The bioavailability and pharmacokinetics of an amoxicillin–clavulanic acid granular combination after intravenous and oral administration in swine
Journal of Veterinary Pharmacology and Therapeutics ( IF 1.3 ) Pub Date : 2020-10-15 , DOI: 10.1111/jvp.12916 Pan Sun 1, 2 , Tingting Zhao 1, 2 , Hongzhi Xiao 1, 2 , Jie Wang 1, 2 , Suxia Zhang 1, 2, 3 , Xingyuan Cao 1, 2, 3
Journal of Veterinary Pharmacology and Therapeutics ( IF 1.3 ) Pub Date : 2020-10-15 , DOI: 10.1111/jvp.12916 Pan Sun 1, 2 , Tingting Zhao 1, 2 , Hongzhi Xiao 1, 2 , Jie Wang 1, 2 , Suxia Zhang 1, 2, 3 , Xingyuan Cao 1, 2, 3
Affiliation
The pharmacokinetic behaviours of amoxicillin (AMX) and clavulanic acid (CA) in swine were studied after either an intravenous or oral administration of AMX (10 mg/kg) and CA (2.5 mg/kg). The concentrations of these two medicines in swine plasma were determined using high‐performance liquid chromatographic‐tandem mass spectrometry, and the data were analysed using a noncompartmental model with the WinNonlin software. After intravenous administration, both substances were absorbed rapidly and reached their effective therapeutic concentration quickly. CA was eliminated more slowly compared with AMX. Moreover, the distribution volume of AMX was larger than that of CA, suggesting that AMX could penetrate tissues better. After oral administration of the granular formulation, no significant difference was observed in the mean elimination half‐life value between AMX and CA. The mean maximal plasma concentrations of AMX and CA, reached after 1.14 and 1.32 hr, were 2.58 and 1.91 μg/m, respectively. The mean oral bioavailability of AMX and CA was 23.6% and 26.4%, respectively. After oral administration, the T>MIC50 for three common respiratory pathogens was over 6.12 hr. Therefore, oral administration could be more effective in the clinical therapy of pigs, especially when administered twice daily.
中文翻译:
阿莫西林-克拉维酸颗粒组合在猪体内静脉和口服给药后的生物利用度和药代动力学
在静脉或口服 AMX (10 mg/kg) 和 CA (2.5 mg/kg) 后,研究了阿莫西林 (AMX) 和克拉维酸 (CA) 在猪体内的药代动力学行为。使用高效液相色谱-串联质谱法测定这两种药物在猪血浆中的浓度,并使用 WinNonlin 软件使用非房室模型分析数据。静脉给药后,两种物质均被迅速吸收并迅速达到其有效治疗浓度。与 AMX 相比,CA 的消除速度更慢。此外,AMX 的分布体积大于 CA,表明 AMX 可以更好地穿透组织。口服颗粒剂后,AMX 和 CA 之间的平均消除半衰期值没有观察到显着差异。在 1.14 和 1.32 小时后达到的 AMX 和 CA 的平均最大血浆浓度分别为 2.58 和 1.91 μg/m。AMX 和 CA 的平均口服生物利用度分别为 23.6% 和 26.4%。口服后,T>MIC三种常见呼吸道病原体的50超过 6.12 小时。因此,口服给药在猪的临床治疗中可能更有效,尤其是每天给药两次。
更新日期:2020-10-15
中文翻译:
阿莫西林-克拉维酸颗粒组合在猪体内静脉和口服给药后的生物利用度和药代动力学
在静脉或口服 AMX (10 mg/kg) 和 CA (2.5 mg/kg) 后,研究了阿莫西林 (AMX) 和克拉维酸 (CA) 在猪体内的药代动力学行为。使用高效液相色谱-串联质谱法测定这两种药物在猪血浆中的浓度,并使用 WinNonlin 软件使用非房室模型分析数据。静脉给药后,两种物质均被迅速吸收并迅速达到其有效治疗浓度。与 AMX 相比,CA 的消除速度更慢。此外,AMX 的分布体积大于 CA,表明 AMX 可以更好地穿透组织。口服颗粒剂后,AMX 和 CA 之间的平均消除半衰期值没有观察到显着差异。在 1.14 和 1.32 小时后达到的 AMX 和 CA 的平均最大血浆浓度分别为 2.58 和 1.91 μg/m。AMX 和 CA 的平均口服生物利用度分别为 23.6% 和 26.4%。口服后,T>MIC三种常见呼吸道病原体的50超过 6.12 小时。因此,口服给药在猪的临床治疗中可能更有效,尤其是每天给药两次。