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Pharmacokinetics of neomycin sulfate after intravenous and oral administrations in swine
Journal of Veterinary Pharmacology and Therapeutics ( IF 1.3 ) Pub Date : 2021-06-24 , DOI: 10.1111/jvp.12981
Yu Liu 1, 2 , Yuxin Yang 1, 2 , Yuying Cao 1, 2 , Jicheng Qiu 1, 2 , Jingyuan Kong 1, 2 , Lu Zhang 1, 2 , Yanying Guo 1, 2 , Mingchuan Zhang 3 , Xingyuan Cao 1, 2, 4 , Suxia Zhang 1, 2, 4
Affiliation  

The aminoglycoside antibiotic neomycin, which is used to treat external or internal bacterial infections, is primarily administered in veterinary medicine as a sulfate salt. However, no information is available on the pharmacokinetic characteristics and absolute availability of neomycin sulfate after intravenous (i.v.) and oral (p.o.) administrations in swine. Here, these parameters were studied in swine after i.v. and p.o. doses of single 15 mg/kg body weight doses. The blood samples were assessed using ultra-high-performance liquid chromatography-tandem mass/mass spectrometry (UPLC-MS/MS) and pharmacokinetic parameters were analyzed using a non-compartmental model. In swine, after the p.o. administration, the elimination half-life, mean residue time from t0 to the last collection point, mean maximum concentration, mean time to reach maximum concentration and area under concentration–time curve from t0 to the last collection point values were 12.43 ± 7.63 h, 10.25 ± 4.32 h, 0.11 ± 0.07 μg/ml, 1.92 ± 0.97 h and 1.23 ± 0.78 μg·h/ml, respectively, whereas after the i.v. administration, the values were 5.87 ± 1.12 h, 6.07 ± 0.49 h, 15.80 ± 1.32 μg/ml, 0.30 ± 0.38 h and 76.14 ± 3.52 μg·h/ml, respectively. The absolute bioavailability of neomycin sulfate B was 4.84%±0.03.

中文翻译:

硫酸新霉素静脉和口服给药后在猪体内的药代动力学

氨基糖苷类抗生素新霉素用于治疗外部或内部细菌感染,主要作为硫酸盐用于兽医。然而,没有关于在猪中静脉(iv)和口服(po)给药后硫酸新霉素的药代动力学特征和绝对可用性的信息。在这里,在 iv 和 po 剂量的单次 15 mg/kg 体重剂量后,在猪中研究了这些参数。使用超高效液相色谱-串联质谱 (UPLC-MS/MS) 评估血液样本,并使用非房室模型分析药代动力学参数。在猪中,po给药后,消除半衰期,从t0到最后一个收集点的平均残留时间,平均最大浓度,达到最大浓度的平均时间和从 t0 到最后一个收集点的浓度-时间曲线下面积值为 12.43 ± 7.63 h、10.25 ± 4.32 h、0.11 ± 0.07 μg/ml、1.92 ± 0.97 h 和 1.23 ± 0.78 μg·h /ml,而在 iv 给药后,值分别为 5.87 ± 1.12 h、6.07 ± 0.49 h、15.80 ± 1.32 μg/ml、0.30 ± 0.38 h 和 76.14 ± 3.52 μg·h/ml。硫酸新霉素 B 的绝对生物利用度为 4.84%±0.03。
更新日期:2021-06-24
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