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伐尼霉素在蛋鸡静脉注射、肌肉注射和口服给药后的药代动力学

Pharmacokinetics of valnemulin after intravenous, intramuscular, and oral administration in layer chickens.

作者信息

Sun F, Fan R, Wang J, Xiong L, Shen J, Zhang S, Cao X

机构信息

Department of Veterinary Pharmacology and Toxicology, China Agricultural University, Beijing, China.

Key Laboratory of Detection for Veterinary Drug Residue and Illegal Additive, Ministry of Agriculture, Beijing, China.

出版信息

J Vet Pharmacol Ther. 2017 Aug;40(4):415-418. doi: 10.1111/jvp.12389. Epub 2017 Feb 15.

Abstract

The pharmacokinetic characteristics of valnemulin in layer chickens were studied after single intravenous, intramuscular, and oral administration at a dose of 15 mg/kg body weight. Plasma samples at certain time points were collected and the drug concentrations in them by ultra high-performance liquid chromatography tandem mass spectrometry (UHPLC-MS). The concentration-time data for each individual were plotted by noncompartmental analysis for the whole three routes. Following intravenous administration, the plasma concentration showed tiny fluctuation. The elimination half-life (T1/2λz), total body clearance (Cl), and area under the plasma concentration-time curve (AUC) were 1.85 ± 0.43 h, 2.2 ± 0.9 L/h, and 7.52 ± 2.46 μg·h/mL, respectively. Following intramuscular administration, the peak concentration (C , 1.40 ± 0.43 μg/mL) was achieved at the time of 0.34 h. A multiple-peak phenomenon existed after oral administration, and the first peak and secondary peak were at 10 min and during 2-4 h, respectively, while the tertiary peak appeared during 5-15 h. The bioavailability (F %) for intramuscular and oral administration was 68.60% and 52.64%, respectively. In present study, the detailed pharmacokinetic profiles showed that this drug is widely distributed and rapidly eliminated, however has a low bioavailability, indicating that valnemulin is likely to be a favorable choice in the clinical practice.

摘要

以15mg/kg体重的剂量对蛋鸡进行单次静脉注射、肌肉注射和口服给药后,研究了伐尼霉素的药代动力学特征。在特定时间点采集血浆样本,并通过超高效液相色谱串联质谱法(UHPLC-MS)测定其中的药物浓度。对三种给药途径的每个个体的浓度-时间数据进行非房室分析并绘制曲线。静脉给药后,血浆浓度波动较小。消除半衰期(T1/2λz)、全身清除率(Cl)和血浆浓度-时间曲线下面积(AUC)分别为1.85±0.43小时、2.2±0.9L/小时和7.52±2.46μg·小时/毫升。肌肉注射后,在0.34小时达到峰浓度(Cmax,1.40±0.43μg/mL)。口服给药后出现多峰现象,第一个峰和第二个峰分别出现在10分钟和2-4小时,而第三个峰出现在5-15小时。肌肉注射和口服给药的生物利用度(F%)分别为68.60%和52.64%。在本研究中,详细的药代动力学特征表明该药物分布广泛且消除迅速,但生物利用度较低,这表明伐尼霉素在临床实践中可能是一个不错的选择。

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