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氟苯尼考在泌乳奶牛静脉注射、肌肉注射和乳房内给药后的药代动力学

Florfenicol pharmacokinetics in lactating cows after intravenous, intramuscular and intramammary administration.

作者信息

Soback S, Paape M J, Filep R, Varma K J

机构信息

National Residue Control Laboratory, Kimron Veterinary Institute, Beit Dagan, Israel.

出版信息

J Vet Pharmacol Ther. 1995 Dec;18(6):413-7. doi: 10.1111/j.1365-2885.1995.tb00618.x.

Abstract

Pharmacokinetics of florfenicol 30% injectable solution was determined in lactating cows after intravenous, intramammary and intramuscular administration. Serum concentration-time data generated in the present study were analysed by non-compartmental methods based on statistical moment theory. Florfenicol half-life was 176 min, mean residence time 129 min, volume of distribution at steady-state 0.35 L/kg, and total body clearance 2.7 mL/min.kg after intravenous administration at 20 mg/kg. The absorption after intramuscular administration appeared slow and the kinetic parameters and the serum concentration vs. time curve were characteristic of absorption rate-dependent elimination. The absorption after intramammary administration of florfenicol at 20 mg/kg was good (53.9%) and resulted in serum concentrations with apparent clinical significance. The intramammary administration resulted in serum florfenicol concentrations that were significantly higher than the respective serum concentrations following intravenous administration 4 h after administration and thereafter. Florfenicol absorption was faster from the mammary gland than from the muscle. The maximum serum concentrations (Cmax) were 6.9 micrograms/mL at 360 min after intramammary administration and 2.3 micrograms/mL at 180 min after intramuscular administration. The bioavailability of florfenicol was 54% and 38% after intramammary and intramuscular administration, respectively. The Cmax in milk was 5.4 micrograms/mL at 180 min after intravenous and 1.6 micrograms/mL at 600 min after intramuscular administration.

摘要

在泌乳奶牛中,分别通过静脉注射、乳房内注射和肌肉注射给药,测定了30%氟苯尼考注射液的药代动力学。本研究生成的血清浓度-时间数据采用基于统计矩理论的非房室方法进行分析。静脉注射20mg/kg后,氟苯尼考的半衰期为176分钟,平均驻留时间为129分钟,稳态分布容积为0.35L/kg,全身清除率为2.7mL/分钟·kg。肌肉注射后吸收似乎较慢,动力学参数以及血清浓度与时间曲线具有吸收速率依赖性消除的特征。乳房内注射20mg/kg氟苯尼考后的吸收良好(53.9%),并产生了具有明显临床意义的血清浓度。乳房内注射后血清氟苯尼考浓度在给药后4小时及之后显著高于静脉注射后的相应血清浓度。氟苯尼考从乳腺的吸收比从肌肉更快。乳房内注射后360分钟时的最大血清浓度(Cmax)为6.9微克/毫升,肌肉注射后180分钟时为2.3微克/毫升。乳房内注射和肌肉注射后氟苯尼考的生物利用度分别为54%和38%。静脉注射后180分钟时牛奶中的Cmax为5.4微克/毫升,肌肉注射后600分钟时为1.6微克/毫升。

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