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氟尼辛透皮剂在母猪体内的药代动力学

Pharmacokinetics of transdermal flunixin in sows.

作者信息

Cramer Mary C, Pairis-Garcia Monique D, Bowman Andrew S, Moeller Steven J, Zhang Yuntao, Sidhu Pritam K, Magnin Geraldine, Coetzee Johann F

机构信息

Department of Animal Sciences, The Ohio State University, Columbus, Ohio.

Department of Preventive Veterinary Medicine, The Ohio State University, Columbus, Ohio.

出版信息

J Vet Pharmacol Ther. 2019 Jul;42(4):492-495. doi: 10.1111/jvp.12772. Epub 2019 Jun 13.

Abstract

The objective of this study was to describe the pharmacokinetics (PK) of flunixin in 12 nonlactating sows following transdermal (TD) flunixin (3.33 mg/kg) and intravenous (IV; 2.20 mg/kg) flunixin meglumine (FM) administration using a crossover design with a 10-day washout period. Blood samples were collected postadministration from sows receiving IV FM (3, 6, 10, 20, 40 min and 1, 3, 6, 12, 16, 24, 36, and 48 hr) and from sows receiving TD flunixin (10, 20, 40 min and 1, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48, 60, and 72 hr). Liquid chromatography and mass spectrometry were used to determine plasma flunixin concentrations, and noncompartmental methods were used for PK analysis. The geometric mean ± SD area under the plasma concentration-time curve (AUC) following IV injection was 26,820.59 ± 9,033.88 and 511.83 ± 213.98 hr ng/ml for TD route. Mean initial plasma concentration (C ) was 26,279.70 ± 3,610.00 ng/ml, and peak concentration (C ) was 14.61 ± 7.85 ng/ml for IV and TD administration, respectively. The percent mean bioavailability of TD flunixin was 1.55 ± 1.00. Our results demonstrate that topical administration is not an efficient route for delivering flunixin in mature sows.

摘要

本研究的目的是采用交叉设计和10天洗脱期,描述12头非泌乳母猪经皮给予氟尼辛(3.33mg/kg)和静脉注射(IV;2.20mg/kg)氟尼辛葡甲胺(FM)后氟尼辛的药代动力学(PK)。给药后,从接受静脉注射FM的母猪(给药后3、6、10、20、40分钟以及1、3、6、12、16、24、36和48小时)和接受经皮氟尼辛的母猪(给药后10、20、40分钟以及1、2、3、4、6、8、12、16、24、36、48、60和72小时)采集血样。采用液相色谱和质谱法测定血浆氟尼辛浓度,并采用非房室方法进行药代动力学分析。静脉注射后血浆浓度-时间曲线下面积(AUC)的几何平均值±标准差,经皮给药途径为26,820.59±9,033.88小时·纳克/毫升,经皮给药途径为511.83±213.98小时·纳克/毫升。静脉注射和经皮给药的平均初始血浆浓度(C)分别为26,279.70±3,610.00纳克/毫升和14.61±7.85纳克/毫升,峰浓度(C)分别为14.61±7.85纳克/毫升。经皮氟尼辛的平均生物利用度百分比为1.55±1.00。我们的结果表明,局部给药不是在成年母猪中递送氟尼辛的有效途径。

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