Bermingham Eden C, Papich Mark G
Department of Anatomy, Physiological Sciences, and Radiology, College of Veterinary Medicine, North Carolina State University, Raleigh 27606, USA.
Am J Vet Res. 2002 Jul;63(7):1012-7. doi: 10.2460/ajvr.2002.63.1012.
To compare pharmacokinetics of enrofloxacin administered IV and in various oral preparations to ewes.
5 mature Katahdin ewes weighing 42 to 50 kg.
Ewes received 4 single-dose treatments of enrofloxacin in a nonrandomized crossover design followed by a multiple-dose oral regimen. Single-dose treatments consisted of an IV bolus of enrofloxacin (5 mg/kg), an oral drench (10 mg/kg) made from crushed enrofloxacin tablets, oral administration in feed (10 mg/kg; mixture of crushed enrofloxacin tablets and grain), and another type of oral administration in feed (10 mg/kg; mixture of enrofloxacin solution and grain). The multiple-dose regimen consisted of feeding a mixture of enrofloxacin solution and grain (10 mg/kg, q 24 h, for 7 days). Plasma concentrations of enrofloxacin and ciprofloxacin were measured by use of high-performance liquid chromatography.
Harmonic mean half-life for oral administration was 14.80, 10.80, and 13.07 hours, respectively, for the oral drench, crushed tablets in grain, and enrofloxacin solution in grain. Oral bioavailability for the oral drench, crushed tablets in grain, and enrofloxacin in grain was 4789, 98.07, and 94.60%, respectively, and median maximum concentration (Cmax) was 1.61, 2.69, and 2.26 microg/ml, respectively. Median Cmax of the multiple-dose regimen was 2.99 microg/ml.
Enrofloxacin administered orally to sheep has a prolonged half-life and high oral bioavailability. Oral administration at 10 mg/kg, q 24 h, was sufficient to achieve a plasma concentration of 8 to 10 times the minimum inhibitory concentration (MIC) of any microorganism with an MIC < or = 0.29 microg/ml.
比较恩诺沙星静脉注射给药与多种口服制剂给药对母羊的药代动力学。
5只体重42至50千克的成年卡他丁母羊。
母羊采用非随机交叉设计接受4次单剂量恩诺沙星治疗,随后采用多剂量口服方案。单剂量治疗包括静脉推注恩诺沙星(5毫克/千克)、由碾碎的恩诺沙星片剂制成的口服灌服剂(10毫克/千克)、在饲料中口服给药(10毫克/千克;碾碎的恩诺沙星片剂与谷物的混合物)以及另一种在饲料中的口服给药方式(10毫克/千克;恩诺沙星溶液与谷物的混合物)。多剂量方案包括投喂恩诺沙星溶液与谷物的混合物(10毫克/千克,每24小时一次,共7天)。采用高效液相色谱法测定血浆中恩诺沙星和环丙沙星的浓度。
口服灌服剂、谷物中的碾碎片剂以及谷物中的恩诺沙星溶液口服给药的谐波平均半衰期分别为14.80、10.80和13.07小时。口服灌服剂、谷物中的碾碎片剂以及谷物中的恩诺沙星的口服生物利用度分别为4789%、98.07%和94.60%,中位最大浓度(Cmax)分别为1.61、2.69和2.26微克/毫升。多剂量方案的中位Cmax为2.99微克/毫升。
绵羊口服恩诺沙星具有较长的半衰期和较高的口服生物利用度。每24小时口服10毫克/千克足以使血浆浓度达到对任何最低抑菌浓度(MIC)≤0.29微克/毫升的微生物的最低抑菌浓度的8至10倍。