Haines G R, Brown M P, Gronwall R R, Merritt K A
Department of Large Animal Clinical Sciences, College of Veterinary Medicine, University of Florida, Gainesville 32610-0136, USA.
Can J Vet Res. 2000 Jul;64(3):171-7.
Serum concentrations and pharmacokinetics of enrofloxacin were studied in 6 mares after intravenous (IV) and intragastric (IG) administration at a single dose rate of 7.5 mg/kg body weight. In experiment 1, an injectable formulation of enrofloxacin (100 mg/mL) was given IV. At 5 min after injection, mean serum concentration was 9.04 microg/mL and decreased to 0.09 microg/mL by 24 h. Elimination half-life was 5.33 +/- 1.05 h and the area under the serum concentration vs time curve (AUC) was 21.03 +/- 5.19 mg x h/L. In experiment 2, the same injectable formulation was given IG. The mean peak serum concentration was 0.94 +/- 0.97 microg/mL at 4 h after administration and declined to 0.29 +/- 0.12 microg/mL by 24 h. Absorption of this enrofloxacin preparation after IG administration was highly variable, and for this reason, pharmacokinetic values for each mare could not be determined. In experiment 3, a poultry formulation (32.3 mg/mL) was given IG. The mean peak serum concentration was 1.85 +/- 1.47 microg/mL at 45 min after administration and declined to 0.19 +/- 0.06 microg/mL by 24 h. Elimination half-life was 10.62 +/- 5.33 h and AUC was 16.30 +/- 4.69 mg x h/L. Bioavailability was calculated at 78.29 +/- 16.55%. Minimum inhibitory concentrations of enrofloxacin were determined for equine bacterial culture specimens submitted to the microbiology laboratory over an 11-month period. The minimum inhibitory concentration of enrofloxacin required to inhibit 90% of isolates (MIC90) was 0.25 microg/mL for Staphylococcus aureus, Escherichia coli, Salmonella spp., Klebsiella spp., and Pasteurella spp. The poultry formulation was well tolerated and could be potentially useful in the treatment of susceptible bacterial infections in adult horses. The injectable enrofloxacin solution should not be used orally.
以7.5mg/kg体重的单剂量速率,对6匹母马静脉注射(IV)和灌胃(IG)恩诺沙星后的血清浓度和药代动力学进行了研究。在实验1中,静脉注射恩诺沙星的注射用制剂(100mg/mL)。注射后5分钟,平均血清浓度为9.04μg/mL,到24小时时降至0.09μg/mL。消除半衰期为5.33±1.05小时,血清浓度-时间曲线下面积(AUC)为21.03±5.19mg·h/L。在实验2中,对相同的注射用制剂进行灌胃。给药后4小时的平均血清峰值浓度为0.94±0.97μg/mL,到24小时时降至0.29±0.12μg/mL。灌胃给药后该恩诺沙星制剂的吸收差异很大,因此,无法确定每匹母马的药代动力学值。在实验3中,灌胃给予家禽用制剂(32.3mg/mL)。给药后45分钟的平均血清峰值浓度为1.85±1.47μg/mL,到24小时时降至0.19±0.06μg/mL。消除半衰期为10.62±5.33小时,AUC为16.30±4.69mg·h/L。计算得出生物利用度为78.29±16.55%。在11个月的时间里,对提交给微生物实验室的马属细菌培养标本测定了恩诺沙星的最低抑菌浓度。对于金黄色葡萄球菌、大肠杆菌、沙门氏菌属、克雷伯氏菌属和巴氏杆菌属,抑制90%分离株所需的恩诺沙星最低抑菌浓度(MIC90)为0.25μg/mL。家禽用制剂耐受性良好,可能对治疗成年马的易感细菌感染有用。注射用恩诺沙星溶液不应口服使用。