Leiberich Marion, Krebber Ralph, Hewetson Michael, Marais Johan, Naidoo Vinny
Faculty of Veterinary Science, Department of Companion Animal Clinical Studies, University of Pretoria, Pretoria, South Africa.
Research & Development-Regulatory Science-Human Safety-Residue Analysis, Bayer Crop Science AG, Monheim am Rhein, Germany.
J Vet Pharmacol Ther. 2019 May;42(3):346-354. doi: 10.1111/jvp.12747. Epub 2019 Jan 17.
South Africa currently loses over 1000 white rhinoceros (Ceratotherium simum) each year to poaching incidents, and numbers of severely injured victims found alive have increased dramatically. However, little is known about the antimicrobial treatment of wounds in rhinoceros. This study explores the applicability of enrofloxacin for rhinoceros through the use of pharmacokinetic-pharmacodynamic modelling. The pharmacokinetics of enrofloxacin and its metabolite ciprofloxacin were evaluated in five white rhinoceros after intravenous (i.v.) and after successive i.v. and oral administration of 12.5 mg/kg enrofloxacin. After i.v. administration, the half-life, area under the curve (AUC ), clearance and the volume of distribution were 12.41 ± 2.62 hr, 64.5 ± 14.44 μg ml hr , 0.19 ± 0.04 L h kg , and 2.09 ± 0.48 L/kg, respectively. Ciprofloxacin reached 26.42 ± 0.05% of the enrofloxacin plasma concentration. After combined i.v. and oral enrofloxacin administration oral bioavailability was 33.30 ± 38.33%. After i.v. enrofloxacin administration, the efficacy marker AUC : MIC exceeded the recommended ratio of 125 against bacteria with an MIC of 0.5 μg/mL. Subsequent intravenous and oral enrofloxacin administration resulted in a low Cmax: MIC ratio of 3.1. The results suggest that intravenous administration of injectable enrofloxacin could be a useful drug with bactericidal properties in rhinoceros. However, the maintenance of the drug plasma concentration at a bactericidal level through additional per os administration of 10% oral solution of enrofloxacin indicated for the use in chickens, turkeys and rabbits does not seem feasible.
南非目前每年因偷猎事件损失超过1000头白犀牛（白犀），且发现存活的重伤犀牛数量急剧增加。然而，关于犀牛伤口的抗菌治疗知之甚少。本研究通过药代动力学-药效学建模探索恩诺沙星对犀牛的适用性。在5头白犀牛静脉注射（i.v.）以及连续静脉注射和口服12.5mg/kg恩诺沙星后，评估了恩诺沙星及其代谢物环丙沙星的药代动力学。静脉注射后，半衰期、曲线下面积（AUC）、清除率和分布容积分别为12.41±2.62小时、64.5±14.44μg/ml·小时、0.19±0.04L/小时·千克和2.09±0.48L/千克。环丙沙星达到恩诺沙星血浆浓度的26.42±0.05%。静脉注射和口服恩诺沙星联合给药后，口服生物利用度为33.30±38.33%。静脉注射恩诺沙星后，疗效指标AUC:MIC超过了针对最低抑菌浓度（MIC）为0.5μg/mL的细菌推荐的125的比例。随后静脉注射和口服恩诺沙星导致低的Cmax:MIC比值3.1。结果表明，静脉注射恩诺沙星注射液可能是一种对犀牛具有杀菌特性的有用药物。然而，通过额外口服用于鸡、火鸡和兔子的10%恩诺沙星口服溶液将药物血浆浓度维持在杀菌水平似乎不可行。
