Kirby A, Lewbart G A, Hancock-Ronemus A, Papich M G
College of Veterinary Medicine, North Carolina State University, Raleigh, NC, USA.
Marine Biological Laboratory, Woods Hole, MA, USA.
J Vet Pharmacol Ther. 2018 Apr;41(2):349-353. doi: 10.1111/jvp.12462. Epub 2017 Oct 25.
The pharmacokinetics of enrofloxacin and the metabolite ciprofloxacin were studied in horseshoe crabs after a single injection of 5 mg/kg. Twelve Atlantic horseshoe crabs (Limulus polyphemus) of undetermined age were injected with enrofloxacin into the dorsal cardiac sinus. Hemolymph samples were collected by syringe and needle at regular intervals for 120 hr. Samples were analyzed by high-pressure liquid chromatography and compartmental analysis performed on the results. Following injection, the elimination half-life (T½), peak concentration, area under the curve (AUC), and volume of distribution (VD) for enrofloxacin were 27.9 (29.13) hr, 8.98 (18.09) μg/ml, 367.38 (35.41) hr μg/ml, and 0.575 (20.48) L/kg, respectively (mean value, CV%). For ciprofloxacin, the elimination T½, peak concentration, and AUC were 61.36 (34.55) hr, 2.34 (24.11) μg/ml, and 304.46 (24.69) μg hr/ml. In these animals, the ciprofloxacin concentrations comprised an average of 45.8% of the total fluoroquinolone concentrations, which is substantial compared to other marine invertebrates. The total AUC produced (sum of enrofloxacin and ciprofloxacin) was 682.69 ± 180.61 μg hr/ml. Concentrations that were achieved after a single dose of 5 mg/kg horseshoe crabs were sufficient to treat bacteria susceptible to enrofloxacin and ciprofloxacin.
在单次注射5mg/kg恩诺沙星后，研究了鲎体内恩诺沙星及其代谢产物环丙沙星的药代动力学。将12只年龄未明的大西洋鲎（美洲鲎）通过背侧心窦注射恩诺沙星。用注射器和针头定期采集血淋巴样本，持续120小时。样本通过高压液相色谱分析，并对结果进行房室分析。注射后，恩诺沙星的消除半衰期（T½）、峰浓度、曲线下面积（AUC）和分布容积（VD）分别为27.9（29.13）小时、8.98（18.09）μg/ml、367.38（35.41）小时·μg/ml和0.575（20.48）L/kg（平均值，CV%）。对于环丙沙星，消除T½、峰浓度和AUC分别为61.36（34.55）小时、2.34（24.11）μg/ml和304.46（24.69）μg·小时/ml。在这些动物中，环丙沙星浓度平均占氟喹诺酮总浓度的45.8%，与其他海洋无脊椎动物相比，这一比例相当可观。产生的总AUC（恩诺沙星和环丙沙星之和）为682.69±180.61μg·小时/ml。单次给予5mg/kg鲎后达到的浓度足以治疗对恩诺沙星和环丙沙星敏感的细菌。
