Broome R L, Brooks D L, Babish J G, Copeland D D, Conzelman G M
Animal Resources Service, School of Veterinary Medicine, University of California, Davis 95616.
Am J Vet Res. 1991 Nov;52(11):1835-41.
The pharmacokinetic properties of the fluoroquinolone antimicrobial enrofloxacin were studied in New Zealand White rabbits. Four rabbits were each given enrofloxacin as a single 5 mg/kg of body weight dosage by IV, SC, and oral routes over 4 weeks. Serum antimicrobial concentrations were determined for 24 hours after dosing. Compartmental modeling of the IV administration indicated that a 2-compartment open model best described the disposition of enrofloxacin in rabbits. Serum enrofloxacin concentrations after SC and oral dosing were best described by a 1- and 2-compartment model, respectively. Overall elimination half-lives for IV, SC, and oral routes of administration were 2.5, 1.71, and 2.41 hours, respectively. The half-life of absorption for oral dosing was 26 times the half-life of absorption after SC dosing (7.73 hours vs 0.3 hour). The observed time to maximal serum concentration was 0.9 hour after SC dosing and 2.3 hours after oral administration. The observed serum concentrations at these times were 2.07 and 0.452 micrograms/ml, respectively. Mean residence times were 1.55 hours for IV injections, 1.46 hours for SC dosing, and 8.46 hours for oral administration. Enrofloxacin was widely distributed in the rabbit as suggested by the volume of distribution value of 2.12 L/kg calculated from the IV study. The volume of distribution at steady-state was estimated at 0.93 L/kg. Compared with IV administration, bioavailability was 77% after SC dosing and 61% for gastrointestinal absorption. Estimates of predicted average steady-state serum concentrations were 0.359, 0.254, and 0.226 micrograms/ml for IV, SC, and oral administration, respectively.(ABSTRACT TRUNCATED AT 250 WORDS)
在新西兰白兔中研究了氟喹诺酮类抗菌药恩诺沙星的药代动力学特性。4只兔子在4周内分别通过静脉注射、皮下注射和口服途径给予单次5mg/kg体重剂量的恩诺沙星。给药后24小时测定血清抗菌浓度。静脉给药的房室模型表明,二房室开放模型最能描述恩诺沙星在兔体内的处置情况。皮下注射和口服给药后的血清恩诺沙星浓度分别以单房室和二房室模型最佳描述。静脉注射、皮下注射和口服给药途径的总体消除半衰期分别为2.5小时、1.71小时和2.41小时。口服给药的吸收半衰期是皮下注射后吸收半衰期的26倍(7.73小时对0.3小时)。观察到的达到最大血清浓度的时间,皮下注射后为0.9小时,口服给药后为2.3小时。此时观察到的血清浓度分别为2.07微克/毫升和0.452微克/毫升。静脉注射的平均驻留时间为1.55小时,皮下注射为1.46小时,口服给药为8.46小时。根据静脉注射研究计算的分布容积值2.12L/kg表明,恩诺沙星在兔体内分布广泛。稳态分布容积估计为0.93L/kg。与静脉给药相比,皮下注射后的生物利用度为77%,胃肠道吸收为61%。静脉注射、皮下注射和口服给药的预测平均稳态血清浓度估计分别为0.359微克/毫升、0.254微克/毫升和0.226微克/毫升。(摘要截选至250字)