Kaartinen L, Panu S, Pyörälä S
Department of Clinical Sciences, Faculty of Veterinary Medicine, University of Helsinki, Finland.
Equine Vet J. 1997 Sep;29(5):378-81. doi: 10.1111/j.2042-3306.1997.tb03143.x.
Pharmacokinetic behaviour of enrofloxacin was studied in 6 horses after intravenous (i.v.) or intramuscular (i.m.) administration of enrofloxacin (5 mg/kg bwt). Concentration of enrofloxacin and ciproflaxin were measured by high performance liquid chromatography in serum. Antimicrobial activity of the samples was determined with an agar-diffusion technique. Reactions at the site of i.m. injection were monitored clinically and by determination of serum creatine kinase (CK) activity. After i.v. administration, elimination half-life of enrofloxacin was 4.4 h and volume of distribution was 2.3 1/kg bwt. Enrofloxacin was rapidly metabolised to ciprofloxacin. The half-life of ciprofloxacin parallelled that of the parent drug, its concentration in serum reached 20-35% of that of the parent drug. After i.m. administration, elimination half-life of enrofloxacin was longer (9.9 h) than after i.v. administration. Mean absorption time of enrofloxacin was also long (9.9 h). No statistically significant differences were found when half-life and mean residence time of antimicrobial activity were compared with those of enrofloxacin and ciprofloxacin from chemically analysed data. Intramuscular injection of enrofloxacin was found to be very irritating. After i.m. administration, CK activity in serum, compared with pre-injection levels, increased over 10-fold. CK activity also stayed high during the 32 h follow-up period. Clinical reactions, such as swelling or tenderness at the i.m. injection sites, were observed in 2 horses.
在6匹马静脉注射(i.v.)或肌肉注射(i.m.)恩诺沙星(5mg/kg体重)后,对其药代动力学行为进行了研究。采用高效液相色谱法测定血清中恩诺沙星和环丙沙星的浓度。用琼脂扩散技术测定样品的抗菌活性。通过临床观察和测定血清肌酸激酶(CK)活性来监测肌肉注射部位的反应。静脉注射后,恩诺沙星的消除半衰期为4.4小时,分布容积为2.3L/kg体重。恩诺沙星迅速代谢为环丙沙星。环丙沙星的半衰期与母体药物平行,其血清浓度达到母体药物的20%-35%。肌肉注射后,恩诺沙星的消除半衰期比静脉注射后更长(9.9小时)。恩诺沙星的平均吸收时间也很长(9.9小时)。将抗菌活性的半衰期和平均驻留时间与化学分析数据中的恩诺沙星和环丙沙星进行比较时,未发现统计学上的显著差异。发现肌肉注射恩诺沙星具有很强的刺激性。肌肉注射后,与注射前水平相比,血清中的CK活性增加了10倍以上。在32小时的随访期内,CK活性也一直很高。在2匹马中观察到了临床反应,如肌肉注射部位的肿胀或压痛。