Wiuff C, Lykkesfeldt J, Aarestrup F M, Svendsen O
Danish Veterinary Institute, Bülowsvej 27, DK-1790 Copenhagen V, Denmark.
J Vet Pharmacol Ther. 2002 Oct;25(5):335-42. doi: 10.1046/j.1365-2885.2002.00430.x.
The concentration of enrofloxacin in plasma, intestinal tissue, lymph nodes and intestinal contents was investigated in healthy pigs after oral (p.o.) and intramuscular (i.m.) administration of a single dose of 2.5 mg/kg bw. Tissue and content samples were collected from jejunum, ileum, caecum and colon from pigs killed at 2, 3 and 6 h after dosing. Intramuscular administration resulted in significantly higher concentrations in plasma, intestinal tissue and lymph nodes at 2 h but not at 3 or 6 h compared with p.o. administration. The absorption and distribution phase was longer after oral administration, and maximum concentrations in tissue and plasma were determined later than after i.m. administration. No difference between route of administration was observed in the intestinal content. Enrofloxacin concentrations in faeces during a 5-day dosing regimen with i.m. and p.o. administration were determined by both HPLC and bio-assay. Higher concentrations were found after i.m. administration during the first day, but the difference was not significant after 2 days. The biologically active concentrations determined by bio-assay constituted 48-75% of the total concentrations determined by HPLC. On the basis of these results it was concluded that in order to ensure an immediate high concentration of enrofloxacin, and thereby avoid an initial selection for resistant mutants, the intramuscular route seems to be preferable to the oral route.
在健康猪口服(p.o.)和肌肉注射(i.m.)单剂量2.5 mg/kg体重的恩诺沙星后,对其血浆、肠组织、淋巴结和肠内容物中的恩诺沙星浓度进行了研究。在给药后2、3和6小时处死猪,从空肠、回肠、盲肠和结肠采集组织和内容物样本。与口服给药相比,肌肉注射在2小时时血浆、肠组织和淋巴结中的浓度显著更高,但在3或6小时时并非如此。口服给药后吸收和分布阶段更长,组织和血浆中的最大浓度比肌肉注射后测定得更晚。在肠内容物中未观察到给药途径之间的差异。通过高效液相色谱法(HPLC)和生物测定法测定了肌肉注射和口服给药5天方案期间粪便中的恩诺沙星浓度。肌肉注射给药后第一天发现浓度更高,但2天后差异不显著。通过生物测定法测定的生物活性浓度占通过HPLC测定的总浓度的48 - 75%。基于这些结果得出结论,为了确保恩诺沙星立即达到高浓度,从而避免对耐药突变体的初始选择,肌肉注射途径似乎比口服途径更可取。