McKellar Q A, Gibson I F, McCormack R Z
Department of Veterinary Pharmacology, University of Glasgow Veterinary School, UK.
Biopharm Drug Dispos. 1998 Mar;19(2):123-9. doi: 10.1002/(sici)1099-081x(199803)19:2<123::aid-bdd89>3.0.co;2-g.
The plasma pharmacokinetics of danofloxacin administered at 1.25 mg kg-1 body weight by the intravenous and intramuscular routes were determined in sheep. Tissue distribution was also determined following administration by the intramuscular route at 1.25 mg kg-1 body weight. Danofloxacin had a large volume of distribution at steady state (Vdss) of 2.76 +/- 0.16 h (mean +/- S.E.M.) L kg-1, an elimination half-life (t1/2 beta) of 3.35 +/- 0.23 h, and a body clearance (C1) of 0.63 +/- 0.04 L kg-1 h-1. Following intramuscular administration it achieved a maximum concentration (Cmax) of 0.32 +/- 0.02 microgram mL-1 at 1.23 +/- 0.34 h (tmax) and had a mean residence time (MRT) of 5.45 +/- 0.19 h. Danofloxacin had an absolute bioavailability (F) of 95.71 +/- 4.41% and a mean absorption time (MAT) of 0.81 +/- 0.20 h following intramuscular administration. Mean plasma concentrations of > 0.06 microgram mL-1 were maintained for more than 8 h following intravenous and intramuscular administration. Following intramuscular administration highest concentrations were measured in plasma (0.43 +/- 0.04 microgram mL-1), lung (1.51 +/- 0.18 micrograms g-1), and interdigital skin (0.64 +/- 0.18 microgram g-1) at 1 h, duodenal contents (0.81 +/- 0.40 microgram mL-1), lymph nodes (4.61 +/- 0.35 micrograms g-1), and brain (0.06 +/- 0.00 microgram mL-1) at 2 h, jejunal (10.50 +/- 4.31 micrograms mL-1) and ileal (5.25 +/- 1.67 micrograms mL-1) contents at 4 h, and colonic contents (8.94 +/- 0.65 micrograms mL-1) at 8 h.
通过静脉注射和肌肉注射途径，以1.25毫克/千克体重的剂量给绵羊注射达氟沙星，测定其血浆药代动力学。还测定了以1.25毫克/千克体重肌肉注射给药后的组织分布情况。达氟沙星稳态时的分布容积（Vdss）为2.76±0.16升/千克（平均值±标准误），消除半衰期（t1/2β）为3.35±0.23小时，机体清除率（C1）为0.63±0.04升/千克/小时。肌肉注射后，在1.23±0.34小时（达峰时间）达到最大浓度（Cmax）为0.32±0.02微克/毫升，平均驻留时间（MRT）为5.45±0.19小时。肌肉注射后，达氟沙星的绝对生物利用度（F）为95.71±4.41%，平均吸收时间（MAT）为0.81±0.20小时。静脉注射和肌肉注射后，血浆平均浓度>0.06微克/毫升可维持8小时以上。肌肉注射后，1小时时血浆（0.43±0.04微克/毫升）、肺（1.51±0.18微克/克）和趾间皮肤（0.64±0.18微克/克）中测得的浓度最高，2小时时十二指肠内容物（0.81±0.40微克/毫升）、淋巴结（4.61±0.35微克/克）和脑（0.06±0.00微克/毫升）中浓度最高，4小时时空肠（10.55±4.31微克/毫升）和回肠（5.25±1.67微克/毫升）内容物中浓度最高，8小时时结肠内容物（8.94±0.65微克/毫升）中浓度最高。
