Craig A J, Ramzan I, Malik R
Department of Veterinary Clinical Sciences, University of Sydney, New South Wales, Australia.
Res Vet Sci. 1994 Nov;57(3):372-6. doi: 10.1016/0034-5288(94)90133-3.
Fluconazole (100 mg) was administered to six adult cats as an intravenous infusion over 30 minutes, and the same cats received 100 mg of the drug orally 16 weeks later. The cats were bled repeatedly through an indwelling jugular catheter, the plasma fluconazole concentrations were assayed by high performance liquid chromatography, and the concentration-time data were subjected to a non-compartmental pharmacokinetic analysis. The mean (SD) intravenous half-life (13.8 [2.6] hours) was similar to that observed after oral dosing (12.4 [3.0] hours). The plasma clearances (intravenous 0.9 [0.1], oral 0.9 [0.2] ml min-1 kg-1) and the volumes of distribution at steady state (intravenous 1.1 [0.1], oral 1.0 [0.1] litre kg-1) were also similar after the two routes of dosing. The peak plasma concentration was reached 2.6 hours after oral dosing and the drug was completely bioavailable (1.09 [0.05]). On the basis of this single dose study, the administration of 50 mg fluconazole every eight hours to a 4 kg cat should produce average steady state plasma fluconazole concentrations of approximately 33 mg litre-1.
将氟康唑(100毫克)以静脉输注的方式在30分钟内给予6只成年猫,16周后相同的猫口服100毫克该药物。通过留置的颈静脉导管对猫进行多次采血,采用高效液相色谱法测定血浆氟康唑浓度,并对浓度-时间数据进行非房室药代动力学分析。静脉给药后的平均(标准差)半衰期(13.8 [2.6]小时)与口服给药后观察到的半衰期(12.4 [3.0]小时)相似。两种给药途径后的血浆清除率(静脉给药0.9 [0.1],口服给药0.9 [0.2]毫升·分钟⁻¹·千克⁻¹)和稳态分布容积(静脉给药1.1 [0.1],口服给药1.0 [0.1]升·千克⁻¹)也相似。口服给药后2.6小时达到血浆峰浓度,且药物完全生物利用(1.09 [0.05])。基于该单剂量研究,对一只4千克的猫每8小时给予50毫克氟康唑,应可产生约33毫克·升⁻¹的平均稳态血浆氟康唑浓度。