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猫体内的氟康唑:静脉注射和口服给药后的药代动力学以及在脑脊液、房水和肺上皮衬液中的渗透情况。

Fluconazole in cats: pharmacokinetics following intravenous and oral administration and penetration into cerebrospinal fluid, aqueous humour and pulmonary epithelial lining fluid.

作者信息

Vaden S L, Heit M C, Hawkins E C, Manaugh C, Riviere J E

机构信息

Department of Companion Animal and Special Species Medicine, College of Veterinary Medicine, North Carolina State University, Raleigh 27606, USA.

出版信息

J Vet Pharmacol Ther. 1997 Jun;20(3):181-6. doi: 10.1111/j.1365-2885.1997.tb00093.x.

Abstract

The pharmacokinetics of fluconazole following intravenous (i.v.) and oral (p.o.) administration and the penetration of fluconazole into cerebrospinal fluid, aqueous humour and epithelial lining fluid (ELF) of the lungs were evaluated in adult male cats. Pharmacokinetic parameters were calculated from serum concentration-time data obtained following i.v. and p.o. administration of 50 mg per cat using a cross-over study design. Fluconazole concentrations were measured using a high-performance liquid chromatography assay. Mean total body clearance of fluconazole was 37.7 mL/h.kg, mean volume of distribution at steady state was 1.14 L/kg, mean residence time was 31.0 h and mean half-life of elimination was 25 h as derived by non-compartmental analysis of data. Absorption was complete. Mean ratios of fluid:serum fluconazole concentrations following administration of 50 mg fluconazole per day for 8 days were as follows: cerebrospinal fluid, 0.88; aqueous humour 0.79; ELF, 1.20. Fluconazole concentrations in cerebrospinal fluid, aqueous humour and ELF exceeded reported minimum inhibitory concentrations of fluconazole for pathogenic fungi. Results of this study suggest fluconazole can effectively be administered to cats at 50 mg per cat per day.

摘要

在成年雄性猫中评估了氟康唑静脉注射(i.v.)和口服(p.o.)给药后的药代动力学,以及氟康唑在脑脊液、房水和肺上皮衬液(ELF)中的渗透情况。采用交叉研究设计,根据每只猫静脉注射和口服50mg后获得的血清浓度 - 时间数据计算药代动力学参数。使用高效液相色谱法测定氟康唑浓度。通过对数据进行非房室分析得出,氟康唑的平均全身清除率为37.7 mL/h.kg,稳态分布容积平均为1.14 L/kg,平均滞留时间为31.0 h,平均消除半衰期为25 h。吸收完全。每天给予50mg氟康唑,连续8天给药后,脑脊液、房水和ELF中氟康唑浓度与血清氟康唑浓度的平均比值如下:脑脊液为0.88;房水为0.79;ELF为1.20。脑脊液、房水和ELF中的氟康唑浓度超过了报道的氟康唑对致病真菌的最低抑菌浓度。本研究结果表明,每天每只猫给予50mg氟康唑可有效地用于猫。

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