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单剂量静脉注射和口服给药后,二氟沙星在日本鹌鹑(Coturnix japonica)体内的药代动力学。

Pharmacokinetics of difloxacin in Japanese quails (Coturnix japonica) after single intravenous and oral administration.

作者信息

Aboubakr M, Elbadawy M

机构信息

Department of Pharmacology, Faculty of Veterinary Medicine, Benha University, 13736, Moshtohor, Toukh, Elqaliobiya, Egypt.

Department of Pharmacology, Faculty of Veterinary Medicine, Benha University, 13736, Moshtohor, Toukh, Elqaliobiya, Egypt.

出版信息

Res Vet Sci. 2019 Feb;122:36-39. doi: 10.1016/j.rvsc.2018.11.012. Epub 2018 Nov 12.

Abstract

Pharmacokinetics of difloxacin (DF), a fluoroquinolone antibiotic, were investigated in Japanese quails (Coturnix japonica) after a single intravenous (IV) and oral (PO) administration of 10 mg/kg bodyweight. Plasma concentration profiles of DF were analyzed by a compartmental pharmacokinetic method. Following IV injection, the plasma concentration vs time profile was best described by a two-compartment open model. Elimination half-life (t), total body clearance (Cl), volume of distribution at steady state (V) and mean residence time (MRT) of DF were 5.45 ± 0.14 h, 0.22 ± 0.01 L/kg/h, 1.54 ± 0.06 L/kg and 6.92 ± 0.19 h, respectively. Following PO administration, DF was rapidly absorbed, with peak plasma concentration (C) of 3.67 μg/mL attained at 1.90 h (T) after administration. Absorption half-life (t), elimination half-life (t), mean absorption time (MAT) were 0.5 h, 5.26 h and 1.11 h, respectively. The bioavailability (F) following PO administration of DF was high (84.40%). For a successful clinical effect of DF in quails, a multiple dosage regimen of 10 mg/kg bodyweight, administered orally every 24 h is recommended to maintain effective plasma concentrations with bacterial infections, in which MIC90 is <0.2 μg/mL.

摘要

在日本鹌鹑(Coturnix japonica)单次静脉注射(IV)和口服(PO)10毫克/千克体重的氟喹诺酮类抗生素双氟沙星(DF)后,对其药代动力学进行了研究。采用房室药代动力学方法分析了DF的血浆浓度曲线。静脉注射后,血浆浓度-时间曲线最适合用二室开放模型描述。DF的消除半衰期(t)、全身清除率(Cl)、稳态分布容积(V)和平均驻留时间(MRT)分别为5.45±0.14小时、0.22±0.01升/千克/小时、1.54±0.06升/千克和6.92±0.19小时。口服给药后,DF迅速吸收,给药后1.90小时(T)达到血浆峰值浓度(C)3.67微克/毫升。吸收半衰期(t)、消除半衰期(t)、平均吸收时间(MAT)分别为0.5小时、5.26小时和1.11小时。口服DF后的生物利用度(F)较高(84.40%)。为使DF在鹌鹑中获得成功的临床效果,建议采用10毫克/千克体重、每24小时口服一次的多剂量方案,以在细菌感染(其中MIC90<0.2微克/毫升)时维持有效的血浆浓度。

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