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在不同给药途径后,野鸭体内莫西沙星的药代动力学、血浆蛋白结合率和生物利用度。

Pharmacokinetics, plasma protein binding and bioavailability of moxifloxacin in Muscovy ducks after different routes of administration.

机构信息

Pharmacology Department, Faculty of Veterinary Medicine, Cairo University, P.O. Box 12211, Giza, Egypt.

出版信息

Res Vet Sci. 2010 Jun;88(3):507-11. doi: 10.1016/j.rvsc.2009.11.009. Epub 2009 Dec 9.

Abstract

In this study the disposition kinetics and plasma availability of moxifloxacin in Muscovy ducks after single intravenous (i.v.), intramuscular (i.m.) and oral (p.o.) administrations of 5 mg kg(-1) b.wt. were investigated. The concentrations of moxifloxacin in the plasma were measured using high-performance liquid chromatography (HPLC) with fluorescence detection on samples collected at frequent intervals after drug administration. Following intravenous injection, the decline in plasma drug concentration was bi-exponential with half-lives of (t(1/2)(alpha)) 0.22+/-0.10h and (t(1/2)(beta)) 2.49+/-0.26h for distribution and elimination phases, respectively. The volume of distribution at steady-state (V(dss)) was 1.02+/-0.14 l kg(-1) and the total body clearance (Cl(tot)) was 0.32+/-0.11 l kg(-1)h(-1), respectively. After intramuscular and oral administration of moxifloxacin at the same dose the peak plasma concentrations (C(max)) were 2.38+/-0.43 and 2.11+/-0.36 microg ml(-1) and were obtained at 1.47+/-0.26 and 1.83+/-0.16h (T(max)), respectively, the elimination half-lives (T(1/2el)) were 3.14+/-0.42 and 2.63+/-0.44h, respectively, and AUC(0-24) were 15.87+/-2.35 and 14.52+/-2.37 microg ml(-1)h(-1), respectively. The systemic bioavailabilities were 96.36+/-11.54% and 86.79+/-12.64%, respectively. In vitro plasma protein binding percent was 32%. We concluded that moxifloxacin might be clinically interesting alternative for the treatment of most sensitive bacterial infections in Muscovy ducks.

摘要

本研究考察了 5mg/kg 体重单次静脉(i.v.)、肌肉(i.m.)和口服(p.o.)给予美罗培南后,麻鸭体内的药物处置动力学和血浆利用度。采用高效液相色谱法(HPLC)结合荧光检测,在给药后频繁采集样本,检测美罗培南在血浆中的浓度。静脉注射后,药物浓度的下降呈双指数衰减,分布相和消除相的半衰期(t(1/2)(alpha))分别为 0.22+/-0.10h 和(t(1/2)(beta))2.49+/-0.26h。稳态分布容积(V(dss))为 1.02+/-0.14 l/kg,总清除率(Cl(tot))为 0.32+/-0.11 l/kg/h。以相同剂量肌肉和口服给予美罗培南后,C(max)分别为 2.38+/-0.43 和 2.11+/-0.36 microg/ml,T(max)分别为 1.47+/-0.26 和 1.83+/-0.16h,消除半衰期(T(1/2el))分别为 3.14+/-0.42 和 2.63+/-0.44h,AUC(0-24)分别为 15.87+/-2.35 和 14.52+/-2.37 microg/ml/h。系统生物利用度分别为 96.36+/-11.54%和 86.79+/-12.64%。体外血浆蛋白结合率为 32%。我们得出结论,美罗培南可能是治疗麻鸭最敏感细菌感染的一种有临床应用前景的替代药物。

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