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达氟沙星在番鸭体内的处置动力学和组织残留。

Disposition kinetics and tissue residues of danofloxacin in Muscovy ducks.

机构信息

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

出版信息

Br Poult Sci. 2009 Sep;50(5):613-9. doi: 10.1080/00071660903147416.

Abstract
  1. The disposition kinetics and plasma availability of danofloxacin in Muscovy ducks after single intravenous (i.v.), intramuscular (i.m.) and oral administrations of 5 mg/kg body weight were investigated. 2. Tissue residue profiles (liver, kidney and muscle) and plasma were also studied after multiple intramuscular and oral administration of 5 mg/kg once daily for 5 consecutive days. 3. The concentrations of the drug in the plasma and tissues were measured using high-performance liquid chromatography (HPLC) with fluorescence detection on samples collected at frequent intervals after drug administration. 4. Following intravenous injection, plasma concentration vs. time curves were best described by a two compartment open model. The decline in plasma drug concentration was bi-exponential with half-lives of (t(1/2alpha)) 0.08 h and (t(1/2beta)) 3.91 h for distribution and elimination phases, respectively. 5. After intramuscular and oral administration of danofloxacin at the same dose the peak plasma concentrations (C(max)) were 0.89 and 0.81 microg/ml and attained at 1.17 and 1.21 h (T(max)), respectively, and the elimination half-lives (T(1/2el)) were 2.91 and 2.39 h, respectively. The systemic bioavailabilities were 103.21 and 89.26%, following i.m. and oral admisistartion, respectively. In vitro protein binding percent of danofloxacin in Muscovy ducks plasma was 17%. 6. The tissue level following i.m. and oral administration were highest in liver and kidney, respectively, and decreased in the following order: plasma and muscle. No danofloxacin residues were detected in tissues and plasma after 96 h with either route of administration except in liver and kidney, after 120 h in case of oral administration.
摘要
  1. 研究了单次静脉(i.v.)、肌肉内(i.m.)和口服给予 5mg/kg 体重后,达氟沙星在麝香鸭体内的处置动力学和血浆可利用度。

  2. 还研究了连续 5 天每天口服或肌肉内给予 5mg/kg 体重 1 次后多剂量的组织残留情况(肝、肾和肌肉)和血浆。

  3. 采用高效液相色谱(HPLC)-荧光检测法,在给药后频繁间隔采集样本,测定血浆和组织中药物的浓度。

  4. 静脉注射后,血浆浓度-时间曲线最好用两室开放模型描述。血浆药物浓度的下降呈双指数衰减,分布和消除相的半衰期(t(1/2alpha))分别为 0.08 小时和 3.91 小时。

  5. 以相同剂量肌肉内和口服给予达氟沙星后,血浆峰浓度(C(max))分别为 0.89 和 0.81μg/ml,达峰时间(T(max))分别为 1.17 和 1.21 小时,消除半衰期(T(1/2el))分别为 2.91 和 2.39 小时,分别为肌肉内和口服给药的 103.21%和 89.26%。达氟沙星在麝香鸭血浆中的体外蛋白结合率为 17%。

  6. 肌肉内和口服给药后的组织水平在肝和肾中最高,分别为:血浆和肌肉。两种给药途径后 96 小时,除肝和肾外,组织和血浆中均未检测到达氟沙星残留,口服给药后 120 小时除外。

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