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达氟沙星在母羊体内的药代动力学及从血液到乳汁的渗透情况。

Pharmacokinetics and penetration of danofloxacin from the blood into the milk of ewes.

作者信息

Shem-Tov M, Ziv G, Glickman A, Saran A

机构信息

Ministry of Agriculture, Kimron Veterinary Institute, Bet-Dagan, Israel.

出版信息

Vet Res. 1997 Nov-Dec;28(6):571-9.

PMID:9428151
Abstract

The single-dose disposition kinetics of danofloxacin were determined in clinically normal, lactating ewes after intravenous (i.v.) and intramuscular (i.m.) administration of 1.25 mg/kg. The drug concentration in the blood serum and milk were determined by microbiological assay and the data were subjected to compartmental and non-compartmental kinetic analyses. The i.v. and im elimination half-lives in serum (t1/2 beta and t1/2el) were 125.0 +/- 38.6 min and 209.4 +/- 56.3 min, respectively. The steady-state volume of distribution (Vss) was 1.9 +/- 0.7 L/kg. The drug was quickly absorbed after the i.m. injection and the i.m. availability was 100%. Penetration of danofloxacin from the blood into the milk was rapid and extensive with drug concentrations in milk exceeding those in serum beginning 60-90 min after administration and onwards. Milk danofloxacin concentrations equal to or higher than the minimal inhibitory concentrations (MIC) for pathogenic Gram-negative bacteria and Mycoplasma species were maintained over approximately 24 h. Concentrations greater than the MIC for Staphylococcus aureus were maintained in the milk for 12 h.

摘要

在临床健康的泌乳母羊静脉注射(i.v.)和肌肉注射(i.m.)1.25mg/kg达氟沙星后,测定了其单剂量处置动力学。通过微生物测定法测定血清和乳汁中的药物浓度,并对数据进行房室和非房室动力学分析。血清中的静脉注射和肌肉注射消除半衰期(t1/2β和t1/2el)分别为125.0±38.6分钟和209.4±56.3分钟。稳态分布容积(Vss)为1.9±0.7L/kg。肌肉注射后药物吸收迅速,肌肉注射的生物利用度为100%。达氟沙星从血液进入乳汁的过程迅速且广泛,给药后60 - 90分钟及之后,乳汁中的药物浓度超过血清中的药物浓度。乳汁中达氟沙星的浓度等于或高于致病性革兰氏阴性菌和支原体的最低抑菌浓度(MIC),并维持约24小时。乳汁中高于金黄色葡萄球菌MIC的浓度维持12小时。

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