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Pharmacokinetics and Efficacy of Tilmicosin in the Treatment of Pasteurella haemolytica Bronchopneumonia in Calves

机译:替米考星治疗小牛溶血性巴斯德氏菌支气管肺炎的药代动力学和疗效

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Tilmicosin was administered intravenously and subcutaneously at a dose rate of 10 mg/kg bwt to determine its concentration in blood and bronchial secretion as well as its kinetic behavior in healthy and Pasteurella haemolytica type A1-infected calves. Sever acute bronchopneumonia was induced in 10 calves by inoculating them intra-tracheally with P. haemolytica type A1. The calves were treated with tilmicosin; 5 of these received the drug intravenously and the other 5 were injected subcutaneously. After a slow intravenous injection, the serum concentration-time curve indicated a two compartment open model with a mean elimination half-lives (t1/2bs) of 22.09 and 22.14 hours before and after infection, respectively. The mean residence time (MRT) corrected for a bolus injection was 2.25 and 2.20 hours and the mean MRTinf was 25.27 and 25.46 hours in healthy and P. haemolytica-infected calves, respectively. After subcutaneous injection, the drug was eliminated more slowly (before and after infection) from serum and bronchial secretions, with t1/2bs of (24.60 and 25.85 hours) and (33.74 and 31.78 hours), respectively. The apparent volume of distribution (Vd(area)) of tilmicosin was more than 1 litre·kg-1. The peak serum and bronchial secretions of tilmicosin concentration were (1.33 and 1.36 mg·ml-1) and (1.40 and 1.70 mg·ml-1) attained at (7.21 and 7.15 hours) and 7.11 and 7.10 hours) after subcutaneous injection, respectively. Tilmicosin was good secreted into bronchial secretions having AUCbronchial secretion/ AUCserum ratio of approximately 1:1.24 and 1:1.22 in healthy and P. haemolytica-
机译:替米考星以10 mg / kg bwt的剂量静脉内和皮下给药,以确定其在血液和支气管分泌物中的浓度,以及在健康和溶血巴斯德氏菌A1型感染小牛中的动力学行为。将10头小牛经气管内接种溶血性P.1型小牛,即可诱发严重急性支气管肺炎。小牛用替米考星处理;其中5例接受静脉注射药物,另外5例经皮下注射。缓慢静脉注射后,血清浓度-时间曲线显示了一个两室开放模型,在感染前后平均消除半衰期(t1 / 2bs)分别为22.09和22.14小时。大剂量注射校正的平均停留时间(MRT)在健康和溶血性疟原虫感染的犊牛中分别为2.25和2.20小时,平均MRTinf为25.27和25.46小时。皮下注射后,从血清和支气管分泌物中清除药物的速度较慢(在感染前后),t1 / 2bs分别为(24.60和25.85小时)和(33.74和31.78小时)。替米考星的表观分布体积(Vd(面积))大于1升·kg-1。皮下注射后,替米考星浓度的峰值血清和支气管分泌浓度分别为(1.33和1.36 mg·ml-1)和(1.40和1.70 mg·ml-1),分别在(7.21和7.15小时)和7.11和7.10小时达到。 。在健康和溶血性疟原虫中,Tilmicosin可良好分泌到支气管分泌物中,其AUC支气管分泌/ AUC血清比率约为1:1.24和1:1.22。

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