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泌乳奶牛、母羊和母山羊血清及乳汁中安普霉素的浓度。

Serum and milk concentrations of apramycin in lactating cows, ewes and goats.

作者信息

Ziv G, Kurtz B, Risenberg R, Glickman A

机构信息

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

出版信息

J Vet Pharmacol Ther. 1995 Oct;18(5):346-51. doi: 10.1111/j.1365-2885.1995.tb00602.x.

Abstract

A 20% solution of apramycin was administered intravenously (i.v.) and intramuscularly (i.m.) to lactating cows with clinically normal and acutely inflamed udders, to lactating ewes with normal or subclinically infected, inflamed udders and i.v. to lactating goats with normal udders. The i.v. disposition kinetics of apramycin was very similar in cows, ewes and goats. The elimination half-life was approximately 2 h and the steady-state volume of distribution was 1.26-1.45 L/kg. The absorption rate of the drug from the i.m. injection site was rapid, the i.m. bioavailability was 60-70% and the mean elimination half-life was 265 min in cows and 145.5 min in ewes. The binding percentage of apramycin to serum protein was low (< 22.5%). Concentrations of apramycin in milk produced by clinically normal mammary glands of cows, ewes and goats were consistently lower than in serum; the kinetic value AUCmilk/AUCserum was < 0.32. Drug penetration into the milk from the acutely inflamed quarters of cows was extensive; mastitis milk Cmax values were more than tenfold greater than the Cmax in normal milk. On the other hand, the drug had limited access to the milk produced by subclinically infected inflamed half-udders of ewes.

摘要

将20%的安普霉素溶液静脉注射和肌肉注射给乳房临床正常和急性发炎的泌乳奶牛,以及乳房正常或亚临床感染发炎的泌乳母羊,并将其静脉注射给乳房正常的泌乳山羊。安普霉素在奶牛、母羊和山羊体内的静脉处置动力学非常相似。消除半衰期约为2小时,稳态分布容积为1.26 - 1.45 L/kg。药物从肌肉注射部位的吸收速度很快,在奶牛中肌肉注射的生物利用度为60 - 70%,平均消除半衰期为265分钟,在母羊中为145.5分钟。安普霉素与血清蛋白的结合率较低(< 22.5%)。奶牛、母羊和山羊临床正常乳腺分泌的乳汁中安普霉素的浓度始终低于血清中的浓度;动力学值AUC乳汁/AUC血清< 0.32。药物从奶牛急性发炎乳腺进入乳汁的程度很大;患乳腺炎乳汁的Cmax值比正常乳汁中的Cmax值大十多倍。另一方面,该药物进入亚临床感染发炎半侧乳房的母羊所产乳汁的量有限。

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