Baggot J D, Love D N, Rose R J, Raus R
Equine Vet J. 1985 Jan;17(1):30-4. doi: 10.1111/j.2042-3306.1985.tb02034.x.
The serum concentrations of the aminoglycosides neomycin, kanamycin and streptomycin were determined after intravenous (iv) and intramuscular (im) administration. These values were then related to the minimum inhibitory concentrations (MIC) of a number of equine pathogenic bacteria to determine the duration of therapeutic serum concentrations of the aminoglycosides in the horse. Pharmacokinetic analysis of the data using neomycin as the example revealed a mean (+/- sd) peak serum concentration of 23.2 +/- 10.2 micrograms/ml present at 30 mins, and at 8 h the serum concentration was 2.8 +/- 0.8 micrograms/ml. From the pharmacological analysis of concentration-time data it was shown that neomycin was very rapidly absorbed from the im injection site, with an absorption half-time of 0.16 +/- 0.05 and was well absorbed (systemic availability was 73.7 +/- 26.9 per cent). A peak tissue level, which represented 40 per cent of the amount of drug in the body, was obtained at 32 mins after injection of the drug. At 8 h, the fractions of the dose in the central and peripheral compartments of the model were 1.5 per cent and 2.5 per cent respectively, and 96 per cent was the cumulative amount eliminated up to that time. Based on the MIC values of the majority of isolates of Corynebacterium equi, and only a few isolates of Klebsiella pneumoniae, Escherichia coli, Salmonella typhimurium and Streptococcus equi, one would expect a serum concentration of more than 2 micrograms neomycin/ml up to 8 h following im dosage (10 mg/kg) to be therapeutically effective.
在静脉注射(iv)和肌肉注射(im)后测定了氨基糖苷类抗生素新霉素、卡那霉素和链霉素的血清浓度。然后将这些值与多种马病原菌的最低抑菌浓度(MIC)相关联,以确定马体内氨基糖苷类抗生素治疗性血清浓度的持续时间。以新霉素为例对数据进行药代动力学分析,结果显示在30分钟时平均(±标准差)血清峰值浓度为23.2±10.2微克/毫升,8小时时血清浓度为2.8±0.8微克/毫升。从浓度 - 时间数据的药理学分析表明,新霉素从肌肉注射部位吸收非常迅速,吸收半衰期为0.16±0.05,并且吸收良好(全身利用率为73.7±26.9%)。在注射药物后32分钟获得了代表体内药物量40%的峰值组织水平。在8小时时,模型中央和外周隔室中剂量的分数分别为1.5%和2.5%,到那时累计消除量为96%。根据马棒状杆菌大多数分离株以及仅少数肺炎克雷伯菌、大肠杆菌、鼠伤寒沙门氏菌和马链球菌分离株的MIC值,预计在肌肉注射剂量(10毫克/千克)后8小时内血清中新霉素浓度超过2微克/毫升将具有治疗效果。