Baggot J D, Love D N, Rose R J, Raus J
J Vet Pharmacol Ther. 1981 Dec;4(4):277-84. doi: 10.1111/j.1365-2885.1981.tb00863.x.
The disposition kinetics and bioavailability of streptomycin, kanamycin and neomycin were determined following their administration as parenteral preparations to horses. Single doses (10 mg/kg) of each aminoglycoside were given by the intravenous (i.v.) and intramuscular (i.m.) routes and, at a later time, seven intramuscular doses were injected at 12-h intervals. The pharmacokinetic behaviour of the three aminoglycosides was similar, in that a rapid distribution phase was followed by a relatively short half-life. The half-life (mean +/- SD, n = 6) of kanamycin (1.80 +/- 0.17 h) was significantly (P less than 0.01; t test, 10 d.f.) shorter than that of streptomycin (3.40 +/- 0.42 h), while neomycin half-life (2.10 +/- 0.97 h) was of an intermediate length. The apparent volume of distribution of neither kanamycin nor neomycin varied significantly (P greater than 0.05) from that of streptomycin and numerically (V1 d congruent to 230 ml/kg) was the same as the extracellular fluid volume. The body clearance of kanamycin (88.5 +/- 11.3 ml/kg.h) was significantly (P less than 0.01) larger than that of streptomycin (47.5 +/- 7.9 ml/kg.h), while a significant difference in this parameter did not exist (P greater than 0.05) between neomycin and streptomycin. Following intramuscular injection, each aminoglycoside was rapidly and completely absorbed from the injection site, although neomycin showed wide individual variation in the fraction absorbed. The administration of multiple doses did not change either the bioavailability or the apparent half-life from the values obtained after a single dose. The only pharmacokinetic difference between these aminoglycosides that is of clinical importance lies in the rate of their elimination. A dosage interval of 8 h would be appropriate for kanamycin compared with a 12-h interval for streptomycin. The dosage interval for neomycin based on half-life should be 8 h but, due to the relatively greater toxicity of this aminoglycoside, an interval of 12 h might be recommended. The height of the peak serum concentration is determined by the size of the dose.
在给马注射链霉素、卡那霉素和新霉素的肠胃外制剂后，测定了它们的处置动力学和生物利用度。每种氨基糖苷类药物均以单剂量（10mg/kg）通过静脉注射（i.v.）和肌肉注射（i.m.）给药，随后在较晚时间以12小时的间隔注射七次肌肉剂量。这三种氨基糖苷类药物的药代动力学行为相似，即快速分布阶段后接着是相对较短的半衰期。卡那霉素的半衰期（平均值±标准差，n = 6）为（1.80±0.17小时），显著（P小于0.01；t检验，自由度为10）短于链霉素（3.40±0.42小时），而新霉素的半衰期（2.10±0.97小时）处于中间长度。卡那霉素和新霉素的表观分布容积与链霉素相比均无显著差异（P大于0.05），且数值上（V1d约等于230ml/kg）与细胞外液容积相同。卡那霉素的机体清除率（88.5±11.3ml/kg·h）显著（P小于0.01）高于链霉素（47.5±7.9ml/kg·h），而新霉素与链霉素在该参数上不存在显著差异（P大于0.05）。肌肉注射后，每种氨基糖苷类药物均从注射部位快速且完全吸收，尽管新霉素在吸收分数上显示出较大的个体差异。多次给药并未改变单次给药后获得的生物利用度或表观半衰期的值。这些氨基糖苷类药物之间唯一具有临床重要性的药代动力学差异在于它们的消除速率。卡那霉素的合适给药间隔为8小时，而链霉素为12小时。基于半衰期，新霉素的给药间隔应为8小时，但由于该氨基糖苷类药物毒性相对较大，可能建议间隔为12小时。血清峰值浓度的高度由剂量大小决定。
