Tokiwa T, Ohashi H
Jpn J Antibiot. 1982 Apr;35(4):987-92.
Pharmacokinetics of netilmicin (NTL), a new aminoglycoside antibiotic, injected intramuscularly to Beagle dogs were compared with those of gentamicin (GM), and the relationship between NTL dosage administered and plasma level and urinary excretion was examined. 1. When administered to 6 male Beagle dogs at a dose of 10 mg/kg, the plasma level showed a broad peak (ca. 23 mcg/ml) at 10 to 45 minutes after administration and declined thereafter with half-life of 65 minutes. On the other hand, the plasma level of GM administered at a dose of 10 mg/kg showed a peak (ca. 24mcg/ml) at 15 to 45 minutes after administration and the elimination half-life was 75 minutes. Both of the urinary concentrations of NTL and GM administered at a dose of 10 mg/kg were highest in the 4- to 6-hour urine, whereas NTL and GM recovered in the 24-hour urine were 51.7% and 57.7% of the dose administered, respectively. The pharmacokinetic profile of NTL administered intramuscularly to Beagle dogs appeared to be almost identical to that of GM. 2. The peak plasma level of ca. 50 mcg/ml was obtained at 10 to 60 minutes after administration of NTL at 20 mg/kg, and the half-life was 74 minutes. NTL recovered in the 24-hour urine was 69.7% of the dose administered. 3. TLC-bioautograms showed no biologically active metabolites of NTL in the urine collected from Beagle dogs given the antibiotic intramuscularly.
将新氨基糖苷类抗生素奈替米星(NTL)肌肉注射给比格犬后的药代动力学与庆大霉素(GM)进行了比较,并研究了NTL给药剂量与血浆水平和尿排泄之间的关系。1. 以10mg/kg的剂量给6只雄性比格犬给药后,血浆水平在给药后10至45分钟出现一个较宽的峰值(约23mcg/ml),此后下降,半衰期为65分钟。另一方面,以10mg/kg的剂量给药的GM血浆水平在给药后15至45分钟出现峰值(约24mcg/ml),消除半衰期为75分钟。以10mg/kg的剂量给药的NTL和GM的尿浓度在4至6小时的尿液中最高,而在24小时尿液中回收的NTL和GM分别为给药剂量的51.7%和57.7%。肌肉注射给比格犬的NTL的药代动力学特征似乎与GM几乎相同。2. 以20mg/kg的剂量给药NTL后,在给药后10至60分钟获得约50mcg/ml的血浆峰值水平,半衰期为74分钟。在24小时尿液中回收的NTL为给药剂量的69.7%。3. TLC-生物自显影图谱显示,从肌肉注射该抗生素的比格犬收集的尿液中没有NTL的生物活性代谢物。