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庆大霉素C1、C1a和C2单次静脉注射后在马体内的药代动力学

Pharmacokinetics of gentamicin C1, C1a and C2 in horses after single intravenous dose.

作者信息

Steinman A, Isoherranen N, Ashoach O, Soback S

机构信息

Koret School of Veterinary Medicine, The Hebrew University of Jerusalem, Rehovot, Israel.

出版信息

Equine Vet J. 2002 Sep;34(6):615-8. doi: 10.2746/042516402776180160.

Abstract

Gentamicin pharmacokinetics has not been studied in horses. Pharmacokinetics of gentamicin C1, C1a and C2 components following i.v. administration of total gentamicin at 6.6 mg/kg bwt to 6 healthy mature horses was determined. Significant differences in clearance, half-life (t 1/2), and mean residence time (MRT) between the gentamicin Cia and the 2 other components were found. The total body clearance (CL) of gentamicin C1a was 1.62 +/- 0.50 ml/min x kg and similar to the glomerular filtration rate (GFR) reported for horses. The CL of gentamicin C1 and C2 were 1.03 +/- 0.08 ml/min x kg and 1.10 +/- 0.15 ml/min x kg, respectively, and significantly slower than that of gentamicin C1a. The values of apparent volume of distribution at steady state were 0.22 +/- 0.05, 0.26 +/- 0.12 and 0.23 +/- 0.05 l/kg for gentamicin C1, C1a and C2, respectively. The MRT values were mean +/- s.d. 3.6 +/- 0.5, 2.7 +/- 0.3 and 3.5 +/- 0.4 h and the t 1/2 values were 3.1 (2.5-4.0), 2.4 (2.0-3.2) and 33 (2.4-4.3) h (harmonic mean and range) for gentamicin C1, C1a and C2, respectively. The MRT and t 1/2 values for gentamicin C1a were significantly shorter than those of gentamicin C1 and C2. It was concluded that the difference in pharmacokinetics between the gentamicin components has potential pharmacological and toxicological implications.

摘要

庆大霉素的药代动力学尚未在马匹中进行研究。测定了给6匹健康成年马静脉注射6.6mg/kg体重的总庆大霉素后,庆大霉素C1、C1a和C2组分的药代动力学。发现庆大霉素Cia与其他两种组分在清除率、半衰期(t 1/2)和平均驻留时间(MRT)方面存在显著差异。庆大霉素C1a的总体清除率(CL)为1.62±0.50ml/min×kg,与报道的马匹肾小球滤过率(GFR)相似。庆大霉素C1和C2的CL分别为1.03±0.08ml/min×kg和1.10±0.15ml/min×kg,明显慢于庆大霉素C1a。稳态时的表观分布容积值分别为庆大霉素C1 0.22±0.05、C1a 0.26±0.12和C2 0.23±0.05l/kg。庆大霉素C1、C1a和C2的MRT值分别为平均±标准差3.6±0.5、2.7±0.3和3.5±0.4小时,t 1/2值分别为3.1(2.5 - 4.0)、2.4(2.0 - 3.2)和3.3(2.4 - 4.3)小时(调和均值和范围)。庆大霉素C1a的MRT和t 1/2值明显短于庆大霉素C1和C2。得出结论,庆大霉素各组分药代动力学的差异具有潜在的药理和毒理学意义。

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