[Absorption, distribution, and excretion of arbekacin after intravenous and intramuscular administration in rats].
[Absorption, distribution, and excretion of arbekacin after intravenous and intramuscular administration in rats].
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阿贝卡星在大鼠静脉和肌内给药后的吸收、分布和排泄[J].
DOI：
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发表时间：
1987
期刊：
影响因子：
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通讯作者：
F. Kai
中科院分区：
文献类型：
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作者：
N. Mitomi;T. Matsumoto;M. Fujigaki;I. Komiya;F. Kai
以10 mg/kg或20 mg/kg剂量静脉或肌肉注射阿贝卡星（HBK）后，研究了HBK在大鼠体内的吸收、分布和排泄。静脉推注给药时，HBK的消除半衰期为0.69小时，恒速静脉输注时为0.55小时，肌内给药时为0.57小时。静脉推注给药后24小时内的累积尿液排泄量为剂量的74.7%，肌内给药为剂量的79.1%。两种给药途径之间的累积尿排泄量未观察到显著差异。给药后24小时内的累积胆汁排泄量约为剂量的0.1%，无论给药途径是静脉推注还是肌内给药。静脉推注给药后，HBK的组织或器官分布与肌肉注射给药后相似。药物分布最多的是肾脏，其次是血浆和肺。在本研究检查的6种组织或器官中，药物在肝脏中的分布最少。通过平衡透析法在3种不同浓度的HBK（5、10和20 μ g/ml）下研究HBK的蛋白结合。HBK与人血清、人血清白蛋白和大鼠血清的结合率均小于15%。
Absorption, distribution, and excretion of arbekacin (HBK) were studied in rats after intravenous or intramuscular administration of HBK at a dose of 10 mg/kg or 20 mg/kg. Elimination half-lives of HBK were 0.69 hour for bolus intravenous administration, 0.55 hour for constant rate intravenous infusion, and 0.57 hour for intramuscular administration. Cumulative urinary excretions within 24 hours after administration were 74.7% of the dose for bolus intravenous administration, and 79.1% of the dose for intramuscular administration. No significant difference was observed in the cumulative urinary excretions between the 2 administration routes. Cumulative biliary excretions within 24 hours after administration were around 0.1% of doses regardless administration routes, bolus intravenous or intramuscular administration. The tissue or organ distribution of HBK after bolus intravenous administration was similar to that after intramuscular administration. The drug was distributed most abundantly into the kidney followed by plasma and the lung. The distribution of the drug into the liver was the least among the 6 tissues or organs examined in this study. The protein binding of HBK was studied by an equilibrium dialysis method at three different concentrations of HBK, 5, 10, and 20 micrograms/ml. Binding ratios of HBK to human serum, human serum albumin, and rat serum were less than 15%.