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[小诺霉素静脉注射剂IV.大鼠、兔及犬静脉滴注后的急性毒性安全性评价]

[Safety evaluation of micronomicin IV. Acute toxicity in rats, rabbits and dogs after drip intravenous infusion].

作者信息

Hara T, Harada S, Ikenaga T, Deguchi T

出版信息

Jpn J Antibiot. 1983 Nov;36(11):3204-7.

PMID:6674532
Abstract

Micronomicin (MCR) is a new aminoglycoside antibiotic produced by Micromonospora sagamiensis var. nonreducans which was isolated from soil collected at Sagamihara City by Nara et al. This antibiotic shows a close similarity to gentamicin C components in physical and chemical properties. The antibacterial activity of MCR is broad-spectrum and almost equal to that of gentamicin C complex. MCR exhibits particularly high activity against Pseudomonas, Proteus, Klebsiella pneumoniae, Serratia, etc, as well as against some Pseudomonas aeruginosa strains resistant to gentamicin C1a. Toxicological studies of MCR were carried out for safety evaluation as follows: Studies were carried out to assess acute toxicity, when administered in 1 hour by drip intravenous infusion to Wistar rats, Japanese White rabbits and Beagle dogs. The results of the studies are summarised as follows: There was no difference on acute toxicity between drip intravenous infusion (d.i.v.) and intramuscular injection (i.m.) in rats. However, acute toxicity of d.i.v. was less than that of bolus intravenous administration (i.v.) in rats. Acute toxicity of d.i.v. was stronger than that of i.m. in dogs when administered in rats. Acute toxicity varied with species, and it was ranked in rabbits not equal to dogs greater than rats. There was no difference on symptoms between d.i.v. and i.m.

摘要

小诺米星(MCR)是由相模小单孢菌非还原变种产生的一种新型氨基糖苷类抗生素,该菌株由奈良等人从相模原市采集的土壤中分离得到。这种抗生素在理化性质上与庆大霉素C组分极为相似。MCR的抗菌活性具有广谱性,几乎与庆大霉素C复合物相当。MCR对假单胞菌、变形杆菌、肺炎克雷伯菌、沙雷氏菌等,以及对庆大霉素C1a耐药的一些铜绿假单胞菌菌株表现出特别高的活性。为进行安全性评估,对MCR开展了如下毒理学研究:通过静脉滴注1小时给药,对Wistar大鼠、日本白兔和比格犬进行急性毒性评估。研究结果总结如下:大鼠静脉滴注(d.i.v.)和肌肉注射(i.m.)的急性毒性无差异。然而,大鼠静脉滴注的急性毒性低于静脉推注(i.v.)。在大鼠给药时,犬静脉滴注的急性毒性强于肌肉注射。急性毒性因物种而异,其排序为兔>犬>大鼠。静脉滴注和肌肉注射的症状无差异。

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