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新型氨基糖苷类抗生素妥布霉素的体外评价

In vitro evaluation of tobramycin, a new aminoglycoside antibiotic.

作者信息

Levison M E, Knight R, Kaye D

出版信息

Antimicrob Agents Chemother. 1972 May;1(5):381-4. doi: 10.1128/AAC.1.5.381.

Abstract

One hundred fifty-two strains of Escherichia coli, Klebsiella-Enterobacter, Pseudomonas aeruginosa, Proteus species, and Staphylococcus aureus were inhibited by 3.1 mug of tobramycin/ml in a broth-dilution method and showed zones of inhibition of 16 mm or more around a 10-mug tobramycin disc in the Kirby-Bauer method. Tobramycin was most active against S. aureus, 100% of strains being inhibited by 0.1 mug/ml. All strains of E. coli, K. pneumoniae, P. aeruginosa, and indole-positive Proteus species, and 80% of Enterobacter species were inhibited by 0.8 mug of tobramycin/ml, whereas only 48% of P. mirabilis strains were inhibited by this concentration. Tobramycin was approximately twice as active as gentamicin against S. aureus, four times as active against P. aeruginosa, slightly more active against E. coli and Enterobacter species, equally active against P. mirabilis, and slightly less active against K. pneumoniae. The minimal bactericidal concentrations of tobramycin and gentamicin were the same as or twice the minimal inhibitory concentrations for all strains except those of P. aeruginosa, against which greater concentrations of both gentamicin and tobramycin were required for bactericidal activity. Tobramycin sterilized cultures of S. aureus, E. coli, and P. aeruginosa, but the rate of bactericidal action was faster with a combination of tobramycin and carbenicillin than with either antibiotic alone in the same concentrations. Tobramycin retained potency in the presence of 200 to 600 mug of carbenicillin/ml for at least 6 hr of incubation at 37 C, but lost potency in the presence of 600 mug of carbenicillin/ml by 24 hr of incubation and in the presence of 800 mug/ml by 2 hr of incubation.

摘要

采用肉汤稀释法时,152株大肠杆菌、克雷伯菌属-肠杆菌属、铜绿假单胞菌、变形杆菌属和金黄色葡萄球菌被3.1μg/ml的妥布霉素抑制,在柯氏-鲍氏法中,围绕10μg妥布霉素纸片的抑菌圈直径为16mm或更大。妥布霉素对金黄色葡萄球菌活性最强,100%的菌株被0.1μg/ml抑制。所有大肠杆菌、肺炎克雷伯菌、铜绿假单胞菌和吲哚阳性变形杆菌属菌株,以及80%的肠杆菌属菌株被0.8μg/ml的妥布霉素抑制,而只有48%的奇异变形杆菌菌株被该浓度抑制。妥布霉素对金黄色葡萄球菌的活性约为庆大霉素的两倍,对铜绿假单胞菌的活性为四倍,对大肠杆菌和肠杆菌属的活性略高,对奇异变形杆菌的活性相同,对肺炎克雷伯菌的活性略低。除铜绿假单胞菌外,妥布霉素和庆大霉素的最低杀菌浓度与所有菌株的最低抑菌浓度相同或为其两倍,对于铜绿假单胞菌,需要更高浓度的庆大霉素和妥布霉素才能产生杀菌活性。妥布霉素可使金黄色葡萄球菌、大肠杆菌和铜绿假单胞菌培养物灭菌,但在相同浓度下,妥布霉素和羧苄西林联合使用时的杀菌作用速率比单独使用任何一种抗生素都要快。在37℃孵育至少6小时的情况下,妥布霉素在200至600μg/ml羧苄西林存在时仍保持效力,但在600μg/ml羧苄西林存在下孵育24小时后效力丧失,在800μg/ml存在下孵育2小时后效力丧失。

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