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羧苄青霉素茚满酯钠,一种羧苄青霉素的口服活性衍生物。

Carbenicillin indanyl sodium, an orally active derivative of carbenicillin.

作者信息

English A R, Retsema J A, Ray V A, Lynch J E

出版信息

Antimicrob Agents Chemother. 1972 Mar;1(3):185-91. doi: 10.1128/AAC.1.3.185.

Abstract

Carbenicillin indanyl sodium, an orally active derivative of carbenicillin, is active against a broad spectrum of bacterial species. Although the ester has in vitro antimicrobial activity per se when evaluated in Brain Heart Infusion broth, the in vivo antibacterial activity seen in mice and rats reflects primarily the efficient hydrolysis of the ester to carbenicillin. With an acute systemic infection in mice as a test system, orally administered carbenicillin indanyl sodium protected mice against lethal infections produced by Escherichia coli, Salmonella choleraesuis, Pasteurella multocida, Proteus vulgaris, Staphylococcus aureus, and Streptococcus pyogenes. The dose that protected 50% of the animals against each of these infections was comparable to that of parenteral carbenicillin. Against experimental urinary-tract disease in rats produced by E. coli, P. vulgaris, and Pseudomonas aeruginosa, it was again observed that carbenicillin indanyl sodium provided activity comparable to that of parenterally administered carbenicillin.

摘要

羧苄西林茚满酯钠是羧苄西林的一种口服活性衍生物,对多种细菌具有活性。尽管该酯在脑心浸液肉汤中进行评估时本身具有体外抗菌活性,但在小鼠和大鼠体内观察到的抗菌活性主要反映了酯高效水解为羧苄西林的过程。以小鼠急性全身感染作为测试系统,口服羧苄西林茚满酯钠可保护小鼠免受由大肠杆菌、猪霍乱沙门氏菌、多杀巴斯德菌、普通变形杆菌、金黄色葡萄球菌和化脓性链球菌引起的致死性感染。保护50%的动物免受上述每种感染的剂量与胃肠外给药的羧苄西林相当。在大鼠中,针对由大肠杆菌、普通变形杆菌和铜绿假单胞菌引起的实验性尿路疾病,再次观察到羧苄西林茚满酯钠提供的活性与胃肠外给药的羧苄西林相当。

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