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聚诺昔林的生物活性——一种不溶性脲醛缩合产物

Biological activity of polynoxylin--an insoluble urea-formaldehyde condensation product.

作者信息

Blenkharn J I

出版信息

J Clin Hosp Pharm. 1985 Dec;10(4):367-72. doi: 10.1111/j.1365-2710.1985.tb00935.x.

Abstract

The antimicrobial activity of polynoxylin, an alkali urea-formaldehyde condensation product, has been examined. The minimum inhibitory concentration (MIC) for 1000 clinical isolates of bacteria and yeasts was in the range 1024-16,384 mg/l. Cidal concentrations of the drug were within one dilution of the corresponding values for MIC, the results suggest a cumulative mode of antimicrobial activity. Formaldehyde, the putative active component of polynoxylin, was released into water from 10% (w/w) cream preparation which gave a maximum yield of 1.56 mg within 6 h. The limited water solubility of polynoxylin, cumulative mode of antimicrobial action and presence of pre-formed formaldehyde in the pharmaceutical preparation, suggest the possibility of sustained activity when applied to skin. The slow solubilization of particulate polynoxylin and gradual liberation of inhibitory degradation products may further enhance the inherent antimicrobial activity afforded by the presence of pre-formed formaldehyde.

摘要

已对碱脲 - 甲醛缩合产物聚氧西林的抗菌活性进行了研究。对1000株临床分离的细菌和酵母菌的最低抑菌浓度(MIC)在1024 - 16384毫克/升范围内。该药物的杀菌浓度在相应MIC值的一个稀释度内,结果表明其抗菌活性具有累积模式。聚氧西林的假定活性成分甲醛从10%(w/w)乳膏制剂中释放到水中,在6小时内最大产量为1.56毫克。聚氧西林有限的水溶性、抗菌作用的累积模式以及药物制剂中预先形成的甲醛的存在,表明其应用于皮肤时具有持续活性的可能性。颗粒状聚氧西林的缓慢溶解和抑制性降解产物的逐渐释放可能会进一步增强预先形成的甲醛所提供的固有抗菌活性。

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