Matsuzawa T, Kondo T, Kita Y
Antimicrob Agents Chemother. 1974 Dec;6(6):685-90. doi: 10.1128/AAC.6.6.685.
The absorption, distribution, metabolism, and excretion of propionylmaridomycin was investigated in the rat by using [(14)C]propionylmaridomycin. Propionylmaridomycin was absorbed from the gastrointestinal tract at a relatively rapid rate and was readily distributed into tissues. Among the tissues examined, liver, kidney, and lung showed a remarkably higher level of the radioactivity than plasma, while distribution of the radioactivity into brain was little. However, a significant accumulation of the radioactivity in tissues was not observed. Excretion of the radioactivity was mainly via the fecal route and the high fecal recovery was accounted for by unabsorbed drug and biliary excretion of the drug and/or its metabolites. Tissue distribution of antimicrobial activity was also investigated and lung was found to show the highest antimicrobial activity among any tissues examined. Propionylmaridomycin was completely converted to several metabolites by the rat and the presence of at least three components was confirmed as biologically active metabolites. Of these metabolites, 4''-depropionyl-9-propionylmaridomycin was identified, which was the major metabolite in tissues, plasma, and urine.
采用[¹⁴C]丙酰马立霉素对大鼠体内丙酰马立霉素的吸收、分布、代谢及排泄情况进行了研究。丙酰马立霉素能以相对较快的速度从胃肠道吸收，并易于分布到组织中。在所检查的组织中，肝脏、肾脏和肺中的放射性水平显著高于血浆，而脑组织中的放射性分布较少。然而，未观察到放射性在组织中的显著蓄积。放射性的排泄主要通过粪便途径，粪便中较高的回收率是由于未吸收的药物以及药物和/或其代谢产物的胆汁排泄所致。还研究了抗菌活性的组织分布，发现在所检查的任何组织中，肺显示出最高的抗菌活性。丙酰马立霉素在大鼠体内完全转化为几种代谢产物，并且确认至少有三种成分作为生物活性代谢产物存在。在这些代谢产物中，鉴定出了4''-去丙酰基-9-丙酰马立霉素，它是组织、血浆和尿液中的主要代谢产物。
