Ullmann U, Wurst W
Infection. 1979;7(4):187-9. doi: 10.1007/BF01640941.
Four-hourly urine from volunteers and patients who had received penicillins orally or intravenously was investigated by means of thin layer chromatography and bioautography. Antibacterially active metabolites were not detected with only two of 12 penicillins, namely amoxicillin and mezlocillin. In the case of the other penicillins the metabolites possessed variable antibacterial activity as could be demonstrated using different test microorganisms. After administration of carbenicillin esters three antibacterially active spots were detected, one of which corresponded to penicillin G; the other two were active against Pseudomonas aeruginosa. The bioautogram after treatment with azlocillin showed two components which were active against Bacillus subtilis, Staphylococcus aureus and Escherichia coli; only the rapid moving component was active against P. aeruginosa, however. The formation and chemical nature of these additional active components is still to a large extent not understood. It is quite possible, however, that they affect the bio-availability of an antibiotic.
通过薄层色谱法和生物自显影法对口服或静脉注射青霉素的志愿者和患者每四小时收集的尿液进行了研究。在12种青霉素中,只有阿莫西林和美洛西林未检测到具有抗菌活性的代谢物。对于其他青霉素,代谢物具有不同的抗菌活性,这可以通过使用不同的测试微生物来证明。给予羧苄青霉素酯后,检测到三个具有抗菌活性的斑点,其中一个对应于青霉素G;另外两个对铜绿假单胞菌有活性。用阿洛西林治疗后的生物自显影图谱显示有两个成分对枯草芽孢杆菌、金黄色葡萄球菌和大肠杆菌有活性;然而,只有快速移动的成分对铜绿假单胞菌有活性。这些额外活性成分的形成和化学性质在很大程度上仍不清楚。然而,它们很可能会影响抗生素的生物利用度。