Swahn A
Eur J Clin Pharmacol. 1976 Feb 6;9(4):299-306. doi: 10.1007/BF00561664.
Two ampicillin esters, 35S-pivampicillin and 35S-carampicillin and polyethylene glycol (nonabsorbable marker) were given orally to healthy subjects with gastrointestinal tubes. The cumulative absorption of radioactivity in both compounds (60-90%) was higher than (25-67%) previously found after administration of 35S-ampicillin. The pek plasma levels of radioactivity were reached earlier and were about twice as high as in the latter study. The amount of radioactivity excreted in urine was about the same as that absorbed from the proximal part of the gastrointestinal tract. Both 35S-pivampicillin and 35S-carampicillin were partly hydrolyzed in the stomach and upper small intestine and labelled ampicillin was released. They were also decomposed after absorption since all the radioactivity recovered from blood and urine appeared to be attached to ampicillin and ampicillin metabolites. Studies in vitro indicated that ampicillin esters absorbed intact may be hydrolyzed not only in the blood but also in the intestinal wall and the liver.
给插有胃肠管的健康受试者口服两种氨苄西林酯（35S-匹氨西林和35S-卡芦莫南）以及聚乙二醇（不可吸收标记物）。两种化合物中放射性的累积吸收（60 - 90%）高于先前给予35S-氨苄西林后发现的吸收量（25 - 67%）。放射性的峰值血浆水平出现得更早，且约为后一项研究中的两倍。尿中排泄的放射性量与从胃肠道近端吸收的量大致相同。35S-匹氨西林和35S-卡芦莫南都在胃和小肠上段部分水解，释放出标记的氨苄西林。它们在吸收后也会分解，因为从血液和尿液中回收的所有放射性似乎都与氨苄西林及其代谢产物结合。体外研究表明，完整吸收的氨苄西林酯不仅可能在血液中水解，还可能在肠壁和肝脏中水解。
