Hobbs D C
Antimicrob Agents Chemother. 1972 Oct;2(4):272-5. doi: 10.1128/AAC.2.4.272.
Indanyl carbenicillin, an ester of carbenicillin with indanol, is absorbed in the intestine after oral administration and is subsequently hydrolyzed to release the parent antibiotic which can be measured in serum and urine. To study the metabolism of indanyl carbenicillin, labeled indanol was prepared by exchange with tritiated water and was used, with phenylmalonyl chloride and 6-aminopenicillanic acid, to prepare labeled indanyl carbenicillin. Labeled indanol and indanyl carbenicillin were orally administered to dogs and rats with good recovery of label in the urine. In the dog, indanol, whether administered as such or as indanyl carbenicillin, was excreted in the urine as the glucuronide and sulfate ester conjugates of indanol and as conjugates of two hydroxyindanones and two hydroxyindanols, as determined by combined gas chromatography-mass spectrometry. Rats, conversely, excreted only the conjugates of indanol, whether indanol or indanyl carbenicillin was administered. After oral administration of unlabeled indanyl carbenicillin to humans, conjugates of indanol were recovered in the urine in excellent yield, as determined by a gas chromatographic assay. None of the other indanol metabolites formed by the dog was observed in human urine.
茚满酯羧苄青霉素，即羧苄青霉素与茚满醇形成的酯，口服后在肠道被吸收，随后水解释放出母体抗生素，该抗生素可在血清和尿液中检测到。为了研究茚满酯羧苄青霉素的代谢情况，通过与氚水交换制备了标记的茚满醇，并将其与苯丙酰氯和6-氨基青霉烷酸一起用于制备标记的茚满酯羧苄青霉素。将标记的茚满醇和茚满酯羧苄青霉素口服给予狗和大鼠，尿液中标记物回收率良好。在狗身上，无论直接给予茚满醇还是给予茚满酯羧苄青霉素，茚满醇都会以茚满醇的葡萄糖醛酸和硫酸酯共轭物以及两种羟基茚满酮和两种羟基茚满醇的共轭物形式随尿液排出，这是通过气相色谱 - 质谱联用测定的。相反，无论给予大鼠茚满醇还是茚满酯羧苄青霉素，大鼠仅排出茚满醇的共轭物。给人类口服未标记的茚满酯羧苄青霉素后，通过气相色谱分析测定，尿液中茚满醇的共轭物回收率很高。在人类尿液中未观察到狗体内形成的其他茚满醇代谢产物。
