Musson D G, Hajdu R, Bayne W F, Rogers J D
Merck Sharp & Dohme Research Laboratories, West Point, Pennsylvania 19486.
Pharm Res. 1991 Jan;8(1):33-9. doi: 10.1023/a:1015818004113.
Imipenem (thienamycin formamidine) is an antibiotic active against a broad spectrum of bacteria. Its primary metabolite arises from cleavage of the lactam ring. The metabolite can be formed in-vitro by acid-catalyzed or enzymatic hydrolysis. In animals and man, this metabolite can be generated systemically as well as in the kidneys following the excretion of imipenem into the urine. In man, this dehydropeptidase-catalyzed renal metabolism is minimized by the coadministration of cilastatin, a competitive inhibitor. A specific HPLC assay has been developed to evaluate the disposition of this metabolite in humans having normal or end-stage renal function. The assay employs ion-pair, reversed-phase chromatography, and post-column acid treatment of the analyte for ultraviolet detection.
亚胺培南（硫霉素甲脒）是一种对多种细菌有效的抗生素。其主要代谢产物源于内酰胺环的裂解。该代谢产物可通过酸催化或酶促水解在体外形成。在动物和人体内，这种代谢产物可在亚胺培南排泄到尿液后在全身以及肾脏中产生。在人体中，通过同时给予竞争性抑制剂西司他丁可使这种脱氢肽酶催化的肾脏代谢降至最低。已开发出一种特定的高效液相色谱法来评估这种代谢产物在具有正常或终末期肾功能的人体内的处置情况。该方法采用离子对反相色谱法，并对分析物进行柱后酸处理以进行紫外检测。
