Diekmann H W, Bühring K U, Garbe A, Nowak H
Arzneimittelforschung. 1976 Apr;26(4b):722-6.
The metabolite patterns of 4,4-diphenyl-N-isopropyl-cyclohexylamine-hydrochloride (pramiverine, Sistalgin) in urine, feces, bile and serum of Wistar rats, beagle dogs, rhesus monkey and man were analyzed with radio thin-layer chromatographic techniques. The structures of six pramiverine metabolites were elucidated. Pramiverine is eliminated unchanged in only minute amounts via the renal, the biliary and the fecal route. Consequently an almost quantitative absorption and metabolism takes place. Metabolite patterns in serum and urine differ considerably indicating that some of the metabolites are excreted preferentially by the kidney while others are reabsorbed to various degrees. The identified metabolites are products of dealkylation, deamination and hydroxylation reactions.
采用放射性薄层色谱技术分析了4,4 -二苯基 - N -异丙基 - 环己胺盐酸盐(普拉米维林,西斯塔金)在Wistar大鼠、比格犬、恒河猴和人类尿液、粪便、胆汁及血清中的代谢物模式。阐明了六种普拉米维林代谢物的结构。普拉米维林仅通过肾脏、胆汁和粪便途径以极少量原样排出。因此,几乎发生了定量吸收和代谢。血清和尿液中的代谢物模式差异很大,表明一些代谢物优先通过肾脏排泄,而其他代谢物则有不同程度的重吸收。鉴定出的代谢物是脱烷基化、脱氨基和羟基化反应的产物。