Hausleiter H J, Achtert G, Khan M A, Kukovetz W R, Beubler E
Eur J Drug Metab Pharmacokinet. 1982 Oct-Dec;7(4):329-39. doi: 10.1007/BF03189637.
10 and 20 mg of N-Propyl-ajmalin-hydrogentartrate (N-PAB, Neo-Gilurytmal) were administered i.v. and orally respectively to healthy volunteers. In the study 14C-labelled N-PAB was used. The pharmacokinetics and the metabolic behaviour was examined. A fast and complete absorption of the compound could be observed. The bioavailability was 78%. The terminal plasma elimination half-life (beta-phase) was in the range of 4 to 6 hours. A total of 33% of the administered radioactivity was excreted via the kidney. 35 to 48% of the radioactivity found in urine was unchanged N-PAB. The excretion-kinetics of the three main metabolites as well as of the parent compound were determined. The possible presence of non-metabolizers is suggested.
分别向健康志愿者静脉注射和口服10毫克和20毫克的N-丙基阿马林氢酒石酸盐(N-PAB,新吉尔鲁特马尔)。在该研究中使用了14C标记的N-PAB。对其药代动力学和代谢行为进行了研究。可以观察到该化合物快速且完全吸收。生物利用度为78%。终末血浆消除半衰期(β相)在4至6小时范围内。总共33%的给药放射性通过肾脏排泄。尿液中发现的放射性的35%至48%是未变化的N-PAB。测定了三种主要代谢物以及母体化合物的排泄动力学。提示可能存在非代谢者。