Haustein K O, Hüller G
Institute of Clinical Pharmacology, Medical Academy Erfurt, GDR.
Eur J Drug Metab Pharmacokinet. 1988 Apr-Jun;13(2):81-90. doi: 10.1007/BF03191308.
The pharmacokinetics of 14C-propiverine was studied in 13 volunteers and in 2 patients after a single i.v. injection of 5 mg or after oral administration of 15 mg. To each dose 1.11 MBq 14C-propiverine was added. The radioactivity measured in plasma, urine (and bile fluid), and the metabolites were estimated by an extraction procedure together with TLC and radiochromatography. Propiverine was eliminated from the plasma with a half-life time (t0.5) of 4.1 h (i.v. and per os), while the plasma radioactivity decreased with a t0.5 of 21.2 (i.v.) or 10.4 h (per os). Within 4 days, 84.5 (i.v.) or 53.5% (per os) of the administered radioactivity was excreted in urine. The absorption of radioactivity of propiverine amounted to 84.5%, while the amount of available propiverine was only 48.9%. In two patients with cannulated ductus choledochus, 21.5 or 14.7% of the administered radioactivity was excreted within 2 days. The metabolic pattern of plasma, urine and bile fluid mainly consisted of amine oxides, substances oxidized in the propyl side chain, desalkylated metabolites, substances with a N-demethylated piperidino group or with ester cleavage, and glucuronide conjugates. Unchanged propiverine appeared in plasma, urine and bile at about 6 to 8% of the administered dose.
在13名志愿者和2名患者中研究了14C-丙哌维林的药代动力学，单次静脉注射5mg或口服15mg后进行研究。每剂添加1.11MBq的14C-丙哌维林。通过萃取程序结合薄层色谱法和放射色谱法估算血浆、尿液（和胆汁）以及代谢物中测得的放射性。丙哌维林从血浆中消除的半衰期（t0.5）为4.1小时（静脉注射和口服），而血浆放射性以21.2（静脉注射）或10.4小时（口服）的t0.5下降。在4天内，84.5%（静脉注射）或53.5%（口服）的给药放射性经尿液排出。丙哌维林的放射性吸收量为84.5%，而可用丙哌维林的量仅为48.9%。在两名胆总管插管患者中，21.5%或14.7%的给药放射性在2天内排出。血浆、尿液和胆汁的代谢模式主要包括氧化胺、丙基侧链氧化的物质、去烷基化代谢物、具有N-去甲基哌啶基团或酯裂解的物质以及葡萄糖醛酸结合物。未变化的丙哌维林在血浆、尿液和胆汁中的出现量约为给药剂量的6%至8%。
