Costa P, Bressolle F, Bromet-Petit M, Mosser J, Sarrazin B
Service d'Urologie Andrologie, Centre Hospitalier Universitaire, Nîmes, France.
J Pharm Sci. 1992 Dec;81(12):1223-6. doi: 10.1002/jps.2600811220.
The concentration-time profiles of metabolites of moxisylyte, an alpha-blocking agent, in the plasma and urine of 12 healthy volunteers were investigated after intravenous (iv) and oral (two formulations) administration. The study was conducted with an open, randomized Latin squares design. Plasma and urine levels of moxisylyte and its biotransformation products were assayed by a specific HPLC method with fluorescence detection. Plasma levels declined in a monophasic or biphasic pattern depending on the subject. Two metabolites, conjugated desacetylmoxisylyte (DAM) and conjugated monodesmethylated DAM (MDAM), were found in plasma and urine. Unconjugated DAM was found in plasma only after iv administration. The apparent elimination half-lives of unconjugated DAM, conjugated DAM, and MDAM were 0.86, 1.7, and 3 h, respectively. The total amounts of metabolites (expressed as the equivalent of DAM) excreted in the urine were 75% after i.v. administration and 68 and 69% after oral administration of the two formulations. Oral absorption appeared to be complete for the two treatments. There was no statistical difference between the two oral formulations studied.
在12名健康志愿者静脉注射（iv）和口服（两种制剂）后，研究了α受体阻滞剂莫西赛利代谢产物在血浆和尿液中的浓度-时间曲线。该研究采用开放、随机拉丁方设计进行。莫西赛利及其生物转化产物的血浆和尿液水平通过具有荧光检测的特定高效液相色谱法进行测定。血浆水平根据受试者呈单相或双相模式下降。在血浆和尿液中发现了两种代谢产物，即结合型去乙酰莫西赛利（DAM）和结合型单去甲基化DAM（MDAM）。仅在静脉注射后血浆中发现了未结合的DAM。未结合的DAM、结合型DAM和MDAM的表观消除半衰期分别为0.86、1.7和3小时。静脉注射后尿液中排泄的代谢产物总量（以DAM当量表示）为75%，口服两种制剂后分别为68%和69%。两种治疗的口服吸收似乎是完全的。所研究的两种口服制剂之间没有统计学差异。
