Costa P, Bressolle F, Jarroux E, Sarrazin B, Mosser J, Navratil H, Galtier M
Service d'Urologie-Andrologie, CHU G. Doumergue, Nîmes, France.
J Pharm Sci. 1993 Sep;82(9):968-71. doi: 10.1002/jps.2600820920.
The pharmacokinetics of moxisylyte in plasma and urine was investigated after oral administration. Twelve subjects were treated orally, twice daily with 240 mg of the drug for 6 days; on day 7, the subjects received a last dose of 240 mg of moxisylyte. Moxisylyte was assayed in plasma and urine by a specific HPLC method with fluorimetric detection. Moxisylyte was absorbed rapidly and changed to its metabolites immediately after drug administration; unchanged moxisylyte was not found in plasma. Two metabolites were found in plasma and urine: conjugated desacetylmoxisylyte (DAM) and the conjugate of desmethylated DAM (MDAM). The pharmacokinetic parameters determined after the first oral administration were not modified on multiple dosing. The apparent elimination half-lives of conjugated DAM and MDAM were 2.3 and 3.5 h, respectively. Elimination of these two metabolites in urine averaged 50 and 10%, respectively.
口服给药后研究了莫西赛利在血浆和尿液中的药代动力学。12名受试者每日口服2次，每次240mg该药物，共6天；在第7天，受试者接受最后一剂240mg莫西赛利。采用具有荧光检测的特定高效液相色谱法测定血浆和尿液中的莫西赛利。给药后莫西赛利迅速吸收并立即转化为其代谢产物；血浆中未发现未变化的莫西赛利。在血浆和尿液中发现了两种代谢产物：共轭去乙酰莫西赛利（DAM）和去甲基化DAM的共轭物（MDAM）。首次口服给药后测定的药代动力学参数在多次给药时未改变。共轭DAM和MDAM的表观消除半衰期分别为2.3小时和3.5小时。这两种代谢产物在尿液中的消除率平均分别为50%和10%。
