Bressolle F, Costa P, Rouzier-Panis R, Marquer C
Faculté de Pharmacie, Université de Montpellier, France.
Eur J Clin Pharmacol. 1996;49(5):411-5. doi: 10.1007/BF00203788.
The concentration-time profiles of specific metabolites of moxisylyte, an alpha-adrenoceptor blocking agent, in the plasma and urine from 18 healthy volunteers were investigated after intracavernous (IC) administrations at three dose levels (10, 20 and 30 mg).
Four metabolites, unconjugated desacetyl-moxisylyte (DAM), DAM glucuronide, and DAM and monodesmethylated DAM (MDAM) sulphates were found in plasma and urine. For all metabolites, t1/2 elimination was independent of the administered dose (1.19 h for unconjugated DAM; 1.51 h for DAM glucuronide; 1.51 h for DAM sulphate; and 2.17 h for MDAM sulphate). Cmax and AUC increased in direct proportion to dose, except for the inactive DAM glucuronide. Any the differences detected were small and equivalence of the three doses can be accepted.
The pharmacokinetics of moxisylyte in humans following intracavernous administration were linear in the dose range 10 to 30 mg.
研究18名健康志愿者在三个剂量水平（10、20和30毫克）海绵体内（IC）给药后，α-肾上腺素受体阻滞剂莫西赛利特定代谢物在血浆和尿液中的浓度-时间曲线。
在血浆和尿液中发现了四种代谢物，即未结合的去乙酰基莫西赛利（DAM）、DAM葡糖醛酸苷以及DAM和单去甲基化DAM（MDAM）的硫酸盐。对于所有代谢物，消除半衰期与给药剂量无关（未结合的DAM为1.19小时；DAM葡糖醛酸苷为1.51小时；DAM硫酸盐为1.51小时；MDAM硫酸盐为2.17小时）。除无活性的DAM葡糖醛酸苷外，Cmax和AUC与剂量成正比增加。检测到的任何差异都很小，三个剂量的等效性可以接受。
海绵体内给药后，莫西赛利在人体中的药代动力学在10至30毫克的剂量范围内呈线性。
