Lukkari E, Hakonen T, Neuvonen P J
Department of Clinical Pharmacology, University of Helsinki, Haartmaninkatu, Finland.
Eur J Clin Pharmacol. 1998 Jan;53(5):351-4. doi: 10.1007/s002280050392.
The effect of gender and concomitant use of contraceptive steroids on the absorption and metabolism of oxybutynin was investigated in 49 healthy volunteers, 24 females and 25 males. Serum concentrations of oxybutynin and its active metabolite, N-desethyloxybutynin, were measured for up to 48 h after ingestion of a single dose of 10 mg oxybutynin.
Intake of oral contraceptive steroids had no significant effect on the pharmacokinetic parameters of oxybutynin or its metabolite. Both in males and females, the mean area under the curve (AUC0-t) of N-desethyloxybutynin was about 13 times higher and the peak concentration (Cmax) 15 to 19 times higher than the AUC0-t and Cmax of the parent oxybutynin, with no significant differences between males and females.
The pharmacokinetics of orally administered oxybutynin shows a considerable interindividual variability, but is unaffected by gender and use of contraceptive steroids.
在49名健康志愿者(24名女性和25名男性)中研究性别及同时使用避孕甾体激素对奥昔布宁吸收和代谢的影响。单次口服10 mg奥昔布宁后,测定长达48小时的奥昔布宁及其活性代谢物N - 去乙基奥昔布宁的血清浓度。
口服避孕甾体激素对奥昔布宁及其代谢物的药代动力学参数无显著影响。在男性和女性中,N - 去乙基奥昔布宁的平均曲线下面积(AUC0 - t)约比母体奥昔布宁的AUC0 - t高13倍,峰浓度(Cmax)高15至19倍,男性和女性之间无显著差异。
口服奥昔布宁的药代动力学存在相当大的个体间差异,但不受性别和避孕甾体激素使用的影响。