Meyer E, Lambert W, De Leenheer A, De Bersaques J, Kint A
Laboratoria voor Medische Biochemie en voor Klinische Analyse, Gent, Belgium.
Br J Clin Pharmacol. 1992 Feb;33(2):187-9. doi: 10.1111/j.1365-2125.1992.tb04023.x.
The concentrations of trans-acitretin and its principal metabolite, cis-acitretin, were measured by h.p.l.c. after single and multiple dosing (50 mg orally for 13 days) in plasma, blister fluid and epidermal samples from four healthy male volunteers. Within-day epidermal concentrations of trans-acitretin exceeded those of the cis-form which were at the limit of assay sensitivity. No accumulation of trans-acitretin was observed in plasma or blister fluid but AUC values for the drug in blister roof cells tended to be higher after multiple dosing.
在4名健康男性志愿者单次和多次给药(口服50 mg,持续13天)后,通过高效液相色谱法测定血浆、水疱液和表皮样本中反式阿维A及其主要代谢物顺式阿维A的浓度。日内表皮中反式阿维A的浓度超过了顺式异构体的浓度,顺式异构体的浓度处于检测灵敏度的极限。在血浆或水疱液中未观察到反式阿维A的蓄积,但多次给药后水疱顶细胞中该药物的AUC值往往更高。