Pharmacokinetics of oral viaminate in healthy Chinese subjects: an open-label, sequential, single-dose, food-effect, and multiple-dose study

Viaminate is a retinoid derivative and possesses the therapeutic effects of retionid but the adverse effects are less than those of other oral retinoids. However, the pharmacokinetic profiles of viaminate following single and multiple oral doses have not yet been fully characterized in human being. An open-label, dose-escalation study was performed to evaluate the pharmacokinetics of oral viaminate in 9 healthy Chinese volunteers. Pharmacokinetics parameters of viaminate were determined using serial blood samples obtained up to 15 hours after administration of single dose (50-, 100-, or 150 mg), multiple doses of 50 mg twice a day or single dose of 50 mg half an hour after a high-fat breakfast. Areas under the curve of plasma concentration vs. time (AUC) and the maximum plasma concentration (Cmax) were found to be proportional to dose. But the elimination half-life (t1/2) and the time reaching maximum plasma concentration (Tmax) were not changed significantly. Food had a positive effect on the extent of absorption (AUC 57.5 [fed] vs. 8.4 ng·h/mL [fasted]), and peak concentration was significantly increased (Cmax 18.4 [fed] vs. 1.4 ng/mL [fasted]), while rate of absorption was similarly (Tmax 3.8 [fed] vs. 3.1 h [fasted]). Viaminate was well tolerated in the studied dose range in healthy Chinese subjects. Viaminate displayed linear pharmacokinetics in the dose range from 50 to 150 mg after a single oral dose. The ingestion of food significantly increased the extent of viaminate absorption. No marked effects of sex on the pharmacokinetic parameters of viaminate were observed.