Pharmacokinetics and safety of a telmisartan/amlodipine/rosuvastatin fixed-dose combination tablet compared to co-administration of telmisartan/amlodipine and rosuvastatin in healthy Korean male volunteers.

内容摘要

This study was conducted to compare the single-dose pharmacokinetic and safety profiles of JLP-1401 (fixed-dose combination (FDC) of telmisartan/amlodipine/rosuvastatin) to those of each constituent co-administered in healthy Korean male volunteers. A total of 40 healthy Korean subjects participated in an open-label, randomized, single-dose, 4-period crossover study. During each treatment period, the subjects received the test drug (FDC tablet of telmisartan/amlodipine/rosuvastatin 80 mg/10 mg/20 mg) or reference drug (co-administration of telmisartan/amlodipine FDC tablet and rosuvastatin tablet). Plasma samples were collected pre dose and at 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12, 24, 48, and 72 hours post dose to evaluate pharmacokinetic profiles. Safety was assessed by the evaluation of adverse events (AEs), laboratory assessments, 12-lead electrocardiograms, physical examinations, and vital sign measurements. The geometric least-square mean ratios and their 90% confidence intervals of AUClast and Cmax were 1.01 (0.94 - 1.07) and 0.83 (0.72 - 0.95) for telmisartan, 1.01 (0.99 - 1.04) and 1.03 (1.01 - 1.06) for amlodipine, and 1.03 (0.98 - 1.08) and 0.94 (0.85 - 1.04) for rosuvastatin, respectively. All AEs were of mild or moderate intensity, and there were no significant differences in the incidence of AEs between the treatments. The pharmacokinetic profiles of the test and reference drugs were within the bioequivalent criteria, and both drugs were safe and well tolerated.