The goal of present study was to compare the pharmacokinetic profiles of single-dose administration of an FDC tablet containing rosuvastatin/olmesartan 20/40 mg (test formulation) with coadministration of a rosuvastatin 20-mg tablet and a olmesartan 40-mg tablet (reference formulation) in healthy Korean male volunteers, for the purpose of determining bioequivalence.
This single-dose, randomized, open-label, 2-period crossover study enrolled subjects aged 20 to 50 years and within 20 % of ideal body weight. Each subject received a single dose of the test and reference formulations orally in a fasted state, with a 7-day washout period between the administrations. Blood samples were collected up to 72 hours after dosing, and pharmacokinetic parameters were determined for rosuvastatin, its active metabolite (N-desmethyl rosuvastatin), and olmesartan. Bioequivalence was concluded if the 90 % CIs of the geometric mean ratios for the primary pharmacokinetic parameters were within the predetermined range of 80 % to 125 % . Adverse events (AEs) were evaluated based on subject interviews and physical examinations.
Among the 58 enrolled subjects, 54 completed the study. The 90 % CIs of the geometric mean ratios of the primary pharmacokinetic parameters were as follows: rosuvastatin: AUClast, 85.60 % to 97.40 % and Cmax, 83.16 % to 98.21 % ; N-desmethyl rosuvastatin: AUClast, 82.08 % to 93.45 % and Cmax, 79.23 % to 93.41 % ; and olmesartan: AUClast, 97.69 % to 105.69 % and Cmax, 100.35 % to 109.42 % . The most frequently noted AE was headache, occurring in 3 and 6 patients with the test and reference formulations, respectively. All of the AEs were expected, and there was no significant difference in the prevalences of AEs between the 2 formulations.
The pharmacokinetic properties of the newly developed FDC tablet of rosuvastatin/olmesartan 20/40 mg suggest that it is bioequivalent to co-administration of each drug as individual tablets in these healthy Korean male subjects. The two formulations were well tolerated, with no serious AEs observed. ClinicalTrials.gov identifier: NCT01823900.