Comparison of relative bioavailability between the fixed dose combination (FDC) of rosuvastatin calcium 20 mg and ezetimibe 10 mg coated tablet (Trezete®) versus rosuvastatin calcium and ezetimibe concomitantly administered to healthy volunteers

Bioavailability comparison between the FDC Trezete® coated tablet and co-administration of rosuvastatin calcium (Crestor®) and ezetimibe (Ezetrol®) in 60 healthy volunteers. This was a typical crossover bioequivalence study in which a group of volunteers received the test formulation and both reference formulations. Blood samples were collected throughout a 72-hour interval. Rosuvastatin calcium and ezetimibe plasmatic concentrations were determined separately by mass spectrometry (HPLC-MS-MS). From the concentration obtained were calculated main pharmacokinetics parameters: AUC0-t and Cmax and secondary parameters. The geometric mean of Trezete®/Crestor® were 93.62% for Cmax (91.34% - 102.36%) and for AUC0-t, 96.19% (90.16% - 102.61%). Trezete®/Ezetrol® AUC0-t was 100.11% (93.89% - 106.74%) and Cmax, 95.54% (86.91% - 105.03%). The 90% confidence intervals for AUC0-t and Cmax were within the range of 80%-125% proposed by ANVISA and FDA for bioequivalence evaluation. It was concluded that Trezete® is bioequivalent to Crestor® and Ezetrol® concomitantly administered.