Pharmacokinetic comparison between the fixed-dose combination of rosuvastatin/ezetimibe 2.5/10 mg and the co-administration of individual formulations in healthy subjects
Year: 2025
Type: article
Study design: Clinical Trial
Abstract: The combination therapy of low-dose rosuvastatin and ezetimibe has shown similar efficacy in decreasing low-density lipoprotein cholesterol (LDL-C) compared to high-dose rosuvastatin monotherapy.This study aimed to compare the pharmacokinetics (PKs) between the fixed-dose combination (FDC) of rosuvastatin/ezetimibe 2.5/10 mg and the co-administration of individual formulations.A randomized, open-label, single-dose, 2-sequence, 2-period, crossover study was conducted in healthy volunteers.Subjects were randomized in each sequence and received a single dose of the FDC of rosuvastatin/ ezetimibe 2.5/10 mg or the co-administration of individual formulations in each period with a 14-day washout.Serial blood samples for PK analysis were collected up to 48 hours post-dose for rosuvastatin and 72 hours post-dose for ezetimibe.The geometric mean ratios (GMRs) and 90% confidence intervals (CIs) of the FDC to the co-administration for maximum plasma concentration (C max ) and area under the curve from zero to the last measurable time point (AUC last ) were calculated.Forty-seven subjects were randomized, and 41 subjects completed the study.The GMRs (90% CIs) of C max and AUC last for rosuvastatin were 0.9789 (0.9020-1.0622) and 0.9741 (0.9105-1.0422).The corresponding values were 1.0419 (0.9219-1.1776) and 0.9983 (0.9522-1.0465) for total ezetimibe, and 1.0396 (0.9087-1.1893) and 0.9743 (0.8997-1.0550) for free ezetimibe, respectively.All the values were within the conventional bioequivalence criteria of 0.8 to 1.25.In conclusion, the FDC of rosuvastatin/ezetimibe 2.5/10 mg showed comparable PK with the co-administration of individual formulations.
Authors: Dowon Lee, Sejung Hwang, Taewon Lee, Kyung-Sang Yu, SeungHwan Lee
Language: English
Subfield: Surgery
Field: Medicine
Domain: Health Sciences
Open Access status: diamond
Funder: Yuhan
OpenAlex ID: W4411680776