Pharmacokinetics and bioequivalence of two different 20 mg olmesartan tablets: A randomized, single-dose, two-period crossover study in healthy Korean male volunteers

Olmesartan is an angiotensin receptor blocker (ARB) and is widely used in clinical practice to treathypertension. To compare the pharmacokinetic (PK) parameters and tolerability of two oral formulationsof olmesartan (test drug: OMETAN® 20 mg tablet, reference drug: OLMETEC® 20 mgtablet) and assess their bioequivalence, a randomized, single dose, two-treatment crossover clinicalstudy was conducted. At each period, 40 subjects received the test drug or the reference drug. Bloodsamples were collected at pre-dose and up to 48 h after study drug administration of each period. Plasma concentrations of olmesartan were measured using liquid chromatography-tandem massspectrometry. To evaluate PK profiles, maximum plasma concentration (Cmax) and area under theconcentration-time curve from zero to last measurable time (AUClast) were estimated using a noncompartmentalmethod. Tolerability was evaluated based on the incidence of adverse events, vitalsigns, electrocardiograms, and laboratory tests. A total of 39 subjects completed the study. Thegeometric mean ratio and 90% confidence intervals (CI) of test drug to reference drug were 1.027(0.969–1.088) for Cmax and 1.014 (0.957–1.074) for AUClast, respectively. There were no serious adverseevents and both formulations of olmesartan were well tolerated. The OMETAN 20 mg tabletwas judged to be bioequivalent to the OLMETEC 20 mg tablet KCI Citation Count: 0