The perception and pharmacokinetics of a 20-mg dose of escitalopram orodispersible tablets in a relative bioavailability study in healthy men

Abstract

Background: Rapidly dissolving oral (orodispersible) drug formulations have been developed to overcome problems related to swallowing.

Objective: The aim of this study was to compare the bioavailability of orodispersible and conventional immediate-release (IR) escitalopram tablets.

Methods: This was a randomized, open-label, 3-way crossover trial in which healthy men received single doses of orodispersible escitalopram formulations (2 ×10 mg and 1 × 20 mg) and conventional (2 × 10 mg) oral escitalopram tablets. Blood samples for pharmacokinetic analysis were obtained during a 168-hour period after dosing. The safety profile and tolerability were assessed by monitoring of adverse events, physical examinations, ECGs, and clinical laboratory and vital signs assessments. A questionnaire was used to assess the perception of the orodispersible tablet (ODT).

Results: The assumed bioequivalence assessment was based on pharmacokinetic and statistical analysis of data from the 29 men who completed the 3 treatments. The serum concentration-time profiles of escitalopram were similar after intake of the 3 treatments. The 90% CI for the mean treatment ratios of the log-transformed C(max), AUC(0-t), and AUC(0-∞) were all within the predefined equivalence range of 80% to 125%. Most subjects (87%) thought that the ODT was pleasant to take, and 85% of subjects thought that it was convenient to take the tablet without water. Most subjects (67%-90%) reported adverse events, with a similar incidence for all treatments. Most adverse events were mild, with somnolence and nausea being the most frequently reported. No clinically relevant changes were observed in physical, biochemical, hematologic, or urinalysis variables during the study.

Conclusions: In this small study population of fasting healthy male volunteers, 2 × 10-mg ODTs or 1 × 20-mg ODT and 2 × 10-mg conventional IR escitalopram tablets met the regulatory criteria for assumed bioequivalence. CLINICALTRIALS.GOV IDENTIFIER: NCT 01395433.

Trial registration: ClinicalTrials.gov NCT01395433.