Single-Dose Oral Bioavailability and Pharmacokinetic Characterization of S-Etodolac 200 mg Modified-Release Film Tablets in Healthy Male Volunteers Under Fasting Conditions
Dr. Bhanu Prakash Reddy
DOI: https://doi.org/10.63712/bpsrj-v2i3p005
ABSTRACT:
Background: Etodolac is a non-steroidal anti-inflammatory drug (NSAID) characterized by a racemic mixture, with the S-enantiomer primarily responsible for therapeutic activity. Modified-release (MR) formulations are designed to prolong drug release, offering the advantage of reduced dosing frequency. Objective: This study aimed to characterize the oral bioavailability and pharmacokinetic (PK) profile of a newly developed S-Etodolac 200 mg MR film tablet. Methods: An open-label, single-dose, single-period study was conducted involving 24 healthy adult male subjects under fasting conditions. Following an overnight fast, each subject received a single 200 mg dose of the test formulation. A total of 23 blood samples were collected over a 48-hour period. Plasma concentrations of S-Etodolac were quantified, and PK parameters were derived using non-compartmental analysis. Safety and tolerability were also assessed. Results: All 24 enrolled subjects completed the study. The drug exhibited a delayed absorption profile consistent with an MR formulation, achieving a median peak plasma concentration (Tmax) at 5.5 hours. The mean peak concentration (Cmax) was 1992.07 ± 503.94 ng/mL. The mean area under the curve from time zero to the last measurable concentration (AUC0-t) and extrapolated to infinity (AUC0-inf) were 37415.07 ± 12775.43 ng·hr/mL and 39521.14 ± 13914.82 ng·hr/mL, respectively. The mean elimination half-life (t1/2) was 8.44 ± 1.91 hours. The formulation was well-tolerated, with no adverse events reported during the study. Conclusion: The S-Etodolac 200 mg MR film tablet demonstrates a prolonged absorption and elimination profile suitable for modified-release drug delivery. The formulation is safe and well-tolerated in healthy male subjects under fasting conditions.