Comparative Pharmacokinetics of a Once‐Daily Tramadol Extended‐Release Tablet and an Immediate‐Release Reference Product Following Single‐Dose and Multiple‐Dose Administration

The pharmacokinetics of a once‐daily formulation of tramadol (Tramadol Contramid OAD 200‐mg tablets) following single‐dose and multiple‐dose administration was compared with that of an immediate‐release product (tramadol IR 50‐mg tablets) in 2 separate studies. In both studies, AUC parameters met bioequivalence criteria, whereas C max of Tramadol Contramid OAD was lower than that of tramadol IR following a 200‐mg daily dosage. After single‐dose administration, the mean tramadol concentration at 1 hour postdose was within the range associated with analgesic efficacy (>100 ng/mL), and the mean concentration remained above this level for the remainder of the dosing interval. Steady state was attained within 48 hours following multiple‐dose administration. Tramadol Contramid OAD provides a rapid rise in plasma concentrations and an equivalent daily systemic exposure as tramadol IR, with a reduction in peak plasma concentrations.