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.
Karhu
David
D
Labopharm, Inc, 480 boul Armand-Frappier, Laval, Québec, H7V 4B4, Canada. dkarhu@labopharm.com
Fradette
Caroline
C
Potgieter
Maria Alida
MA
Ferreira
Maria M
MM
Terblanché
Johann
J
D000284:Administration, Oral; D000293:Adolescent; D000328:Adult; D000701:Analgesics, Opioid / Q000008:administration & dosage / Q000493:pharmacokinetics*; D019540:Area Under Curve; D018592:Cross-Over Studies; D003692:Delayed-Action Preparations; D004334:Drug Administration Schedule; D005260:Female; D006801:Humans; D008297:Male; D013607:Tablets; D013997:Time Factors; D014147:Tramadol / Q000008:administration & dosage / Q000493:pharmacokinetics*; D055815:Young Adult
D000701:Analgesics, Opioid; D003692:Delayed-Action Preparations; D013607:Tablets; D014147:Tramadol