Format

Send to

Choose Destination
J Opioid Manag. 2013 Jul-Aug;9(4):291-300. doi: 10.5055/jom.2013.0171.

Pharmacokinetic evaluation of tapentadol extended-release tablets in healthy subjects.

Author information

1
Janssen Research & Development, LLC, New Jersey.
2
Janssen Research & Development, LLC, Beerse, Belgium.
3
GrĂ¼nenthal GmbH, Aachen, Germany.

Abstract

OBJECTIVE:

To evaluate serum pharmacokinetics of tapentadol administered to healthy subjects as extended-release (ER) tablets.

DESIGN:

Seven single-dose studies (five randomized, crossover, bioequivalence studies; a study in Japanese men; and a randomized, crossover, effects-of-food study) and one repeated-dose study.

SETTING:

Clinical research settings in the United States and The Netherlands.

PATIENTS OR PARTICIPANTS:

Healthy males and females were enrolled into seven studies; one study enrolled only Japanese males.

INTERVENTIONS:

In the bioequivalence studies, subjects first received one polyethylene oxide- or hypromellose-based tapentadol ER tablet (50, 100, 150, 200, or 250 mg; one dose per study), then (after washout) the other formulation (matching dose). In all other studies, subjects received polyethylene oxide-based tapentadol ER tablets. In the repeated-dose study, subjects received one 250 mg tablet, then (after washout) one 250 mg tablet every 12 hours (five doses). In the food-effect study, subjects received one 250 mg tablet within 30 minutes after a high-fat meal or after 10 hours of fasting. In the study in Japanese men, subjects received one 100 mg tablet.

MAIN OUTCOME MEASURES:

Maximum tapentadol concentrations (Cmax) were typically observed 5 hours after dosing. Mean terminal half-life values ranged from 4.4 to 5.9 hours. Tapentadol Cmax and AUC values increased proportionally following single ER (polyethylene oxide-based tablets) doses of 50 to 250 mg. Trough tapentadol concentrations increased during repeat dosing until reaching steady-state by the third dose. Serum Cmax and area under the concentration-time curve (AUC) values at steady state were 1.6 and 1.9 times higher relative to single-dose administration. Coadministration of the 250 mg dose with a high-fat meal increased Cmax and AUC values by an average of < 17 percent.

CONCLUSIONS:

The pharmacokinetics of tapentadol ER are consistent after repeated and single-dose administration. Tapentadol ER may be administered without regard to food intake. No clinically significant differences were observed in the pharmacokinetics of tapentadol between Japanese and Caucasian subjects.

PMID:
24353023
DOI:
10.5055/jom.2013.0171
[Indexed for MEDLINE]

Supplemental Content

Loading ...
Support Center