A Study to Assess Bioequivalence of a New Tapentadol Extended-Release Tablet With Respect to a Tapentadol Extended Release Tablet Under Fasted Conditions in Healthy Subjects

A Single-Dose, Open-Label, Randomized, 2-Way Crossover Pivotal Study to Assess Bioequivalence of a New Tapentadol Extended-Release (TRF) 100-mg Tablet With Respect to a Tapentadol Extended-Release (PR2) 100-mg Tablet Under Fasted Conditions in Healthy Subjects

Status

Completed

Phases

Phase 1

Study type

Interventional

Source

ClinicalTrials.gov

Registry ID

NCT02019485

Enrollment

Registered

2013-12-24

Start date

2010-07-31

Completion date

2010-08-31

Last updated

2013-12-24

For informational purposes only — not medical advice. Sourced from public registries and may not reflect the latest updates. Terms

Conditions

Healthy

Keywords

Healthy, Tapentadol, Tapentadol extended-release tamper-resistant formulation, Tapentadol extended-release prolonged-release formulation, Bioequivalence, Fasted Conditions

Brief summary

The purpose of this study is to evaluate bioequivalence (biological equivalence of two formulations of a study medication) of a new tapentadol Extended release (ER) 100 mg tamper-resistant formulation (TRF) tablet, to the current tapentadol ER 100 mg, prolonged-release formulation 2 (PR2) tablet used in healthy participants under fasted (without food) conditions.

Detailed description

This is an open-label (all people know the identity of the intervention), randomized (the study medication is assigned by chance), 2-way crossover (method used to switch participants from one treatment arm to another in a clinical study), single-dose, and single-center study. The study consists of 3 phases: the screening phase, treatment phase, and end-of-study or withdrawal assessment phase. In the treatment phase, participants will receive a single dose of new tapentadol ER 100-mg TRF tablet (Treatment A) and current tapentadol ER 100-mg PR2 (Treatment B) under fasted conditions in 2 treatment sequences (AB and BA). Administration of the study medication will be separated by a washout period (no treatment) of 7 to14 days. Approximately 64 participants will be enrolled in this study. Safety will be evaluated by the assessment of adverse events, clinical laboratory tests, electrocardiogram, vital signs, and physical examination. The duration of participation in the study for an individual participant will be approximately 5.5 weeks.

Interventions

DRUGTapentadol Extended Release (ER) Tamper-Resistant Formulation (TRF)

Participants will receive a single dose of tapentadol ER TRF 100 mg tablet orally (by mouth) in treatment sequences AB and BA appropriately.

DRUGTapentadol Prolonged-Release Formulation 2 (PR2)

Participants will receive a single dose of tapentadol PR2 100 mg tablet orally in treatment sequences AB and BA appropriately.

Study design

Allocation

RANDOMIZED

Intervention model

CROSSOVER

Primary purpose

TREATMENT

Masking

NONE

Eligibility

Sex/Gender

ALL

Age

19 Years to 55 Years

Healthy volunteers

Yes

Inclusion criteria

* Agrees to protocol-defined use of effective contraception * Body mass index (BMI) between 20 and 28 kilograms per square meter, inclusive, and body weight not less than 50 kg (BMI is calculated as weight \[kilogram\] divided by square of height \[meter\]) * Habitually smokes no more than 10 cigarettes, or 2 cigars, or 2 pipes of tobacco per day for at least 6 months before the first study medication administration

Exclusion criteria

* History of seizure disorder or epilepsy or mild or severe traumatic brain injury * Men with hemoglobin concentrations below 12.5 g/dL or women with hemoglobin concentrations below 11.5 g/dL * Positive test for drugs of abuse, such as cannabinoids, alcohol, opiates, cocaine, amphetamines, benzodiazepines, or barbiturates at screening or Day -1 of each treatment period * Positive test for human immunodeficiency virus antibodies, hepatitis B surface antigen, or hepatitis C antibodies * History of a gastrointestinal disease affecting absorption, gastric surgery or history of or current significant medical illness

Design outcomes

Primary

Measure	Time frame
Maximum serum concentration of tapentadol	Predose; 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 24, 36, and 48 hours postdose (at each single-dose of study medication)
Time to reach the observed maximum serum concentration of tapentadol	Predose; 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 24, 36, and 48 hours postdose (at each single-dose of study medication
Area under the serum concentration-time curve of tapentadol from time 0 to the time of the last quantifiable concentration	Predose; 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 24, 36, and 48 hours postdose (at each single-dose of study medication
Area under the serum concentration-time curve of tapentadol from time 0 to infinite time	Predose; 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 24, 36, and 48 hours postdose (at each single-dose of study medication
Percentage of area under the serum concentration-time curve of tapentadol from time 0 to infinite time	Predose; 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 24, 36, and 48 hours postdose (at each single-dose of study medication
Elimination half-life associated with the terminal slope of the semilogarithmic tapentadol concentration-time curve	Predose; 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 24, 36, and 48 hours postdose (at each single-dose of study medication
First-order rate constant associated with the terminal portion of tapentadol concentration curve	Predose; 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 24, 36, and 48 hours postdose (at each single-dose of study medication
Time to last quantifiable serum concentration of tapentadol	Predose; 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 24, 36, and 48 hours postdose (at each single-dose of study medication
Number of participants with adverse events	Up to end-of-study (Day 3 of last single-dose of study medication)

Countries

United States

Outcome results

None listed

Source: ClinicalTrials.gov · Data processed: Feb 4, 2026