The purpose of this study is to evaluate bio-equivalence of tapentadol extended-release (ER) tamper-resistant formulation (TRF) tablet, to the current tapentadol ER, prolonged-release formulation 2 (PR2) tablet, in healthy participants.
This is a single-dose, open-label (a medical research study in which participants and researchers are told which treatments the participants are receiving, "unblinded"), single-centre, randomized (like the flip of a coin; 50/50 chance of receiving a study treatment), and 2-way crossover (groups of participants receive two or more interventions in a particular order) study of a single-dose tapentadol in healthy participants under fasted conditions. The study consists of 3 parts: Screening (2 to 21 days before the study commences), Open-label Treatment (single-dose treatment on Day 1 of each period separated with wash-out period of 7 to 14 days) and End of study (Day 3 of treatment Period 2). The duration of participation in the study for an individual participant will be up to 5.5 weeks (including Screening). Participants will be randomly assigned to one of the 2 treatment sequence groups. Participants assigned to the first treatment sequence will receive tapentadol TRF 50 milligram (mg) tablet, and after a washout period, participants will receive tapentadol PR2 50-mg tablet. Participants assigned to the second treatment sequence will receive tapentadol PR2 50-mg tablet, and after washout period, participants will receive tapentadol TRF 50-mg tablet. Bio-equivalence will be primarily evaluated by pharmacokinetics parameters. Participant's safety will be monitored throughout the study.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
TREATMENT
Masking
NONE
Enrollment
64
Single dose of tapentadol ER 50 milligram (mg), will be administered under fasted condition.
Single dose of tapentadol ER 50 milligram (mg), prolonged release tablet will be administered under fasted condition.
Unnamed facility
Lincoln, Nebraska, United States
Maximum Serum Concentration (C[max])
The C(max) is the maximum serum concentration which will be observed at the defined time points.
Time frame: Pre-dose and 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 24, 36 and 48 hours post-dose of study medication
Area Under the Serum Concentration-Time Curve From Time Zero to Infinite Time (AUC [infinity])
The AUC (infinity) is the area under the serum concentration-time curve from time zero to infinite time, calculated as the sum of AUC(last) and C(last)/lambda(z), wherein AUC(last) is area under the plasma concentration-time curve from time zero to last quantifiable time; and C(last) is the last observed quantifiable concentration; and lambda(z) is elimination rate constant.
Time frame: Pre-dose and 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 24, 36 and 48 hours post-dose of study medication
Area Under the Serum Concentration-Time Curve From Time Zero to Infinite Time (AUC [last])
The AUC (last) is the area under the serum concentration-time curve from time zero time of the last quantifiable concentration C(last), and C(last) is the last observed quantifiable concentration.
Time frame: Pre-dose and 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 24, 36 and 48 hours post-dose of study medication
Time to Reach the Maximum Serum Concentration (T[max])
The T\[max\] is time to reach the observed maximum serum concentration.
Time frame: Pre-dose and 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 24, 36 and 48 hours post-dose of study medication
Percentage of AUC(infinity)
Percentage of AUC(infinity) is calculated as (AUC\[infinity\] minus AUC\[last\] divided by AUC\[infinity\]) multiplied by 100.
Time frame: Pre-dose and 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 24, 36 and 48 hours post-dose of study medication
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Elimination half-life period (t1/2)
Elimination half-life associated with the terminal slope (lambda\[z\]) of the semi logarithmic drug concentration-time curve, calculated as 0.693/lambda (z).
Time frame: Pre-dose and 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 24, 36 and 48 hours post-dose of study medication
Terminal slope (Lambda [z])
Terminal slope is defined by first-order rate constant associated with the terminal portion of the curve, determined as the negative slope of the terminal log-linear phase of the drug concentration-time curve.
Time frame: Pre-dose and 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 24, 36 and 48 hours post-dose of study medication
Time to Last Quantifiable Serum Concentration (T[last])
The T(last) is the time to reach last quantifiable serum concentration.
Time frame: Pre-dose and 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 24, 36 and 48 hours post-dose of study medication
Relative Bioavailability of Tapentadol (F[rel])
The F(rel) of tapentadol is calculated as the Area Under the Serum Concentration-Time Curve (AUC) and Cmax ratios of the two Treatments(that is, treatment effect).
Time frame: Pre-dose and 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 24, 36 and 48 hours post-dose of study medication