This was a single center, open-label, two-way crossover, drug-drug-interaction study to determine the effect of multiple dosing of omeprazole on 4 consecutive days on the pharmacokinetics of a single dose of an immediate-release capsule of CG5503 (tapentadol) in healthy participants.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
TREATMENT
Masking
NONE
Enrollment
32
Tapentadol IR capsule containing 93 mg tapentadol hydrochloride.
Omeprazole capsule containing 40 mg omeprazole.
J&JPRD Clinical Pharmacology Unit
Merksem, Belgium
Pharmacokinetic parameter: Cmax of CG5503 base
14 blood samples for the determination of serum concentrations were taken at pre-dose and up to 48 hours after administration of the CG5503 IR capsule. The evaluation of the maximum observed serum concentration (Cmax) was based on the CG5503 base concentrations measured in serum samples using a validated liquid chromatography/tandem mass spectrometry (LC-MS/MS) method.
Time frame: Pre-dose up to 48 hours post-dose
Pharmacokinetic parameter: AUC0-t of CG5503 base
14 blood samples for the determination of serum concentrations were taken at pre-dose and up to 48 hours after administration of the CG5503 IR capsule. The evaluation of the area under the concentration time curve (AUC) from 0 hours to time t (=48 hours) (AUC0-t) was based on the CG5503 base concentrations measured in serum samples.
Time frame: Pre-dose up to 48 hours post-dose
Pharmacokinetic parameter: AUC0-inf of CG5503 base
14 blood samples for the determination of serum concentrations were taken at pre-dose and up to 48 hours after administration of the CG5503 IR capsule. The AUC from 0 hours to infinity (AUC0-inf) was extrapolated from the AUC from administration to the last measured concentration.
Time frame: Pre-dose up to 48 hours post-dose
Pharmacokinetic parameter: Cmax of CG5503-O-glucuronide
14 blood samples for the determination of serum concentrations were taken at pre-dose and up to 48 hours after administration of the CG5503 IR capsule. The evaluation of the maximum observed serum concentration (Cmax) was based on the CG5503-O-glucuronide concentrations measured in serum samples using a validated liquid chromatography/tandem mass spectrometry (LC-MS/MS) method.
Time frame: Pre-dose up to 48 hours post-dose
Pharmacokinetic parameter: AUC0-t of CG5503-O-glucuronide
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14 blood samples for the determination of serum concentrations were taken at pre-dose and up to 48 hours after administration of the CG5503 IR capsule. The evaluation of the area under the concentration time curve (AUC) from 0 hours to time t (=48 hours) (AUC0-t) was based on the CG5503-O-glucuronide concentrations measured in serum samples.
Time frame: Pre-dose up to 48 hours post-dose
Pharmacokinetic parameter: AUC0-inf of CG5503-O-glucuronide
14 blood samples for the determination of serum concentrations were taken at pre-dose and up to 48 hours after administration of the CG5503 IR capsule. The AUC from 0 hours to infinity (AUC0-inf) was extrapolated from the AUC from administration to the last measured concentration.
Time frame: Pre-dose up to 48 hours post-dose
Incidence of treatment emergent adverse events
Number of adverse events and number of participants with adverse events.
Time frame: Day 1 to Day 4