CompletedNCT03956134Updated May 20, 2019

Pharmacokinetic Characterization of Two Novel CG5503 Tablet Formulations in Healthy Volunteers

A Phase 1 interventional study of Tapentadol Test Product 1 and Tapentadol Test Product 2 in Pharmacokinetics, sponsored by Grünenthal GmbH. Completed at 1 site in Germany. Open to male participants aged 18 Years to 55 Years, including healthy volunteers. Per ClinicalTrials.gov, last updated 2019-05-20.

Sponsored by Grünenthal GmbH · Phase 1, Interventional, and Treatment

From the registry’s dates

Registered 14 years 1 month after the study started (first participant enrolled Apr 2005, registered May 2019).

Phase: Phase 1
Study type: Interventional
Enrollment: 10
Allocation: Randomized
Ages: 18 Years to 55 Years
Sex: Male

Study summary

This study investigated the pharmacokinetics (how a drug is taken up and excreted from the body), safety, and tolerability of 2 new tapentadol (CG5503) tablet formulations compared to a previously characterized tapentadol prolonged-release (PR) tablet formulation.

Read the detailed description

The study was performed to evaluate the pharmacokinetic characteristics (relative bioavailability) of 2 new tapentadol (CG5503) tablet formulations (Test Product 1 and Test Product 2) containing 116 mg tapentadol hydrochloride each, as compared to a 116-mg tapentadol hydrochloride PR tablet (Reference Product) and to explore the effect of food on the bioavailability of the 2 new tapentadol formulations. Participants received a single dose of each of the test formulations under fasting or fed conditions and of the reference formulation under fasting conditions in a randomized order. There was a wash-out period of at least 3 days between consecutive treatments. Blood samples were taken from pre-dose up to 32 hours post-dose for pharmacokinetic analyses.

Furthermore, the study compared the safety and tolerability of the test formulations with that of the reference. Adverse events and vital signs were documented at screening, pre-dose, and up to 32 hours post-dose. Clinical laboratory parameters were determined and 12-lead electrocardiograms (ECG) were recorded at screening and at discharge. A final medical examination was performed at 2-14 days after discharge following the last treatment.

Conditions studied

Pharmacokinetics

In context

Lead sponsor

Grünenthal GmbH is the lead sponsor of 65 studies on the registry; 2 are open to participants now.

Of its 13 completed or terminated interventional studies of FDA-regulated products, 8 (62%) have results posted.

Counted across the registry records on this site, refreshed daily.

Who can participate

Ages eligible: 18 Years to 55 Years
Sexes eligible: Male
Accepts healthy volunteers: Yes

Inclusion criteria

Male Caucasian participants, aged 18-55 years;
Body Mass Index between 18 and 30 kg/m2 inclusive;
Participants must be in good health as determined by medical history, physical examination, 12-lead electrocardiogram, vital signs, and clinical laboratory parameters;
Participants giving written informed consent to participate within this study.

Exclusion criteria

Exclusion Criteria:

Resting pulse rate equal to or less than 45 or equal to or above 95 beats / min;
Resting blood pressure: systolic blood pressure equal to or less than 100 and equal to or above 140 mmHg, diastolic blood pressure equal to or less than 50 and equal to or above 90 mmHg;
Positive human immunodeficiency virus (HIV) type 1/2 antibodies, hepatitis B surface (HBs) antigen, hepatitis B core (HBc) antibodies, hepatitis C virus (HCV) antibodies;
History or presence of orthostatic hypotension;
Participation in another clinical study in the last three months before starting this study (exception: characterization of metabolizer status);
Positive screening of drug abuse;
Diseases or condition known to interfere with the absorption, distribution, metabolism or excretion of drugs;
Marked repolarization abnormality (e.g., suspicious or definite congenital long QT syndrome);
Bronchial asthma;
Definite or suspected history of drug allergy or hypersensitivity;
Participants who have received any prescribed and non-prescribed systemic or topical medication two weeks before and during the study with the exception of short term medication, e.g. headache with paracetamol;
Evidence of alcohol or drug abuse;
Not able to abstain from drinking of caffeine containing beverages (tea, coffee, chocolate or cola),
Consumption of any quinine containing beverages (bitter lemon, tonic water) or food within two weeks before and during the study;
Drinking of alcohol containing beverages within 48 hours before administration of investigational product(s);
Blood donation (above 100 mL) or comparable blood losses during the last 3 months;
History of seizures or at risk (i.e. head trauma, epilepsy in family anamnesis, unclear loss of consciousness);
Known or suspected of not being able to comply with the study protocol;
Not able to communicate meaningfully with the investigator and staff;
Smoking of more than 20 cigarettes/day.

Study design

Phase: Phase 1
Primary purpose: Treatment
Allocation: Randomized
Intervention model: Crossover assignment
Masking: None (open label)
Enrollment: 10 participants (actual)

Study arms

Experimental
Tapentadol Test Product 1 (fasting)
Tapentadol new tablet formulation, given as single oral dose with 240 mL of still mineral water under fasting condition.
Drug: Tapentadol Test Product 1
Experimental
Tapentadol Test Product 2 (fasting)
Tapentadol new tablet formulation, given as single oral dose with 240 mL of still mineral water under fasting condition.
Drug: Tapentadol Test Product 2
Experimental
Tapentadol Test Product 1 (fed)
Tapentadol new tablet formulation, given as single oral dose with 240 mL of still mineral water under fed condition.
Drug: Tapentadol Test Product 1
Experimental
Tapentadol Test Product 2 (fed)
Tapentadol new tablet formulation, given as single oral dose with 240 mL of still mineral water under fed condition.
Drug: Tapentadol Test Product 2
Active comparator
Tapentadol PR Reference Product
Tapentadol PR tablet formulation given as single oral dose with 240 mL of still mineral water under fasting condition.
Drug: Tapentadol Prolonged-release Reference Product

Interventions

DrugTapentadol Test Product 1
Tapentadol tablet containing 116 mg of tapentadol hydrochloride; Tapentadol Test Product 1 contains different amounts of excipients than Tapentadol Test Product 2
DrugTapentadol Test Product 2
Tapentadol tablet containing 116 mg of tapentadol hydrochloride; Tapentadol Test Product 2 contains different amounts of excipients than Tapentadol Test Product 1
DrugTapentadol Prolonged-release Reference Product
Tapentadol PR tablet containing 116 mg of tapentadol hydrochloride

What researchers measure

Primary outcomes

Pharmacokinetic parameter: Cmax
19 Blood samples were collected from pre-dose up to 32 hours post-dose. The evaluation of the maximum observed serum concentration (Cmax) was based on the tapentadol base concentrations measured in serum samples using a validated liquid chromatography/tandem mass spectrometry (LC-MS/MS) method.
Time frame: Pre-dose up to 32 hours post-dose
Pharmacokinetic parameter: AUC0-t
19 Blood samples were collected from pre-dose up to 32 hours post-dose. The evaluation of the area under the concentration time curve (AUC) from 0 hours to time t (=32 hours) (AUC0-t) was based on the tapentadol base concentrations measured in serum samples.
Time frame: Pre-dose up to 32 hours post-dose
Pharmacokinetic parameter: AUC0-inf
19 Blood samples were collected from pre-dose up to 32 hours post-dose. 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 32 hours post-dose
Pharmacokinetic parameter: tmax
19 Blood samples were collected from pre-dose up to 32 hours post-dose. The evaluation of the time to reach Cmax (tmax) was determined based on the tapentadol base concentrations measured in serum samples.
Time frame: Pre-dose up to 32 hours post-dose

Secondary outcomes

Pharmacokinetic parameter: MRT
19 Blood samples were collected from pre-dose up to 32 hours post-dose. The evaluation of the mean residence time (MRT) was based on the tapentadol base concentrations measured in serum samples using a validated LC-MS/MS method.
Time frame: Pre-dose up to 32 hours post-dose
Pharmacokinetic parameter: CL/f
19 Blood samples were collected from pre-dose up to 32 hours post-dose. The evaluation of the apparent total clearance from serum after oral administration (CL/f) of tapentadol base was calculated based on available dose and AUC data.
Time frame: Pre-dose up to 32 hours post-dose
Pharmacokinetic parameter: Vz/f
19 Blood samples were collected from pre-dose up to 32 hours post-dose. The evaluation of the apparent volume of distribution during the terminal disposition phase (Vz/f) was calculated based on CL/f and terminal elimination rate constant lambda z.
Time frame: Pre-dose up to 32 hours post-dose
Pharmacokinetic parameter: tlag
19 Blood samples were collected from pre-dose up to 32 hours post-dose. The evaluation of the lag time (tlag) was based on the tapentadol base concentrations measured in serum samples. Tlag was taken as the time point prior to that of the first quantifiable serum concentration.
Time frame: Pre-dose up to 32 hours post-dose
Pharmacokinetic parameter: t1/2z
19 Blood samples were collected from pre-dose up to 32 hours post-dose. The evaluation of the apparent terminal half life (t1/2z) was based on the tapentadol base concentrations measured in serum samples.
Time frame: Pre-dose up to 32 hours post-dose

Study locations

1 site

Department of Clinical Pharmacology, Grünenthal GmbH
Aachen, 52099, Germany

References and documents

Individual participant data

Plan to share: No

No publications or documents are linked to this record.

Updates

Tracking since Sep 25, 2026

No changes since tracking began. The registry record was last updated on May 20, 2019, before this site started recording changes on Sep 25, 2026. Its history is on ClinicalTrials.gov ↗

Registry details

Key details

Study ID: NCT03956134
Lead sponsor: Grünenthal GmbH
Responsible party: Sponsor
First posted: May 20, 2019
Start date: Apr 2005
Primary completion: Jun 2005
Completion: Jun 2005
Last update: May 20, 2019

Study contacts

Grünenthal Study Director

study director · Grünenthal GmbH

Oversight

Data monitoring committee: No
FDA-regulated drug: No
FDA-regulated device: No

View the source record on ClinicalTrials.gov ↗

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