PharmacokineticsPhase 1NCT03956134
Pharmacokinetic Characterization of Two Novel CG5503 Tablet Formulations in Healthy Volunteers
A Phase 1 study testing Tapentadol Test Product 1, Tapentadol Test Product 2 and Tapentadol Prolonged-release Reference Product in people with Pharmacokinetics, run by Grünenthal GmbH at 1 site in Germany.
Trial 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 more about this study
- Who is it for?
- Ages 18 to 55 years, men onlyHealthy volunteers can take part
- Conditions the study is for
- Pharmacokinetics
- What is being tested?
- Tapentadol Test Product 1, Tapentadol Test Product 2 and Tapentadol Prolonged-release Reference Product
- Type of treatment
- Pill or oral medicine
- Could I receive a placebo?
- No, everyone receives an active treatment
- How many people
- 10 participants
- Where
- 1 siteGermany
- Study dates
- Apr 2005to Jun 2005
- Phase
- Phase 1
- Are there results?
- None posted in the registry
Key requirements
Who can take part, as listed by the sponsor. Only the study team can confirm whether you are eligible, so take this list to your doctor.
- Ages 18 to 55 years
- Men only
- Healthy volunteers accepted
- Adult
Who may be able to join
- 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.
Who cannot join
- 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;
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- 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.
Trial locations and contacts
1 site in 1 country.
Germany1 site
Department of Clinical Pharmacology, Grünenthal GmbH
Aachen, 52099
About this study
Official title: Investigation of the Pharmacokinetic Characteristics of Two New CG5503 Formulations as Compared to CG5503 PR Tablets and Exploration of the Effect of Food on the Bioavailability of the Two New CG5503 Formulations Following Single Oral Administration of 116 mg CG5503 in a Single Center, Open, Randomized, 5-way-crossover, Single Dose, Phase I Study in 10 Healthy Male Subjects
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
- Pharmacokinetics
- Being tested
- Tapentadol Test Product 1, Tapentadol Test Product 2, Tapentadol Prolonged-release Reference Product
What participants receive
What participants receive. In a randomised study each person is assigned to one group by chance.
Tapentadol Test Product 1Drug
Tapentadol tablet containing 116 mg of tapentadol hydrochloride; Tapentadol Test Product 1 contains different amounts of excipients than Tapentadol Test Product 2
Tapentadol Test Product 2Drug
Tapentadol tablet containing 116 mg of tapentadol hydrochloride; Tapentadol Test Product 2 contains different amounts of excipients than Tapentadol Test Product 1
Tapentadol Prolonged-release Reference ProductDrug
Tapentadol PR tablet containing 116 mg of tapentadol hydrochloride
| Study group | Role | What they receive |
|---|---|---|
| Tapentadol Test Product 1 (fasting) | Experimental | Tapentadol new tablet formulation, given as single oral dose with 240 mL of still mineral water under fasting condition. Receives: Drug: Tapentadol Test Product 1 |
| Tapentadol Test Product 2 (fasting) | Experimental | Tapentadol new tablet formulation, given as single oral dose with 240 mL of still mineral water under fasting condition. Receives: Drug: Tapentadol Test Product 2 |
| Tapentadol Test Product 1 (fed) | Experimental | Tapentadol new tablet formulation, given as single oral dose with 240 mL of still mineral water under fed condition. Receives: Drug: Tapentadol Test Product 1 |
| Tapentadol Test Product 2 (fed) | Experimental | Tapentadol new tablet formulation, given as single oral dose with 240 mL of still mineral water under fed condition. Receives: Drug: Tapentadol Test Product 2 |
| Tapentadol PR Reference Product | Active comparator | Tapentadol PR tablet formulation given as single oral dose with 240 mL of still mineral water under fasting condition. Receives: Drug: Tapentadol Prolonged-release Reference Product |
What is being measured
The primary outcome is the main question the study is designed to answer.
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.
Measured: 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.
Measured: 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.
Measured: 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.
Measured: Pre-dose up to 32 hours post-dose
Secondary outcomes (5)
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.
Measured: 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.
Measured: 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.
Measured: 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.
Measured: 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.
Measured: Pre-dose up to 32 hours post-dose
Timeline
From the start of the study to its completion; the mark is today. Estimated dates are the sponsor’s plan.
- First posted20 May 2019
- Study startApr 2005
- Primary completionJun 2005
- Study completionJun 2005
Resources
- Official record on ClinicalTrials.govThe registry entry this page is built from, with its full change history.
- Other trials for PharmacokineticsStudies of the same condition, open and under way.
- What the trial phases meanHow a treatment moves from first tests in people to approval.
More details
For doctors and researchers: how the study is designed, who runs it, and its registry IDs.
Study design
- Study type
- Interventional
- Phase
- Phase 1
- Primary purpose
- Treatment
- Allocation
- Randomised
- Intervention model
- Crossover
- Model description
- Randomization was performed according to Williams' design, with 5 periods and 10 sequences. There was a washout of at least 3 days between the consecutive administrations.
- Masking
- None (open label)
- Enrolment
- 10 participants (actual)
Sponsor and investigators
- Lead sponsor
- Grünenthal GmbH
- Sponsor type
- Industry (pharma, biotech, devices)
- Responsible party
- Sponsor
- Investigators
- Grünenthal Study Director, Study director, Grünenthal GmbH
IDs, dates and publications
- ClinicalTrials.gov ID
- NCT03956134
- Sponsor's protocol ID
- HP5503/12
- Status last verified
- May 2019
- First submitted
- 14 May 2019
- Last updated
- 20 May 2019
- Results posted
- No
- Data monitoring committee
- No
- FDA-regulated drug
- No
- FDA-regulated device
- No
- Individual data sharing
- No
Study at a glance
From the registry record, last updated by the sponsor on 20 May 2019. Recruitment status is as the sponsor reported it: confirm with the study team.
- Official title
- Investigation of the Pharmacokinetic Characteristics of Two New CG5503 Formulations as Compared to CG5503 PR Tablets and Exploration of the Effect of Food on the Bioavailability of the Two New CG5503 Formulations Following Single Oral Administration of 116 mg CG5503 in a Single Center, Open, Randomized, 5-way-crossover, Single Dose, Phase I Study in 10 Healthy Male Subjects
- ClinicalTrials.gov ID
- NCT03956134
- Acronym / sponsor ID
- HP5503/12
- Conditions
- Pharmacokinetics
- Phase
- Phase 1
- Study type
- Interventional
- Recruitment status
- Completed
- Enrolment
- 10 participants (actual)
- Lead sponsor
- Grünenthal GmbHIndustry (pharma, biotech, devices)
- Study start
- Apr 2005 (actual)
- Primary completion
- Jun 2005 (actual)
- Study completion
- Jun 2005 (actual)
- First posted
- 20 May 2019 (actual)
- Results
- Not posted in the source record
Clinical summary
The research question as the sponsor registered it. This describes what the study plans to test, not what it found.
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.
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.
Study design
- Primary purpose
- Treatment
- Allocation
- Randomised
- Intervention model
- Crossover
- Masking
- None (open label)
- Number of arms
- 5
- Model description
- Randomization was performed according to Williams' design, with 5 periods and 10 sequences. There was a washout of at least 3 days between the consecutive administrations.
| Arm | Type | Receives |
|---|---|---|
| Tapentadol Test Product 1 (fasting) | Experimental | Drug: Tapentadol Test Product 1Tapentadol new tablet formulation, given as single oral dose with 240 mL of still mineral water under fasting condition. |
| Tapentadol Test Product 2 (fasting) | Experimental | Drug: Tapentadol Test Product 2Tapentadol new tablet formulation, given as single oral dose with 240 mL of still mineral water under fasting condition. |
| Tapentadol Test Product 1 (fed) | Experimental | Drug: Tapentadol Test Product 1Tapentadol new tablet formulation, given as single oral dose with 240 mL of still mineral water under fed condition. |
| Tapentadol Test Product 2 (fed) | Experimental | Drug: Tapentadol Test Product 2Tapentadol new tablet formulation, given as single oral dose with 240 mL of still mineral water under fed condition. |
| Tapentadol PR Reference Product | Active comparator | Drug: Tapentadol Prolonged-release Reference ProductTapentadol PR tablet formulation given as single oral dose with 240 mL of still mineral water under fasting condition. |
Who may qualify
- Ages
- 18 to 55 years
- Sex
- Male only
- Healthy volunteers
- Accepted
- Age groups
- Adult
Key inclusion criteria (4 listed)
- 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.
Key exclusion criteria (20 listed)
- 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);
Eligibility is decided by the study team after screening; this overview does not establish that a patient qualifies. Full inclusion and exclusion criteria.
Interventions
| Intervention | Type | Arms |
|---|---|---|
| Tapentadol Test Product 1Tapentadol tablet containing 116 mg of tapentadol hydrochloride; Tapentadol Test Product 1 contains different amounts of excipients than Tapentadol Test Product 2 | Drug | Tapentadol Test Product 1 (fasting), Tapentadol Test Product 1 (fed) |
| Tapentadol Test Product 2Tapentadol tablet containing 116 mg of tapentadol hydrochloride; Tapentadol Test Product 2 contains different amounts of excipients than Tapentadol Test Product 1 | Drug | Tapentadol Test Product 2 (fasting), Tapentadol Test Product 2 (fed) |
| Tapentadol Prolonged-release Reference ProductTapentadol PR tablet containing 116 mg of tapentadol hydrochloride | Drug | Tapentadol PR Reference Product |
Primary outcome
Pharmacokinetic parameter: Cmax
Time frame: Pre-dose up to 32 hours post-dose
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.
Pharmacokinetic parameter: AUC0-t
Time frame: Pre-dose up to 32 hours post-dose
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.
Pharmacokinetic parameter: AUC0-inf
Time frame: Pre-dose up to 32 hours post-dose
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.
Pharmacokinetic parameter: tmax
Time frame: Pre-dose up to 32 hours post-dose
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.
5 secondary outcomes
Pharmacokinetic parameter: MRT
Time frame: Pre-dose up to 32 hours post-dose
Pharmacokinetic parameter: CL/f
Time frame: Pre-dose up to 32 hours post-dose
Pharmacokinetic parameter: Vz/f
Time frame: Pre-dose up to 32 hours post-dose
Pharmacokinetic parameter: tlag
Time frame: Pre-dose up to 32 hours post-dose
Pharmacokinetic parameter: t1/2z
Time frame: Pre-dose up to 32 hours post-dose
Results and safety
The study is completed, but results are not available in the source record. That does not mean the treatment did or did not work.
Research links
- Official record on ClinicalTrials.govLast updated by the sponsor 20 May 2019.
- Individual participant dataSharing planned: No
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Referral and contact
AzTrials does not enrol participants or take referrals. Contact the study team or a site listed below; they decide who can take part. This study is not recruiting at the moment.
Grünenthal Study Director study director
Grünenthal GmbH
1 site in 1 country: see every site and its status.
Questions about this trial
What is this clinical trial studying?
A Phase 1 study testing Tapentadol Test Product 1, Tapentadol Test Product 2 and Tapentadol Prolonged-release Reference Product in people with Pharmacokinetics, run by Grünenthal GmbH at 1 site in Germany.
The full registered description is in the About this study section and the official record.
Who may be eligible to take part?
The sponsor lists 4 inclusion and 20 exclusion criteria. Eligibility is decided by the study team after screening, so read the full criteria and contact a listed site.
Is this clinical trial currently recruiting?
The record says: finished, as of the sponsor's last update on 20 May 2019. Status can change between updates, so confirm with the study contact before making plans.
Where is the study taking place?
The record lists 1 site in Germany. Whether a site is taking part right now should be confirmed with that site. See every site.
What are the possible benefits and risks?
They depend on the study and the treatment, and no study can promise a benefit. The study team explains the known risks during informed consent, before anyone joins; the record itself does not list them.
What does this phase mean?
Phase 1 studies test a treatment in a small group of people for the first time or in a new way, mainly to check safety and find the right dose.
Not every study follows the same path, and some studies (observational studies, device studies) have no phase.
Are results available for this study?
The study is completed, but results are not available in the source record. That does not mean the treatment did or did not work.
How can a doctor refer a patient or contact the research team?
The record lists no contact. The official record names the sponsor, who can be asked directly. AzTrials does not enrol participants or take referrals.
What does the primary outcome measure?
Pharmacokinetic parameter: Cmax (time frame: Pre-dose up to 32 hours post-dose). The study lists 4 primary outcomes in all. It is what the study was designed to measure, not a finding.
Where can I read the original study information?
Does a listing mean the treatment is approved or proven to work?
No. A listing means the study is registered. It does not show that the treatment is safe, works, or is approved by a regulator.
How often is this information updated?
AzTrials copies changed records from ClinicalTrials.gov every night and reloads the whole registry every week. The sponsor last updated this record on 20 May 2019.