PharmacokineticPhase 1NCT03951987
Investigation How CG5503 is Taken up and Excreted From the Body After 2 Minutes Intravenous Infusion With and Without Oral Co-administration of Charcoal
A Phase 1 study testing 4 ml CG5503 and 5 g charcoal powder in people with Pharmacokinetic, run by Grünenthal GmbH at 1 site in Germany.
Trial summary
This was a Phase I study in 12 healthy male participants to compare the pharmacokinetic properties of CG5503 (how it is taken up and excreted from the body) after 2 minutes intravenous (i.v.) infusion with and without oral co-administration of charcoal to investigate a potential gastrointestinal secretion of CG5503. Read more about this study
- Who is it for?
- Ages 18 to 65 years, men onlyHealthy volunteers can take part
- Conditions the study is for
- Pharmacokinetic
- What is being tested?
- 4 ml CG5503 and 5 g charcoal powder
- Type of treatment
- Pill or oral medicine, Injection or infusion
- Could I receive a placebo?
- No, everyone receives an active treatment
- How many people
- 14 participants
- Where
- 1 siteGermany
- Study dates
- Feb 2004to Apr 2004
- 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 65 years
- Men only
- Healthy volunteers accepted
- Adult, Older adult
Who may be able to join
- Male Caucasian participants aged 18 - 65 years.
- Body mass index (BMI) between 20 and 30 kilograms/square meter inclusive.
- Participants must be in good health as determined by medical history, physical examination, 12-lead electrocardiogram, vital signs, and clinical laboratory parameters (serum/urine biochemistry, serology and haematology). Minor deviations of laboratory values from the normal range may be accepted, if judged by the investigator to have no clinical relevance and if not considered to interfere with the study objectives.
- Negative human immunodeficiency virus (HIV)-1/-2 antibodies, hepatitis B surface (HBs)-antigen, hepatitis B core (HBc)-antibodies, hepatitis C virus (HCV)-antibodies at the screening examination.
- Participants giving written consent to participate within this trial.
Who cannot join
- Use of any medication within four weeks prior to commencement of the study (self-medication or prescription), if not on a stable basis.
- Diseases and functional disorders of the gastrointestinal tract, liver, cardiovascular system or kidneys.
- Malignancy.
- History of orthostatic hypotension.
- Resting pulse rate equal to or below 45 beats/min or equal to or above 100 beats/min.
- Systolic blood pressure equal to or below 100 mmHg or equal to or above 160 mmHg.
Show all 21Show fewer
- Diastolic blood pressure equal to or below 50 mmHg or equal to or above 95 mmHg.
- Clinically relevant deviations in laboratory parameters.
- Drug allergy.
- Bronchial asthma.
- Participation in another clinical study in the last three months before starting this study (exception: characterization of metabolizer status).
- Blood donation (more than 100 milliliter) in the last three months before the start of the study.
- Evidence of alcohol or drug abuse.
- Positive drug abuse screening test.
- Extremely unbalanced diet (in the opinion of the investigator).
- Excessive consumption of food or beverages containing caffeine (more than five cups of coffee per day or other equivalent amounts of caffeine).
- Consumption of grapefruit juice two weeks before the start of the study.
- Known or suspected of not being able to comply with the study protocol.
- Not able to communicate meaningfully with the investigator and staff.
- Neurotic personality, psychiatric illness, or suicide risk.
- History of seizures or at risk (i.e. head trauma, epilepsy in family anamnesis, unclear loss of consciousness).
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 Properties of CG5503 After 2 Minutes Intravenous Infusion With and Without Oral Coadministration of Charcoal in a Randomised, Open, Single Dose, 2-way Crossover, Phase I Study in 12 Healthy Male Volunteers
This was a Phase I study in 12 healthy male participants to compare the pharmacokinetic properties of CG5503 (how it is taken up and excreted from the body) after 2 minutes intravenous (i.v.) infusion with and without oral co-administration of charcoal to investigate a potential gastrointestinal secretion of CG5503.
During the course of the study each participant received two infusions of 40 mg CG5503 without (treatment A) and with (treatment B) oral co-administration of charcoal. In treatment B, eight doses of 5 grams charcoal powder were co-administered orally at defined time points. The wash out phases were to be at least 4 to 14 days between the treatment periods.
- Conditions
- Pharmacokinetic
- Being tested
- 4 ml CG5503, 5 g charcoal powder
What participants receive
What participants receive. In a randomised study each person is assigned to one group by chance.
4 ml CG5503Drug
4 ml of the CG5503 infusion solution corresponding to 40 mg CG5503 (tapentadol hydrochloride).
5 g charcoal powderDrug
Also called Tradename: Kohle-Pulvis Pulver
Oral administration of 5 g charcoal powder suspended in 100 ml tap water.
| Study group | Role | What they receive |
|---|---|---|
| Treatment A: 4 ml CG5503 | Experimental | 4 ml of the CG5503 i.v. infusion solution corresponding to 40 mg CG5503 (tapentadol hydrochloride) was administered as a 2 minutes infusion. Receives: Drug: 4 ml CG5503 |
| Treatment B: 4 ml CG5503; 5 g charcoal powder | Experimental | 4 ml of the CG5503 i.v. infusion solution corresponding to 40 mg CG5503 (tapentadol hydrochloride) with oral co-administration of charcoal (5 g charcoal were co-administered orally at 1, 0.5 hours and 10 minutes before the start of CG5503 infusion and 0.5, 1, 1.5, 2 and 4 hours thereafter) Receives: Drug: 4 ml CG5503; Drug: 5 g charcoal powder |
What is being measured
The primary outcome is the main question the study is designed to answer.
Pharmacokinetic parameter Serum: area under the concentration-time curve extrapolated to infinity (AUC0-inf) for CG5503 base
26 PK blood samples were obtained from each participant. Serum concentrations were determined using validated high-performance liquid chromatography-tandem mass spectrometry bioanalytical assays. The AUC0-inf was calculated based on serum concentration-time data (using the actual blood sampling times).
Measured: Pre-dose and up to 23 hours post-dose
Pharmacokinetic parameter Saliva: area under the concentration-time curve extrapolated to infinity (AUC0-inf) for CG5503 base
16 PK saliva samples were obtained from each participant. Saliva concentrations were determined using validated high-performance liquid chromatography-tandem mass spectrometry bioanalytical assays. Participants were asked to donate saliva as much as possible in approximately 0.5 minutes. The AUC0-inf was calculated based on saliva concentration-time data (using the actual saliva sampling time intervals).
Measured: Pre-dose and up to 23 hours post-dose
Pharmacokinetic parameter Serum: area under the concentration-time curve extrapolated to infinity (AUC0-inf) for CG5503-glucuronide
26 PK blood samples were obtained from each participant. Serum concentrations were determined using validated high-performance liquid chromatography-tandem mass spectrometry bioanalytical assays. The AUC0-inf was calculated based on serum concentration-time data (using the actual blood sampling times).
Measured: Pre-dose and up to 23 hours post-dose
Pharmacokinetic parameter Serum: area under the concentration-time curve extrapolated to infinity (AUC0-inf) for CG5503-sulphate
26 PK blood samples were obtained from each participant. Serum concentrations were determined using validated high-performance liquid chromatography-tandem mass spectrometry bioanalytical assays. The AUC0-inf was calculated based on serum concentration-time data (using the actual blood sampling times).
Measured: Pre-dose and up to 23 hours post-dose
Pharmacokinetic parameter Serum: area under the concentration-time curve from 0 to time t (AUC0-t) for CG5503 base
26 PK blood samples were obtained from each participant. Serum concentrations were determined using validated high-performance liquid chromatography-tandem mass spectrometry bioanalytical assays. The AUC0-t was calculated based on serum concentration-time data (using the actual blood sampling times).
Measured: Pre-dose and up to 23 hours post-dose
Pharmacokinetic parameter Saliva: area under the concentration-time curve from 0 to time t (AUC0-t) for CG5503 base
16 PK saliva samples were obtained from each participant. Saliva concentrations were determined using validated high-performance liquid chromatography-tandem mass spectrometry bioanalytical assays. Participants were asked to donate saliva as much as possible in approximately 0.5 minutes. The AUC0-t was calculated based on saliva concentration-time data (using the actual saliva sampling time intervals).
Measured: Pre-dose and up to 23 hours post-dose
Pharmacokinetic parameter Serum: area under the concentration-time curve from 0 to time t (AUC0-t) for CG5503-glucuronide
26 PK blood samples were obtained from each participant. Serum concentrations were determined using validated high-performance liquid chromatography-tandem mass spectrometry bioanalytical assays. The AUC0-t was calculated based on serum concentration-time data (using the actual blood sampling times).
Measured: Pre-dose and up to 23 hours post-dose
Pharmacokinetic parameter Serum: area under the concentration-time curve from 0 to time t (AUC0-t) for CG5503-sulphate
26 PK blood samples were obtained from each participant. Serum concentrations were determined using validated high-performance liquid chromatography-tandem mass spectrometry bioanalytical assays. The AUC0-t was calculated based on serum concentration-time data (using the actual blood sampling times).
Measured: Pre-dose and up to 23 hours post-dose
Pharmacokinetic parameter Serum: maximum concentration (Cmax) for CG5503 base
26 PK blood samples were obtained from each participant. Serum concentrations were determined using validated high-performance liquid chromatography-tandem mass spectrometry bioanalytical assays. The Cmax was calculated based on serum concentration-time data (using the actual blood sampling times).
Measured: Pre-dose and up to 23 hours post-dose
Pharmacokinetic parameter Saliva: maximum concentration (Cmax) for CG5503 base
16 PK saliva samples were obtained from each participant. Saliva concentrations were determined using validated high-performance liquid chromatography-tandem mass spectrometry bioanalytical assays. Participants were asked to donate saliva as much as possible in approximately 0.5 minutes. tubes. The Cmax was calculated based on saliva concentration-time data (using the actual saliva sampling time intervals).
Measured: Pre-dose and up to 23 hours post-dose
Pharmacokinetic parameter Serum: maximum concentration (Cmax) for CG5503-glucuronide
26 PK blood samples were obtained from each participant. Serum concentrations were determined using validated high-performance liquid chromatography-tandem mass spectrometry bioanalytical assays. The Cmax was calculated based on serum concentration-time data (using the actual blood sampling times).
Measured: Pre-dose and up to 23 hours post-dose
Pharmacokinetic parameter Serum: maximum concentration (Cmax) for CG5503-sulphate
26 PK blood samples were obtained from each participant. Serum concentrations were determined using validated high-performance liquid chromatography-tandem mass spectrometry bioanalytical assays. The Cmax was calculated based on serum concentration-time data (using the actual blood sampling times).
Measured: Pre-dose and up to 23 hours post-dose
Pharmacokinetic parameter Serum: time to maximum concentration (tmax) for CG5503 base
26 PK blood samples were obtained from each participant. Serum concentrations were determined using validated high-performance liquid chromatography-tandem mass spectrometry bioanalytical assays. The tmax was calculated based on serum concentration-time data (using the actual blood sampling times).
Measured: Pre-dose and up to 23 hours post-dose
Pharmacokinetic parameter Saliva: time to maximum concentration (tmax) for CG5503 base
16 PK saliva samples were obtained from each participant. Saliva concentrations were determined using validated high-performance liquid chromatography-tandem mass spectrometry bioanalytical assays. Participants were asked to donate saliva as much as possible in approximately 0.5 minutes. The tmax was calculated based on saliva concentration-time data (using the actual saliva sampling time intervals).
Measured: Pre-dose and up to 23 hours post-dose
Pharmacokinetic parameter Serum: time to maximum concentration (tmax) for CG5503-glucuronide
26 PK blood samples were obtained from each participant. Serum concentrations were determined using validated high-performance liquid chromatography-tandem mass spectrometry bioanalytical assays. The tmax was calculated based on serum concentration-time data (using the actual blood sampling times).
Measured: Pre-dose and up to 23 hours post-dose
Pharmacokinetic parameter Serum: time to maximum concentration (tmax) for CG5503-sulphate
26 PK blood samples were obtained from each participant. Serum concentrations were determined using validated high-performance liquid chromatography-tandem mass spectrometry bioanalytical assays. The tmax was calculated based on serum concentration-time data (using the actual blood sampling times).
Measured: Pre-dose and up to 23 hours post-dose
Secondary outcomes (23)
Pharmacokinetic parameter Serum: extrapolated AUC expressed as a percentage of total AUC0-inf (AUC%extr) for CG5503 base
26 PK blood samples were obtained from each participant. Serum concentrations were determined using validated high-performance liquid chromatography-tandem mass spectrometry bioanalytical assays. The AUC%extr was calculated based on serum concentration-time data (using the actual blood sampling times).
Measured: Pre-dose and up to 23 hours post-dose
Pharmacokinetic parameter Saliva: extrapolated AUC expressed as a percentage of total AUC0-inf (AUC%extr) for CG5503 base
16 PK saliva samples were obtained from each participant. Saliva concentrations were determined using validated high-performance liquid chromatography-tandem mass spectrometry bioanalytical assays. Participants were asked to donate saliva as much as possible in approximately 0.5 minutes. The AUC%extr was calculated based on saliva concentration-time data (using the actual saliva sampling time intervals).
Measured: Pre-dose and up to 23 hours post-dose
Pharmacokinetic parameter Serum: extrapolated AUC expressed as a percentage of total AUC0-inf (AUC%extr) for CG5503-glucuronide
26 PK blood samples were obtained from each participant. Serum concentrations were determined using validated high-performance liquid chromatography-tandem mass spectrometry bioanalytical assays. The AUC%extr was calculated based on serum concentration-time data (using the actual blood sampling times).
Measured: Pre-dose and up to 23 hours post-dose
Pharmacokinetic parameter Serum: extrapolated AUC expressed as a percentage of total AUC0-inf (AUC%extr) for CG5503-sulphate
26 PK blood samples were obtained from each participant. Serum concentrations were determined using validated high-performance liquid chromatography-tandem mass spectrometry bioanalytical assays. The AUC%extr was calculated based on serum concentration-time data (using the actual blood sampling times).
Measured: Pre-dose and up to 23 hours post-dose
Pharmacokinetic parameter Serum: apparent terminal elimination rate constant (λz) for CG5503 base
26 PK blood samples were obtained from each participant. Serum concentrations were determined using validated high-performance liquid chromatography-tandem mass spectrometry bioanalytical assays. The λz was calculated based on serum concentration-time data (using the actual blood sampling times).
Measured: Pre-dose and up to 23 hours post-dose
Pharmacokinetic parameter Saliva: apparent terminal elimination rate constant (λz) for CG5503 base
16 PK saliva samples were obtained from each participant. Saliva concentrations were determined using validated high-performance liquid chromatography-tandem mass spectrometry bioanalytical assays. Participants were asked to donate saliva as much as possible in approximately 0.5 minutes. The λz was calculated based on saliva concentration-time data (using the actual saliva sampling time intervals).
Measured: Pre-dose and up to 23 hours post-dose
Pharmacokinetic parameter Serum: apparent terminal elimination rate constant (λz) for CG5503-glucuronide
26 PK blood samples were obtained from each participant. Serum concentrations were determined using validated high-performance liquid chromatography-tandem mass spectrometry bioanalytical assays. The λz was calculated based on serum concentration-time data (using the actual blood sampling times).
Measured: Pre-dose and up to 23 hours post-dose
Pharmacokinetic parameter Serum: apparent terminal elimination rate constant (λz) for CG5503-sulphate
26 PK blood samples were obtained from each participant. Serum concentrations were determined using validated high-performance liquid chromatography-tandem mass spectrometry bioanalytical assays. The λz was calculated based on serum concentration-time data (using the actual blood sampling times).
Measured: Pre-dose and up to 23 hours post-dose
Pharmacokinetic parameter Serum: the apparent half-life associated with the terminal elimination phase (t1/2,z) for CG5503 base
26 PK blood samples were obtained from each participant. Serum concentrations were determined using validated high-performance liquid chromatography-tandem mass spectrometry bioanalytical assays. The t½z was calculated based on serum concentration-time data (using the actual blood sampling times).
Measured: Pre-dose and up to 23 hours post-dose
Pharmacokinetic parameter Saliva: the apparent half-life associated with the terminal elimination phase (t1/2,z) for CG5503 base
16 PK saliva samples were obtained from each participant. Saliva concentrations were determined using validated high-performance liquid chromatography-tandem mass spectrometry bioanalytical assays. Participants were asked to donate saliva as much as possible in approximately 0.5 minutes. The t½z was calculated based on saliva concentration-time data (using the actual saliva sampling time intervals).
Measured: Pre-dose and up to 23 hours post-dose
Pharmacokinetic parameter Serum: the apparent half-life associated with the terminal elimination phase (t1/2,z) for CG5503-glucuronide
26 PK blood samples were obtained from each participant. Serum concentrations were determined using validated high-performance liquid chromatography-tandem mass spectrometry bioanalytical assays. The t½z was calculated based on serum concentration-time data (using the actual blood sampling times).
Measured: Pre-dose and up to 23 hours post-dose
Pharmacokinetic parameter Serum: the apparent half-life associated with the terminal elimination phase (t1/2,z) for CG5503-sulphate
26 PK blood samples were obtained from each participant. Serum concentrations were determined using validated high-performance liquid chromatography-tandem mass spectrometry bioanalytical assays. The t½z was calculated based on serum concentration-time data (using the actual blood sampling times).
Measured: Pre-dose and up to 23 hours post-dose
Pharmacokinetic parameter Serum: total serum or blood clearance of drug after intravenous administration (CL) for CG5503 base
26 PK blood samples were obtained from each participant. Serum concentrations were determined using validated high-performance liquid chromatography-tandem mass spectrometry bioanalytical assays. The CL was calculated based on serum concentration-time data (using the actual blood sampling times).
Measured: Pre-dose and up to 23 hours post-dose
Pharmacokinetic parameter Saliva: total clearance of drug after intravenous administration (CL) for CG5503 base
16 PK saliva samples were obtained from each participant. Saliva concentrations were determined using validated high-performance liquid chromatography-tandem mass spectrometry bioanalytical assays. Participants were asked to donate saliva as much as possible in approximately 0.5 minutes. The CL was calculated based on saliva concentration-time data (using the actual saliva sampling time intervals).
Measured: Pre-dose and up to 23 hours post-dose
Pharmacokinetic parameter Serum: total serum or blood clearance of drug after intravenous administration (CL) for CG5503-glucuronide
26 PK blood samples were obtained from each participant. Serum concentrations were determined using validated high-performance liquid chromatography-tandem mass spectrometry bioanalytical assays. The CL was calculated based on serum concentration-time data (using the actual blood sampling times).
Measured: Pre-dose and up to 23 hours post-dose
Pharmacokinetic parameter Serum: total serum or blood clearance of drug after intravenous administration (CL) for CG5503-sulphate
26 PK blood samples were obtained from each participant. Serum concentrations were determined using validated high-performance liquid chromatography-tandem mass spectrometry bioanalytical assays. The CL was calculated based on serum concentration-time data (using the actual blood sampling times).
Measured: Pre-dose and up to 23 hours post-dose
Pharmacokinetic parameter Serum: the apparent volume of distribution associated with terminal phase after intravenous administration (Vz) for CG5503 base
26 PK blood samples were obtained from each participant. Serum concentrations were determined using validated high-performance liquid chromatography-tandem mass spectrometry bioanalytical assays. The Vz was calculated based on serum concentration-time data (using the actual blood sampling times).
Measured: Pre-dose and up to 23 hours post-dose
Pharmacokinetic parameter Saliva: the apparent volume of distribution associated with terminal phase after intravenous administration (Vz) for CG5503 base
16 PK saliva samples were obtained from each participant. Saliva concentrations were determined using validated high-performance liquid chromatography-tandem mass spectrometry bioanalytical assays. Participants were asked to donate saliva as much as possible in approximately 0.5 minutes. The Vz was calculated based on saliva concentration-time data (using the actual saliva sampling time intervals).
Measured: Pre-dose and up to 23 hours post-dose
Pharmacokinetic parameter Serum: the apparent volume of distribution associated with terminal phase after intravenous administration (Vz) for CG5503-glucuronide
26 PK blood samples were obtained from each participant. Serum concentrations were determined using validated high-performance liquid chromatography-tandem mass spectrometry bioanalytical assays. The Vz was calculated based on serum concentration-time data (using the actual blood sampling times).
Measured: Pre-dose and up to 23 hours post-dose
Pharmacokinetic parameter Serum: the apparent volume of distribution associated with terminal phase after intravenous administration (Vz) for CG5503-sulphate
26 PK blood samples were obtained from each participant. Serum concentrations were determined using validated high-performance liquid chromatography-tandem mass spectrometry bioanalytical assays. The Vz was calculated based on serum concentration-time data (using the actual blood sampling times).
Measured: Pre-dose and up to 23 hours post-dose
Pharmacokinetic parameter Urine: renal excretion (Ae % of dose) for CG5503 base
12 PK urine samples were obtained from each participant. Urine concentrations were determined using validated high-performance liquid chromatography-tandem mass spectrometry bioanalytical assays. The Ae (% of dose) was calculated based on urine concentration-time data (using the actual urine sampling time intervals).
Measured: Pre-dose and up to 23 hours post-dose
Pharmacokinetic parameter Urine: renal excretion (Ae % of dose) for CG5503-glucuronide
12 PK urine samples were obtained from each participant. Urine concentrations were determined using validated high-performance liquid chromatography-tandem mass spectrometry bioanalytical assays. The Ae (% of dose) was calculated based on urine concentration-time data (using the actual urine sampling time intervals).
Measured: Pre-dose and up to 23 hours post-dose
Pharmacokinetic parameter Urine: renal excretion (Ae % of dose) for CG5503-sulphate
12 PK urine samples were obtained from each participant. Urine concentrations were determined using validated high-performance liquid chromatography-tandem mass spectrometry bioanalytical assays. The Ae (% of dose) was calculated based on urine concentration-time data (using the actual urine sampling time intervals).
Measured: Pre-dose and up to 23 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 posted16 May 2019
- Study startFeb 2004
- Primary completionApr 2004
- Study completionApr 2004
Resources
- Official record on ClinicalTrials.govThe registry entry this page is built from, with its full change history.
- Other trials for PharmacokineticStudies 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
- The randomization was in the ratio 1:1.
- Masking
- None (open label)
- Enrolment
- 14 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
- NCT03951987
- Sponsor's protocol ID
- HP5503/11
- Status last verified
- May 2019
- First submitted
- 14 May 2019
- Last updated
- 16 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 16 May 2019. Recruitment status is as the sponsor reported it: confirm with the study team.
- Official title
- Investigation of the Pharmacokinetic Properties of CG5503 After 2 Minutes Intravenous Infusion With and Without Oral Coadministration of Charcoal in a Randomised, Open, Single Dose, 2-way Crossover, Phase I Study in 12 Healthy Male Volunteers
- ClinicalTrials.gov ID
- NCT03951987
- Acronym / sponsor ID
- HP5503/11
- Conditions
- Pharmacokinetic
- Phase
- Phase 1
- Study type
- Interventional
- Recruitment status
- Completed
- Enrolment
- 14 participants (actual)
- Lead sponsor
- Grünenthal GmbHIndustry (pharma, biotech, devices)
- Study start
- Feb 2004 (actual)
- Primary completion
- Apr 2004 (actual)
- Study completion
- Apr 2004 (actual)
- First posted
- 16 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 was a Phase I study in 12 healthy male participants to compare the pharmacokinetic properties of CG5503 (how it is taken up and excreted from the body) after 2 minutes intravenous (i.v.) infusion with and without oral co-administration of charcoal to investigate a potential gastrointestinal secretion of CG5503.
During the course of the study each participant received two infusions of 40 mg CG5503 without (treatment A) and with (treatment B) oral co-administration of charcoal. In treatment B, eight doses of 5 grams charcoal powder were co-administered orally at defined time points. The wash out phases were to be at least 4 to 14 days between the treatment periods.
Study design
- Primary purpose
- Treatment
- Allocation
- Randomised
- Intervention model
- Crossover
- Masking
- None (open label)
- Number of arms
- 2
- Model description
- The randomization was in the ratio 1:1.
| Arm | Type | Receives |
|---|---|---|
| Treatment A: 4 ml CG5503 | Experimental | Drug: 4 ml CG55034 ml of the CG5503 i.v. infusion solution corresponding to 40 mg CG5503 (tapentadol hydrochloride) was administered as a 2 minutes infusion. |
| Treatment B: 4 ml CG5503; 5 g charcoal powder | Experimental | Drug: 4 ml CG5503, Drug: 5 g charcoal powder4 ml of the CG5503 i.v. infusion solution corresponding to 40 mg CG5503 (tapentadol hydrochloride) with oral co-administration of charcoal (5 g charcoal were co-administered orally at 1, 0.5 hours and 10 minutes before the start of CG5503 infusion and 0.5, 1, 1.5, 2 and 4 hours thereafter) |
Who may qualify
- Ages
- 18 to 65 years
- Sex
- Male only
- Healthy volunteers
- Accepted
- Age groups
- Adult, Older adult
Key inclusion criteria (5 listed)
- Male Caucasian participants aged 18 - 65 years.
- Body mass index (BMI) between 20 and 30 kilograms/square meter inclusive.
- Participants must be in good health as determined by medical history, physical examination, 12-lead electrocardiogram, vital signs, and clinical laboratory parameters (serum/urine biochemistry, serology and haematology). Minor deviations of laboratory values from the normal range may be accepted, if judged by the investigator to have no clinical relevance and if not considered to interfere with the study objectives.
- Negative human immunodeficiency virus (HIV)-1/-2 antibodies, hepatitis B surface (HBs)-antigen, hepatitis B core (HBc)-antibodies, hepatitis C virus (HCV)-antibodies at the screening examination.
- Participants giving written consent to participate within this trial.
Key exclusion criteria (21 listed)
- Use of any medication within four weeks prior to commencement of the study (self-medication or prescription), if not on a stable basis.
- Diseases and functional disorders of the gastrointestinal tract, liver, cardiovascular system or kidneys.
- Malignancy.
- History of orthostatic hypotension.
- Resting pulse rate equal to or below 45 beats/min or equal to or above 100 beats/min.
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 |
|---|---|---|
| 4 ml CG55034 ml of the CG5503 infusion solution corresponding to 40 mg CG5503 (tapentadol hydrochloride). | Drug | Treatment A: 4 ml CG5503, Treatment B: 4 ml CG5503; 5 g charcoal powder |
| 5 g charcoal powderAlso: Tradename: Kohle-Pulvis PulverOral administration of 5 g charcoal powder suspended in 100 ml tap water. | Drug | Treatment B: 4 ml CG5503; 5 g charcoal powder |
Primary outcome
Pharmacokinetic parameter Serum: area under the concentration-time curve extrapolated to infinity (AUC0-inf) for CG5503 base
Time frame: Pre-dose and up to 23 hours post-dose
26 PK blood samples were obtained from each participant. Serum concentrations were determined using validated high-performance liquid chromatography-tandem mass spectrometry bioanalytical assays. The AUC0-inf was calculated based on serum concentration-time data (using the actual blood sampling times).
Pharmacokinetic parameter Saliva: area under the concentration-time curve extrapolated to infinity (AUC0-inf) for CG5503 base
Time frame: Pre-dose and up to 23 hours post-dose
16 PK saliva samples were obtained from each participant. Saliva concentrations were determined using validated high-performance liquid chromatography-tandem mass spectrometry bioanalytical assays. Participants were asked to donate saliva as much as possible in approximately 0.5 minutes. The AUC0-inf was calculated based on saliva concentration-time data (using the actual saliva sampling time intervals).
Pharmacokinetic parameter Serum: area under the concentration-time curve extrapolated to infinity (AUC0-inf) for CG5503-glucuronide
Time frame: Pre-dose and up to 23 hours post-dose
26 PK blood samples were obtained from each participant. Serum concentrations were determined using validated high-performance liquid chromatography-tandem mass spectrometry bioanalytical assays. The AUC0-inf was calculated based on serum concentration-time data (using the actual blood sampling times).
Pharmacokinetic parameter Serum: area under the concentration-time curve extrapolated to infinity (AUC0-inf) for CG5503-sulphate
Time frame: Pre-dose and up to 23 hours post-dose
26 PK blood samples were obtained from each participant. Serum concentrations were determined using validated high-performance liquid chromatography-tandem mass spectrometry bioanalytical assays. The AUC0-inf was calculated based on serum concentration-time data (using the actual blood sampling times).
Pharmacokinetic parameter Serum: area under the concentration-time curve from 0 to time t (AUC0-t) for CG5503 base
Time frame: Pre-dose and up to 23 hours post-dose
26 PK blood samples were obtained from each participant. Serum concentrations were determined using validated high-performance liquid chromatography-tandem mass spectrometry bioanalytical assays. The AUC0-t was calculated based on serum concentration-time data (using the actual blood sampling times).
Pharmacokinetic parameter Saliva: area under the concentration-time curve from 0 to time t (AUC0-t) for CG5503 base
Time frame: Pre-dose and up to 23 hours post-dose
16 PK saliva samples were obtained from each participant. Saliva concentrations were determined using validated high-performance liquid chromatography-tandem mass spectrometry bioanalytical assays. Participants were asked to donate saliva as much as possible in approximately 0.5 minutes. The AUC0-t was calculated based on saliva concentration-time data (using the actual saliva sampling time intervals).
Pharmacokinetic parameter Serum: area under the concentration-time curve from 0 to time t (AUC0-t) for CG5503-glucuronide
Time frame: Pre-dose and up to 23 hours post-dose
26 PK blood samples were obtained from each participant. Serum concentrations were determined using validated high-performance liquid chromatography-tandem mass spectrometry bioanalytical assays. The AUC0-t was calculated based on serum concentration-time data (using the actual blood sampling times).
Pharmacokinetic parameter Serum: area under the concentration-time curve from 0 to time t (AUC0-t) for CG5503-sulphate
Time frame: Pre-dose and up to 23 hours post-dose
26 PK blood samples were obtained from each participant. Serum concentrations were determined using validated high-performance liquid chromatography-tandem mass spectrometry bioanalytical assays. The AUC0-t was calculated based on serum concentration-time data (using the actual blood sampling times).
Pharmacokinetic parameter Serum: maximum concentration (Cmax) for CG5503 base
Time frame: Pre-dose and up to 23 hours post-dose
26 PK blood samples were obtained from each participant. Serum concentrations were determined using validated high-performance liquid chromatography-tandem mass spectrometry bioanalytical assays. The Cmax was calculated based on serum concentration-time data (using the actual blood sampling times).
Pharmacokinetic parameter Saliva: maximum concentration (Cmax) for CG5503 base
Time frame: Pre-dose and up to 23 hours post-dose
16 PK saliva samples were obtained from each participant. Saliva concentrations were determined using validated high-performance liquid chromatography-tandem mass spectrometry bioanalytical assays. Participants were asked to donate saliva as much as possible in approximately 0.5 minutes. tubes. The Cmax was calculated based on saliva concentration-time data (using the actual saliva sampling time intervals).
Pharmacokinetic parameter Serum: maximum concentration (Cmax) for CG5503-glucuronide
Time frame: Pre-dose and up to 23 hours post-dose
26 PK blood samples were obtained from each participant. Serum concentrations were determined using validated high-performance liquid chromatography-tandem mass spectrometry bioanalytical assays. The Cmax was calculated based on serum concentration-time data (using the actual blood sampling times).
Pharmacokinetic parameter Serum: maximum concentration (Cmax) for CG5503-sulphate
Time frame: Pre-dose and up to 23 hours post-dose
26 PK blood samples were obtained from each participant. Serum concentrations were determined using validated high-performance liquid chromatography-tandem mass spectrometry bioanalytical assays. The Cmax was calculated based on serum concentration-time data (using the actual blood sampling times).
Pharmacokinetic parameter Serum: time to maximum concentration (tmax) for CG5503 base
Time frame: Pre-dose and up to 23 hours post-dose
26 PK blood samples were obtained from each participant. Serum concentrations were determined using validated high-performance liquid chromatography-tandem mass spectrometry bioanalytical assays. The tmax was calculated based on serum concentration-time data (using the actual blood sampling times).
Pharmacokinetic parameter Saliva: time to maximum concentration (tmax) for CG5503 base
Time frame: Pre-dose and up to 23 hours post-dose
16 PK saliva samples were obtained from each participant. Saliva concentrations were determined using validated high-performance liquid chromatography-tandem mass spectrometry bioanalytical assays. Participants were asked to donate saliva as much as possible in approximately 0.5 minutes. The tmax was calculated based on saliva concentration-time data (using the actual saliva sampling time intervals).
Pharmacokinetic parameter Serum: time to maximum concentration (tmax) for CG5503-glucuronide
Time frame: Pre-dose and up to 23 hours post-dose
26 PK blood samples were obtained from each participant. Serum concentrations were determined using validated high-performance liquid chromatography-tandem mass spectrometry bioanalytical assays. The tmax was calculated based on serum concentration-time data (using the actual blood sampling times).
Pharmacokinetic parameter Serum: time to maximum concentration (tmax) for CG5503-sulphate
Time frame: Pre-dose and up to 23 hours post-dose
26 PK blood samples were obtained from each participant. Serum concentrations were determined using validated high-performance liquid chromatography-tandem mass spectrometry bioanalytical assays. The tmax was calculated based on serum concentration-time data (using the actual blood sampling times).
23 secondary outcomes
Pharmacokinetic parameter Serum: extrapolated AUC expressed as a percentage of total AUC0-inf (AUC%extr) for CG5503 base
Time frame: Pre-dose and up to 23 hours post-dose
Pharmacokinetic parameter Saliva: extrapolated AUC expressed as a percentage of total AUC0-inf (AUC%extr) for CG5503 base
Time frame: Pre-dose and up to 23 hours post-dose
Pharmacokinetic parameter Serum: extrapolated AUC expressed as a percentage of total AUC0-inf (AUC%extr) for CG5503-glucuronide
Time frame: Pre-dose and up to 23 hours post-dose
Pharmacokinetic parameter Serum: extrapolated AUC expressed as a percentage of total AUC0-inf (AUC%extr) for CG5503-sulphate
Time frame: Pre-dose and up to 23 hours post-dose
Pharmacokinetic parameter Serum: apparent terminal elimination rate constant (λz) for CG5503 base
Time frame: Pre-dose and up to 23 hours post-dose
Pharmacokinetic parameter Saliva: apparent terminal elimination rate constant (λz) for CG5503 base
Time frame: Pre-dose and up to 23 hours post-dose
Pharmacokinetic parameter Serum: apparent terminal elimination rate constant (λz) for CG5503-glucuronide
Time frame: Pre-dose and up to 23 hours post-dose
Pharmacokinetic parameter Serum: apparent terminal elimination rate constant (λz) for CG5503-sulphate
Time frame: Pre-dose and up to 23 hours post-dose
Pharmacokinetic parameter Serum: the apparent half-life associated with the terminal elimination phase (t1/2,z) for CG5503 base
Time frame: Pre-dose and up to 23 hours post-dose
Pharmacokinetic parameter Saliva: the apparent half-life associated with the terminal elimination phase (t1/2,z) for CG5503 base
Time frame: Pre-dose and up to 23 hours post-dose
Pharmacokinetic parameter Serum: the apparent half-life associated with the terminal elimination phase (t1/2,z) for CG5503-glucuronide
Time frame: Pre-dose and up to 23 hours post-dose
Pharmacokinetic parameter Serum: the apparent half-life associated with the terminal elimination phase (t1/2,z) for CG5503-sulphate
Time frame: Pre-dose and up to 23 hours post-dose
Pharmacokinetic parameter Serum: total serum or blood clearance of drug after intravenous administration (CL) for CG5503 base
Time frame: Pre-dose and up to 23 hours post-dose
Pharmacokinetic parameter Saliva: total clearance of drug after intravenous administration (CL) for CG5503 base
Time frame: Pre-dose and up to 23 hours post-dose
Pharmacokinetic parameter Serum: total serum or blood clearance of drug after intravenous administration (CL) for CG5503-glucuronide
Time frame: Pre-dose and up to 23 hours post-dose
Pharmacokinetic parameter Serum: total serum or blood clearance of drug after intravenous administration (CL) for CG5503-sulphate
Time frame: Pre-dose and up to 23 hours post-dose
Pharmacokinetic parameter Serum: the apparent volume of distribution associated with terminal phase after intravenous administration (Vz) for CG5503 base
Time frame: Pre-dose and up to 23 hours post-dose
Pharmacokinetic parameter Saliva: the apparent volume of distribution associated with terminal phase after intravenous administration (Vz) for CG5503 base
Time frame: Pre-dose and up to 23 hours post-dose
Pharmacokinetic parameter Serum: the apparent volume of distribution associated with terminal phase after intravenous administration (Vz) for CG5503-glucuronide
Time frame: Pre-dose and up to 23 hours post-dose
Pharmacokinetic parameter Serum: the apparent volume of distribution associated with terminal phase after intravenous administration (Vz) for CG5503-sulphate
Time frame: Pre-dose and up to 23 hours post-dose
Pharmacokinetic parameter Urine: renal excretion (Ae % of dose) for CG5503 base
Time frame: Pre-dose and up to 23 hours post-dose
Pharmacokinetic parameter Urine: renal excretion (Ae % of dose) for CG5503-glucuronide
Time frame: Pre-dose and up to 23 hours post-dose
Pharmacokinetic parameter Urine: renal excretion (Ae % of dose) for CG5503-sulphate
Time frame: Pre-dose and up to 23 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 16 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 4 ml CG5503 and 5 g charcoal powder in people with Pharmacokinetic, 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 5 inclusion and 21 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 16 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 Serum: area under the concentration-time curve extrapolated to infinity (AUC0-inf) for CG5503 base (time frame: Pre-dose and up to 23 hours post-dose). The study lists 16 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 16 May 2019.