Investigation How CG5503 is Taken up and Excreted From th... | NCT03951987

Status Module

Description Module

Arms/Interventions Module

Arm Groups

Label	Type	Description	Intervention Names
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.	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)	Drug: 4 ml CG5503 Drug: 5 g charcoal powder

Interventions

Name	Type	Description	Arm Group Labels	Other Names
4 ml CG5503	Drug	4 ml of the CG5503 infusion solution corresponding to 40 mg CG5503 (tapentadol hydrochloride).	Treatment A: 4 ml CG5503 Treatment B: 4 ml CG5503; 5 g charcoal powder

Outcomes Module

Primary Outcomes

Measure	Description	Time Frame
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).	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).	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).	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).

Secondary Outcomes

Measure	Description	Time Frame
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).

Eligibility Module

Eligibility Criteria

Inclusion Criteria:

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.

Exclusion Criteria:

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.
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).

ID	Term
D010636	Phenols
D001555	Benzene Derivatives
D006841	Hydrocarbons, Aromatic
D006844	Hydrocarbons, Cyclic
D006838	Hydrocarbons
D009930	Organic Chemicals