Investigation How CG5503 is Taken up and Excreted From the Body After 2 Minutes Intravenous Infusion With and Without Oral Co-administration of Charcoal

Grünenthal

Status and phase: Completed; Phase 1

Conditions: Pharmacokinetic

Treatments: Drug: 5 g charcoal powder; Drug: 4 ml CG5503

Study type: Interventional

Funder types: Industry

Identifiers

NCT03951987

HP5503/11

Details and patient eligibility

About

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.

Enrollment: 14 patients

Sex: Male

Ages: 18 to 65 years old

Volunteers: Accepts Healthy Volunteers

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).

Trial design

Primary purpose: Treatment

Allocation: Randomized

Interventional model: Crossover Assignment

Masking: None (Open label)

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14 participants in 2 patient groups

Treatment A: 4 ml CG5503

Experimental group

Description:

4 ml of the CG5503 i.v. infusion solution corresponding to 40 mg CG5503 (tapentadol hydrochloride) was administered as a 2 minutes infusion.

Treatment:

Drug: 4 ml CG5503

Treatment B: 4 ml CG5503; 5 g charcoal powder

Experimental group

Description:

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)

Treatment:

Drug: 4 ml CG5503

Drug: 5 g charcoal powder