Study to determine the basic pharmacokinetics of ambroxol and \[14C\]-radioactivity including mass balance, excretion pathways and complete metabolism in healthy male volunteers following administration of a lozenge of 20 mg ambroxol together with an oral solution of 0.4 mg \[14C\]-ambroxol labelled in two different positions
Study Type
INTERVENTIONAL
Allocation
NON_RANDOMIZED
Purpose
TREATMENT
Masking
NONE
Enrollment
12
Individual time course profiles of [14C]-radioactivity (in nmoleq/L or nmoleq/kg for faeces) in plasma
Time frame: up to 120 hours after drug administration
Individual time course profiles of ambroxol in plasma
Time frame: up to 120 hours after drug administration
Rate and extent of excretion mass balance based on the total radioactivity in urine and faeces
Time frame: up to 216 hours after drug administration
Identification of major metabolites in urine, feces and plasma in comparison with various animal species
Time frame: up to 48 hours after drug administration
Cblood cells/Cplasma ratio of [14C]-radioactivity and Cblood /Cplasma ratio of [14C]-radioactivity
Time frame: up to 120 hours after drug administration
Cmax (maximum concentration of the analyte(s) in plasma)
Time frame: up to 120 hours after drug administration
tmax (time from dosing to the maximum concentration of the analyte(s) in plasma)
Time frame: up to 120 hours after drug administration
AUC0-tz (area under the concentration-time curve of the analyte(s) in plasma over the time interval from 0 to the time of the last quantifiable data point)
Time frame: up to 120 hours after drug administration
AUC0-∞ (area under the concentration-time curve of the analyte(s) in plasma over the time interval from 0 to infinity)
Time frame: up to 120 hours after drug administration
λz (terminal rate constant in plasma)
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Time frame: up to 120 hours after drug administration
t1/2 (terminal half-life of the analyte(s) in plasma)
Time frame: up to 120 hours after drug administration
MRTpo (mean residence time of the analyte(s) in the body after oral administration)
Time frame: up to 120 hours after drug administration
CL/F (total clearance of the analyte in plasma after oral administration)
Time frame: up to 120 hours after drug administration
Vz/F (apparent volume of distribution during the terminal phase λz following an oral dose)
Time frame: up to 120 hours after drug administration
Ae0-tz (amount of analyte that is eliminated in urine within the time interval zero to tz)
Time frame: up to 216 hours after drug administration
Aefaeces,0-tz (amount of analyte excreted in faeces within the time interval zero to tz)
Time frame: up to 216 hours after drug administration
fefaeces,0-tz (fraction of analyte excreted in faeces within the time interval zero to tz in % of dose)
Time frame: up to 216 hours after drug administration
CLR,t1-t2 (renal clearance of analyte from the within the time interval t1 to t2)
Time frame: up to 216 hours after drug administration
fe0-tz (fraction of analyte excreted in urine within the time interval zero to tz in % of dose)
Time frame: up to 216 hours after drug administration
Individual time course profiles of [14C]-radioactivity (in nmoleq/L or nmoleq/kg for faeces) in urine
Time frame: up to 216 hours after drug administration
Individual time course profiles of [14C]-radioactivity (in nmoleq/L or nmoleq/kg for faeces) in faeces
Time frame: up to 216 hours after drug administration
Individual time course profiles of ambroxol in urine
Time frame: up to 216 hours after drug administration
Number of patients with clinically significant changes vital signs (blood pressure [BP], pulse rate [PR])
Time frame: up to 39 days
Number of patients with adverse events
Time frame: up to 39 days
Number of patients with clinically significant changes in 12-lead electrocardiogram (ECG)
Time frame: up to 39 days
Number of patients with abnormal changes in laboratory parameters
Time frame: up to 39 days
Assessment of tolerability on a 4-point scale
Time frame: Day 14