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Study to Evaluate Safety, Tolerability and Pharmacokinetics of Increasing Repeated Oral Doses of Ambroxol Lozenges in Healthy Male Volunteers

Phase 1
Completed
Conditions
Healthy
Interventions
Registration Number
NCT02194283
Lead Sponsor
Boehringer Ingelheim
Brief Summary

The main objectives of the present study are to determine pharmacokinetics of ambroxol in healthy male volunteers following repeated administration of lozenges of 20 mg ambroxol for four days

Detailed Description

Not available

Recruitment & Eligibility

Status
COMPLETED
Sex
Male
Target Recruitment
34
Inclusion Criteria
  • Healthy males according to the following criteria: Based upon a complete medical history, including the physical examination, vital signs, 12-lead Electrocardiogram (ECG), clinical laboratory tests
  • Age ≥21 and Age ≤50 year
  • BMI ≥18.5 and BMI ≤29.9 kg/m2 (Body Mass Index)
  • Signed and dated written informed consent prior to admission to the study in accordance with Good Clinical Practice (GCP) and the local legislation
Exclusion Criteria
  • Any finding of the medical examination (including vital signs and ECG) deviating from normal and of clinical relevance
  • Any evidence of a clinically relevant concomitant disease
  • Gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunological or hormonal disorders
  • Surgery of the gastrointestinal tract (except appendectomy)
  • Diseases of the central nervous system (such as epilepsy) or psychiatric disorders or neurological disorders
  • History of relevant orthostatic hypotension, fainting spells or blackouts
  • Chronic or relevant acute infections
  • History of relevant allergy/hypersensitivity (including allergy to drug or its excipients)
  • Intake of drugs with a long half-life (> 24 hours) within at least one month or less than 10 half-lives of the respective drug prior to administration or during the trial
  • Use of drugs which might reasonably influence the results of the trial or that prolong the QT/QTc interval based on the knowledge at the time of protocol preparation within 10 days prior to administration or during the trial
  • Participation in another trial with an investigational drug within two months prior to administration or during the trial
  • Actual smoker
  • Alcohol abuse (more than 40 g/day)
  • Drug abuse
  • Blood donation (more than 100 mL within four weeks prior to administration or during the trial)
  • Excessive physical activities (within one week prior to administration or during the trial)
  • Any laboratory value outside the reference range that is of clinical relevance
  • Inability to comply with dietary regimen of trial site
  • A marked baseline prolongation of QT/QTc interval (e.g., repeated demonstration of a QTc interval >450 ms)
  • A history of additional risk factors for torsade de pointes (e.g., heart failure, hypokalaemia, family history of Long QT Syndrome)

Study & Design

Study Type
INTERVENTIONAL
Study Design
SINGLE_GROUP
Arm && Interventions
GroupInterventionDescription
Ambroxol - in single rising dosesAmbroxol - in single rising doses-
PlaceboPlacebo-
Primary Outcome Measures
NameTimeMethod
Cmin,ss (minimum concentration of the analyte in plasma at steady state)up to 120 hours after first drug administration
tmax (time from dosing to the maximum concentration of the analyte in plasma)up to 24 hours after drug administration
AUC0-24 (area under the concentration-time curve of the analyte in plasma over the time interval from 0 to 24 hours)up to 24 hours after drug administration
Cmax,ss (maximum concentration of the analyte in plasma at steady state)up to 120 hours after first drug administration
RA (accumulation ratio)up to 96 hours after first drug administration
Cmax (maximum measured concentration of the analyte in plasma)up to 24 hours after drug administration
AUC72-96,ss (area under the concentration-time curve of the analyte in plasma at steady state over a uniform 24 hour interval matching Day 1)up to 96 hours after first drug administration
Ae72-96,ss (amount of analyte that is eliminated in urine at steady state from the time point 72 to time point 96)up to 96 hours after first drug administration
λz,ss (terminal rate constant in plasma at steady state)up to 120 hours after first drug administration
Ae0-24 (amount of the analyte that is eliminated in urine from the time point 0 until time point 24)up to 24 hours after drug administration
tmax,ss (time from last dosing to maximum concentration at steady state)up to 120 hours after first drug administration
t1/2,ss (terminal half-life of the analyte in plasma at steady state)up to 120 hours after first drug administration
CLR,0-24 (renal clearance of the analyte determined from the time point 0 until time point 24) using AUC0-24 and Ae0-24up to 24 hours after drug administration
CLR,72-96,ss (renal clearance of the analyte in plasma from the time point 72 until the time point 96 at steady state) using AUC72-96 and Ae72-96up to 96 hours after first drug administration
LI (linearity index)up to 96 hours after first drug administration
Secondary Outcome Measures
NameTimeMethod
Number of patients with abnormal changes in laboratory parametersup to 36 days
Number of patients with clinically significant changes in vital signs (blood pressure [BP], pulse rate [PR])up to 36 days
Assessment of tolerability on a 4-point scale10 days after last drug administration
Number of patients with adverse eventsup to 36 days
Number of patients with clinically significant changes in 12-lead electrocardiogram (ECG)up to 36 days
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