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Relative Bioavailability of Single Oral Doses of Dabigatran Etexilate With or Without Oral Administration of Verapamil in Two Different Dosages in Healthy Male and Female Volunteers

Phase 1
Completed
Conditions
Healthy
Interventions
Registration Number
NCT02171533
Lead Sponsor
Boehringer Ingelheim
Brief Summary

To investigate whether and to what extent the P-glycoprotein inhibitor (P-gp) verapamil affects the pharmacokinetic parameters of dabigatran with verapamil given at different dosages, in different formulations (immediate release (IR) and extended release (ER)), and in different intervals in relation to the dabigatran dose.

Detailed Description

Not available

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
40
Inclusion Criteria

Not provided

Exclusion Criteria

Not provided

Study & Design

Study Type
INTERVENTIONAL
Study Design
CROSSOVER
Arm && Interventions
GroupInterventionDescription
Fixed sequenceVerapamilTreatments will be given in a fixed sequence
CrossoverVerapamil ERTreatments will be given in randomized sequences
Fixed sequencedabigatranTreatments will be given in a fixed sequence
CrossoverVerapamilTreatments will be given in randomized sequences
CrossoverdabigatranTreatments will be given in randomized sequences
Primary Outcome Measures
NameTimeMethod
AUC0-infinity (area under the concentration-time curve of total dabigatran over the time interval from 0 extrapolated to infinity)up to 107 hours
Cmax (maximum measured concentration of total dabigatran)up to 107 hours
Secondary Outcome Measures
NameTimeMethod
Occurence of Adverse Eventswithin 5 days after last drug administration
Cmax (maximum measured concentration of free dabigatran)up to 107 hours
AUC0-infinity (area under the concentration-time curve of free dabigatran over the time interval from 0 extrapolated to infinity)up to 107 hours
t1/2 (terminal half-life of the analyte in plasma)up to 107 hours
Vz/F (apparent volume of distribution during the terminal phase λz following an extravascular dose)up to 107 hours
tmin,ss (time from last dosing to the minimum concentration of verapamil at steady state over a uniform dosing interval τ)up to 107 hours
Cpre,ss (predose concentration of verapamil at steady state immediately before administration of the next dose)up to 107 hours
Cavg (Average concentration of verapamil at steady state)up to 107 hours
MRTpo,ss (mean residence time of verapamil in the body at steady state after oral administration)up to 107 hours
Vz/F,ss (apparent volume of distribution during the terminal phase λz at steady state following an extravascular administration)up to 107 hours
Ae0-24 (amount of dabigatran that is eliminated in urine from the time interval 0-24h)up to 107 hours
fe0-24 (fraction of administered drug excreted unchanged in urine from time point 0- 24h)up to 107 hours
CLR0-24 (renal clearance of dabigatran from the time point 0 until the time point 24h )up to 107 hours
AUEC0-24 (area under the effect curve)up to 107 hours

for ecarin clotting time and thrombin time

ERmax (maximum effect ratio)up to 107 hours

for ecarin clotting time and thrombin time

AUC0-infinity (area under the concentration-time curve of verapamil over the time interval from 0 extrapolated to infinity)up to 107 hours
Cmax (maximum measured concentration of verapamil)up to 107 hours
tmax (time from dosing to the maximum concentration of the analyte in plasma)up to 107 hours
λz (terminal rate constant in plasma)up to 107 hours
AUC0-24 (area under the concentration-time curve of the analyte in plasma over the time interval from 0 to 24 h after the administration)up to 107 hours
AUC0-tz (area under the concentration-time curve of the analyte in plasma over the time interval from 0 to the time of the last quantifiable data point)up to 107 hours
MRTpo (mean residence time of the analyte in the body after oral administration)up to 107 hours
CL/F (apparent clearance of the analyte in the plasma after extravascular administration)up to 107 hours
AUC0-tz,ss (area under the concentration-time curve of verapamil from the time point 0 after the last dose at steady state to the last quantifiable analyte plasma concentration within the uniform dosing interval τ)up to 107 hours
Cmax,ss (maximum concentration of verapamil at steady state)up to 107 hours
tz,ss (time of last measureable concentration of verapamil within the dosing interval τ at steady state)up to 107 hours
tmax,ss (time from last dosing to the maximum concentration of verapamil at steady state on day 4)up to 107 hours
CL/F,ss (apparent clearance of verapamil at steady state after extravascular multiple dose administration)up to 107 hours
Cmin,ss (minimum measured concentration of verapamil at steady state over a uniform dosing interval τ)up to 107 hours
AUCτ,ss (area under the concentration-time curve of verapamil within the uniform dosing interval τ)up to 107 hours
Assessment of Tolerability by investigatorwithin 5 days after last drug administration
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