The objective of this study was to investigate the effect of multiple doses BI 1356 given once daily in the estimated highest therapeutic dose of 5 mg until steady state on the pharmacokinetics, safety, and tolerability of a single oral conventional therapeutic dose of 1.75 mg glyburide. In addition, the effect of glyburide as a single oral dose of 1.75 mg being a conventional therapeutic dose on the multiple dose pharmacokinetics of BI 1356 was investigated. Pharmacokinetic profiles of glyburide were determined when given alone or in combination with BI 1356. Pharmacokinetic profiles of BI 1356 and its inactive metabolite CD 1750 were determined at steady state of BI 1356 when given alone or in combination with glyburide.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
TREATMENT
Masking
NONE
Enrollment
20
AUC0-infinity (area under the concentration-time curve of glyburide in plasma) for several time points
Time frame: up to 48 hours after drug administration
Cmax (maximum measured concentration of glyburide in plasma) for several time points
Time frame: up to 48 hours after drug administration
AUCτ,ss (area under the concentration-time curve of the analyte in plasma at steady state over a uniform dosing interval τ) of BI 1356
Time frame: up to 48 h after drug administration
Cmax,ss (maximum measured concentration of the analyte in plasma at steady state over a uniform dosing interval τ) of BI 1356
Time frame: up to 48 h after drug administration
tmax (time from dosing to the maximum concentration of the analyte in plasma) for several time points
Time frame: up to 48 hours after drug administration
λz (terminal rate constant in plasma)
Time frame: up to 48 hours after drug administration
t1/2 (terminal half-life of the analyte in plasma)
Time frame: up to 48 hours after drug administration
MRTpo (mean residence time of the analyte in the body after po administration) for several time points
Time frame: up to 48 hours after drug administration
CL/F (apparent clearance of the analyte in the plasma after extravascular administration) for several time points
Time frame: up to 48 hours after drug administration
Vz/F (apparent volume of distribution during the terminal phase λz following an extravascular dose) for several time points
Time frame: up to 48 hours after drug administration
Number of patients with adverse events
Time frame: up to 11 weeks
Assessment of tolerability by investigator on a 4-point scale
Time frame: Day 1 of treatment B, day 3 of treatment B and C
AUC (area under the concentration-time curve of the analyte in plasma) for several time points
Time frame: up to 48 h after drug administration
Cmax,ss (maximum measured concentration of the analyte in plasma at steady state over a uniform dosing interval τ) of CD 1750
Time frame: up to 48 h after drug administration
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