Two substudies to assess (1) the tolerability of BIBR 953 ZW intravenous infusion at 0.1, 1 and 5 mg BIBR 953 ZW and (2) the absolute bioavailability of 100mg BIBR 1048 administered as 'acid free' tablet formulation (TF1) and (3) the bioavailability of the 100 mg tablet of BIBR 1048 relative to the tartaric acid solution of 100 mg dose strength and (4) the absolute bioavailability of the 100 mg tartaric acid solution of BIBR 1048 MS.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
TREATMENT
Masking
DOUBLE
Enrollment
30
AUC0-inf (Area under the plasma concentration-time curve extrapolated to infinity)
Time frame: up to 48 hours after drug administration
AUC0-tf (Area under the plasma concentration-time curve up to the last quantifiable plasma concentration)
Time frame: up to 48 hours after drug administration
Cmax (Maximum plasma concentration after oral administration)
Time frame: up to 48 hours after drug administration
Cumulative urinary excretion of BIBR 953 ZW administered intravenously
Time frame: up to 48 hours after drug administration
changes in activated partial thromboplastin time (aPTT )
Time frame: up to 48 hours after drug administration
changes in prothrombin time (PT)
Time frame: up to 48 hours after drug administration
C29 (Plasma concentration of BIBR 953 ZW at 29 minutes after the start of the 30 min. infusion)
Time frame: 29 minutes after start of infusion
t1/2 (terminal half-life)
Time frame: up to 48 hours after infusion
CLtot (total clearance of drug from plasma)
Time frame: up to 48 hours after infusion
CLren (renal clearance from plasma)
Time frame: up to 48 hours after infusion
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MRTdisp (Mean time of residence of drug molecules in the body after intravascular administration)
Time frame: up to 48 hours after infusion
Vss (apparent volume of distribution at steady state)
Time frame: up to 48 hours after infusion
Vz (Apparent volume of distribution during the terminal elimination phase)
Time frame: up to 48 hours after infusion
MRTtot (total mean residence time)
Time frame: up to 48 hours after oral administration
CLtot/F (total clearance after oral administration)
Time frame: up to 48 hours after oral administration
tmax (time to reach the peak plasma concentration)
Time frame: up to 48 hours after oral administration
Vz/F (apparent volume of distribution of the terminal elimination phase after oral administration)
Time frame: up to 48 hours after oral administration
changes in Ecarin clotting time (ECT)
Time frame: up to 48 hours after drug administration
changes in thrombin time (TT)
Time frame: up to 48 hours after drug administration
changes in vital signs (systolic and diastolic blood pressure, pulse rate)
Time frame: up to 1 month
changes in electrocardiogram
Time frame: up to 1 month
occurrence of adverse events
Time frame: up to 1 month