The pharmacokinetics of 50 mg BIBR 1048 administered as two newly developed capsule formulation using melt extrusion technology was assessed in two separate, single dose, 3-way crossover, open design, randomised studies. The 3-way crossover treatments included administration of the tartaric acid solution of 50 mg BIBR 1048, the capsule formulation A or B and administration of the capsules with coadministration of pantoprazole.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
TREATMENT
Masking
NONE
Enrollment
24
BIBR 1048 MS, formulation A 50 mg
BIBR 1048 MS, formulation B 50 mg
BIBR 1048 MS, powder plus solution 50 mg
AUC0-∞ (Area under the concentration-time curve the time interval from 0 extrapolated to infinity) of BIBR 953 ZW
Time frame: Before and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24 and 48 hours after administration of study drug
AUC0-tf (Area under the concentration-time curve over the time interval from 0 to the time of the last quantifiable concentration) of BIBR 953 ZW
Time frame: Before and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24 and 48 hours after administration of study drug
Cmax (Maximum measured concentration) of BIBR 953 ZW
Time frame: Before and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24 and 48 hours after administration of study drug
tmax (Time from dosing to the maximum concentration) of BIBR 953 ZW
Time frame: Before and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24 and 48 hours after administration of study drug
t1/2 (Terminal half-life) of BIBR 953 ZW
Time frame: Before and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24 and 48 hours after administration of study drug
MRTtot (Total mean residence time) of BIBR 953 ZW
Time frame: Before and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24 and 48 hours after administration of study drug
CLtot/F (Total apparent clearance) of BIBR 953 ZW
Time frame: Before and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24 and 48 hours after administration of study drug
Vz/F (Apparent volume of distribution) of BIBR 953 ZW
Time frame: Before and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24 and 48 hours after administration of study drug
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Pantoprazole 40 mg
λz (terminal elimination rate constant) of BIBR 953 ZW
Time frame: Before and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24 and 48 hours after administration of study drug
Changes in aPTT (activated partial thromboplastin time)
Time frame: Before and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24 and 48 hours after administration of study drug
Changes in PT (prothrombin time)
Time frame: Before and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24 and 48 hours after administration of study drug