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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.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Substudy 1 | Experimental | Three treatments of single administrations of BIBR 1048 MS 50 mg with or without pantoprazole; randomised sequence
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| Substudy 2 | Experimental | Three treatments of single administrations of BIBR 1048 MS 50 mg with or without pantoprazole; randomised sequence
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| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| BIBR 1048 MS capsule formulation A | Drug | BIBR 1048 MS, formulation A 50 mg |
| |
| Measure | Description | Time Frame |
|---|---|---|
| AUC0-∞ (Area under the concentration-time curve the time interval from 0 extrapolated to infinity) of BIBR 953 ZW | 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 | Before and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24 and 48 hours after administration of study drug |
| Measure | Description | Time Frame |
|---|---|---|
| Cmax (Maximum measured concentration) of BIBR 953 ZW | 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 | 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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Inclusion Criteria:
Exclusion Criteria:
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| ID | Term |
|---|---|
| D012996 | Solutions |
| D000077402 | Pantoprazole |
| ID | Term |
|---|---|
| D004364 | Pharmaceutical Preparations |
| D053799 | 2-Pyridinylmethylsulfinylbenzimidazoles |
| D013454 | Sulfoxides |
| D013457 | Sulfur Compounds |
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| BIBR 1048 MS capsule formulation B |
| Drug |
BIBR 1048 MS, formulation B 50 mg |
|
| BIBR 1048 MS powder plus solution | Drug | BIBR 1048 MS, powder plus solution 50 mg |
|
| Pantoprazole | Drug | Pantoprazole 40 mg |
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| t1/2 (Terminal half-life) of BIBR 953 ZW | 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 | 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 | 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 | Before and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24 and 48 hours after administration of study drug |
| λz (terminal elimination rate constant) of BIBR 953 ZW | 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) | 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) | Before and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24 and 48 hours after administration of study drug |
| D009930 | Organic Chemicals |
| D011725 | Pyridines |
| D006573 | Heterocyclic Compounds, 1-Ring |
| D006571 | Heterocyclic Compounds |
| D001562 | Benzimidazoles |
| D006574 | Heterocyclic Compounds, 2-Ring |
| D000072471 | Heterocyclic Compounds, Fused-Ring |