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The aim of this study were to investigate the metabolism and pharmacokinetics of BIBR 1048 MS and BIBR 953 ZW in man.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| BIBR 953 ZW Intravenously | Experimental |
| |
| BIBR 1048 Oral Solution | Active Comparator |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| BIBR 953 ZW Intravenously | Drug | 5 mg, 2.8 MBq (76 µCi) |
| |
| Measure | Description | Time Frame |
|---|---|---|
| Total radioactivity in plasma and whole blood | 168 hours | |
| Total radioactivity in urine and faeces (excretion balance) over 168 h or until < 1% excreted in urine/faeces samples in a 24 h period | over 168 hours or 24 hour period | |
| Concentrations of BIBR 953 ZW in plasma over 168 h, estimation of the extent of gastrointestinal absorption | 168 hours | |
| Concentrations of BIBR 953 ZW in urine | 168 hours | |
| [14C] metabolic pattern and identification of metabolites in urine and if feasible, in plasma and faeces in comparison with various animal species | -12, 0 hours, 0-24, 24-48, 48-72, 72-96, 96-120, 120-144, 144-168 post dose |
| Measure | Description | Time Frame |
|---|---|---|
| Ratio of radioactivity in blood cells and plasma (CE/CP) | 0.5, 1, 2 ,4 ,8, 24 hours after oral study drug administration, 31min, 1, 2, 4, 8, 24h after start of infusion | |
| Measurement of in vitro plasma protein binding of [14C]-BIBR 953 ZW | Screening, day-1, day 1-day 8 |
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Inclusion Criteria:
Exclusion Criteria:
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| BIBR 1048 Oral Solution |
| Drug |
200 mg free base, 2.8 MBq (76 µCi) |
|
| Cmax - Peak (maximum) plasma concentration of BIBR 953 ZW | Screening, day-1, day 1-day 8 |
| tmax - time to reach the peak plasma concentration of BIBR 953 ZW | Screening, day-1, day 1-day 8 |
| t1/2 - Terminal half-life derived from non-compartmental analysis of BIBR 953 ZW | Screening, day-1, day 1-day 8 |
| AUC0-t - area under the plasma concentration vs. time curve from time zero to the time point for the last sample on the pharmacokinetic profile in which total radioactivity or active drug were reliably quantified) BIBR 953 ZW | Screening, day-1, day 1-day 8 |
| AUC0-infinity - Area under the plasma concentration vs. time curve from time zero to infinity - BIBR 953 ZW | Screening, day-1, day 1-day 8 |
| MRT0-inf - the average amount of time a particle remains in a compartment or system, derived when the drug concentration profile is extrapolated to infinity) - BIBR 953 ZW | Screening, day-1, day 1-day 8 |
| MRT0-t - the average amount of time a particle remains in a compartment or system - BIBR 953 ZW | Screening, day-1, day 1-day 8 |
| CL renal - the apparent volume of the central compartment cleared of drug via renal excretion into the urine, per unit time - BIBR 953 ZW | Screening, day-1, day 1-day 8 |
| CLtot - the apparent volume of the central compartment cleared of drug per unit tim after intravenous dosing - BIBR 953 ZW | Screening, day-1, day 1-day 8 |
| CLtot/F - the apparent volume of the central compartment cleared of drug per unit time after extravascular dosing - BIBR 953 ZW | Screening, day-1, day 1-day 8 |
| Vss - apparent volume of distribution at steady state following intravenous administration - BIBR 953 ZW | Screening, day-1, day 1-day 8 |
| Vz/f - Volume of distribution during terminal phase after oral administration - BIBR 953 ZW | Screening, day-1, day 1-day 8 |
| Cmax - Peak (maximum) plasma concentration for total radioactivity | up to day 8 |
| tmax - time to reach the peak plasma concentration for total radioactivity | up to day 8 |
| Occurence of Adverse events | Screening, upt to 10 days after study drug administration |
| Change from Baseline in physical examination | Screening, 8 to 10 days after study drug administration |
| Changes from Baseline in vital signs | Screening, 8 to 10 days after study drug administration |
| Change from Baseline in systolic and diastolic blood pressure | Screening, Day-1, day1, day2, day 8-10 after study drug administration |
| Change from Baseline in Pulse rate | Screening, Day-1, day1, day2, day 8-10 after study drug administration |
| Change from Baseline in 12-lead electrocardiogram (ECG) | Screening, Day-1, day1, day2, day 8-10 after study drug administration |
| Change from Baseline in clinical laboratory tests (hematology, clinical chemistry and urinanalysis) | Screening, day-1, day1, day2, day3, day 8-10 after study drug administration |
| Changes from baseline in activated partial thromboplastin time - aPTT | Screening, 1, 2, 24, 48 and 168 hours post dose administration |
| Changes from baseline in coagulation parameter INR - international normalized ratio prothrombin time | Screening, 1, 2, 24, 48 and 168 hours post dose administration |
| ID | Term |
|---|---|
| D000069604 | Dabigatran |
| ID | Term |
|---|---|
| D011725 | Pyridines |
| D006573 | Heterocyclic Compounds, 1-Ring |
| D006571 | Heterocyclic Compounds |
| D001562 | Benzimidazoles |
| D006574 | Heterocyclic Compounds, 2-Ring |
| D000072471 | Heterocyclic Compounds, Fused-Ring |
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