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To compare the oral bioavailability and rate of absorption of four prototype extended-release (ER) formulations with BI 11634 (single doses) to immediate-release (IR) tablets in healthy male volunteers.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| BI 11634 ER formulation A | Experimental |
| |
| BI 11634 ER formulation B | Experimental |
| |
| BI 11634 ER formulation M | Experimental |
| |
| BI 11634 ER formulation C | Experimental |
| |
| BI 11634 IR tablet | Active Comparator |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| BI 11634 ER formulation A | Drug |
| ||
| BI 11634 ER formulation B |
| Measure | Description | Time Frame |
|---|---|---|
| AUC0-∞ (area under the concentration time curve of the analyte in plasma over the time interval from 0 extrapolated to infinity) | up to 48 hours after drug administraton | |
| Cmax (maximum measured concentration of analyte in plasma) | up to 48 hours after drug administraton |
| Measure | Description | Time Frame |
|---|---|---|
| AUC0-tz (area under the concentration-time curve of the analyte in plasma over the time interval from 0 to the time of the last quantifiable data point) | up to 48 hours after drug administration | |
| tmax (time from dosing to the maximum concentration of the analyte in plasma) |
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Inclusion Criteria:
Exclusion Criteria:
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| Drug |
|
| BI 11634 ER formulation M | Drug |
|
| BI 11634 ER formulation C | Drug |
|
| BI 11634 IR tablet | Drug |
|
| up to 48 hours after drug administration |
| λz (terminal rate constant in plasma) | up to 48 hours after drug administration |
| t1/2 (terminal half-life of the analyte in plasma) | up to 48 hours after drug administration |
| MRTpo (mean residence time of the analyte in the body after oral administration) | up to 48 hours after drug administration |
| CL/F (apparent clearance of the analyte in the plasma after extravascular administration) | up to 48 hours after drug administration |
| Vz/F (apparent volume of distribution during the terminal phase λz following an extravascular dose) | up to 48 hours after drug administration |
| Fluctuation parameter Cmax/C24 ratio | up to 48 hours after drug administration |
| Maximum prolongation of blood coagulation time | by HepTest® (Haemachem Inc.) | up to 48 hours after drug administration |
| Number of subjects with adverse events | up to 8 days after last drug administration |
| Number of subjects with clinically significant findings in vital signs (blood pressure, pulse rate) | up to 8 days after last drug administration |
| Number of subjects with clinically significant findings in ECG | up to 8 days after last drug administration |
| Number of subjects with clinically significant findings in laboratory tests | up to 8 days after last drug administration |
| Assessment of tolerability by investigator on a 4-point scale | up to 8 days after last drug administration |
| % Inhibition of Factor Xa | by Russel's Viper Venom test (RVV) | up to 48 hours after drug administration |