Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Part 1: To investigate the effect of quinidine, a P-glycoprotein (P-gp) probe inhibitor on the bioavailability of dabigatran etexilate,
Part 2: To determine the effect of quinidine on the bioavailability of fexofenadine, a probe substrate for P-gp
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Dabigatran etexilate capsules | Active Comparator |
| |
| Dabigatran etexilate capsules and quinidine sulfate tablets | Experimental |
| |
| Fexofenadine tablets | Active Comparator |
| |
| Fexofenadine and quinidine sulfate tablets | Experimental |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| Dabigatran etexilate capsules | Drug |
| ||
| Measure | Description | Time Frame |
|---|---|---|
| AUCτ,ss (area under the concentration-time curve of dabigatran in plasma at steady state over one dosing interval) | Before dose, 0:30, 1:00, 1:30, 2:00, 3:00, 4:00, 6:00, 8:00, 10:00 and 12:00 hours after dosing on day 3 | |
| Cmax,ss (maximum concentration of dabigatran in plasma at steady state) | Before dose on day 1, day 2, before dose, 0:30, 1:00, 1:30, 2:00, 3:00, 4:00, 6:00, 8:00, 10:00, 12:00, 24:00 and 48:00 hours after dosing on Day 3 | |
| AUC0-∞ (area under the concentration-time curve of fexofenadine in plasma over the time interval from 0 to infinity) | Before dose, 0:30, 1:00,1:30, 2:00, 3:00, 4:00, 6:00, 8:00, 10:00, 12:00, 24:00 and 48:00 hours after dosing on day 1 | |
| Cmax (maximum measured concentration of fexofenadine in plasma) | Before dose, 0:30, 1:00,1:30, 2:00, 3:00, 4:00, 6:00, 8:00, 10:00, 12:00, 24:00 and 48:00 hours after dosing on day 1 |
| Measure | Description | Time Frame |
|---|---|---|
| AUC0-tz,ss (area under the concentration-time curve of dabigatran in plasma from the time point 0 after the last dose at steady state to the last quantifiable dabigatran plasma concentration within the uniform dosing interval τ) | 0:30, 1:00, 1:30, 2:00, 3:00, 4:00, 6:00, 8:00, 10:00, 12:00, 24 and 48 hours after dosing on day 3 | |
| tz,ss (time of last measurable concentration of dabigatran in plasma within the dosing interval τ at steady state) |
Not provided
Inclusion Criteria:
Exclusion Criteria:
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
| Quinidine sulfate tablets |
| Drug |
|
| Fexofenadine tablets | Drug |
|
| 0:30, 1:00, 1:30, 2:00, 3:00, 4:00, 6:00, 8:00, 10:00, 12:00, 24 and 48 hours after dosing on day 3 |
| tmax,ss (time from last dosing to the maximum concentration of dabigatran in plasma at steady state) | 0:30, 1:00, 1:30, 2:00, 3:00, 4:00, 6:00, 8:00, 10:00, 12:00, 24 and 48 hours after dosing on day 3 |
| CL/Fss (apparent clearance of dabigatran in the plasma at steady state) | Before dose on day 1, day 2, before dose, 0:30, 1:00, 1:30, 2:00, 3:00, 4:00, 6:00, 8:00, 10:00, 12:00, 24:00 and 48:00 hours after dosing on Day 3 |
| Cmin,ss (minimum measured concentration of dabigatran in plasma at steady state) | Before dose on day 1, day 2, before dose, 0:30, 1:00, 1:30, 2:00, 3:00, 4:00, 6:00, 8:00, 10:00, 12:00, 24:00 and 48:00 hours after dosing on Day 3 |
| Cavg (average concentration of dabigatran at steady state) | Before dose on day 1, day 2, before dose, 0:30, 1:00, 1:30, 2:00, 3:00, 4:00, 6:00, 8:00, 10:00, 12:00, 24:00 and 48:00 hours after dosing on Day 3 |
| C10,2 (total dabigatran concentration 10 hours after the second dabigatran etexilate administration) | Day 2, 22 hours after the first dose on day 1 |
| tmin,ss (time from last dosing to the minimum concentration of dabigatran in plasma at steady state over a uniform dosing interval τ) | Before dose on day 1, day 2, before dose, 0:30, 1:00, 1:30, 2:00, 3:00, 4:00, 6:00, 8:00, 10:00, 12:00, 24:00 and 48:00 hours after dosing on Day 3 |
| MRTpo,ss (mean residence time of dabigatran in the body at steady state after oral administration) | Before dose on day 1, day 2, before dose, 0:30, 1:00, 1:30, 2:00, 3:00, 4:00, 6:00, 8:00, 10:00, 12:00, 24:00 and 48:00 hours after dosing on Day 3 |
| Vz/Fss (apparent volume of distribution of dabigatran during the terminal phase λz at steady state following an extravascular administration) | Before dose on day 1, day 2, before dose, 0:30, 1:00, 1:30, 2:00, 3:00, 4:00, 6:00, 8:00, 10:00, 12:00, 24:00 and 48:00 hours after dosing on Day 3 |
| Cmax (maximum measured concentration of quinidine in plasma) | Pre-dose, 0:30, 1:00, 2:00, 3:00, 4:00, 6:00, 8:00, 11:00, 13:00, 25:00 and 49 hours after dosing |
| AUC0-∞ (area under the concentration-time curve of quinidine in plasma over the time interval from 0 to infinity) | Pre-dose, 0:30, 1:00, 2:00, 3:00, 4:00, 6:00, 8:00, 11:00, 13:00, 25:00 and 49 hours after dosing |
| AUC0-tz (area under the concentration-time curve of fexofenadine in plasma from the time point 0 after the last dose to the last quantifiable analyte plasma concentration within the uniform dosing interval τ) | Before dose, 0:30, 1:00,1:30, 2:00, 3:00, 4:00, 6:00, 8:00, 10:00, 12:00, 24:00 and 48:00 hours after dosing on day 1 |
| tmax (time from last dosing to the maximum measured concentration of fexofenadine in plasma) | Before dose, 0:30, 1:00,1:30, 2:00, 3:00, 4:00, 6:00, 8:00, 10:00, 12:00, 24:00 and 48:00 hours after dosing on day 1 |
| t½ (terminal half-life of fexofenadine in plasma) | Before dose, 0:30, 1:00,1:30, 2:00, 3:00, 4:00, 6:00, 8:00, 10:00, 12:00, 24:00 and 48:00 hours after dosing on day 1 |
| MRTpo (mean residence time of fexofenadine in the body after p.o. administration) | Before dose, 0:30, 1:00,1:30, 2:00, 3:00, 4:00, 6:00, 8:00, 10:00, 12:00, 24:00 and 48:00 hours after dosing on day 1 |
| CL/F (apparent clearance of fexofenadine in plasma following extravascular administration) | Before dose, 0:30, 1:00,1:30, 2:00, 3:00, 4:00, 6:00, 8:00, 10:00, 12:00, 24:00 and 48:00 hours after dosing on day 1 |
| Vz/F (apparent volume of distribution of fexofenadine during the terminal phase λz following an extravascular dose) | Before dose, 0:30, 1:00,1:30, 2:00, 3:00, 4:00, 6:00, 8:00, 10:00, 12:00, 24:00 and 48:00 hours after dosing on day 1 |
| t½ (terminal half-life of dabigatran in plasma at steady state) | Before dose, 0:30, 1:00,1:30, 2:00, 3:00, 4:00, 6:00, 8:00, 10:00, 12:00, 24:00 and 48:00 hours after dosing on day 3 |
| Cpre,ss (pre-dose concentration of dabigatran in plasma immediately before administration of the following dose at steady state) | Before dose on day 3, day 4, and day 5 |
| ID | Term |
|---|---|
| D000069604 | Dabigatran |
| D011802 | Quinidine |
| C093230 | fexofenadine |
| ID | Term |
|---|---|
| D011725 | Pyridines |
| D006573 | Heterocyclic Compounds, 1-Ring |
| D006571 | Heterocyclic Compounds |
| D001562 | Benzimidazoles |
| D006574 | Heterocyclic Compounds, 2-Ring |
| D000072471 | Heterocyclic Compounds, Fused-Ring |
| D002930 | Cinchona Alkaloids |
| D000470 | Alkaloids |
| D011812 | Quinuclidines |
| D006572 | Heterocyclic Compounds, Bridged-Ring |
| D011804 | Quinolines |
Not provided
Not provided