Trial Outcomes & Findings for Bioavailability of Different Applications of Dabigatran in Healthy Volunteers (NCT NCT02171611)
NCT ID: NCT02171611
Last Updated: 2017-05-23
Results Overview
Area under the concentration-time curve of the analyte in plasma over the time interval from 0 extrapolated to infinity (AUC0-inf) for total dabigatran.
Recruitment status
COMPLETED
Study phase
PHASE1
Target enrollment
30 participants
Primary outcome timeframe
-0:30 hour(h) before drug administration and 0:30h, 1:00h, 1:30h, 2:00h, 2:30h, 3:00h, 3:30h, 4:00h, 6:00h, 8:00h, 12:00h, 24:00h, 36:00h and 48:00h after drug administration.
Results posted on
2017-05-23
Participant Flow
Participant milestones
| Measure |
A/B/C
Subjects were treated after an overnight fast of at least 10 hours with single oral dose, started in Period 1 with Dabigatran etexilate 150 mg capsule: Reference (A) with about 240 mL of water and in Period 2 with Dabigatran etexilate 150 mg pellets: Test 1 (B) by sprinkling the pellets on a teaspoon of food and administered immediately to the subject, followed in period 3 with Dabigatran etexilate 150 mg powder: Test 2 (C) resolved in 24 mL reconstitution solution.
Treatments were separated by washout period of at least 7 days after drug administration.
|
A/C/B
Subjects were treated after an overnight fast of at least 10 hours with single oral dose, started in Period 1 with Dabigatran etexilate 150 mg capsule: Reference (A) with about 240 mL of water and in period 2 with Dabigatran etexilate 150 mg powder: Test 2 (C) resolved in 24 mL reconstitution solution, followed in Period 3 with Dabigatran etexilate 150 mg pellets: Test 1 (B) by sprinkling the pellets on a teaspoon of food and administered immediately to the subject.
Treatments were separated by washout period of at least 7 days after drug administration.
|
B/A/C
Subjects were treated after an overnight fast of at least 10 hours with single oral dose, started in Period 1 with Dabigatran etexilate 150 mg pellets: Test 1 (B) by sprinkling the pellets on a teaspoon of food and administered immediately to the subject and in period 2 with Dabigatran etexilate 150 mg capsule: Reference (A) with about 240 mL of water, followed in Period 3 with Dabigatran etexilate 150 mg powder: Test 2 (C) resolved in 24 mL reconstitution solution.
Treatments were separated by washout period of at least 7 days after drug administration.
|
B/C/A
Subjects were treated after an overnight fast of at least 10 hours with single oral dose, started in Period 1 with Dabigatran etexilate 150 mg pellets: Test 1 (B) by sprinkling the pellets on a teaspoon of food and administered immediately to the subject and in period 2 with Dabigatran etexilate 150 mg powder: Test 2 (C) resolved in 24 mL reconstitution solution, followed in period 3 with Dabigatran etexilate 150 mg capsule: Reference (A) with about 240 mL of water.
Treatments were separated by washout period of at least 7 days after drug administration.
|
C/A/B
Subjects were treated after an overnight fast of at least 10 hours with single oral dose, started in Period 1 with Dabigatran etexilate 150 mg powder: Test 2 (C) resolved in 24 mL reconstitution solution and in period 2 with Dabigatran etexilate 150 mg capsule: Reference (A) with about 240 mL of water, followed in Period 3 with Dabigatran etexilate 150 mg pellets: Test 1 (B) by sprinkling the pellets on a teaspoon of food and administered immediately to the subject. Treatments were separated by washout period of at least 7 days after drug administration.
|
C/B/A
Subjects were treated after an overnight fast of at least 10 hours with single oral dose, started in Period 1 with Dabigatran etexilate 150 mg powder: Test 2 (C) resolved in 24 mL reconstitution solution and in period 2 with Dabigatran etexilate 150 mg pellets: Test 1 (B) by sprinkling the pellets on a teaspoon of food and administered immediately to the subject, followed in Period 3 with Dabigatran etexilate 150 mg capsule: Reference (A) with about 240 mL of water.
Treatments were separated by washout period of at least 7 days after drug administration.
|
|---|---|---|---|---|---|---|
|
Overall Study
STARTED
|
5
|
5
|
5
|
5
|
5
|
5
|
|
Overall Study
COMPLETED
|
5
|
5
|
5
|
5
|
5
|
5
|
|
Overall Study
NOT COMPLETED
|
0
|
0
|
0
|
0
|
0
|
0
|
Reasons for withdrawal
Withdrawal data not reported
Baseline Characteristics
Bioavailability of Different Applications of Dabigatran in Healthy Volunteers
Baseline characteristics by cohort
| Measure |
Overall
n=30 Participants
This study is open-label, single dose, randomised, three-way crossover design having 3 treatment periods ie., Dabigatran etexilate 150 mg formulation capsule: Reference (A), Dabigatran etexilate 150 mg formulation pellets: Test 1 (B) and Dabigatran etexilate 150 mg formulation powder: Test 2 (C)
|
|---|---|
|
Age, Continuous
|
39.8 Years
STANDARD_DEVIATION 8.2 • n=99 Participants
|
|
Sex: Female, Male
Female
|
10 Participants
n=99 Participants
|
|
Sex: Female, Male
Male
|
20 Participants
n=99 Participants
|
PRIMARY outcome
Timeframe: -0:30 hour(h) before drug administration and 0:30h, 1:00h, 1:30h, 2:00h, 2:30h, 3:00h, 3:30h, 4:00h, 6:00h, 8:00h, 12:00h, 24:00h, 36:00h and 48:00h after drug administration.Population: PK-Per protocol set (PK-PPS): This subject set included all subjects in the treated set who provided at least one observation for at least one primary (PK) endpoint without important protocol violations with respect to the evaluation of relative bioavailability and who did not vomit at or before 2 times the median tmax.
Area under the concentration-time curve of the analyte in plasma over the time interval from 0 extrapolated to infinity (AUC0-inf) for total dabigatran.
Outcome measures
| Measure |
Dabigatran Etexilate 150 mg Capsule: Reference (A)
n=30 Participants
Subjects were treated with single oral dose of Dabigatran etexilate 150 mg formulation capsule: Reference (A) after an overnight fast of at least 10 hours with about 240 milliliter (mL) of water.
|
Dabigatran Etexilate 150 mg Pellets: Test 1 (B)
n=30 Participants
Subjects were treated with single oral dose of Dabigatran etexilate 150 mg formulation pellets: Test 1 (B) after an overnight fast of at least 10 hours. Pellets were sprinkled on a teaspoon of food and administered immediately to the subject.
|
Dabigatran Etexilate 150 mg Powder: Test 2 (C)
n=30 Participants
Subjects were treated with single oral dose of Dabigatran etexilate 150 mg formulation powder: Test 2 (C) resolved in 24 mL reconstitution solution after an overnight fast of at least 10 hours.
|
|---|---|---|---|
|
AUC0-inf for Total Dabigatran
|
599 ng(nanogram)*h(hour)/mL(milliliter)
Geometric Coefficient of Variation 93.3
|
1050 ng(nanogram)*h(hour)/mL(milliliter)
Geometric Coefficient of Variation 33.8
|
928 ng(nanogram)*h(hour)/mL(milliliter)
Geometric Coefficient of Variation 32.8
|
PRIMARY outcome
Timeframe: -0:30 hour(h) before drug administration and 0:30h, 1:00h, 1:30h, 2:00h, 2:30h, 3:00h, 3:30h, 4:00h, 6:00h, 8:00h, 12:00h, 24:00h, 36:00h and 48:00h after drug administration.Population: pharmacokinetic per-protocol set
Area under the concentration-time curve of the analyte in plasma over the time interval from 0 extrapolated to infinity (AUC0-inf) for free dabigatran.
Outcome measures
| Measure |
Dabigatran Etexilate 150 mg Capsule: Reference (A)
n=30 Participants
Subjects were treated with single oral dose of Dabigatran etexilate 150 mg formulation capsule: Reference (A) after an overnight fast of at least 10 hours with about 240 milliliter (mL) of water.
|
Dabigatran Etexilate 150 mg Pellets: Test 1 (B)
n=30 Participants
Subjects were treated with single oral dose of Dabigatran etexilate 150 mg formulation pellets: Test 1 (B) after an overnight fast of at least 10 hours. Pellets were sprinkled on a teaspoon of food and administered immediately to the subject.
|
Dabigatran Etexilate 150 mg Powder: Test 2 (C)
n=30 Participants
Subjects were treated with single oral dose of Dabigatran etexilate 150 mg formulation powder: Test 2 (C) resolved in 24 mL reconstitution solution after an overnight fast of at least 10 hours.
|
|---|---|---|---|
|
AUC0-inf for Free Dabigatran
|
464 ng*h/mL
Geometric Coefficient of Variation 97.3
|
815 ng*h/mL
Geometric Coefficient of Variation 40
|
734 ng*h/mL
Geometric Coefficient of Variation 38.2
|
PRIMARY outcome
Timeframe: -0:30 hour(h) before drug administration and 0:30h, 1:00h, 1:30h, 2:00h, 2:30h, 3:00h, 3:30h, 4:00h, 6:00h, 8:00h, 12:00h, 24:00h, 36:00h and 48:00h after drug administration.Population: pharmacokinetic per-protocol set
Maximum measured concentration of the analyte in plasma (Cmax) for total dabigatran.
Outcome measures
| Measure |
Dabigatran Etexilate 150 mg Capsule: Reference (A)
n=30 Participants
Subjects were treated with single oral dose of Dabigatran etexilate 150 mg formulation capsule: Reference (A) after an overnight fast of at least 10 hours with about 240 milliliter (mL) of water.
|
Dabigatran Etexilate 150 mg Pellets: Test 1 (B)
n=30 Participants
Subjects were treated with single oral dose of Dabigatran etexilate 150 mg formulation pellets: Test 1 (B) after an overnight fast of at least 10 hours. Pellets were sprinkled on a teaspoon of food and administered immediately to the subject.
|
Dabigatran Etexilate 150 mg Powder: Test 2 (C)
n=30 Participants
Subjects were treated with single oral dose of Dabigatran etexilate 150 mg formulation powder: Test 2 (C) resolved in 24 mL reconstitution solution after an overnight fast of at least 10 hours.
|
|---|---|---|---|
|
Cmax for Total Dabigatran
|
74.6 ng/mL
Geometric Coefficient of Variation 110
|
139 ng/mL
Geometric Coefficient of Variation 37.8
|
124 ng/mL
Geometric Coefficient of Variation 37
|
PRIMARY outcome
Timeframe: -0:30 hour(h) before drug administration and 0:30h, 1:00h, 1:30h, 2:00h, 2:30h, 3:00h, 3:30h, 4:00h, 6:00h, 8:00h, 12:00h, 24:00h, 36:00h and 48:00h after drug administration.Population: pharmacokinetic per-protocol set
Maximum measured concentration of the analyte in plasma (Cmax) for free dabigatran
Outcome measures
| Measure |
Dabigatran Etexilate 150 mg Capsule: Reference (A)
n=30 Participants
Subjects were treated with single oral dose of Dabigatran etexilate 150 mg formulation capsule: Reference (A) after an overnight fast of at least 10 hours with about 240 milliliter (mL) of water.
|
Dabigatran Etexilate 150 mg Pellets: Test 1 (B)
n=30 Participants
Subjects were treated with single oral dose of Dabigatran etexilate 150 mg formulation pellets: Test 1 (B) after an overnight fast of at least 10 hours. Pellets were sprinkled on a teaspoon of food and administered immediately to the subject.
|
Dabigatran Etexilate 150 mg Powder: Test 2 (C)
n=30 Participants
Subjects were treated with single oral dose of Dabigatran etexilate 150 mg formulation powder: Test 2 (C) resolved in 24 mL reconstitution solution after an overnight fast of at least 10 hours.
|
|---|---|---|---|
|
Cmax for Free Dabigatran
|
61.5 ng/mL
Geometric Coefficient of Variation 110
|
112 ng/mL
Geometric Coefficient of Variation 40.4
|
103 ng/mL
Geometric Coefficient of Variation 40.7
|
SECONDARY outcome
Timeframe: -0:30 hour(h) before drug administration and 0:30h, 1:00h, 1:30h, 2:00h, 2:30h, 3:00h, 3:30h, 4:00h, 6:00h, 8:00h, 12:00h, 24:00h, 36:00h and 48:00h after drug administration.Population: pharmacokinetic per-protocol set
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 (AUC0-tz) for total dabigatran.
Outcome measures
| Measure |
Dabigatran Etexilate 150 mg Capsule: Reference (A)
n=30 Participants
Subjects were treated with single oral dose of Dabigatran etexilate 150 mg formulation capsule: Reference (A) after an overnight fast of at least 10 hours with about 240 milliliter (mL) of water.
|
Dabigatran Etexilate 150 mg Pellets: Test 1 (B)
n=30 Participants
Subjects were treated with single oral dose of Dabigatran etexilate 150 mg formulation pellets: Test 1 (B) after an overnight fast of at least 10 hours. Pellets were sprinkled on a teaspoon of food and administered immediately to the subject.
|
Dabigatran Etexilate 150 mg Powder: Test 2 (C)
n=30 Participants
Subjects were treated with single oral dose of Dabigatran etexilate 150 mg formulation powder: Test 2 (C) resolved in 24 mL reconstitution solution after an overnight fast of at least 10 hours.
|
|---|---|---|---|
|
AUC0-tz for Total Dabigatran
|
565 ng*h/mL
Geometric Coefficient of Variation 106
|
1030 ng*h/mL
Geometric Coefficient of Variation 34.2
|
908 ng*h/mL
Geometric Coefficient of Variation 33.5
|
SECONDARY outcome
Timeframe: -0:30 hour(h) before drug administration and 0:30h, 1:00h, 1:30h, 2:00h, 2:30h, 3:00h, 3:30h, 4:00h, 6:00h, 8:00h, 12:00h, 24:00h, 36:00h and 48:00h after drug administration.Population: pharmacokinetic per-protocol set
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 (AUC0-tz) for free dabigatran.
Outcome measures
| Measure |
Dabigatran Etexilate 150 mg Capsule: Reference (A)
n=30 Participants
Subjects were treated with single oral dose of Dabigatran etexilate 150 mg formulation capsule: Reference (A) after an overnight fast of at least 10 hours with about 240 milliliter (mL) of water.
|
Dabigatran Etexilate 150 mg Pellets: Test 1 (B)
n=30 Participants
Subjects were treated with single oral dose of Dabigatran etexilate 150 mg formulation pellets: Test 1 (B) after an overnight fast of at least 10 hours. Pellets were sprinkled on a teaspoon of food and administered immediately to the subject.
|
Dabigatran Etexilate 150 mg Powder: Test 2 (C)
n=30 Participants
Subjects were treated with single oral dose of Dabigatran etexilate 150 mg formulation powder: Test 2 (C) resolved in 24 mL reconstitution solution after an overnight fast of at least 10 hours.
|
|---|---|---|---|
|
AUC0-tz for Free Dabigatran
|
436 ng*h/mL
Geometric Coefficient of Variation 110
|
794 ng*h/mL
Geometric Coefficient of Variation 41.3
|
715 ng*h/mL
Geometric Coefficient of Variation 39.5
|
SECONDARY outcome
Timeframe: -0:30 hour(h) before drug administration and 0:30h, 1:00h, 1:30h, 2:00h, 2:30h, 3:00h, 3:30h, 4:00h, 6:00h, 8:00h, 12:00h, 24:00h, 36:00h and 48:00h after drug administration.Population: pharmacokinetic per-protocol set
Time from dosing to the maximum concentration of the analyte in plasma (tmax) for total dabigatran
Outcome measures
| Measure |
Dabigatran Etexilate 150 mg Capsule: Reference (A)
n=30 Participants
Subjects were treated with single oral dose of Dabigatran etexilate 150 mg formulation capsule: Reference (A) after an overnight fast of at least 10 hours with about 240 milliliter (mL) of water.
|
Dabigatran Etexilate 150 mg Pellets: Test 1 (B)
n=30 Participants
Subjects were treated with single oral dose of Dabigatran etexilate 150 mg formulation pellets: Test 1 (B) after an overnight fast of at least 10 hours. Pellets were sprinkled on a teaspoon of food and administered immediately to the subject.
|
Dabigatran Etexilate 150 mg Powder: Test 2 (C)
n=30 Participants
Subjects were treated with single oral dose of Dabigatran etexilate 150 mg formulation powder: Test 2 (C) resolved in 24 mL reconstitution solution after an overnight fast of at least 10 hours.
|
|---|---|---|---|
|
Tmax for Total Dabigatran
|
2.0 hour
Interval 1.5 to 6.0
|
1.5 hour
Interval 1.0 to 3.0
|
1.5 hour
Interval 1.0 to 2.5
|
SECONDARY outcome
Timeframe: -0:30 hour(h) before drug administration and 0:30h, 1:00h, 1:30h, 2:00h, 2:30h, 3:00h, 3:30h, 4:00h, 6:00h, 8:00h, 12:00h, 24:00h, 36:00h and 48:00h after drug administration.Population: pharmacokinetic per-protocol set
Time from dosing to the maximum concentration of the analyte in plasma (tmax) for free dabigatran
Outcome measures
| Measure |
Dabigatran Etexilate 150 mg Capsule: Reference (A)
n=30 Participants
Subjects were treated with single oral dose of Dabigatran etexilate 150 mg formulation capsule: Reference (A) after an overnight fast of at least 10 hours with about 240 milliliter (mL) of water.
|
Dabigatran Etexilate 150 mg Pellets: Test 1 (B)
n=30 Participants
Subjects were treated with single oral dose of Dabigatran etexilate 150 mg formulation pellets: Test 1 (B) after an overnight fast of at least 10 hours. Pellets were sprinkled on a teaspoon of food and administered immediately to the subject.
|
Dabigatran Etexilate 150 mg Powder: Test 2 (C)
n=30 Participants
Subjects were treated with single oral dose of Dabigatran etexilate 150 mg formulation powder: Test 2 (C) resolved in 24 mL reconstitution solution after an overnight fast of at least 10 hours.
|
|---|---|---|---|
|
Tmax for Free Dabigatran
|
2.0 hour
Interval 1.5 to 6.0
|
1.51 hour
Interval 1.0 to 3.0
|
1.5 hour
Interval 1.0 to 2.0
|
SECONDARY outcome
Timeframe: -0:30 hour(h) before drug administration and 0:30h, 1:00h, 1:30h, 2:00h, 2:30h, 3:00h, 3:30h, 4:00h, 6:00h, 8:00h, 12:00h, 24:00h, 36:00h and 48:00h after drug administration.Population: pharmacokinetic per-protocol set
Terminal rate constant in plasma (λz) for total dabigatran.
Outcome measures
| Measure |
Dabigatran Etexilate 150 mg Capsule: Reference (A)
n=30 Participants
Subjects were treated with single oral dose of Dabigatran etexilate 150 mg formulation capsule: Reference (A) after an overnight fast of at least 10 hours with about 240 milliliter (mL) of water.
|
Dabigatran Etexilate 150 mg Pellets: Test 1 (B)
n=30 Participants
Subjects were treated with single oral dose of Dabigatran etexilate 150 mg formulation pellets: Test 1 (B) after an overnight fast of at least 10 hours. Pellets were sprinkled on a teaspoon of food and administered immediately to the subject.
|
Dabigatran Etexilate 150 mg Powder: Test 2 (C)
n=30 Participants
Subjects were treated with single oral dose of Dabigatran etexilate 150 mg formulation powder: Test 2 (C) resolved in 24 mL reconstitution solution after an overnight fast of at least 10 hours.
|
|---|---|---|---|
|
λz for Total Dabigatran
|
0.079 1/hour
Geometric Coefficient of Variation 13.5
|
0.074 1/hour
Geometric Coefficient of Variation 14.5
|
0.0756 1/hour
Geometric Coefficient of Variation 16.4
|
SECONDARY outcome
Timeframe: -0:30 hour(h) before drug administration and 0:30h, 1:00h, 1:30h, 2:00h, 2:30h, 3:00h, 3:30h, 4:00h, 6:00h, 8:00h, 12:00h, 24:00h, 36:00h and 48:00h after drug administration.Population: pharmacokinetic per-protocol set
Outcome measures
| Measure |
Dabigatran Etexilate 150 mg Capsule: Reference (A)
n=30 Participants
Subjects were treated with single oral dose of Dabigatran etexilate 150 mg formulation capsule: Reference (A) after an overnight fast of at least 10 hours with about 240 milliliter (mL) of water.
|
Dabigatran Etexilate 150 mg Pellets: Test 1 (B)
n=30 Participants
Subjects were treated with single oral dose of Dabigatran etexilate 150 mg formulation pellets: Test 1 (B) after an overnight fast of at least 10 hours. Pellets were sprinkled on a teaspoon of food and administered immediately to the subject.
|
Dabigatran Etexilate 150 mg Powder: Test 2 (C)
n=30 Participants
Subjects were treated with single oral dose of Dabigatran etexilate 150 mg formulation powder: Test 2 (C) resolved in 24 mL reconstitution solution after an overnight fast of at least 10 hours.
|
|---|---|---|---|
|
λz for Free Dabigatran
|
0.091 1/hour
Geometric Coefficient of Variation 16
|
0.0811 1/hour
Geometric Coefficient of Variation 18.6
|
0.0893 1/hour
Geometric Coefficient of Variation 15.7
|
SECONDARY outcome
Timeframe: -0:30 hour(h) before drug administration and 0:30h, 1:00h, 1:30h, 2:00h, 2:30h, 3:00h, 3:30h, 4:00h, 6:00h, 8:00h, 12:00h, 24:00h, 36:00h and 48:00h after drug administration.Population: pharmacokinetic per-protocol set
Terminal half-life of the analyte in plasma (t1/2) for total dabigatran
Outcome measures
| Measure |
Dabigatran Etexilate 150 mg Capsule: Reference (A)
n=30 Participants
Subjects were treated with single oral dose of Dabigatran etexilate 150 mg formulation capsule: Reference (A) after an overnight fast of at least 10 hours with about 240 milliliter (mL) of water.
|
Dabigatran Etexilate 150 mg Pellets: Test 1 (B)
n=30 Participants
Subjects were treated with single oral dose of Dabigatran etexilate 150 mg formulation pellets: Test 1 (B) after an overnight fast of at least 10 hours. Pellets were sprinkled on a teaspoon of food and administered immediately to the subject.
|
Dabigatran Etexilate 150 mg Powder: Test 2 (C)
n=30 Participants
Subjects were treated with single oral dose of Dabigatran etexilate 150 mg formulation powder: Test 2 (C) resolved in 24 mL reconstitution solution after an overnight fast of at least 10 hours.
|
|---|---|---|---|
|
t1/2 for Total Dabigatran
|
8.77 hour
Geometric Coefficient of Variation 13.5
|
9.37 hour
Geometric Coefficient of Variation 14.5
|
9.16 hour
Geometric Coefficient of Variation 16.4
|
SECONDARY outcome
Timeframe: -0:30 hour(h) before drug administration and 0:30h, 1:00h, 1:30h, 2:00h, 2:30h, 3:00h, 3:30h, 4:00h, 6:00h, 8:00h, 12:00h, 24:00h, 36:00h and 48:00h after drug administration.Population: pharmacokinetic per-protocol set
Terminal half-life of the analyte in plasma (t1/2) for free dabigatran.
Outcome measures
| Measure |
Dabigatran Etexilate 150 mg Capsule: Reference (A)
n=30 Participants
Subjects were treated with single oral dose of Dabigatran etexilate 150 mg formulation capsule: Reference (A) after an overnight fast of at least 10 hours with about 240 milliliter (mL) of water.
|
Dabigatran Etexilate 150 mg Pellets: Test 1 (B)
n=30 Participants
Subjects were treated with single oral dose of Dabigatran etexilate 150 mg formulation pellets: Test 1 (B) after an overnight fast of at least 10 hours. Pellets were sprinkled on a teaspoon of food and administered immediately to the subject.
|
Dabigatran Etexilate 150 mg Powder: Test 2 (C)
n=30 Participants
Subjects were treated with single oral dose of Dabigatran etexilate 150 mg formulation powder: Test 2 (C) resolved in 24 mL reconstitution solution after an overnight fast of at least 10 hours.
|
|---|---|---|---|
|
t1/2 for Free Dabigatran
|
7.62 hour
Geometric Coefficient of Variation 16
|
8.54 hour
Geometric Coefficient of Variation 18.6
|
7.76 hour
Geometric Coefficient of Variation 15.7
|
SECONDARY outcome
Timeframe: -0:30 hour(h) before drug administration and 0:30h, 1:00h, 1:30h, 2:00h, 2:30h, 3:00h, 3:30h, 4:00h, 6:00h, 8:00h, 12:00h, 24:00h, 36:00h and 48:00h after drug administration.Population: pharmacokinetic per-protocol set
Mean residence time of the analyte in the body after po administration (MRTpo) for total dabigatran.
Outcome measures
| Measure |
Dabigatran Etexilate 150 mg Capsule: Reference (A)
n=30 Participants
Subjects were treated with single oral dose of Dabigatran etexilate 150 mg formulation capsule: Reference (A) after an overnight fast of at least 10 hours with about 240 milliliter (mL) of water.
|
Dabigatran Etexilate 150 mg Pellets: Test 1 (B)
n=30 Participants
Subjects were treated with single oral dose of Dabigatran etexilate 150 mg formulation pellets: Test 1 (B) after an overnight fast of at least 10 hours. Pellets were sprinkled on a teaspoon of food and administered immediately to the subject.
|
Dabigatran Etexilate 150 mg Powder: Test 2 (C)
n=30 Participants
Subjects were treated with single oral dose of Dabigatran etexilate 150 mg formulation powder: Test 2 (C) resolved in 24 mL reconstitution solution after an overnight fast of at least 10 hours.
|
|---|---|---|---|
|
MRTpo for Total Dabigatran
|
10.8 hour
Geometric Coefficient of Variation 12
|
10.1 hour
Geometric Coefficient of Variation 11.4
|
10 hour
Geometric Coefficient of Variation 12.2
|
SECONDARY outcome
Timeframe: -0:30 hour(h) before drug administration and 0:30h, 1:00h, 1:30h, 2:00h, 2:30h, 3:00h, 3:30h, 4:00h, 6:00h, 8:00h, 12:00h, 24:00h, 36:00h and 48:00h after drug administration.Population: pharmacokinetic per-protocol set
Mean residence time of the analyte in the body after po administration (MRTpo) for free dabigatran.
Outcome measures
| Measure |
Dabigatran Etexilate 150 mg Capsule: Reference (A)
n=30 Participants
Subjects were treated with single oral dose of Dabigatran etexilate 150 mg formulation capsule: Reference (A) after an overnight fast of at least 10 hours with about 240 milliliter (mL) of water.
|
Dabigatran Etexilate 150 mg Pellets: Test 1 (B)
n=30 Participants
Subjects were treated with single oral dose of Dabigatran etexilate 150 mg formulation pellets: Test 1 (B) after an overnight fast of at least 10 hours. Pellets were sprinkled on a teaspoon of food and administered immediately to the subject.
|
Dabigatran Etexilate 150 mg Powder: Test 2 (C)
n=30 Participants
Subjects were treated with single oral dose of Dabigatran etexilate 150 mg formulation powder: Test 2 (C) resolved in 24 mL reconstitution solution after an overnight fast of at least 10 hours.
|
|---|---|---|---|
|
MRTpo for Free Dabigatran
|
9.9 hour
Geometric Coefficient of Variation 14.0
|
9.58 hour
Geometric Coefficient of Variation 14.1
|
9.15 hour
Geometric Coefficient of Variation 12.2
|
SECONDARY outcome
Timeframe: -0:30 hour(h) before drug administration and 0:30h, 1:00h, 1:30h, 2:00h, 2:30h, 3:00h, 3:30h, 4:00h, 6:00h, 8:00h, 12:00h, 24:00h, 36:00h and 48:00h after drug administration.Population: pharmacokinetic per-protocol set
Apparent clearance of the analyte in plasma following extravascular administration (CL/F) for total dabigatran.
Outcome measures
| Measure |
Dabigatran Etexilate 150 mg Capsule: Reference (A)
n=30 Participants
Subjects were treated with single oral dose of Dabigatran etexilate 150 mg formulation capsule: Reference (A) after an overnight fast of at least 10 hours with about 240 milliliter (mL) of water.
|
Dabigatran Etexilate 150 mg Pellets: Test 1 (B)
n=30 Participants
Subjects were treated with single oral dose of Dabigatran etexilate 150 mg formulation pellets: Test 1 (B) after an overnight fast of at least 10 hours. Pellets were sprinkled on a teaspoon of food and administered immediately to the subject.
|
Dabigatran Etexilate 150 mg Powder: Test 2 (C)
n=30 Participants
Subjects were treated with single oral dose of Dabigatran etexilate 150 mg formulation powder: Test 2 (C) resolved in 24 mL reconstitution solution after an overnight fast of at least 10 hours.
|
|---|---|---|---|
|
CL/F for Total Dabigatran
|
3130 mL (milliliter)/min (minute)
Geometric Coefficient of Variation 93.3
|
1790 mL (milliliter)/min (minute)
Geometric Coefficient of Variation 33.8
|
2020 mL (milliliter)/min (minute)
Geometric Coefficient of Variation 32.8
|
SECONDARY outcome
Timeframe: -0:30 hour(h) before drug administration and 0:30h, 1:00h, 1:30h, 2:00h, 2:30h, 3:00h, 3:30h, 4:00h, 6:00h, 8:00h, 12:00h, 24:00h, 36:00h and 48:00h after drug administration.Population: pharmacokinetic per-protocol set
Apparent clearance of the analyte in plasma following extravascular administration (CL/F) for free dabigatran.
Outcome measures
| Measure |
Dabigatran Etexilate 150 mg Capsule: Reference (A)
n=30 Participants
Subjects were treated with single oral dose of Dabigatran etexilate 150 mg formulation capsule: Reference (A) after an overnight fast of at least 10 hours with about 240 milliliter (mL) of water.
|
Dabigatran Etexilate 150 mg Pellets: Test 1 (B)
n=30 Participants
Subjects were treated with single oral dose of Dabigatran etexilate 150 mg formulation pellets: Test 1 (B) after an overnight fast of at least 10 hours. Pellets were sprinkled on a teaspoon of food and administered immediately to the subject.
|
Dabigatran Etexilate 150 mg Powder: Test 2 (C)
n=30 Participants
Subjects were treated with single oral dose of Dabigatran etexilate 150 mg formulation powder: Test 2 (C) resolved in 24 mL reconstitution solution after an overnight fast of at least 10 hours.
|
|---|---|---|---|
|
CL/F for Free Dabigatran
|
4040 mL (milliliter)/min (minute)
Geometric Coefficient of Variation 97.3
|
2310 mL (milliliter)/min (minute)
Geometric Coefficient of Variation 40
|
2560 mL (milliliter)/min (minute)
Geometric Coefficient of Variation 38.2
|
SECONDARY outcome
Timeframe: -0:30 hour(h) before drug administration and 0:30h, 1:00h, 1:30h, 2:00h, 2:30h, 3:00h, 3:30h, 4:00h, 6:00h, 8:00h, 12:00h, 24:00h, 36:00h and 48:00h after drug administration.Population: pharmacokinetic per-protocol set
Apparent volume of distribution during the terminal phase λz following an extravascular dose (Vz/F) for total dabigatran.
Outcome measures
| Measure |
Dabigatran Etexilate 150 mg Capsule: Reference (A)
n=30 Participants
Subjects were treated with single oral dose of Dabigatran etexilate 150 mg formulation capsule: Reference (A) after an overnight fast of at least 10 hours with about 240 milliliter (mL) of water.
|
Dabigatran Etexilate 150 mg Pellets: Test 1 (B)
n=30 Participants
Subjects were treated with single oral dose of Dabigatran etexilate 150 mg formulation pellets: Test 1 (B) after an overnight fast of at least 10 hours. Pellets were sprinkled on a teaspoon of food and administered immediately to the subject.
|
Dabigatran Etexilate 150 mg Powder: Test 2 (C)
n=30 Participants
Subjects were treated with single oral dose of Dabigatran etexilate 150 mg formulation powder: Test 2 (C) resolved in 24 mL reconstitution solution after an overnight fast of at least 10 hours.
|
|---|---|---|---|
|
Vz/F for Total Dabigatran
|
2380 Liter
Geometric Coefficient of Variation 92.8
|
1450 Liter
Geometric Coefficient of Variation 35
|
1610 Liter
Geometric Coefficient of Variation 35.9
|
SECONDARY outcome
Timeframe: -0:30 hour(h) before drug administration and 0:30h, 1:00h, 1:30h, 2:00h, 2:30h, 3:00h, 3:30h, 4:00h, 6:00h, 8:00h, 12:00h, 24:00h, 36:00h and 48:00h after drug administration.Population: pharmacokinetic per-protocol set
Apparent volume of distribution during the terminal phase λz following an extravascular dose (Vz/F) for free dabigatran.
Outcome measures
| Measure |
Dabigatran Etexilate 150 mg Capsule: Reference (A)
n=30 Participants
Subjects were treated with single oral dose of Dabigatran etexilate 150 mg formulation capsule: Reference (A) after an overnight fast of at least 10 hours with about 240 milliliter (mL) of water.
|
Dabigatran Etexilate 150 mg Pellets: Test 1 (B)
n=30 Participants
Subjects were treated with single oral dose of Dabigatran etexilate 150 mg formulation pellets: Test 1 (B) after an overnight fast of at least 10 hours. Pellets were sprinkled on a teaspoon of food and administered immediately to the subject.
|
Dabigatran Etexilate 150 mg Powder: Test 2 (C)
n=30 Participants
Subjects were treated with single oral dose of Dabigatran etexilate 150 mg formulation powder: Test 2 (C) resolved in 24 mL reconstitution solution after an overnight fast of at least 10 hours.
|
|---|---|---|---|
|
Vz/F for Free Dabigatran
|
2670 Liter
Geometric Coefficient of Variation 91
|
1700 Liter
Geometric Coefficient of Variation 41.4
|
1720 Liter
Geometric Coefficient of Variation 37.6
|
SECONDARY outcome
Timeframe: From first drug administration until 7 days after the last drug administration of Dabigatran, ie., up to 10 days.Population: Treated Set
Percentage of participants with findings in Physical examination, Vital signs (blood pressure (BP), pulse rate (PR)), 12-lead ECG (electrocardiogram), Clinical laboratory tests (haematology, clinical chemistry and urinalysis). Relevant findings or worsening of baseline conditions were reported as Adverse events. There were no clinically relevant finding reported for Physical examination, Vital signs (blood pressure, pulse rate), 12-lead ECG and Clinical laboratory tests.
Outcome measures
| Measure |
Dabigatran Etexilate 150 mg Capsule: Reference (A)
n=30 Participants
Subjects were treated with single oral dose of Dabigatran etexilate 150 mg formulation capsule: Reference (A) after an overnight fast of at least 10 hours with about 240 milliliter (mL) of water.
|
Dabigatran Etexilate 150 mg Pellets: Test 1 (B)
n=30 Participants
Subjects were treated with single oral dose of Dabigatran etexilate 150 mg formulation pellets: Test 1 (B) after an overnight fast of at least 10 hours. Pellets were sprinkled on a teaspoon of food and administered immediately to the subject.
|
Dabigatran Etexilate 150 mg Powder: Test 2 (C)
n=30 Participants
Subjects were treated with single oral dose of Dabigatran etexilate 150 mg formulation powder: Test 2 (C) resolved in 24 mL reconstitution solution after an overnight fast of at least 10 hours.
|
|---|---|---|---|
|
Percentage of Participants With Findings in Physical Examination, Vital Signs , Pulse Rate (PR)), 12-lead ECG, Clinical Laboratory Tests.
|
0.0 Percentage of participants
|
0.0 Percentage of participants
|
0.0 Percentage of participants
|
SECONDARY outcome
Timeframe: From first drug administration until 7 days after the last drug administration of Dabigatran, ie., up to 10 days.Population: Treated set
Percentage of participants with investigator defined drug-releated Adverse events.
Outcome measures
| Measure |
Dabigatran Etexilate 150 mg Capsule: Reference (A)
n=30 Participants
Subjects were treated with single oral dose of Dabigatran etexilate 150 mg formulation capsule: Reference (A) after an overnight fast of at least 10 hours with about 240 milliliter (mL) of water.
|
Dabigatran Etexilate 150 mg Pellets: Test 1 (B)
n=30 Participants
Subjects were treated with single oral dose of Dabigatran etexilate 150 mg formulation pellets: Test 1 (B) after an overnight fast of at least 10 hours. Pellets were sprinkled on a teaspoon of food and administered immediately to the subject.
|
Dabigatran Etexilate 150 mg Powder: Test 2 (C)
n=30 Participants
Subjects were treated with single oral dose of Dabigatran etexilate 150 mg formulation powder: Test 2 (C) resolved in 24 mL reconstitution solution after an overnight fast of at least 10 hours.
|
|---|---|---|---|
|
Percentage of Participants With Drug-related Adverse Events
|
6.7 Percentage of participants
|
23.3 Percentage of participants
|
26.7 Percentage of participants
|
SECONDARY outcome
Timeframe: From first drug administration until 7 days after the last drug administration of Dabigatran, ie., up to 10 days.Population: Treated Set
Tolerability will be assessed by the investigator according to the categories good, satisfactory, not satisfactory and bad.
Outcome measures
| Measure |
Dabigatran Etexilate 150 mg Capsule: Reference (A)
n=30 Participants
Subjects were treated with single oral dose of Dabigatran etexilate 150 mg formulation capsule: Reference (A) after an overnight fast of at least 10 hours with about 240 milliliter (mL) of water.
|
Dabigatran Etexilate 150 mg Pellets: Test 1 (B)
n=30 Participants
Subjects were treated with single oral dose of Dabigatran etexilate 150 mg formulation pellets: Test 1 (B) after an overnight fast of at least 10 hours. Pellets were sprinkled on a teaspoon of food and administered immediately to the subject.
|
Dabigatran Etexilate 150 mg Powder: Test 2 (C)
n=30 Participants
Subjects were treated with single oral dose of Dabigatran etexilate 150 mg formulation powder: Test 2 (C) resolved in 24 mL reconstitution solution after an overnight fast of at least 10 hours.
|
|---|---|---|---|
|
Assessment of Tolerability by Investigator.
Satisfactory
|
0.0 Percentage of Participants
|
0.0 Percentage of Participants
|
0.0 Percentage of Participants
|
|
Assessment of Tolerability by Investigator.
Good
|
100.0 Percentage of Participants
|
100.0 Percentage of Participants
|
100.0 Percentage of Participants
|
|
Assessment of Tolerability by Investigator.
Not satisfactory
|
0.0 Percentage of Participants
|
0.0 Percentage of Participants
|
0.0 Percentage of Participants
|
|
Assessment of Tolerability by Investigator.
Bad
|
0.0 Percentage of Participants
|
0.0 Percentage of Participants
|
0.0 Percentage of Participants
|
|
Assessment of Tolerability by Investigator.
Not assessable
|
0.0 Percentage of Participants
|
0.0 Percentage of Participants
|
0.0 Percentage of Participants
|
Adverse Events
Dabigatran Etexilate 150 mg Capsule: Reference (A)
Serious events: 0 serious events
Other events: 2 other events
Deaths: 0 deaths
Dabigatran Etexilate 150 mg Pellets: Test 1 (B)
Serious events: 0 serious events
Other events: 7 other events
Deaths: 0 deaths
Dabigatran Etexilate 150 mg Powder: Test 2 (C)
Serious events: 0 serious events
Other events: 8 other events
Deaths: 0 deaths
Serious adverse events
Adverse event data not reported
Other adverse events
| Measure |
Dabigatran Etexilate 150 mg Capsule: Reference (A)
n=30 participants at risk
Subjects were treated with single oral dose of Dabigatran etexilate 150 mg formulation capsule: Reference (A) after an overnight fast of at least 10 hours with about 240 milliliter (mL) of water.
|
Dabigatran Etexilate 150 mg Pellets: Test 1 (B)
n=30 participants at risk
Subjects were treated with single oral dose of Dabigatran etexilate 150 mg formulation pellets: Test 1 (B) after an overnight fast of at least 10 hours. Pellets were sprinkled on a teaspoon of food and administered immediately to the subject.
|
Dabigatran Etexilate 150 mg Powder: Test 2 (C)
n=30 participants at risk
Subjects were treated with single oral dose of Dabigatran etexilate 150 mg formulation powder: Test 2 (C) resolved in 24 mL reconstitution solution after an overnight fast of at least 10 hours.
|
|---|---|---|---|
|
Gastrointestinal disorders
Abdominal pain upper
|
0.00%
0/30 • From first drug administration until 7 days after the last drug administration of Dabigatran, ie., up to 10 days.
|
6.7%
2/30 • From first drug administration until 7 days after the last drug administration of Dabigatran, ie., up to 10 days.
|
0.00%
0/30 • From first drug administration until 7 days after the last drug administration of Dabigatran, ie., up to 10 days.
|
|
Nervous system disorders
Headache
|
6.7%
2/30 • From first drug administration until 7 days after the last drug administration of Dabigatran, ie., up to 10 days.
|
16.7%
5/30 • From first drug administration until 7 days after the last drug administration of Dabigatran, ie., up to 10 days.
|
26.7%
8/30 • From first drug administration until 7 days after the last drug administration of Dabigatran, ie., up to 10 days.
|
Additional Information
Boehringer Ingelheim, Call Center
Boehringer Ingelheim
Phone: 1-800-243-0127
Email: [email protected]
Results disclosure agreements
- Principal investigator is a sponsor employee Boehringer Ingelheim (BI) acknowledges that investigators have the right to publish the study results. Investigators shall provide BI with a copy of any publication or presentation for review prior to any submission. Such review will be done with regard to proprietary information, information related to patentable inventions, medical, scientific, and statistical accuracy within 60 days. BI may request a delay of the publication in order to protect BI's intellectual property rights.
- Publication restrictions are in place
Restriction type: OTHER