Trial Outcomes & Findings for A Study in Healthy Humans to Assess the Relative Bioavailability of One Fixed-dose Combination Tablet Empagliflozin/Metformin Versus Jardiance® Tablet and Glifage® Tablet Administered Together (NCT NCT05083949)

NCT ID: NCT05083949

Last Updated: 2023-07-27

Results Overview

Area under the concentration-time curve of empagliflozin in plasma over the time interval from 0 to the last quantifiable data point (AUC0-tz) normalized to the actual administered dose is presented. The AUC0-tz was divided by the actual dose strength to get the normalized area under the concentration-time curve. The statistical model used for the analysis of the primary endpoints was an analysis of variance (ANOVA) on the logarithmic scale. That is, the PK endpoints were log-transformed (natural logarithm) prior to fitting the ANOVA model. This model included effects accounting for the following sources of variation: sequence, subjects within sequences, period and treatment. The effect 'subjects within sequences' was considered as random, whereas the other effects were considered as fixed. Unit of measure:(hour\*nanogram/milliliter)/milligram.

Recruitment status

COMPLETED

Study phase

PHASE1

Target enrollment

32 participants

Primary outcome timeframe

Within 5 minutes (min) before and 15min, 30min, 45min, 1h, 1h15min, 1h30min, 1h45min, 2h, 2h20min, 2h40min, 3h, 3h30min, 4h, 4h30min, 5h, 5h30min, 6h, 7h, 8h, 10h, 12h, 24h, 48h, and 72h after treatment administration for both arms.

Results posted on

2023-07-27

Participant Flow

This was a phase I, randomised, open label, 2x2 crossover trial in healthy male and female subjects to establish the bioequivalence of 1 Fixed dose combination tablet 12.5 mg empagliflozin/850 mg metformin (treatment B) to the reference treatments (treatment A) which consisted in 1 tablet empagliflozin10 mg (Reference 1) + 1 tablet Glifage® 850 mg (Reference 2).

All subjects were screened for eligibility prior to participation in the trial. Subjects attended a specialist site which ensured that they (the subjects) strictly met all inclusion and none of the exclusion criteria. Subjects were not to be allocated to a treatment group if any of the entry criteria were violated.

Participant milestones

Participant milestones
Measure
(A): Empagliflozin 10mg (R1)+Glifage® 850mg (R2),Then (B): FDC 12.5mg Empagliflozin/850mg Metformin
On Day 1 of Period 1 participants received treatment A: Single dose tablet of 10 milligram(mg) empagliflozin film-coated and a 850mg of metformin hydrochloride (HCl) (Glifage®) tablet, orally with 200 milliliter(mL) of water. On Day 1 of Period 2 participants received treatment B: Fixed dose combination (FDC) tablet of 12.5mg empagliflozin/850 mg metformin HCl, orally with 200mL of water. A high-fat, high-calorie meal was served 30 minutes(min) before drug administration. The treatments were separated by a wash-out phase of at least 7 days.
(B): FDC 12.5mg Empagliflozin/850mg Metformin,Then (A): Empagliflozin 10mg(R1) + Glifage® 850mg(R2)
On Day 1 of Period 1 participants received treatment B: Fixed dose combination (FDC) tablet containing 12.5 milligram (mg) empagliflozin/850 mg metformin hydrochloride (HCl), orally with 200 milliliter (mL) of water. On Day 1 of Period 2 participants received treatment A: Single dose tablet of 10mg empagliflozin and 850 mg of metformin HCl (Glifage®) tablet, orally with 200mL of water. A high-fat, high-calorie meal was served 30 minutes (min) before drug administration. The treatments were separated by a wash-out phase of at least 7 days.
Period 1
STARTED
16
16
Period 1
COMPLETED
13
14
Period 1
NOT COMPLETED
3
2
Wash-out
STARTED
13
14
Wash-out
COMPLETED
13
14
Wash-out
NOT COMPLETED
0
0
Period 2
STARTED
13
14
Period 2
COMPLETED
12
12
Period 2
NOT COMPLETED
1
2

Reasons for withdrawal

Reasons for withdrawal
Measure
(A): Empagliflozin 10mg (R1)+Glifage® 850mg (R2),Then (B): FDC 12.5mg Empagliflozin/850mg Metformin
On Day 1 of Period 1 participants received treatment A: Single dose tablet of 10 milligram(mg) empagliflozin film-coated and a 850mg of metformin hydrochloride (HCl) (Glifage®) tablet, orally with 200 milliliter(mL) of water. On Day 1 of Period 2 participants received treatment B: Fixed dose combination (FDC) tablet of 12.5mg empagliflozin/850 mg metformin HCl, orally with 200mL of water. A high-fat, high-calorie meal was served 30 minutes(min) before drug administration. The treatments were separated by a wash-out phase of at least 7 days.
(B): FDC 12.5mg Empagliflozin/850mg Metformin,Then (A): Empagliflozin 10mg(R1) + Glifage® 850mg(R2)
On Day 1 of Period 1 participants received treatment B: Fixed dose combination (FDC) tablet containing 12.5 milligram (mg) empagliflozin/850 mg metformin hydrochloride (HCl), orally with 200 milliliter (mL) of water. On Day 1 of Period 2 participants received treatment A: Single dose tablet of 10mg empagliflozin and 850 mg of metformin HCl (Glifage®) tablet, orally with 200mL of water. A high-fat, high-calorie meal was served 30 minutes (min) before drug administration. The treatments were separated by a wash-out phase of at least 7 days.
Period 1
Positive doping for Tetrahydrocannabinol (THC)
2
1
Period 1
Adverse Event
1
1
Period 2
The patient was not able to eat the full content of the breakfast
1
0
Period 2
Adverse Event
0
2

Baseline Characteristics

A Study in Healthy Humans to Assess the Relative Bioavailability of One Fixed-dose Combination Tablet Empagliflozin/Metformin Versus Jardiance® Tablet and Glifage® Tablet Administered Together

Baseline characteristics by cohort

Baseline characteristics by cohort
Measure
(A): Empagliflozin 10mg (R1)+Glifage® 850mg (R2),Then (B): FDC 12.5mg Empagliflozin/850mg Metformin
n=16 Participants
On Day 1 of Period 1 participants received treatment A: Single dose tablet of 10 milligram(mg) empagliflozin film-coated and a 850mg of metformin hydrochloride (HCl) (Glifage®) tablet, orally with 200 milliliter(mL) of water. On Day 1 of Period 2 participants received treatment B: Fixed dose combination (FDC) tablet of 12.5mg empagliflozin/850 mg metformin HCl, orally with 200mL of water. A high-fat, high-calorie meal was served 30 minutes(min) before drug administration. The treatments were separated by a wash-out phase of at least 7 days.
(B): FDC 12.5mg Empagliflozin/850mg Metformin,Then (A): Empagliflozin 10mg(R1) + Glifage® 850mg(R2)
n=16 Participants
On Day 1 of Period 1 participants received treatment B: Fixed dose combination (FDC) tablet containing 12.5 milligram (mg) empagliflozin/850 mg metformin hydrochloride (HCl), orally with 200 milliliter (mL) of water. On Day 1 of Period 2 participants received treatment A: Single dose tablet of 10mg empagliflozin and 850 mg of metformin HCl (Glifage®) tablet, orally with 200mL of water. A high-fat, high-calorie meal was served 30 minutes (min) before drug administration. The treatments were separated by a wash-out phase of at least 7 days.
Total
n=32 Participants
Total of all reporting groups
Age, Continuous
32.0 Years
STANDARD_DEVIATION 7.2 • n=39 Participants
31.7 Years
STANDARD_DEVIATION 8.3 • n=41 Participants
31.8 Years
STANDARD_DEVIATION 7.9 • n=35 Participants
Sex: Female, Male
Female
8 Participants
n=39 Participants
8 Participants
n=41 Participants
16 Participants
n=35 Participants
Sex: Female, Male
Male
8 Participants
n=39 Participants
8 Participants
n=41 Participants
16 Participants
n=35 Participants
Race (NIH/OMB)
American Indian or Alaska Native
0 Participants
n=39 Participants
0 Participants
n=41 Participants
0 Participants
n=35 Participants
Race (NIH/OMB)
Asian
0 Participants
n=39 Participants
0 Participants
n=41 Participants
0 Participants
n=35 Participants
Race (NIH/OMB)
Native Hawaiian or Other Pacific Islander
0 Participants
n=39 Participants
0 Participants
n=41 Participants
0 Participants
n=35 Participants
Race (NIH/OMB)
Black or African American
3 Participants
n=39 Participants
2 Participants
n=41 Participants
5 Participants
n=35 Participants
Race (NIH/OMB)
White
7 Participants
n=39 Participants
11 Participants
n=41 Participants
18 Participants
n=35 Participants
Race (NIH/OMB)
More than one race
6 Participants
n=39 Participants
3 Participants
n=41 Participants
9 Participants
n=35 Participants
Race (NIH/OMB)
Unknown or Not Reported
0 Participants
n=39 Participants
0 Participants
n=41 Participants
0 Participants
n=35 Participants

PRIMARY outcome

Timeframe: Within 5 minutes (min) before and 15min, 30min, 45min, 1h, 1h15min, 1h30min, 1h45min, 2h, 2h20min, 2h40min, 3h, 3h30min, 4h, 4h30min, 5h, 5h30min, 6h, 7h, 8h, 10h, 12h, 24h, 48h, and 72h after treatment administration for both arms.

Population: Pharmacokinetic (PK) parameter analysis set (PKS): This set included all subjects who provided all PK endpoints for all treatment periods that were defined as primary (Cmax and AUCo-tz) and was not excluded due to a protocol violation relevant to the evaluation of PK or due to PK non-evaluability. Only subjects with non-missing values were included.

Area under the concentration-time curve of empagliflozin in plasma over the time interval from 0 to the last quantifiable data point (AUC0-tz) normalized to the actual administered dose is presented. The AUC0-tz was divided by the actual dose strength to get the normalized area under the concentration-time curve. The statistical model used for the analysis of the primary endpoints was an analysis of variance (ANOVA) on the logarithmic scale. That is, the PK endpoints were log-transformed (natural logarithm) prior to fitting the ANOVA model. This model included effects accounting for the following sources of variation: sequence, subjects within sequences, period and treatment. The effect 'subjects within sequences' was considered as random, whereas the other effects were considered as fixed. Unit of measure:(hour\*nanogram/milliliter)/milligram.

Outcome measures

Outcome measures
Measure
(A): Empagliflozin 10mg (R1) + Metformin (Glifage®) 850mg (R2)
n=24 Participants
Participants received treatment A: Single dose tablet of 10 milligram (mg) empagliflozin film-coated and a 850mg of metformin HCl (Glifage®) tablet, orally with 200 milliliter (mL) of water. A high-fat, high-calorie meal was served 30 minutes (min) before drug administration.
(B): FDC 12.5mg Empagliflozin/850mg Metformin
n=24 Participants
Participants were administered the treatment B which consisted of a single Fixed dose combination (FDC) tablet containing 12.5 milligram (mg) empagliflozin/850 mg metformin HCl, orally with 200 milliliter (mL) of water. A high-fat, high-calorie meal was served 30 minutes (min) before drug administration.
Dose-normalized Area Under the Concentration-time Curve of Empagliflozin in Plasma Over the Time Interval From 0 to the Last Quantifiable Data Point (AUC0-tz)
117.15 (h*ng/mL)/mg
Standard Error NA
The standard error is actually the geometric standard error and is equal to 1.04.
116.65 (h*ng/mL)/mg
Standard Error NA
The standard error is actually the geometric standard error and is equal to 1.04.

PRIMARY outcome

Timeframe: Within 5 minutes (min) before and 15min, 30min, 45min, 1h, 1h15min, 1h30min, 1h45min, 2h, 2h20min, 2h40min, 3h, 3h30min, 4h, 4h30min, 5h, 5h30min, 6h, 7h, 8h, 10h, 12h, 24h, 48h, and 72h after treatment administration for both arms.

Population: Pharmacokinetic (PK) parameter analysis set (PKS): This set included all subjects who provided all PK endpoints for all treatment periods that were defined as primary (Cmax and AUCo-tz) and was not excluded due to a protocol violation relevant to the evaluation of PK or due to PK non-evaluability. Only subjects with non-missing values were included.

Dose-normalized Maximum measured concentration of empagliflozin in plasma is presented. The maximum measured concentration was divided by the actual dose strength to get the dose-normalised Cmax. The statistical model used for the analysis of the primary endpoints was an analysis of variance (ANOVA) on the logarithmic scale. That is, the PK endpoints were log-transformed (natural logarithm) prior to fitting the ANOVA model. This model included effects accounting for the following sources of variation: sequence, subjects within sequences, period and treatment. The effect 'subjects within sequences' was considered as random, whereas the other effects were considered as fixed. The unit of measure reported is: (nanogram/milliliter)/milligram.

Outcome measures

Outcome measures
Measure
(A): Empagliflozin 10mg (R1) + Metformin (Glifage®) 850mg (R2)
n=24 Participants
Participants received treatment A: Single dose tablet of 10 milligram (mg) empagliflozin film-coated and a 850mg of metformin HCl (Glifage®) tablet, orally with 200 milliliter (mL) of water. A high-fat, high-calorie meal was served 30 minutes (min) before drug administration.
(B): FDC 12.5mg Empagliflozin/850mg Metformin
n=24 Participants
Participants were administered the treatment B which consisted of a single Fixed dose combination (FDC) tablet containing 12.5 milligram (mg) empagliflozin/850 mg metformin HCl, orally with 200 milliliter (mL) of water. A high-fat, high-calorie meal was served 30 minutes (min) before drug administration.
Dose-normalized Maximum Measured Concentration of Empagliflozin (Cmax)
13.42 (ng/mL)/mg
Standard Error NA
The standard error is actually the geometric standard error and is equal to 1.03.
13.60 (ng/mL)/mg
Standard Error NA
The standard error is actually the geometric standard error and is equal to 1.03.

PRIMARY outcome

Timeframe: Within 5 minutes(min) before and 15min, 30min, 45min, 1h, 1h15min, 1h30min, 1h45min, 2h, 2h20min, 2h40min, 3h, 3h30min, 4h, 4h30min, 5h, 5h30min, 6h, 7h, 8h, 10h, 12h, 24h, 48h, and 72h after treatment administration for both arms.

Population: Pharmacokinetic (PK) parameter analysis set (PKS): This set included all subjects who provided all PK endpoints for all treatment periods that were defined as primary (Cmax and AUCo-tz) and was not excluded due to a protocol violation relevant to the evaluation of PK or due to PK non-evaluability. Only subjects with non-missing values were included.

Area under the concentration-time curve of metformin in plasma over the time interval from 0 to the last quantifiable data point (AUC0-tz) is presented. The statistical model used for the analysis of the primary endpoints was an analysis of variance (ANOVA) on the logarithmic scale. That is, the PK endpoints were log-transformed (natural logarithm) prior to fitting the ANOVA model. This model included effects accounting for the following sources of variation: sequence, subjects within sequences, period and treatment. The effect 'subjects within sequences' was considered as random, whereas the other effects were considered as fixed.

Outcome measures

Outcome measures
Measure
(A): Empagliflozin 10mg (R1) + Metformin (Glifage®) 850mg (R2)
n=24 Participants
Participants received treatment A: Single dose tablet of 10 milligram (mg) empagliflozin film-coated and a 850mg of metformin HCl (Glifage®) tablet, orally with 200 milliliter (mL) of water. A high-fat, high-calorie meal was served 30 minutes (min) before drug administration.
(B): FDC 12.5mg Empagliflozin/850mg Metformin
n=24 Participants
Participants were administered the treatment B which consisted of a single Fixed dose combination (FDC) tablet containing 12.5 milligram (mg) empagliflozin/850 mg metformin HCl, orally with 200 milliliter (mL) of water. A high-fat, high-calorie meal was served 30 minutes (min) before drug administration.
Area Under the Concentration-time Curve of Metformin in Plasma Over the Time Interval From 0 to the Last Quantifiable Data Point (AUC0-tz)
10299.45 hour*nanogram/milliliter (h*ng/mL)
Standard Error NA
The standard error is actually the geometric standard error and is equal to 1.05.
10467.41 hour*nanogram/milliliter (h*ng/mL)
Standard Error NA
The standard error is actually the geometric standard error and is equal to 1.05.

PRIMARY outcome

Timeframe: Within 5 minutes(min) before and 15min, 30min, 45min, 1h, 1h15min, 1h30min, 1h45min, 2h, 2h20min, 2h40min, 3h, 3h30min, 4h, 4h30min, 5h, 5h30min, 6h, 7h, 8h, 10h, 12h, 24h, 48h, and 72h after treatment administration for both arms.

Population: Pharmacokinetic (PK) parameter analysis set (PKS): This set included all subjects who provided all PK endpoints for all treatment periods that were defined as primary (Cmax and AUCo-tz) and was not excluded due to a protocol violation relevant to the evaluation of PK or due to PK non-evaluability. Only subjects with non-missing values were included.

Maximum measured concentration of metformin in plasma is presented. The statistical model used for the analysis of the primary endpoints was an analysis of variance (ANOVA) on the logarithmic scale. That is, the PK endpoints were log-transformed (natural logarithm) prior to fitting the ANOVA model. This model included effects accounting for the following sources of variation: sequence, subjects within sequences, period and treatment. The effect 'subjects within sequences' was considered as random, whereas the other effects were considered as fixed.

Outcome measures

Outcome measures
Measure
(A): Empagliflozin 10mg (R1) + Metformin (Glifage®) 850mg (R2)
n=24 Participants
Participants received treatment A: Single dose tablet of 10 milligram (mg) empagliflozin film-coated and a 850mg of metformin HCl (Glifage®) tablet, orally with 200 milliliter (mL) of water. A high-fat, high-calorie meal was served 30 minutes (min) before drug administration.
(B): FDC 12.5mg Empagliflozin/850mg Metformin
n=24 Participants
Participants were administered the treatment B which consisted of a single Fixed dose combination (FDC) tablet containing 12.5 milligram (mg) empagliflozin/850 mg metformin HCl, orally with 200 milliliter (mL) of water. A high-fat, high-calorie meal was served 30 minutes (min) before drug administration.
Maximum Measured Concentration of Metformin (Cmax)
1333.58 nanogram/milliliter (ng/mL )
Standard Error NA
The standard error is actually the geometric standard error and is equal to 1.04.
1308.39 nanogram/milliliter (ng/mL )
Standard Error NA
The standard error is actually the geometric standard error and is equal to 1.04.

SECONDARY outcome

Timeframe: Within 5 minutes(min) before and 15min, 30min, 45min, 1h, 1h15min, 1h30min, 1h45min, 2h, 2h20min, 2h40min, 3h, 3h30min, 4h, 4h30min, 5h, 5h30min, 6h, 7h, 8h, 10h, 12h, 24h, 48h, and 72h after treatment administration for both arms.

Population: Pharmacokinetic (PK) parameter analysis set (PKS): This set included all subjects who provided all PK endpoints for all treatment periods that were defined as primary (Cmax and AUCo-tz) and was not excluded due to a protocol violation relevant to the evaluation of PK or due to PK non-evaluability. Only subjects with non-missing values were included.

Area under the concentration-time curve of empagliflozin in plasma over the time interval from 0 extrapolated to infinity from the last quantifiable data point (AUC0-inf) normalized to the actual administered dose is presented. The AUC0-oo was divided by the actual dose strength to get the normalized area under the concentration-time curve. The statistical model used for the analysis of the primary endpoints was an analysis of variance (ANOVA) on the logarithmic scale. That is, the PK endpoints were log-transformed (natural logarithm) prior to fitting the ANOVA model. This model included effects accounting for the following sources of variation: sequence, subjects within sequences, period and treatment. The effect 'subjects within sequences' was considered as random, whereas the other effects were considered as fixed. Unit of measure: (hour\*nanogram/milliliter)/milligram.

Outcome measures

Outcome measures
Measure
(A): Empagliflozin 10mg (R1) + Metformin (Glifage®) 850mg (R2)
n=24 Participants
Participants received treatment A: Single dose tablet of 10 milligram (mg) empagliflozin film-coated and a 850mg of metformin HCl (Glifage®) tablet, orally with 200 milliliter (mL) of water. A high-fat, high-calorie meal was served 30 minutes (min) before drug administration.
(B): FDC 12.5mg Empagliflozin/850mg Metformin
n=24 Participants
Participants were administered the treatment B which consisted of a single Fixed dose combination (FDC) tablet containing 12.5 milligram (mg) empagliflozin/850 mg metformin HCl, orally with 200 milliliter (mL) of water. A high-fat, high-calorie meal was served 30 minutes (min) before drug administration.
Dose-normalized Area Under the Concentration-time Curve of Empagliflozin in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-∞ )
118.25 (h*ng/mL)/mg
Standard Error NA
The standard error is actually the geometric standard error and is equal to 1.03.
117.64 (h*ng/mL)/mg
Standard Error NA
The standard error is actually the geometric standard error and is equal to 1.03.

SECONDARY outcome

Timeframe: Within 5 minutes(min) before and 15min, 30min, 45min, 1h, 1h15min, 1h30min, 1h45min, 2h, 2h20min, 2h40min, 3h, 3h30min, 4h, 4h30min, 5h, 5h30min, 6h, 7h, 8h, 10h, 12h, 24h, 48h, and 72h after treatment administration for both arms.

Population: Pharmacokinetic (PK) parameter analysis set (PKS): This set included all subjects who provided all PK endpoints for all treatment periods that were defined as primary (Cmax and AUCo-tz) and was not excluded due to a protocol violation relevant to the evaluation of PK or due to PK non-evaluability. Only subjects with non-missing values were included.

Area under the concentration-time curve of metformin in plasma over the time interval from 0 extrapolated to infinity (AUC0-∞ ) is presented. The statistical model used for the analysis was an analysis of variance (ANOVA) on the logarithmic scale. That is, the PK endpoints were log-transformed (natural logarithm) prior to fitting the ANOVA model. This model included effects accounting for the following sources of variation: sequence, subjects within sequences, period and treatment. The effect 'subjects within sequences' was considered as random, whereas the other effects were considered as fixed.

Outcome measures

Outcome measures
Measure
(A): Empagliflozin 10mg (R1) + Metformin (Glifage®) 850mg (R2)
n=24 Participants
Participants received treatment A: Single dose tablet of 10 milligram (mg) empagliflozin film-coated and a 850mg of metformin HCl (Glifage®) tablet, orally with 200 milliliter (mL) of water. A high-fat, high-calorie meal was served 30 minutes (min) before drug administration.
(B): FDC 12.5mg Empagliflozin/850mg Metformin
n=24 Participants
Participants were administered the treatment B which consisted of a single Fixed dose combination (FDC) tablet containing 12.5 milligram (mg) empagliflozin/850 mg metformin HCl, orally with 200 milliliter (mL) of water. A high-fat, high-calorie meal was served 30 minutes (min) before drug administration.
Area Under the Concentration-time Curve of Metformin in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-∞)
10440.79 hour*nanogram/milliliter (hr*ng/mL)
Standard Error NA
The standard error is actually the geometric standard error and is equal to 1.05.
10570.45 hour*nanogram/milliliter (hr*ng/mL)
Standard Error NA
The standard error is actually the geometric standard error and is equal to 1.05.

SECONDARY outcome

Timeframe: Within 5 minutes(min) before and 15min, 30min, 45min, 1h, 1h15min, 1h30min, 1h45min, 2h, 2h20min, 2h40min, 3h, 3h30min, 4h, 4h30min, 5h, 5h30min, 6h, 7h, 8h, 10h, 12h, 24h, 48h, and 72h after treatment administration for both arms.

Population: Pharmacokinetic (PK) parameter analysis set (PKS): This set included all subjects who provided all PK endpoints for all treatment periods that were defined as primary (Cmax and AUCo-tz) and was not excluded due to a protocol violation relevant to the evaluation of PK or due to PK non-evaluability. Only subjects with non-missing values were included.

Time from last dosing to the maximum measured concentration of empagliflozin in plasma (tmax) is presented.

Outcome measures

Outcome measures
Measure
(A): Empagliflozin 10mg (R1) + Metformin (Glifage®) 850mg (R2)
n=24 Participants
Participants received treatment A: Single dose tablet of 10 milligram (mg) empagliflozin film-coated and a 850mg of metformin HCl (Glifage®) tablet, orally with 200 milliliter (mL) of water. A high-fat, high-calorie meal was served 30 minutes (min) before drug administration.
(B): FDC 12.5mg Empagliflozin/850mg Metformin
n=24 Participants
Participants were administered the treatment B which consisted of a single Fixed dose combination (FDC) tablet containing 12.5 milligram (mg) empagliflozin/850 mg metformin HCl, orally with 200 milliliter (mL) of water. A high-fat, high-calorie meal was served 30 minutes (min) before drug administration.
Time From Last Dosing to the Maximum Measured Concentration of Empagliflozin in Plasma (Tmax)
2.33 Hours (hr)
Interval 1.25 to 5.0
2.17 Hours (hr)
Interval 1.0 to 5.5

SECONDARY outcome

Timeframe: Within 5 minutes(min) before and 15min, 30min, 45min, 1h, 1h15min, 1h30min, 1h45min, 2h, 2h20min, 2h40min, 3h, 3h30min, 4h, 4h30min, 5h, 5h30min, 6h, 7h, 8h, 10h, 12h, 24h, 48h, and 72h after treatment administration for both arms.

Population: Pharmacokinetic (PK) parameter analysis set (PKS): This set included all subjects who provided all PK endpoints for all treatment periods that were defined as primary (Cmax and AUCo-tz) and was not excluded due to a protocol violation relevant to the evaluation of PK or due to PK non-evaluability. Only subjects with non-missing values were included.

Time from last dosing to the maximum measured concentration of metformin in plasma (tmax) is presented.

Outcome measures

Outcome measures
Measure
(A): Empagliflozin 10mg (R1) + Metformin (Glifage®) 850mg (R2)
n=24 Participants
Participants received treatment A: Single dose tablet of 10 milligram (mg) empagliflozin film-coated and a 850mg of metformin HCl (Glifage®) tablet, orally with 200 milliliter (mL) of water. A high-fat, high-calorie meal was served 30 minutes (min) before drug administration.
(B): FDC 12.5mg Empagliflozin/850mg Metformin
n=24 Participants
Participants were administered the treatment B which consisted of a single Fixed dose combination (FDC) tablet containing 12.5 milligram (mg) empagliflozin/850 mg metformin HCl, orally with 200 milliliter (mL) of water. A high-fat, high-calorie meal was served 30 minutes (min) before drug administration.
Time From Last Dosing to the Maximum Measured Concentration of Metformin in Plasma (Tmax)
4.00 Hours (hr)
Interval 3.0 to 4.5
4.00 Hours (hr)
Interval 1.0 to 5.0

SECONDARY outcome

Timeframe: Within 5 minutes(min) before and 15min, 30min, 45min, 1h, 1h15min, 1h30min, 1h45min, 2h, 2h20min, 2h40min, 3h, 3h30min, 4h, 4h30min, 5h, 5h30min, 6h, 7h, 8h, 10h, 12h, 24h, 48h, and 72h after treatment administration for both arms.

Population: Pharmacokinetic (PK) parameter analysis set (PKS): This set included all subjects who provided all PK endpoints for all treatment periods that were defined as primary (Cmax and AUCo-tz) and was not excluded due to a protocol violation relevant to the evaluation of PK or due to PK non-evaluability. Only subjects with non-missing values were included.

The percentage (%) of the AUC of empagliflozin that has been derived after extrapolation is reported.

Outcome measures

Outcome measures
Measure
(A): Empagliflozin 10mg (R1) + Metformin (Glifage®) 850mg (R2)
n=24 Participants
Participants received treatment A: Single dose tablet of 10 milligram (mg) empagliflozin film-coated and a 850mg of metformin HCl (Glifage®) tablet, orally with 200 milliliter (mL) of water. A high-fat, high-calorie meal was served 30 minutes (min) before drug administration.
(B): FDC 12.5mg Empagliflozin/850mg Metformin
n=24 Participants
Participants were administered the treatment B which consisted of a single Fixed dose combination (FDC) tablet containing 12.5 milligram (mg) empagliflozin/850 mg metformin HCl, orally with 200 milliliter (mL) of water. A high-fat, high-calorie meal was served 30 minutes (min) before drug administration.
Percentage (%) of the AUC of Empagliflozin That Has Been Derived After Extrapolation
9.77 Percentage (%)
Standard Deviation 3.04
9.31 Percentage (%)
Standard Deviation 1.87

SECONDARY outcome

Timeframe: Within 5 minutes(min) before and 15min, 30min, 45min, 1h, 1h15min, 1h30min, 1h45min, 2h, 2h20min, 2h40min, 3h, 3h30min, 4h, 4h30min, 5h, 5h30min, 6h, 7h, 8h, 10h, 12h, 24h, 48h, and 72h after treatment administration for both arms.

Population: Pharmacokinetic (PK) parameter analysis set (PKS): This set included all subjects who provided all PK endpoints for all treatment periods that were defined as primary (Cmax and AUCo-tz) and was not excluded due to a protocol violation relevant to the evaluation of PK or due to PK non-evaluability. Only subjects with non-missing values were included.

The percentage (%) of the AUC of metformin that has been derived after extrapolation is reported.

Outcome measures

Outcome measures
Measure
(A): Empagliflozin 10mg (R1) + Metformin (Glifage®) 850mg (R2)
n=24 Participants
Participants received treatment A: Single dose tablet of 10 milligram (mg) empagliflozin film-coated and a 850mg of metformin HCl (Glifage®) tablet, orally with 200 milliliter (mL) of water. A high-fat, high-calorie meal was served 30 minutes (min) before drug administration.
(B): FDC 12.5mg Empagliflozin/850mg Metformin
n=24 Participants
Participants were administered the treatment B which consisted of a single Fixed dose combination (FDC) tablet containing 12.5 milligram (mg) empagliflozin/850 mg metformin HCl, orally with 200 milliliter (mL) of water. A high-fat, high-calorie meal was served 30 minutes (min) before drug administration.
Percentage (%) of the AUC of Metformin That Has Been Derived After Extrapolation
14.35 Percentage (%)
Standard Deviation 8.50
13.04 Percentage (%)
Standard Deviation 5.58

SECONDARY outcome

Timeframe: Within 5 minutes(min) before and 15min, 30min, 45min, 1h, 1h15min, 1h30min, 1h45min, 2h, 2h20min, 2h40min, 3h, 3h30min, 4h, 4h30min, 5h, 5h30min, 6h, 7h, 8h, 10h, 12h, 24h, 48h, and 72h after treatment administration for both arms.

Population: Pharmacokinetic (PK) parameter analysis set (PKS): This set included all subjects who provided all PK endpoints for all treatment periods that were defined as primary (Cmax and AUCo-tz) and was not excluded due to a protocol violation relevant to the evaluation of PK or due to PK non-evaluability. Only subjects with non-missing values were included.

The terminal half-life of empagliflozin in plasma (t1/2) is presented.

Outcome measures

Outcome measures
Measure
(A): Empagliflozin 10mg (R1) + Metformin (Glifage®) 850mg (R2)
n=24 Participants
Participants received treatment A: Single dose tablet of 10 milligram (mg) empagliflozin film-coated and a 850mg of metformin HCl (Glifage®) tablet, orally with 200 milliliter (mL) of water. A high-fat, high-calorie meal was served 30 minutes (min) before drug administration.
(B): FDC 12.5mg Empagliflozin/850mg Metformin
n=24 Participants
Participants were administered the treatment B which consisted of a single Fixed dose combination (FDC) tablet containing 12.5 milligram (mg) empagliflozin/850 mg metformin HCl, orally with 200 milliliter (mL) of water. A high-fat, high-calorie meal was served 30 minutes (min) before drug administration.
Terminal Half-life of Empagliflozin in Plasma (t1/2)
0.08 Hours (hr)
Interval 0.04 to 0.11
0.08 Hours (hr)
Interval 0.05 to 0.11

SECONDARY outcome

Timeframe: Within 5 minutes(min) before and 15min, 30min, 45min, 1h, 1h15min, 1h30min, 1h45min, 2h, 2h20min, 2h40min, 3h, 3h30min, 4h, 4h30min, 5h, 5h30min, 6h, 7h, 8h, 10h, 12h, 24h, 48h, and 72h after treatment administration for both arms.

Population: Pharmacokinetic (PK) parameter analysis set (PKS): This set included all subjects who provided all PK endpoints for all treatment periods that were defined as primary (Cmax and AUCo-tz) and was not excluded due to a protocol violation relevant to the evaluation of PK or due to PK non-evaluability. Only subjects with non-missing values were included.

The terminal half-life of metformin in plasma (t1/2) is presented.

Outcome measures

Outcome measures
Measure
(A): Empagliflozin 10mg (R1) + Metformin (Glifage®) 850mg (R2)
n=24 Participants
Participants received treatment A: Single dose tablet of 10 milligram (mg) empagliflozin film-coated and a 850mg of metformin HCl (Glifage®) tablet, orally with 200 milliliter (mL) of water. A high-fat, high-calorie meal was served 30 minutes (min) before drug administration.
(B): FDC 12.5mg Empagliflozin/850mg Metformin
n=24 Participants
Participants were administered the treatment B which consisted of a single Fixed dose combination (FDC) tablet containing 12.5 milligram (mg) empagliflozin/850 mg metformin HCl, orally with 200 milliliter (mL) of water. A high-fat, high-calorie meal was served 30 minutes (min) before drug administration.
Terminal Half-life of Metformin in Plasma (t1/2)
0.06 Hours (hr)
Interval 0.02 to 0.13
0.06 Hours (hr)
Interval 0.02 to 0.11

SECONDARY outcome

Timeframe: Within 5 minutes(min) before and 15min, 30min, 45min, 1h, 1h15min, 1h30min, 1h45min, 2h, 2h20min, 2h40min, 3h, 3h30min, 4h, 4h30min, 5h, 5h30min, 6h, 7h, 8h, 10h, 12h, 24h, 48h, and 72h after treatment administration for both arms.

Population: Pharmacokinetic (PK) parameter analysis set (PKS): This set included all subjects who provided all PK endpoints for all treatment periods that were defined as primary (Cmax and AUCo-tz) and was not excluded due to a protocol violation relevant to the evaluation of PK or due to PK non-evaluability. Only subjects with non-missing values were included.

The elimination rate constant (Kel) for empagliflozin is reported.

Outcome measures

Outcome measures
Measure
(A): Empagliflozin 10mg (R1) + Metformin (Glifage®) 850mg (R2)
n=24 Participants
Participants received treatment A: Single dose tablet of 10 milligram (mg) empagliflozin film-coated and a 850mg of metformin HCl (Glifage®) tablet, orally with 200 milliliter (mL) of water. A high-fat, high-calorie meal was served 30 minutes (min) before drug administration.
(B): FDC 12.5mg Empagliflozin/850mg Metformin
n=24 Participants
Participants were administered the treatment B which consisted of a single Fixed dose combination (FDC) tablet containing 12.5 milligram (mg) empagliflozin/850 mg metformin HCl, orally with 200 milliliter (mL) of water. A high-fat, high-calorie meal was served 30 minutes (min) before drug administration.
Elimination Rate Constant (Kel) for Empagliflozin
0.93 1/hours (1/hr)
Standard Deviation 0.61
0.84 1/hours (1/hr)
Standard Deviation 0.44

SECONDARY outcome

Timeframe: Within 5 minutes(min) before and 15min, 30min, 45min, 1h, 1h15min, 1h30min, 1h45min, 2h, 2h20min, 2h40min, 3h, 3h30min, 4h, 4h30min, 5h, 5h30min, 6h, 7h, 8h, 10h, 12h, 24h, 48h, and 72h after treatment administration for both arms.

Population: Pharmacokinetic (PK) parameter analysis set (PKS): This set included all subjects who provided all PK endpoints for all treatment periods that were defined as primary (Cmax and AUCo-tz) and was not excluded due to a protocol violation relevant to the evaluation of PK or due to PK non-evaluability. Only subjects with non-missing values were included.

The elimination rate constant (Kel) for metformin is reported.

Outcome measures

Outcome measures
Measure
(A): Empagliflozin 10mg (R1) + Metformin (Glifage®) 850mg (R2)
n=24 Participants
Participants received treatment A: Single dose tablet of 10 milligram (mg) empagliflozin film-coated and a 850mg of metformin HCl (Glifage®) tablet, orally with 200 milliliter (mL) of water. A high-fat, high-calorie meal was served 30 minutes (min) before drug administration.
(B): FDC 12.5mg Empagliflozin/850mg Metformin
n=24 Participants
Participants were administered the treatment B which consisted of a single Fixed dose combination (FDC) tablet containing 12.5 milligram (mg) empagliflozin/850 mg metformin HCl, orally with 200 milliliter (mL) of water. A high-fat, high-calorie meal was served 30 minutes (min) before drug administration.
Elimination Rate Constant (Kel) for Metformin
1.33 1/hours (1/hr)
Standard Deviation 2.14
0.97 1/hours (1/hr)
Standard Deviation 1.02

Adverse Events

(A): Empagliflozin 10mg (R1) + Metformin (Glifage®) 850mg (R2)

Serious events: 0 serious events
Other events: 5 other events
Deaths: 0 deaths

(B): FDC 12.5mg Empagliflozin/850mg Metformin

Serious events: 0 serious events
Other events: 2 other events
Deaths: 0 deaths

Serious adverse events

Adverse event data not reported

Other adverse events

Other adverse events
Measure
(A): Empagliflozin 10mg (R1) + Metformin (Glifage®) 850mg (R2)
n=30 participants at risk
Participants received treatment A: Single dose tablet of 10 milligram (mg) empagliflozin film-coated and a 850mg of metformin HCl (Glifage®) tablet, orally with 200 milliliter (mL) of water. A high-fat, high-calorie meal was served 30 minutes (min) before drug administration.
(B): FDC 12.5mg Empagliflozin/850mg Metformin
n=29 participants at risk
Participants were administered the treatment B which consisted of a single Fixed dose combination (FDC) tablet containing 12.5 milligram (mg) empagliflozin/850 mg metformin HCl, orally with 200 milliliter (mL) of water. A high-fat, high-calorie meal was served 30 minutes (min) before drug administration.
Investigations
White blood cells in urine
10.0%
3/30 • Up to 14 days after the last treatment administration.
Treated Set (TS): The treated set included all participants in the research that were randomized and treated with at least one dose of study medication.
0.00%
0/29 • Up to 14 days after the last treatment administration.
Treated Set (TS): The treated set included all participants in the research that were randomized and treated with at least one dose of study medication.
Metabolism and nutrition disorders
Hyperglycaemia
6.7%
2/30 • Up to 14 days after the last treatment administration.
Treated Set (TS): The treated set included all participants in the research that were randomized and treated with at least one dose of study medication.
0.00%
0/29 • Up to 14 days after the last treatment administration.
Treated Set (TS): The treated set included all participants in the research that were randomized and treated with at least one dose of study medication.
Nervous system disorders
Headache
3.3%
1/30 • Up to 14 days after the last treatment administration.
Treated Set (TS): The treated set included all participants in the research that were randomized and treated with at least one dose of study medication.
6.9%
2/29 • Up to 14 days after the last treatment administration.
Treated Set (TS): The treated set included all participants in the research that were randomized and treated with at least one dose of study medication.

Additional Information

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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.
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Restriction type: OTHER