Trial Outcomes & Findings for A Study to Assess the Food Effect on Bioavailability of Metformin/Gliclazide in Healthy Participants (NCT NCT03467971)

NCT ID: NCT03467971

Last Updated: 2019-07-08

Results Overview

AUC (0-inf) is defined as the area under the plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time (0-inf).

Recruitment status

COMPLETED

Study phase

PHASE1

Target enrollment

21 participants

Primary outcome timeframe

Pre-dose, 0.5, 1.0, 2.0, 3.0, 4.0, 5.0, 6.0, 7.0, 8.0, 10.0, 12.0, 16.0, 24.0, 28.0, 32.0, 48.0, 72.0, 96.0, 120.0, 144.0 and 168.0 hour post-dose

Results posted on

2019-07-08

Participant Flow

Participant milestones

Participant milestones
Measure
Metformin-Gliclazide (Fasted), Then Metformin-Gliclazide (Fed)
Participants received single dose of Metformin 1000 milligram (mg) and Gliclazide 30 mg fixed combination tablet in fasting state in treatment period 1 followed by single dose of Metformin 1000 mg and Gliclazide 30 mg fixed combination tablet in fed state in treatment period 2. Each treatment period was separated by a 14-day wash-out period.
Metformin-Gliclazide (Fed), Then Metformin-Gliclazide (Fasted)
Participants received single dose of Metformin 1000 mg and Gliclazide 30 mg fixed combination tablet in fed state in treatment period 1 followed by single dose of Metformin 1000 mg and Gliclazide 30 mg fixed combination tablet in fasting state in treatment period 2. Each treatment period will be separated by a 14-day wash-out period.
Treatment Period 1
STARTED
10
11
Treatment Period 1
COMPLETED
10
11
Treatment Period 1
NOT COMPLETED
0
0
Treatment Period 2
STARTED
10
11
Treatment Period 2
COMPLETED
10
10
Treatment Period 2
NOT COMPLETED
0
1

Reasons for withdrawal

Reasons for withdrawal
Measure
Metformin-Gliclazide (Fasted), Then Metformin-Gliclazide (Fed)
Participants received single dose of Metformin 1000 milligram (mg) and Gliclazide 30 mg fixed combination tablet in fasting state in treatment period 1 followed by single dose of Metformin 1000 mg and Gliclazide 30 mg fixed combination tablet in fed state in treatment period 2. Each treatment period was separated by a 14-day wash-out period.
Metformin-Gliclazide (Fed), Then Metformin-Gliclazide (Fasted)
Participants received single dose of Metformin 1000 mg and Gliclazide 30 mg fixed combination tablet in fed state in treatment period 1 followed by single dose of Metformin 1000 mg and Gliclazide 30 mg fixed combination tablet in fasting state in treatment period 2. Each treatment period will be separated by a 14-day wash-out period.
Treatment Period 2
Withdrawal by Subject
0
1

Baseline Characteristics

A Study to Assess the Food Effect on Bioavailability of Metformin/Gliclazide in Healthy Participants

Baseline characteristics by cohort

Baseline characteristics by cohort
Measure
Metformin-Gliclazide (Fasted), Then Metformin-Gliclazide (Fed)
n=10 Participants
Participants received single dose of Metformin 1000 milligram (mg) and Gliclazide 30 mg fixed combination tablet in fasting state in treatment period 1 followed by single dose of Metformin 1000 mg and Gliclazide 30 mg fixed combination tablet in fed state in treatment period 2. Each treatment period was separated by a 14-day wash-out period.
Metformin-Gliclazide (Fed), Then Metformin-Gliclazide (Fasted)
n=11 Participants
Participants received single dose of Metformin 1000 mg and Gliclazide 30 mg fixed combination tablet in fed state in treatment period 1 followed by single dose of Metformin 1000 mg and Gliclazide 30 mg fixed combination tablet in fasting state in treatment period 2. Each treatment period will be separated by a 14-day wash-out period.
Total
n=21 Participants
Total of all reporting groups
Age, Continuous
37.2 Years
STANDARD_DEVIATION 10.9 • n=5 Participants
32.5 Years
STANDARD_DEVIATION 8.0 • n=7 Participants
34.7 Years
STANDARD_DEVIATION 9.6 • n=5 Participants
Sex: Female, Male
Female
3 Participants
n=5 Participants
3 Participants
n=7 Participants
6 Participants
n=5 Participants
Sex: Female, Male
Male
7 Participants
n=5 Participants
8 Participants
n=7 Participants
15 Participants
n=5 Participants
Ethnicity (NIH/OMB)
Hispanic or Latino
10 Participants
n=5 Participants
11 Participants
n=7 Participants
21 Participants
n=5 Participants
Ethnicity (NIH/OMB)
Not Hispanic or Latino
0 Participants
n=5 Participants
0 Participants
n=7 Participants
0 Participants
n=5 Participants
Ethnicity (NIH/OMB)
Unknown or Not Reported
0 Participants
n=5 Participants
0 Participants
n=7 Participants
0 Participants
n=5 Participants

PRIMARY outcome

Timeframe: Pre-dose, 0.5, 1.0, 2.0, 3.0, 4.0, 5.0, 6.0, 7.0, 8.0, 10.0, 12.0, 16.0, 24.0, 28.0, 32.0, 48.0, 72.0, 96.0, 120.0, 144.0 and 168.0 hour post-dose

Population: The Pharmacokinetics (PK) analysis set included all participants who completed the study with adequate study medication compliance, without any relevant protocol violations with respect to factors likely to affect the comparability of PK results.

AUC (0-inf) is defined as the area under the plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time (0-inf).

Outcome measures

Outcome measures
Measure
Metformin-Gliclazide (Fasted)
n=21 Participants
Participants received single dose of Metformin 1000 mg and Gliclazide 30 mg fixed combination tablet in fasting state in treatment period 1 or in treatment period 2.
Metformin-Gliclazide (Fed)
n=21 Participants
Participants received single dose of Metformin 1000 mg and Gliclazide 30 mg fixed combination tablet in fed state in treatment period 1 or in treatment period 2.
Area Under the Plasma Concentration-time Curve From Time Zero to Infinity (AUC0-inf) of Metformin and Gliclazide
Metformin
4974.2507 Nanogram*hour per milliliter (ng*h/mL)
Standard Deviation 1599.3290
8556.7752 Nanogram*hour per milliliter (ng*h/mL)
Standard Deviation 2544.6658
Area Under the Plasma Concentration-time Curve From Time Zero to Infinity (AUC0-inf) of Metformin and Gliclazide
Gliclazide
21192.1682 Nanogram*hour per milliliter (ng*h/mL)
Standard Deviation 9220.3044
21815.4021 Nanogram*hour per milliliter (ng*h/mL)
Standard Deviation 8369.0107

PRIMARY outcome

Timeframe: Pre-dose, 0.5, 1.0, 2.0, 3.0, 4.0, 5.0, 6.0, 7.0, 8.0, 10.0, 12.0, 16.0, 24.0, 28.0, 32.0, 48.0, 72.0, 96.0, 120.0, 144.0 and 168.0 hour post-dose

Population: PK analysis set included all participants who completed the study with adequate study medication compliance, without any relevant protocol violations with respect to factors likely to affect the comparability of PK results.

AUC (0-t) is defined as the area under the plasma concentration versus time curve from time zero (pre-dose) to time of last quantifiable concentration (0-t)

Outcome measures

Outcome measures
Measure
Metformin-Gliclazide (Fasted)
n=21 Participants
Participants received single dose of Metformin 1000 mg and Gliclazide 30 mg fixed combination tablet in fasting state in treatment period 1 or in treatment period 2.
Metformin-Gliclazide (Fed)
n=21 Participants
Participants received single dose of Metformin 1000 mg and Gliclazide 30 mg fixed combination tablet in fed state in treatment period 1 or in treatment period 2.
Area Under the Plasma Concentration-Time Curve From Time Zero to Last Measurable Concentration (AUC0-t) of Metformin and Gliclazide
Metformin
4722.4546 ng*h/mL
Standard Deviation 1598.1082
8298.5628 ng*h/mL
Standard Deviation 2422.9059
Area Under the Plasma Concentration-Time Curve From Time Zero to Last Measurable Concentration (AUC0-t) of Metformin and Gliclazide
Gliclazide
20348.8381 ng*h/mL
Standard Deviation 9154.5509
20997.1704 ng*h/mL
Standard Deviation 8244.2743

PRIMARY outcome

Timeframe: Pre-dose, 0.5, 1.0, 2.0, 3.0, 4.0, 5.0, 6.0, 7.0, 8.0, 10.0, 12.0, 16.0, 24.0, 28.0, 32.0, 48.0, 72.0, 96.0, 120.0, 144.0 and 168.0 hour post-dose

Population: PK analysis set included all participants who completed the study with adequate study medication compliance, without any relevant protocol violations with respect to factors likely to affect the comparability of PK results.

Cmax is defined as the maximum observed plasma concentration.

Outcome measures

Outcome measures
Measure
Metformin-Gliclazide (Fasted)
n=21 Participants
Participants received single dose of Metformin 1000 mg and Gliclazide 30 mg fixed combination tablet in fasting state in treatment period 1 or in treatment period 2.
Metformin-Gliclazide (Fed)
n=21 Participants
Participants received single dose of Metformin 1000 mg and Gliclazide 30 mg fixed combination tablet in fed state in treatment period 1 or in treatment period 2.
Maximum Observed Plasma Concentration (Cmax) of Metformin and Gliclazide
Metformin
717.5017 ng/mL
Standard Deviation 304.8105
870.7288 ng/mL
Standard Deviation 272.6886
Maximum Observed Plasma Concentration (Cmax) of Metformin and Gliclazide
Gliclazide
968.0305 ng/mL
Standard Deviation 261.8362
1013.9753 ng/mL
Standard Deviation 243.1601

SECONDARY outcome

Timeframe: Pre-dose, 0.5, 1.0, 2.0, 3.0, 4.0, 5.0, 6.0, 7.0, 8.0, 10.0, 12.0, 16.0, 24.0, 28.0, 32.0, 48.0, 72.0, 96.0, 120.0, 144.0 and 168.0 hour post-dose

Population: The PK analysis set included all participants who completed the study with adequate study medication compliance, without any relevant protocol violations with respect to factors likely to affect the comparability of PK results.

Tmax is defined as the time to reach maximum plasma concentration.

Outcome measures

Outcome measures
Measure
Metformin-Gliclazide (Fasted)
n=21 Participants
Participants received single dose of Metformin 1000 mg and Gliclazide 30 mg fixed combination tablet in fasting state in treatment period 1 or in treatment period 2.
Metformin-Gliclazide (Fed)
n=21 Participants
Participants received single dose of Metformin 1000 mg and Gliclazide 30 mg fixed combination tablet in fed state in treatment period 1 or in treatment period 2.
Time to Reach Maximum Plasma Concentration (Tmax) of Metformin and Gliclazide
Metformin
3.6698 Hours
Standard Deviation 0.6600
7.2389 Hours
Standard Deviation 0.7693
Time to Reach Maximum Plasma Concentration (Tmax) of Metformin and Gliclazide
Gliclazide
6.5254 Hours
Standard Deviation 1.7474
8.5238 Hours
Standard Deviation 2.1822

SECONDARY outcome

Timeframe: Pre-dose, 0.5, 1.0, 2.0, 3.0, 4.0, 5.0, 6.0, 7.0, 8.0, 10.0, 12.0, 16.0, 24.0, 28.0, 32.0, 48.0, 72.0, 96.0, 120.0, 144.0 and 168.0 hour post-dose

Population: The PK analysis set included all participants who completed the study with adequate study medication compliance, without any relevant protocol violations with respect to factors likely to affect the comparability of PK results.

Elimination Half Life (t1/2) is defined as the time required for the concentration or amount of drug in the body to be reduced by one-half.

Outcome measures

Outcome measures
Measure
Metformin-Gliclazide (Fasted)
n=21 Participants
Participants received single dose of Metformin 1000 mg and Gliclazide 30 mg fixed combination tablet in fasting state in treatment period 1 or in treatment period 2.
Metformin-Gliclazide (Fed)
n=21 Participants
Participants received single dose of Metformin 1000 mg and Gliclazide 30 mg fixed combination tablet in fed state in treatment period 1 or in treatment period 2.
Elimination Half Life (t1/2) of Metformin and Gliclazide
Metformin
6.2547 Hours
Standard Deviation 2.9771
7.4892 Hours
Standard Deviation 8.7276
Elimination Half Life (t1/2) of Metformin and Gliclazide
Gliclazide
16.6222 Hours
Standard Deviation 6.2627
17.1044 Hours
Standard Deviation 7.5000

SECONDARY outcome

Timeframe: Pre-dose, 0.5, 1.0, 2.0, 3.0, 4.0, 5.0, 6.0, 7.0, 8.0, 10.0, 12.0, 16.0, 24.0, 28.0, 32.0, 48.0, 72.0, 96.0, 120.0, 144.0 and 168.0 hour post-dose

Population: The PK analysis set included all participants who completed the study with adequate study medication compliance, without any relevant protocol violations with respect to factors likely to affect the comparability of PK results.

Vz/f is defined as apparent volume of distribution during terminal phase after non-intravenous administration

Outcome measures

Outcome measures
Measure
Metformin-Gliclazide (Fasted)
n=21 Participants
Participants received single dose of Metformin 1000 mg and Gliclazide 30 mg fixed combination tablet in fasting state in treatment period 1 or in treatment period 2.
Metformin-Gliclazide (Fed)
n=21 Participants
Participants received single dose of Metformin 1000 mg and Gliclazide 30 mg fixed combination tablet in fed state in treatment period 1 or in treatment period 2.
Apparent Volume of Distribution (Vz/f) of Metformin and Gliclazide
Gliclazide
35189.3864 Milliliter (mL)
Standard Deviation 8855.9499
33813.7843 Milliliter (mL)
Standard Deviation 6970.7706
Apparent Volume of Distribution (Vz/f) of Metformin and Gliclazide
Metformin
2003389.9474 Milliliter (mL)
Standard Deviation 1157828.4547
1200933.2647 Milliliter (mL)
Standard Deviation 949837.2019

SECONDARY outcome

Timeframe: Pre-dose, 0.5, 1.0, 2.0, 3.0, 4.0, 5.0, 6.0, 7.0, 8.0, 10.0, 12.0, 16.0, 24.0, 28.0, 32.0, 48.0, 72.0, 96.0, 120.0, 144.0 and 168.0 hour post-dose

Population: The PK analysis set included all participants who completed the study with adequate study medication compliance, without any relevant protocol violations with respect to factors likely to affect the comparability of PK results.

CL/f is defined as apparent total clearance of the drug from plasma after oral administration.

Outcome measures

Outcome measures
Measure
Metformin-Gliclazide (Fasted)
n=21 Participants
Participants received single dose of Metformin 1000 mg and Gliclazide 30 mg fixed combination tablet in fasting state in treatment period 1 or in treatment period 2.
Metformin-Gliclazide (Fed)
n=21 Participants
Participants received single dose of Metformin 1000 mg and Gliclazide 30 mg fixed combination tablet in fed state in treatment period 1 or in treatment period 2.
Apparent Total Body Clearance (CL/f) of Metformin and Gliclazide From Plasma
Metformin
226.79 Liters
Standard Deviation 88.58
125.93 Liters
Standard Deviation 33.92
Apparent Total Body Clearance (CL/f) of Metformin and Gliclazide From Plasma
Glilclazide
1.63 Liters
Standard Deviation 0.57
1.55 Liters
Standard Deviation 0.52

SECONDARY outcome

Timeframe: Baseline up to Day 39

Population: The safety population included all participants who received at least 1 dose of the study treatment in either treatment period 1 or treatment period 2.

Adverse event(AE) was defined as any untoward medical occurrence in participants which does not necessarily have causal relationship with treatment. AE was any unfavorable and unintended sign(including abnormal laboratory finding), symptom/disease temporally associated with use of medicinal product, whether/not considered related to medicinal product. A serious adverse event(SAE) was AE that resulted in any of the following outcomes: death; life threatening; persistent/significant disability/incapacity; initial/prolonged inpatient hospitalization; congenital anomaly/birth defect or was otherwise considered medically important. Term TEAE is defined as AEs starting/worsening after first intake of the study drug. TEAEs included both Serious TEAEs and non-serious TEAEs.

Outcome measures

Outcome measures
Measure
Metformin-Gliclazide (Fasted)
n=21 Participants
Participants received single dose of Metformin 1000 mg and Gliclazide 30 mg fixed combination tablet in fasting state in treatment period 1 or in treatment period 2.
Metformin-Gliclazide (Fed)
n=21 Participants
Participants received single dose of Metformin 1000 mg and Gliclazide 30 mg fixed combination tablet in fed state in treatment period 1 or in treatment period 2.
Number of Participants With Adverse Events (AEs) and Serious Adverse Events (SAEs)
Adverse Events
8 Participants
7 Participants
Number of Participants With Adverse Events (AEs) and Serious Adverse Events (SAEs)
Serious Adverse Events (SAEs)
0 Participants
0 Participants

Adverse Events

Metformin-Gliclazide (Fasted)

Serious events: 0 serious events
Other events: 8 other events
Deaths: 0 deaths

Metformin-Gliclazide (Fed)

Serious events: 0 serious events
Other events: 7 other events
Deaths: 0 deaths

Serious adverse events

Adverse event data not reported

Other adverse events

Other adverse events
Measure
Metformin-Gliclazide (Fasted)
n=21 participants at risk
Participants received single dose of Metformin 1000 mg and Gliclazide 30 mg fixed combination tablet in fasting state in treatment period 1 or in treatment period 2.
Metformin-Gliclazide (Fed)
n=21 participants at risk
Participants received single dose of Metformin 1000 mg and Gliclazide 30 mg fixed combination tablet in fed state in treatment period 1 or in treatment period 2.
Investigations
Elevated triglycerides
9.5%
2/21 • Baseline up to Day 39
The safety population included all participants who received at least 1 dose of the study treatment.
14.3%
3/21 • Baseline up to Day 39
The safety population included all participants who received at least 1 dose of the study treatment.
Investigations
Elevated total bilirubin
4.8%
1/21 • Baseline up to Day 39
The safety population included all participants who received at least 1 dose of the study treatment.
0.00%
0/21 • Baseline up to Day 39
The safety population included all participants who received at least 1 dose of the study treatment.
Investigations
Elevated direct bilirubin
4.8%
1/21 • Baseline up to Day 39
The safety population included all participants who received at least 1 dose of the study treatment.
0.00%
0/21 • Baseline up to Day 39
The safety population included all participants who received at least 1 dose of the study treatment.
Investigations
Elevated indirect bilirubin
4.8%
1/21 • Baseline up to Day 39
The safety population included all participants who received at least 1 dose of the study treatment.
0.00%
0/21 • Baseline up to Day 39
The safety population included all participants who received at least 1 dose of the study treatment.
Investigations
High cholesterol
4.8%
1/21 • Baseline up to Day 39
The safety population included all participants who received at least 1 dose of the study treatment.
0.00%
0/21 • Baseline up to Day 39
The safety population included all participants who received at least 1 dose of the study treatment.
Blood and lymphatic system disorders
Anemia
0.00%
0/21 • Baseline up to Day 39
The safety population included all participants who received at least 1 dose of the study treatment.
14.3%
3/21 • Baseline up to Day 39
The safety population included all participants who received at least 1 dose of the study treatment.
Nervous system disorders
Headache
4.8%
1/21 • Baseline up to Day 39
The safety population included all participants who received at least 1 dose of the study treatment.
0.00%
0/21 • Baseline up to Day 39
The safety population included all participants who received at least 1 dose of the study treatment.
Gastrointestinal disorders
Vomiting
0.00%
0/21 • Baseline up to Day 39
The safety population included all participants who received at least 1 dose of the study treatment.
4.8%
1/21 • Baseline up to Day 39
The safety population included all participants who received at least 1 dose of the study treatment.
Musculoskeletal and connective tissue disorders
Myalgia
4.8%
1/21 • Baseline up to Day 39
The safety population included all participants who received at least 1 dose of the study treatment.
0.00%
0/21 • Baseline up to Day 39
The safety population included all participants who received at least 1 dose of the study treatment.

Additional Information

Communication Center

Merck KGaA, Darmstadt, Germany

Phone: +49-6151-72-5200

Results disclosure agreements

  • Principal investigator is a sponsor employee
  • Publication restrictions are in place