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Bioequivalence of Metformin Under Fed Conditions After Administration of Linagliptin / Metformin Fixed Dose Combination Tablet and Single Tablets

Bioequivalence of Metformin Under Fed Conditions After Administration of a 2.5 mg Linagliptin / 500 mg Metformin Fixed Dose Combination Tablet Compared With Single Linagliptin 2.5 mg and Metformin 500 mg Tablets Administered Together in Healthy Male and Female Volunteers, (an Open-label, Randomised, Single Dose, Two-way Crossover, Phase I Trial)

Status
Completed
Phases
Phase 1
Study type
Interventional
Source
ClinicalTrials.gov
Registry ID
NCT01581931
Enrollment
32
Registered
2012-04-20
Start date
2012-04-30
Completion date
2012-06-30
Last updated
2013-08-20

For informational purposes only — not medical advice. Sourced from public registries and may not reflect the latest updates. Terms

Conditions

Healthy

Brief summary

To establish bioequivalence (BE) under fed conditions between metformin in linagliptin/metformin fixed dose combination tablet and metformin reference product administered in free combination togther with linagliptin

Interventions

DRUGLinagliptin/metformin

FDC

DRUGMetformin

single tablet Metformin

DRUGLinagliptin

single tablet Linagliptin

Sponsors

Boehringer Ingelheim
Lead SponsorINDUSTRY

Study design

Allocation
RANDOMIZED
Intervention model
CROSSOVER
Primary purpose
TREATMENT
Masking
NONE

Eligibility

Sex/Gender
ALL
Age
18 Years to 55 Years
Healthy volunteers
Yes

Inclusion criteria

1\. Healthy male and female subjects

Exclusion criteria

1\. Any relevant deviation from healthy conditions

Design outcomes

Primary

MeasureTime frameDescription
Area Under Curve From 0 to tz Hours (AUC0-tz) of Metformin0:20, 0:40, 1, 1:30, 2, 3, 4, 5, 6, 8, 12, 24, 34, 48, 72 hoursAUC0-tz represents the area under the concentration curve of metformin in plasma from 0 to the time of the last quantifiable plasma contentration of the analyte. Note, the geometric mean is actually an adjusted geometric mean.
Maximum Concentration (Cmax) of Metformin0:20, 0:40, 1, 1:30, 2, 3, 4, 5, 6, 8, 12, 24, 34, 48, 72 hoursCmax represents the maximum concentration of metformin in plasma. Note, the geometric mean is actually an adjusted geometric mean.

Secondary

MeasureTime frameDescription
Area Under Curve From 0 to Infinity Hours (AUC0-infty) of Metformin0:20, 0:40, 1, 1:30, 2, 3, 4, 5, 6, 8, 12, 24, 34, 48, 72 hoursAUC0-infty represents the area under the concentration curve of metformin in plasma from time 0 extrapolated to infinity. Note, the geometric mean is actually an adjusted geometric mean.
Time to Maximum Concentration (Tmax) of Metformin0:20, 0:40, 1, 1:30, 2, 3, 4, 5, 6, 8, 12, 24, 34, 48, 72 hoursTime from dosing to the maximum concentration of metformin in plasma.
Terminal Half-life t1/2 of Metformin0:20, 0:40, 1, 1:30, 2, 3, 4, 5, 6, 8, 12, 24, 34, 48, 72 hoursThe terminal half-life of metformin in plasma is denoted by t1/2.

Countries

Germany

Participant flow

Participants by arm

ArmCount
Overall Study
This was an open-label, randomised, single dose, 2-way crossover trial with 2 treatments and 2 treatment sequences. The single dose administrations in each treatment period were separated by a washout period of at least 35 days.
32
Total32

Withdrawals & dropouts

PeriodReasonFG000FG001
WashoutAdverse Event01

Baseline characteristics

CharacteristicOverall Study
Age Continuous38.8 years
STANDARD_DEVIATION 9.9
Sex: Female, Male
Female
17 Participants
Sex: Female, Male
Male
15 Participants

Adverse events

Event typeEG000
affected / at risk
EG001
affected / at risk
deaths
Total, all-cause mortality
— / —— / —
other
Total, other adverse events
6 / 319 / 32
serious
Total, serious adverse events
0 / 311 / 32

Outcome results

Primary

Area Under Curve From 0 to tz Hours (AUC0-tz) of Metformin

AUC0-tz represents the area under the concentration curve of metformin in plasma from 0 to the time of the last quantifiable plasma contentration of the analyte. Note, the geometric mean is actually an adjusted geometric mean.

Time frame: 0:20, 0:40, 1, 1:30, 2, 3, 4, 5, 6, 8, 12, 24, 34, 48, 72 hours

Population: Treated set - all subjects taking at least 1 dose of trial medication

ArmMeasureValue (GEOMETRIC_MEAN)Dispersion
Lina+Met Single TabletsArea Under Curve From 0 to tz Hours (AUC0-tz) of Metformin7219.03 ng·h/mLGeometric Coefficient of Variation 9.8
Lina+Met FDC TabletArea Under Curve From 0 to tz Hours (AUC0-tz) of Metformin7057.52 ng·h/mLGeometric Coefficient of Variation 9.8
90% CI: [93.64, 102.07]ANOVA
Primary

Maximum Concentration (Cmax) of Metformin

Cmax represents the maximum concentration of metformin in plasma. Note, the geometric mean is actually an adjusted geometric mean.

Time frame: 0:20, 0:40, 1, 1:30, 2, 3, 4, 5, 6, 8, 12, 24, 34, 48, 72 hours

Population: Treated set - all subjects taking at least 1 dose of trial medication

ArmMeasureValue (GEOMETRIC_MEAN)Dispersion
Lina+Met Single TabletsMaximum Concentration (Cmax) of Metformin855.09 ng/mLGeometric Coefficient of Variation 10
Lina+Met FDC TabletMaximum Concentration (Cmax) of Metformin844.72 ng/mLGeometric Coefficient of Variation 10
90% CI: [94.55, 103.21]ANOVA
Secondary

Area Under Curve From 0 to Infinity Hours (AUC0-infty) of Metformin

AUC0-infty represents the area under the concentration curve of metformin in plasma from time 0 extrapolated to infinity. Note, the geometric mean is actually an adjusted geometric mean.

Time frame: 0:20, 0:40, 1, 1:30, 2, 3, 4, 5, 6, 8, 12, 24, 34, 48, 72 hours

Population: Treated set - all subjects taking at least 1 dose of trial medication

ArmMeasureValue (GEOMETRIC_MEAN)Dispersion
Lina+Met Single TabletsArea Under Curve From 0 to Infinity Hours (AUC0-infty) of Metformin7343.59 ng·h/mLGeometric Coefficient of Variation 9.7
Lina+Met FDC TabletArea Under Curve From 0 to Infinity Hours (AUC0-infty) of Metformin7174.30 ng·h/mLGeometric Coefficient of Variation 9.7
95% CI: [93.63, 101.94]ANOVA
Secondary

Terminal Half-life t1/2 of Metformin

The terminal half-life of metformin in plasma is denoted by t1/2.

Time frame: 0:20, 0:40, 1, 1:30, 2, 3, 4, 5, 6, 8, 12, 24, 34, 48, 72 hours

Population: Treated set - all subjects taking at least 1 dose of trial medication

ArmMeasureValue (GEOMETRIC_MEAN)Dispersion
Lina+Met Single TabletsTerminal Half-life t1/2 of Metformin9.14 HoursGeometric Coefficient of Variation 87.4
Lina+Met FDC TabletTerminal Half-life t1/2 of Metformin8.03 HoursGeometric Coefficient of Variation 86
Secondary

Time to Maximum Concentration (Tmax) of Metformin

Time from dosing to the maximum concentration of metformin in plasma.

Time frame: 0:20, 0:40, 1, 1:30, 2, 3, 4, 5, 6, 8, 12, 24, 34, 48, 72 hours

Population: Treated set - all subjects taking at least 1 dose of trial medication

ArmMeasureValue (MEDIAN)
Lina+Met Single TabletsTime to Maximum Concentration (Tmax) of Metformin4.00 Hours
Lina+Met FDC TabletTime to Maximum Concentration (Tmax) of Metformin4.00 Hours

Source: ClinicalTrials.gov · Data processed: Feb 4, 2026