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The Purpose of the Study is to Compare Two Fixed Dose Combination Tablets of Dapagliflozin/Metformin XR in Healthy Subjects Under Fasting and Fed Conditions

Phase 1
Completed
Conditions
Healthy Subjects in Fasted and Fed State
Interventions
Drug: Dapagliflozin/metformin XR 5/500mg
Drug: Dapagliflozin/metformin XR 10/1000mg
Drug: Dapagliflozin/metformin XR 5/500 mg
Registration Number
NCT03216278
Lead Sponsor
AstraZeneca
Brief Summary

This is a bioequivalence study of two doses of the dapagliflozin/metformin XR tablet manufactured at two different plants.

Detailed Description

This is a two part, open-label, randomized, 4-period, 4-treatment (per study part) crossover study in healthy subjects (males and females of non-childbearing potential), performed at a single study center, conducted to establish the bioequivalence of 2 strengths of dapagliflozin/metformin XR tablets manufactured at two different plants.

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
284
Inclusion Criteria

Not provided

Exclusion Criteria

Not provided

Study & Design

Study Type
INTERVENTIONAL
Study Design
CROSSOVER
Arm && Interventions
GroupInterventionDescription
Treatment ADapagliflozin/metformin XR 5/500mgDapagliflozin/metformin XR 5/500 Mount Vernon Test Product Fed
Treatment CDapagliflozin/metformin XR 5/500mgDapagliflozin/metformin XR 5/500 Mount Vernon Test Product Fasted
Treatment GDapagliflozin/metformin XR 10/1000mgDapagliflozin/metformin XR 10/1000 Mount Vernon Test Product Fasted
Treatment EDapagliflozin/metformin XR 10/1000mgDapagliflozin/metformin XR 10/1000 Mount Vernon Test Product Fed
Treatment BDapagliflozin/metformin XR 5/500 mgDapagliflozin/metformin XR 5/500 Humacao Reference Product Fed
Treatment DDapagliflozin/metformin XR 5/500mgDapagliflozin/metformin XR 5/500 Humacao Reference Product Fasted
Treatment HDapagliflozin/metformin XR 10/1000mgDapagliflozin/metformin XR 10/1000 Humacao Reference Product Fasted
Treatment FDapagliflozin/metformin XR 10/1000mgDapagliflozin/metformin XR 10/1000 Humacao Reference Product Fed
Primary Outcome Measures
NameTimeMethod
Part 1 - Area under the plasma concentration versus time curve (AUC) for each analyte and each stateBased on pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 36, 48 and 72 hours post-dose sampling times

To demonstrate the bioequivalence of dapagliflozin/metformin XR 5/500 mg manufactured at Mount Vernon plant and dapagliflozin/metformin XR 5/500 mg manufactured at Humacao plant in metformin and in dapagliflozin plasma concentrations for the fed state and, separately, the fasted state.

Part 2 - Area under the plasma concentration versus time curve (AUC) for each analyte and each stateBased on pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 36, 48 and 72 hours post-dose sampling times

To demonstrate the bioequivalence of dapagliflozin/metformin XR 10/1000 mg manufactured at Mount Vernon plant and dapagliflozin/metformin XR 10/1000 mg manufactured at Humacao plant in metformin and dapagliflozin plasma concentrations for the fed state and, separately, the fasted state.

Part 1 - Peak Plasma Concentration (Cmax) for each analyte and each stateBased on pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 36, 48 and 72 hours post-dose sampling times

To demonstrate the bioequivalence of dapagliflozin/metformin XR 5/500 mg manufactured at Mount Vernon plant and dapagliflozin/metformin XR 5/500 mg manufactured at Humacao plant in metformin and in dapagliflozin plasma concentrations for the fed state and, separately, the fasted state.

Part 2 - Peak Plasma Concentration (Cmax) for each analyte and each stateBased on pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 36, 48 and 72 hours post-dose sampling times

To demonstrate the bioequivalence of dapagliflozin/metformin XR 10/1000 mg manufactured at Mount Vernon plant and dapagliflozin/metformin XR 10/1000 mg manufactured at Humacao plant in metformin and in dapagliflozin plasma concentrations for the fed state and, separately, the fasted state.

Secondary Outcome Measures
NameTimeMethod
Time to reach maximum plasma concentration (tmax)Based on pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 36, 48 and 72 hours post-dose sampling times

Measurements of tmax for dapagliflozin and metformin when administered in both fed and fasted states as single doses of dapagliflozin/metformin 5/500 mg or 10/1000 mg formulation from both the Mount Vernon and Humacao plants.

Area under plasma concentration - time curve from time zero to infinity (AUC)Based on pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 36, 48 and 72 hours post-dose sampling times

Measurements of AUC from time zero to infinity for dapagliflozin and metformin when administered as single doses of dapagliflozin/metformin 5/500 mg or 10/1000 mg formulation from both the Mount Vernon and Humacao plants both fed and fasted states.

Blood pressure10,5 weeks

To evaluate the safety of single doses of dapagliflozin/metformin 5/500 mg or 10/1000 mg formulation from both the Mount Vernon and Humacao plants both fed and fasted states by assessing changes from baseline in mmHg of systolic and diastolic blood pressure.

Apparent total body clearance after extravascular administration (CL/F)Based on pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 36, 48 and 72 hours post-dose sampling times

Measurements of apparent total body clearance after extravascular administration (CL/F) for dapagliflozin and metformin when administered in both fed and fasted states as single doses of dapagliflozin/metformin 5/500 mg or 10/1000 mg formulation from both the Mount Vernon and Humacao plants.

Laboratory assessments - hematology10,5 weeks

To evaluate the safety of single doses of dapagliflozin/metformin 5/500 mg or 10/1000 mg formulation from both the Mount Vernon and Humacao plants both fed and fasted states by assessing changes from baseline in hematology.

Electrocardiogram (ECG)10,5 weeks

To evaluate the safety of single doses of dapagliflozin/metformin 5/500 mg or 10/1000 mg formulation from both the Mount Vernon and Humacao plants both fed and fasted states by assessing changes from baseline in overall ECG evaluation.

Terminal elimination rate constant (λz)Based on pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 36, 48 and 72 hours post-dose sampling times

Measurements of terminal elimination rate constant (λz) for dapagliflozin and metformin when administered in both fed and fasted states as single doses of dapagliflozin/metformin 5/500 mg or 10/1000 mg formulation from both the Mount Vernon and Humacao plants.

Apparent volume of distribution during the terminal phase after extravascular administration (Vz/F)Based on pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 36, 48 and 72 hours post-dose sampling times

Measurements of apparent volume of distribution during the terminal phase after extravascular administration (Vz/F) for dapagliflozin and metformin when administered in both fed and fasted states as single doses of dapagliflozin/metformin 5/500 mg or 10/1000 mg formulation from both the Mount Vernon and Humacao plants.

Adverse events10,5 weeks

To evaluate the safety of single doses of dapagliflozin/metformin 5/500 mg or 10/1000 mg formulation from both the Mount Vernon and Humacao plants both fed and fasted states by assessing the number of subjects with adverse events.

Half-life associated with terminal slope (λz) of a semi-logarithmic concentration-time curve (t½λz)Based on pre-dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 24, 36, 48 and 72 hours post-dose sampling times

Measurements of half-life associated with terminal slope (t½λz) for dapagliflozin and metformin when administered in both fed and fasted states as single doses of dapagliflozin/metformin 5/500 mg or 10/1000 mg formulation from both the Mount Vernon and Humacao plants.

Heart rate10,5 weeks

To evaluate the safety of single doses of dapagliflozin/metformin 5/500 mg or 10/1000 mg formulation from both the Mount Vernon and Humacao plants both fed and fasted states by assessing changes from baseline in heart rate measured as beats per minute.

Laboratory assessments - clinical chemistry10,5 weeks

To evaluate the safety of single doses of dapagliflozin/metformin 5/500 mg or 10/1000 mg formulation from both the Mount Vernon and Humacao plants both fed and fasted states by assessing changes from baseline in clinical chemistry.

Laboratory assessments - urinalysis10,5 weeks

To evaluate the safety of single doses of dapagliflozin/metformin 5/500 mg or 10/1000 mg formulation from both the Mount Vernon and Humacao plants both fed and fasted states by assessing changes from baseline in urinalysis.

Trial Locations

Locations (1)

Research Site

🇧🇷

Aparecida de Goiania, Brazil

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