Bioequivalence Study of Sitagliptin/Metformin Combination Tablet (MK0431A-122)

This study has been completed.
Sponsor:
Information provided by:
Merck Sharp & Dohme Corp.
ClinicalTrials.gov Identifier:
NCT01093794
First received: March 19, 2010
Last updated: June 3, 2011
Last verified: June 2011
  Purpose

This study will test the hypothesis that the Final Market Image (FMI) sitagliptin/metformin 50 mg/500 mg and 50 mg/850 mg (Fixed Dose Combination) FDC tablet and co-administration of corresponding doses of sitagliptin and China-sourced metformin as individual tablets will be bioequivalent based on assessment of the AUC(0-t) and Cmax, for both sitagliptin and metformin.


Condition Intervention Phase
Type 2 Diabetes
Drug: Co-administration of 50 mg sitagliptin and 500 mg metformin
Drug: sitagliptin/metformin 50 mg/500 mg tablet
Drug: Co-administration of 50 mg sitagliptin and 850 mg metformin
Drug: sitagliptin/metformin 50 mg/850 mg tablet
Phase 1

Study Type: Interventional
Study Design: Allocation: Randomized
Endpoint Classification: Bio-equivalence Study
Intervention Model: Crossover Assignment
Masking: Open Label
Primary Purpose: Treatment
Official Title: A Bioequivalence Study With Two Tablet Strengths of the Final Market Image (FMI) Sitagliptin/Metformin Fixed Dose Combination (FDC) Tablet

Resource links provided by NLM:


Further study details as provided by Merck Sharp & Dohme Corp.:

Primary Outcome Measures:
  • Area Under the Curve (AUC(0-t)) for Sitagliptin [ Time Frame: baseline through 72 hours postdose ] [ Designated as safety issue: No ]
    AUC (0-t) is the area under the curve for the plot showing plasma concentration against time from time zero to the time of the last quantifiable concentration for sitagliptin 50 mg, metformin 500 mg and metformin 850 mg.

  • Cmax for Sitagliptin and Metformin [ Time Frame: baseline through 72 hours postdose ] [ Designated as safety issue: No ]
    Cmax is the peak serum concentration of a therapeutic drug after administration; and is used to determine the rate and extent of drug absorption. Cmax is reported for sitagliptin 50 mg, metformin 500 mg and metformin 850 mg.


Enrollment: 28
Study Start Date: April 2010
Study Completion Date: June 2010
Primary Completion Date: June 2010 (Final data collection date for primary outcome measure)
Arms Assigned Interventions
Experimental: 1. Sit + Met500 / SitMet500 FDC / SitMet850 FDC / Sit + Met850

Participants were administered treatment in the following sequence with a minimum 7 day washout period between treatments:

  • Co-administration of 50 mg sitagliptin and 500 mg metformin
  • sitagliptin/metformin 50 mg/500 mg FDC tablet
  • sitagliptin/metformin 50 mg/850 mg FDC tablet
  • Co-administration of 50 mg sitagliptin and 850 mg metformin
Drug: Co-administration of 50 mg sitagliptin and 500 mg metformin
Co-administration of 50 mg sitagliptin and 500 mg China-sourced metformin as individual tablets with 240 ml water on Day 1 of the relevant treatment period (Sit + Met500) after fasting for at least 10 hours.
Drug: sitagliptin/metformin 50 mg/500 mg tablet
Single dose administration of the final marketing image (FMI) sitagliptin/metformin 50 mg/500 mg fixed-dose combination (FDC) tablet with 240 ml water on Day 1 of the relevant treatment period (SitMet850 FDC) after fasting for at least 10 hours.
Drug: Co-administration of 50 mg sitagliptin and 850 mg metformin
Co-administration of 50 mg sitagliptin and 850 mg China sourced metformin as individual tablets with 240 ml water on Day 1 of the relevant treatment period (Sit + Met850) after fasting for at least 10 hours.
Drug: sitagliptin/metformin 50 mg/850 mg tablet
Single dose administration of the FMI sitagliptin/metformin 50 mg/850 mg FDC tablet with 240 ml water on Day 1 of the relevant treatment period (SitMet850 FDC) after fasting for at least 10 hours.
Experimental: 2. SitMet500 FDC / Sit + Met850 / Sit + Met500 / SitMet850 FDC

Participants were administered treatment in the following sequence with a minimum 7 day washout period between treatments:

  • sitagliptin/metformin 50 mg/500 mg FDC tablet
  • Co-administration of 50 mg sitagliptin and 850 mg metformin
  • Co-administration of 50 mg sitagliptin and 500mg metformin
  • sitagliptin/metformin 50 mg/850 mg FDC tablet
Drug: Co-administration of 50 mg sitagliptin and 500 mg metformin
Co-administration of 50 mg sitagliptin and 500 mg China-sourced metformin as individual tablets with 240 ml water on Day 1 of the relevant treatment period (Sit + Met500) after fasting for at least 10 hours.
Drug: sitagliptin/metformin 50 mg/500 mg tablet
Single dose administration of the final marketing image (FMI) sitagliptin/metformin 50 mg/500 mg fixed-dose combination (FDC) tablet with 240 ml water on Day 1 of the relevant treatment period (SitMet850 FDC) after fasting for at least 10 hours.
Drug: Co-administration of 50 mg sitagliptin and 850 mg metformin
Co-administration of 50 mg sitagliptin and 850 mg China sourced metformin as individual tablets with 240 ml water on Day 1 of the relevant treatment period (Sit + Met850) after fasting for at least 10 hours.
Drug: sitagliptin/metformin 50 mg/850 mg tablet
Single dose administration of the FMI sitagliptin/metformin 50 mg/850 mg FDC tablet with 240 ml water on Day 1 of the relevant treatment period (SitMet850 FDC) after fasting for at least 10 hours.
Experimental: 3. Sit + Met850 / SitMet850 FDC / SitMet500 FDC / Sit + Met500

Participants were administered treatment in the following sequence with a minimum 7 day washout period between treatments:

  • Co-administration of 50 mg sitagliptin and 850 mg metformin
  • sitagliptin/metformin 50 mg/850 mg FDC tablet
  • sitagliptin/metformin 50 mg/500 mg FDC tablet
  • Co-administration of 50 mg sitagliptin and 500mg metformin
Drug: Co-administration of 50 mg sitagliptin and 500 mg metformin
Co-administration of 50 mg sitagliptin and 500 mg China-sourced metformin as individual tablets with 240 ml water on Day 1 of the relevant treatment period (Sit + Met500) after fasting for at least 10 hours.
Drug: sitagliptin/metformin 50 mg/500 mg tablet
Single dose administration of the final marketing image (FMI) sitagliptin/metformin 50 mg/500 mg fixed-dose combination (FDC) tablet with 240 ml water on Day 1 of the relevant treatment period (SitMet850 FDC) after fasting for at least 10 hours.
Drug: Co-administration of 50 mg sitagliptin and 850 mg metformin
Co-administration of 50 mg sitagliptin and 850 mg China sourced metformin as individual tablets with 240 ml water on Day 1 of the relevant treatment period (Sit + Met850) after fasting for at least 10 hours.
Drug: sitagliptin/metformin 50 mg/850 mg tablet
Single dose administration of the FMI sitagliptin/metformin 50 mg/850 mg FDC tablet with 240 ml water on Day 1 of the relevant treatment period (SitMet850 FDC) after fasting for at least 10 hours.
Experimental: 4. SitMet850 FDC / Sit + Met500 / Sit + Met850 / SitMet500 FDC

Participants were administered treatment in the following sequence with a minimum 7 day washout period between treatments:

  • sitagliptin/metformin 50 mg/850 mg FDC tablet
  • Co-administration of 50 mg sitagliptin and 500 mg metformin
  • Co-administration of 50 mg sitagliptin and 850 mg metformin
  • sitagliptin/metformin 50 mg/500 mg FDC tablet
Drug: Co-administration of 50 mg sitagliptin and 500 mg metformin
Co-administration of 50 mg sitagliptin and 500 mg China-sourced metformin as individual tablets with 240 ml water on Day 1 of the relevant treatment period (Sit + Met500) after fasting for at least 10 hours.
Drug: sitagliptin/metformin 50 mg/500 mg tablet
Single dose administration of the final marketing image (FMI) sitagliptin/metformin 50 mg/500 mg fixed-dose combination (FDC) tablet with 240 ml water on Day 1 of the relevant treatment period (SitMet850 FDC) after fasting for at least 10 hours.
Drug: Co-administration of 50 mg sitagliptin and 850 mg metformin
Co-administration of 50 mg sitagliptin and 850 mg China sourced metformin as individual tablets with 240 ml water on Day 1 of the relevant treatment period (Sit + Met850) after fasting for at least 10 hours.
Drug: sitagliptin/metformin 50 mg/850 mg tablet
Single dose administration of the FMI sitagliptin/metformin 50 mg/850 mg FDC tablet with 240 ml water on Day 1 of the relevant treatment period (SitMet850 FDC) after fasting for at least 10 hours.

  Eligibility

Ages Eligible for Study:   18 Years to 40 Years
Genders Eligible for Study:   Male
Accepts Healthy Volunteers:   Yes
Criteria

Inclusion Criteria:

  • Subject is of Chinese descent
  • Subject is in good health
  • Subject is a non-smoker

Exclusion Criteria:

  • Subject has a history of stroke or chronic seizures
  • Subject has a history of cancer
  • Subject has had major surgery, donated blood or participated in another investigational study within the past 4 weeks
  Contacts and Locations
Please refer to this study by its ClinicalTrials.gov identifier: NCT01093794

Sponsors and Collaborators
Merck Sharp & Dohme Corp.
Investigators
Study Director: Medical Monitor Merck Sharp & Dohme Corp.
  More Information

No publications provided

Responsible Party: Vice President, Late Stage Development Group Leader, Merck Sharp & Dohme Corp
ClinicalTrials.gov Identifier: NCT01093794     History of Changes
Other Study ID Numbers: MK-0431A-122, 2010_518
Study First Received: March 19, 2010
Results First Received: June 3, 2011
Last Updated: June 3, 2011
Health Authority: China: Ministry of Health

Keywords provided by Merck Sharp & Dohme Corp.:
Type 2 Diabetes

Additional relevant MeSH terms:
Diabetes Mellitus
Diabetes Mellitus, Type 2
Glucose Metabolism Disorders
Metabolic Diseases
Endocrine System Diseases
Sitagliptin
Metformin
Hypoglycemic Agents
Physiological Effects of Drugs
Pharmacologic Actions
Dipeptidyl-Peptidase IV Inhibitors
Protease Inhibitors
Enzyme Inhibitors
Molecular Mechanisms of Pharmacological Action

ClinicalTrials.gov processed this record on April 14, 2014