Pharmacokinetics of Fixed Dose Combination (FDC) Tablets of Linagliptin /Metformin - Full Text View

Purpose

The aim of the trial is to assess the relative bioavailability of fixed dose combination tablets of linagliptin and metformin compared to the administration of two single tablets (linagliptin and metformin ) in Chinese subjects. The availability of a fixed dose combination tablet is expected to significantly enhance patients` compliance with antidiabetic treatment., in particular with concern to the frequent polypharmacy in diabetic patients.

Condition	Intervention	Phase
Healthy	Drug: linagliptin/metformin(high dose) Drug: Linagliptin/metformin(low dose)	Phase 1

Study Type:	Interventional
Study Design:	Allocation: Randomized Endpoint Classification: Pharmacokinetics Study Intervention Model: Crossover Assignment Masking: Open Label Primary Purpose: Treatment
Official Title:	Characterisation of Fixed Dose Combination Tablets of Linagliptin 2.5 mg/Metformin 850 mg or Linagliptin 2.5 mg/Metformin 500 mg and Relative Oral Bioavailability Compared With Single Linagliptin 2.5 mg and Metformin 850 mg or 500 mg Tablets Administered Together to Healthy Chinese Male and Female Volunteers in an Open Label, Randomised, Single-dose, Two-way Crossover, Phase I Study

Resource links provided by NLM:

Drug Information available for: Metformin Metformin hydrochloride Linagliptin

U.S. FDA Resources

Further study details as provided by Boehringer Ingelheim Pharmaceuticals:

Primary Outcome Measures:

relative bioavailability of linagliptin is primarily investigated on the basis of Area under curve (AUC)0-72 h; [ Time Frame: up to 8 weeks ] [ Designated as safety issue: No ]
relative bioavailability of metformin is primarily investigated on the basis of AUC0-tz [ Time Frame: up to 8 weeks ] [ Designated as safety issue: No ]
relative bioavailability of linagliptin is primarily investigated on the basis of Cmax; [ Time Frame: up to 8 weeks ] [ Designated as safety issue: No ]
relative bioavailability of metformin is primarily investigated on the basis of Cmax [ Time Frame: up to 8 weeks ] [ Designated as safety issue: No ]

Secondary Outcome Measures:

Linagliptin and metformin:AUC0-infinity [ Time Frame: up to 8 weeks ] [ Designated as safety issue: No ]
Linagliptin only:AUC0-tz [ Time Frame: up to 8 weeks ] [ Designated as safety issue: No ]
Linagliptin and metformin:tmax(time from dosing to maximum concentration of linagliptin and metformin in plasma) [ Time Frame: up to 8 weeks ] [ Designated as safety issue: No ]
Linagliptin and metformin:lambda-z (terminal elimination rate constant of linagliptin and metformin in plasma) [ Time Frame: up to 8 weeks ] [ Designated as safety issue: No ]
Linagliptin and metformin:t1/2 (terminal half-life of linagliptin and metformin in plasma) [ Time Frame: up to 8 weeks ] [ Designated as safety issue: No ]
Linagliptin and metformin:MRTpo (mean residence time of linagliptin / metformin in the body after po administration) [ Time Frame: up to 8 weeks ] [ Designated as safety issue: No ]
Linagliptin and metformin:CL/F (apparent clearance of linagliptin and metformin in the plasma after extravascular administration) [ Time Frame: up to 8 weeks ] [ Designated as safety issue: No ]
Linagliptin and metformin:Vz/F (apparent volume of distribution during the terminal phase of linagliptin and metformin following an extravascular dose) [ Time Frame: up to 8 weeks ] [ Designated as safety issue: No ]

Enrollment:	48
Study Start Date:	February 2012
Study Completion Date:	June 2012
Primary Completion Date:	June 2012 (Final data collection date for primary outcome measure)

Arms	Assigned Interventions
Experimental: linagliptin/metformin(high dose) 24 subjects (12 male and 12 female) will be assigned to 2 treatment sequences. cross-over design was adopted to ensure each patient would take fixed dose combination tablets of linagliptin /metformin (high dose) and single linagliptin and metformin (high dose) tablets single dose in randomized order	Drug: linagliptin/metformin(high dose) patient would take fixed dose combination tablets of linagliptin /metformin (high dose) and single linagliptin and metformin (High dose) tablets single dose in random order, and each dosage will be separated in 42 days interval.
Experimental: linagliptin/metformin(low dose) 24 subjects (12 male and 12 female) will be assigned to 2 treatment sequences. cross-over design was adopted to ensure each patient would take fixed dose combination tablets of linagliptin /metformin (low dose) and single linagliptin and metformin (low dose) tablets single dose in randomized order	Drug: Linagliptin/metformin(low dose) patient would take fixed dose combination tablets of linagliptin /metformin (low dose) and single linagliptin and metformin (Low dose) tablets single dose in random order, and each dosage will be separated in 42 days interval.

Eligibility

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

Criteria

Inclusion criteria:

1. Healthy male and female subjects

Exclusion criteria:

1. Any relevant deviation from healthy conditions

Contacts and Locations

Please refer to this study by its ClinicalTrials.gov identifier: NCT01540487

Locations

China
1288.5.86001 Boehringer Ingelheim Investigational Site
Beijing, China

Sponsors and Collaborators

Boehringer Ingelheim Pharmaceuticals

Investigators

Study Chair:

Boehringer Ingelheim

Boehringer Ingelheim Pharmaceuticals

More Information

No publications provided

Responsible Party:	Boehringer Ingelheim Pharmaceuticals
ClinicalTrials.gov Identifier:	NCT01540487 History of Changes
Other Study ID Numbers:	1288.5
Study First Received:	February 23, 2012
Last Updated:	November 14, 2012
Health Authority:	China: Food and Drug Administration

Additional relevant MeSH terms:

BI 1356
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 June 18, 2013