Comparative Bioavailability Study of Metformin/Sitagliptin 850 mg/50 mg Tablets in Healthy Male and Female Volunteers

Galenicum Health

Status and phase: Completed; Phase 1

Conditions: Bioequivalence; Diabetes Mellitus, Type 2

Treatments: Drug: Sitagliptin/Metformin HCl 50/850 mg film-coated tablet

Study type: Interventional

Funder types: Industry

Identifiers

NCT05549570

GLU-P6-810

Details and patient eligibility

About

The objective of this study was to evaluate and compare the bioavailability and therefore to assess the bioequivalence of two different formulations of metformin/sitagliptin after a single oral dose administration under fed conditions.

Enrollment: 26 patients

Sex: All

Ages: 18 to 65 years old

Volunteers: Accepts Healthy Volunteers

Inclusion and exclusion criteria

The main Inclusion Criteria were:

• non- or ex-smokers
• body mass index (BMI) within 18.5 to 30.0 kg/m2, inclusively
• no clinically significant abnormality found in the 12-lead electrocardiogram (ECG) performed at study entry
• negative pregnancy test for female subjects
• healthy according to medical history, complete physical examination (including vital signs) and laboratory tests (general biochemistry, hematology and urinalysis)

Exclusion Criteria:

• Females who were pregnant or were lactating
• History of significant hypersensitivity to metformin, sitagliptin or any related products (including excipients of the formulations) as well as severe hypersensitivity reactions (like angioedema) to any drugs
• Presence of significant gastrointestinal, liver or kidney disease, or any other conditions known to interfere with the absorption, distribution, metabolism or excretion of drugs or known to potentiate or predispose to undesired effects
• History of significant gastrointestinal, liver or kidney disease that may have affected drug bioavailability
• Presence of significant cardiovascular, pulmonary, hematologic, neurological, psychiatric, endocrine, immunologic or dermatologic disease
• History of or disposition to seizures, state of confusion, clinically relevant psychiatric diseases
• Presence of out-of-range cardiac interval (PR < 110 msec, PR > 200 msec, QRS < 60 msec, QRS >119 msec and QTc > 450 msec for males and QTc > 460 for females) on the screening ECG or other clinically significant ECG abnormalities
• Maintenance therapy with any drug or significant history of drug dependency or alcohol abuse (> 3 units of alcohol per day, intake of excessive alcohol, acute or chronic)
• Any clinically significant illness in the previous 28 days before day 1 of this study
• Use of any enzyme-modifying drugs, including strong inhibitors of cytochrome P450 (CYP) enzymes (such as cimetidine, fluoxetine, quinidine, erythromycin, ciprofloxacin, fluconazole, ketoconazole, diltiazem and HIV antivirals) and strong inducers of CYP enzymes (such as barbiturates, carbamazepine, glucocorticoids, phenytoin, rifampin and St John's Wort), in the previous 28 days before day 1 of this study
• Any history of tuberculosis and/or prophylaxis for tuberculosis
• Positive screening of alcohol and/or drugs of abuse
• Positive results to HIV Ag/Ab Combo, Hepatitis B surface Antigen (HBsAG (B) (hepatitis B)) or Hepatitis C Virus (HCV (C)) tests
• Females who were pregnant according to a positive pregnancy test
• Volunteers who took metformin and/or sitagliptin in the previous 28 days before day 1 of this study
• Volunteers who took an Investigational Product (in another clinical trial) in the previous 28 days before day 1 of this study
• Volunteers who had already participated in this clinical study
• Volunteers who donated 50 mL or more of blood in the previous 28 days before day 1 of this study
• Donation of 500 mL or more of blood (Canadian Blood Services, Hema-Quebec, clinical studies, etc.) in the previous 56 days before day 1 of this study

Trial design

Primary purpose: Other

Allocation: Randomized

Interventional model: Crossover Assignment

Masking: None (Open label)

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26 participants in 2 patient groups

Reference group

Experimental group

Description:

Thirty minutes after the start of the breakfast, a single dose of the Reference formulation was administered with approximately 240 mL of water at ambient temperature

Treatment:

Drug: Sitagliptin/Metformin HCl 50/850 mg film-coated tablet

Test group

Experimental group

Description:

Thirty minutes after the start of the breakfast, a single dose of the Test formulation was administered with approximately 240 mL of water at ambient temperature

Treatment:

Drug: Sitagliptin/Metformin HCl 50/850 mg film-coated tablet