Bioequivalence Study of Sitagliptin/Metformin Extended-Release Tablets in Healthy Subjects

NCT07679711 | Completed Phase 1

• 1 other identifier: QLG1061-01
• Study Type: interventional
• Target: 76
• Locations: 1 country
• Sites: 1

Brief Summary

The main purpose of this study is to compare the pharmacokinetics (how the body absorbs and clears the drug) and evaluate the bioequivalence of two formulations of sitagliptin/metformin hydrochloride extended-release tablets (50 mg/500 mg) in healthy adult subjects. The test product is manufactured by Qilu Pharmaceutical (Hainan) Co., Ltd., and the reference product is Janumet® XR. The study is designed as a single-center, open-label, randomized, single-dose, two-period, two-sequence crossover trial. It consists of two separate parts: a fasting study and a fed study. Participants will be randomly assigned to receive either the test formulation or the reference formulation in the first period. After a washout period of at least 5 days, participants will receive the alternate formulation in the second period. Blood samples will be collected at designated time points before and after dosing to measure the blood concentration of sitagliptin and metformin. Safety will also be continuously monitored throughout the study by assessing adverse events, vital signs, electrocardiograms (ECGs), and clinical laboratory tests.

Conditions

Healthy Volunteers

Outcome Measures

Primary Outcomes (3)

• Maximum Observed Plasma Concentration (Cmax) of Sitagliptin and Metformin

  Cmax will be obtained directly from the observed plasma concentration-time profiles of sitagliptin and metformin.

  Pre-dose (0 hours) and multiple time points up to 48.0 hours post-dose in each period

• Area Under the Plasma Concentration-Time Curve From Time Zero to the Last Quantifiable Concentration (AUC0-t) of Sitagliptin and Metformin

  AUC0-t is calculated using the linear trapezoidal rule.

  Pre-dose (0 hours) and multiple time points up to 48.0 hours post-dose in each period

• Area Under the Plasma Concentration-Time Curve From Time Zero to Infinity (AUC0-infty) of Sitagliptin and Metformin

  AUC0-infty is calculated as AUC0-t + Ct/λz, where Ct is the last quantifiable concentration and λz is the terminal elimination rate constant.

  Pre-dose (0 hours) and multiple time points up to 48.0 hours post-dose in each period

Study Arms (4)

Fasting, Sequence T-R

EXPERIMENTAL

Participants in the fasting cohort receive the test product (Sitagliptin/Metformin extended-release tablet) in Period 1, followed by a washout period of at least 5 days, and then receive the reference product (Janumet XR) in Period 2.

Drug: Sitagliptin / Metformin hydrochloride extended-release tablet (Test); Drug: Sitagliptin / Metformin hydrochloride extended-release tablet (Reference)

Fasting, Sequence R-T

ACTIVE COMPARATOR

Arm Description: Participants in the fasting cohort receive the reference product (Janumet XR) in Period 1, followed by a washout period of at least 5 days, and then receive the test product (Sitagliptin/Metformin extended-release tablet) in Period 2.

Drug: Sitagliptin / Metformin hydrochloride extended-release tablet (Test); Drug: Sitagliptin / Metformin hydrochloride extended-release tablet (Reference)

Fed, Sequence T-R

EXPERIMENTAL

Participants in the fed cohort (after a high-fat, high-calorie meal) receive the test product (Sitagliptin/Metformin extended-release tablet) in Period 1, followed by a washout period of at least 5 days, and then receive the reference product (Janumet XR) in Period 2.

Drug: Sitagliptin / Metformin hydrochloride extended-release tablet (Test); Drug: Sitagliptin / Metformin hydrochloride extended-release tablet (Reference)

Fed, Sequence R-T

ACTIVE COMPARATOR

Participants in the fed cohort (after a high-fat, high-calorie meal) receive the reference product (Janumet XR) in Period 1, followed by a washout period of at least 5 days, and then receive the test product (Sitagliptin/Metformin extended-release tablet) in Period 2.

Drug: Sitagliptin / Metformin hydrochloride extended-release tablet (Test); Drug: Sitagliptin / Metformin hydrochloride extended-release tablet (Reference)

Interventions

Sitagliptin / Metformin hydrochloride extended-release tablet (Test) DRUG

A single oral dose of sitagliptin 50 mg / metformin hydrochloride 500 mg extended-release tablet manufactured by Qilu Pharmaceutical (Hainan) Co., Ltd., administered with 240 mL of warm water.

Fasting, Sequence R-T; Fasting, Sequence T-R; Fed, Sequence R-T; Fed, Sequence T-R

Sitagliptin / Metformin hydrochloride extended-release tablet (Reference) DRUG

A single oral dose of sitagliptin 50 mg / metformin hydrochloride 500 mg extended-release tablet (Janumet XR) manufactured by Merck Sharp \& Dohme Corp., administered with 240 mL of warm water.

Fasting, Sequence R-T; Fasting, Sequence T-R; Fed, Sequence R-T; Fed, Sequence T-R

Eligibility Criteria

• Age: 18 Years+
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64), Older Adult (65+)

You may qualify if:

• Sign the informed consent form before the trial, and fully understand the trial content, process, and possible adverse reactions.
• Able to complete the study according to the requirements of the study protocol.
• Subjects voluntarily agree to use effective non-pharmacological contraception methods from the signing of informed consent (14 days prior to signing for female subjects) until 3 months after the last dose, with no plans for pregnancy, sperm donation, or egg donation.
• Male and female subjects aged 18 years and above.
• Male subjects weighing ≥ 50.0 kg and female subjects weighing ≥ 45.0 kg; Body Mass Index (BMI) within the range of 19.0 to 27.0 kg/m\^2 (inclusive).

You may not qualify if:

• History of specific allergies (e.g., urticaria, exfoliative dermatitis, angioedema, or bronchial hyperresponsiveness), or allergic constitution (e.g., allergic to two or more drugs, foods such as milk and pollen), or known allergy to the components or analogs of this drug.
• Serious history of cardiovascular, hepatic, renal, gastrointestinal, neurological, endocrine, respiratory, or psychiatric abnormalities, which the investigator considers inappropriate for participation.
• Clinically significant abnormal findings as judged by the investigator, including physical examination, vital signs, electrocardiogram, or clinical laboratory tests.
• History of or current pancreatitis.
• History of hypoglycemia.
• Estimated glomerular filtration rate (eGFR) \< 90 mL/min/1.73 m\^2.
• History of dysphagia or any gastrointestinal disease affecting drug absorption (e.g., gastric or small bowel resection, atrophic gastritis, gastrointestinal bleeding, obstruction, etc.).
• Difficulty in blood collection, intolerance to venipuncture, or history of needle/blood phobia.
• Female subjects who are pregnant, lactating, or have a positive pregnancy test result.
• Positive for any one or more of the following: Hepatitis B surface antigen, Hepatitis C antibody, HIV antibody, or Syphilis antibody.
• History of drug abuse within 5 years, use of illicit drugs within 3 months prior to screening, or positive urine drug screen.
• Consumption of more than 14 units of alcohol per week on average within 3 months prior to screening, or refusal to abstain from alcohol from 48 hours prior to dosing in each period until the end of blood collection for that period, or positive alcohol breath test.
• Smoking more than 5 cigarettes per day on average within 3 months prior to screening, or refusal to abstain from using any tobacco products during the clinical stay.
• History of surgery within 3 months prior to screening, or planned surgery during the study.
• Blood donation or massive blood loss (\>400 mL, excluding physiological blood loss in females) within 3 months prior to the first dose, or donation of 2 therapeutic units of platelets within 1 month.

Sponsors & Collaborators

• The Affiliated Hospital of Qingdao University: lead
• Qilu Pharmaceutical (Hainan) Co., Ltd.: collaborator

Study Sites (1)

The Affiliated Hospital of Qingdao University

Qingdao, Shandong, 266000, China

Location

MeSH Terms

Interventions

Sitagliptin Phosphate

Intervention Hierarchy (Ancestors)

Triazoles; Azoles; Heterocyclic Compounds, 1-Ring; Heterocyclic Compounds; Pyrazines

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: NONE
• Purpose: OTHER
• Intervention Model: CROSSOVER
• Sponsor Type: OTHER
• Responsible Party: PRINCIPAL INVESTIGATOR
• PI Title: Professor

Study Record Dates

• First Submitted: June 24, 2026
• First Posted: July 1, 2026
• Study Start: February 14, 2023
• Primary Completion: March 22, 2023
• Study Completion: March 22, 2023
• Last Updated: July 1, 2026

Record last verified: 2026-06

Locations

CN (1)