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Fed Bioequivalence Study of 2 Metformin 1000 mg Prolonged Release Tablets in 28 Healthy Male and Female Volunteers

Registration Number
NCT05125575
Lead Sponsor
Joint Stock Company "Farmak"
Brief Summary

This study was designed to compare the bioavailability of the Test Product Metformin 1000 mg Prolonged Release Tablets (JSC Farmak, Ukraine) and Reference Product Glucophage® XR 1000 mg Prolonged Release Tablets (Merck Serono Ltd, UK) in healthy male and female volunteers under fed conditions.

Detailed Description

An Open, Comparative, Randomized, Crossover Clinical Trial to Evaluate the Bioequivalence of Single Doses of Test Product Metformin 1000 mg Prolonged Release Tablets (JSC Farmak, Ukraine) and Reference Product Glucophage® XR 1000 mg Prolonged Release Tablets (Merck Serono Ltd, UK) in Healthy, Adult Male and Female Subjects Under Fed Conditions.

During each period 21 blood samples were taken: prior to dosing (-1.0) and 1.0, 2.0, 3.0, 4.0, 4.5, 5.0, 5.5, 6.0, 6.5, 7.0, 7.5, 8.0, 8.5, 9.0, 10.0, 12.0, 16.0, 24.0, 32.0 and 36.0 hours after IMP administration.

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
28
Inclusion Criteria
  • Healthy males and non-pregnant and no breast-feeding females (must have a negative pregnancy test result prior to dosing), Caucasian race.
  • Non-smoker or past-smoker (who has stopped smoking at least 6 months before the first dosing).
  • Body Mass Index (BMI) 18.5 to 30.0 kg/m2, inclusive and body weight between 50 kg and 100 kg(on the day of screening).
  • Subject was available for the whole study and had provided his/her written informed consent.
  • Subjects in good health, as determined by screening medical history, physical examination, vital signs assessments (pulse rate, systolic and diastolic blood pressure, and body temperature) and 12-lead ECG (electrocardiogram). Minor deviations outside the reference ranges were acceptable, if deemed not clinically significant by the Investigator.
  • Subjects in good health, as determined by screening clinical laboratory evaluations. Minor deviations outside the reference ranges were acceptable, if deemed not clinically significant by the Investigator.
  • Acceptance of use of contraceptive measures during the whole study by both female and male subjects.
Exclusion Criteria
  • Known cardiovascular disease, history of hypotension.
  • Factors in the subject's history that might predispose to ketoacidosis (including pancreatic insulin deficiency, history of pancreatitis, caloric restriction disorders, restricted food intake, alcohol abuse)
  • Gastrointestinal, renal or hepatic diseases and/or pathological findings present or in history, which might interfere with the drug pharmacokinetics.
  • Previous liver disease with elevations in serum transaminases.
  • Acute or chronic diseases and/or clinical finding which might interfere with the aims of the study or with the drug's safety, tolerability, bioavailability and/or pharmacokinetics of the Investigational Medicinal Product (IMP).
  • History of kidney disease and with impaired renal function.
  • History of severe allergy or allergic reactions to the study IMP, its excipients or related drugs.
  • Clinically significant illness within 28 days before the first dosing, including major surgery.
  • Any significant clinical abnormality including Hepatitis B surface antigen (HBsAg), hepatitis C virus (HCV), and / or (human immunodeficiency virus) HIV. (On screening)
  • Positive screening urine drugs abuse test or/and alcohol breath test or urine cotinine test, and positive pregnancy test on screening.
  • Serious mental disease and/or inability to cooperate with clinical team.
  • Sitting blood pressure after a minimum of 5 minutes of rest is out of the range of 100-140 mmHg for systolic blood pressure (BP) and/or 60-100 mmHg for diastolic BP and/or heart rate out of the range of 50-100 bpm during the screening procedure.
  • Body ear temperature was out of the range of 35.7-37.6°C at screening.
  • Orthostatic hypotension during the screening procedure.
  • Drug, alcohol (of ≥ 40 g per day pure ethanol), solvents or caffeine abuse.
  • Use of organ-toxic drugs or systemic drugs known to substantially alter liver metabolism within 90 days before the first dosing.
  • Use of any prescription medication for a period of 28 days before the first dosing.
  • Any systemic over-the-counter (OTC) drug treatment and/or vitamins and/or herbal treatment/or food supplements within 14 days before the first dosing.
  • Getting a tattoo, body piercing or any cosmetic treatment involving skin piercing within 90 days before the screening unless evaluated by Investigator as non-significant for inclusion in the study.
  • Donation or loss of at least 500 mL of blood within 90 days or donation of plasma or platelets within 14 days before the first dosing.
  • Anaemia, haemoglobin below 120 g/L for women and 130 g/L for men at screening.
  • Less than 30 days between exit procedure in previous study and the first dosing in this study.

Study & Design

Study Type
INTERVENTIONAL
Study Design
CROSSOVER
Arm && Interventions
GroupInterventionDescription
Treatment BGlucophage® XR 1000 mg Prolonged Release TabletsReference Product Glucophage® XR 1000 mg Prolonged Release Tablets (Merck Serono Ltd, UK)
Treatment AMetformin 1000 mg Prolonged Release Tablets (JSC Farmak, Ukraine)Test Product Metformin 1000 mg Prolonged Release Tablets (JSC Farmak, Ukraine)
Primary Outcome Measures
NameTimeMethod
Cmaxup to 36 hours post-administration

maximum plasma concentration observed (Cmax)

AUC0-tup to 36 hours post-administration

Area under the plasma concentration versus time curve calculated by the trapezoidal rule from sampling time zero to sampling time of the last measurable plasma concentration (AUC0-t)

Secondary Outcome Measures
NameTimeMethod
AUC0-∞up to 36 hours post-administration

Area under the plasma concentration versus time curve from time zero to infinity (AUC0-∞)

tmaxup to 36 hours post-administration

The time of the maximum plasma concentration (tmax).

λzup to 36 hours post-administration

Apparent first-order elimination (λz)

t1/2up to 36 hours post-administration

the elimination or terminal half-life (t1/2)

AUCresup to 36 hours post-administration

Residual area AUCres = 100 (AUC0-∞ - AUC0-t) / AUC0-∞ \[%\]

Trial Locations

Locations (1)

QUINTA-ANALYTICA s.r.o.

🇨🇿

Prague, Czechia

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