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Fasting Bioequivalence Study of 2 Metformin 500 mg Prolonged Release Tablets in 44 Healthy Male and Female Volunteers

Registration Number
NCT05124730
Lead Sponsor
Joint Stock Company "Farmak"
Brief Summary

This study was designed to compare the bioavailability of the Test Product Metformin 500mg Prolonged Release Tablets (JSC Farmak, Ukraine) and Reference Product Glucophage® XR 500 mg Prolonged Release Tablets (Merck Serono Ltd, UK) in healthy male and female volunteers under fasting conditions.

Detailed Description

An Open, Comparative, Randomized, Crossover Clinical Trial to Evaluate the Bioequivalence of Single Doses of Test Product Metformin 500mg Prolonged Release Tablets (JSC Farmak, Ukraine) and Reference Product Glucophage® XR 500 mg Prolonged Release Tablets (Merck Serono Ltd, UK) in Healthy, Adult Male and Female Subjects under Fasting 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 Investigational Medicinal Product (IMP) administration.

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
44
Inclusion Criteria
  • Healthy males and non-pregnant and no breast-feeding females (must have a negative pregnansy 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 has 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. Minor deviations outside the reference ranges were acceptable, if deemed not clinically significant by the Investigator.
  • All laboratory screening results within the normal range. Minor deviations outside the reference ranges were acceptable, if deemed not clinically significant by the Clinical 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 may 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.
  • Glucose level out of the limit 3.3 mmol/L - 5.5 mmol/Lat screening, as determined by screening clinical laboratory evaluations.
  • Previous liver disease or clinically significant elevations in serum transaminases at the screening.
  • Acute or chronic diseases and/or clinical finding which may interfere with the aims of the study or with the drug's safety, tolerability, bioavailability and/or pharmacokinetics of the 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 result of blood pregnancy test at screening or positive urine pregnancy test at check-in or breast-feeding or lack of results of pregnancy test.
  • Positive results of drugs of abuse in urine at screening and at check-in.
  • Positive result of alcohol breath test at screening and at check-in.
  • Positive result of urine cotinine test at screening and at check-in.
  • 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 90-140 mmHg for systolic blood pressure (BP) and/or 60-90 mmHg for diastolic BP and/or heart rate out of the range of 50-100 bpm during the screening procedure.
  • Body ear temperature is out of the range of 35.7 - 37.3°C at screening and at check-in.
  • 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.
  • Use of any OTC (over-the-counter) medication including vitamins, herbal medications and food supplements less than 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.
  • Anemia, 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 in this study.

Study & Design

Study Type
INTERVENTIONAL
Study Design
CROSSOVER
Arm && Interventions
GroupInterventionDescription
Treatment AMetformin 500mg prolonged release tablets (JSC Farmak, Ukraine)Metformin 500 mg Prolonged Release Tablets (JSC Farmak, Ukraine)
Treatment BGlucophage® XR 500 mg prolonged release tablets (Merck Serono Ltd, UK)Glucophage® XR 500 mg prolonged release tablets (Merck Serono Ltd, UK)
Primary Outcome Measures
NameTimeMethod
Cmaxup to 36 hours post-administration

Maximum plasma concentration observed.

AUC0-tup to 36 hours post-administration

Area under the plasma drug concentration versus time curve

Secondary Outcome Measures
NameTimeMethod
AUC(12h-t)from time 12 hours after dosing up to 36 hours post-administration

The area under the plasma drug concentration versus time curve calculated from time 12 hours after dosing to time of the last sample above LLOQ

AUC(0-12h)from time zero to time 12 hours after dosing.

The area under the plasma drug concentration versus time curve calculated from time zero to time 12 hours after dosing.

λzup to 36 hours post-administration

Apparent first-order elimination

AUC(0-∞)up to 36 hours post-administration

Area under the plasma drug concentration versus time curve from time zero to infinity

AUC(0-24h)from time zero to time 24 hours after dosing

The area under the plasma drug concentration versus time curve calculated from time zero to time 24 hours after dosing.

tmaxup to 36 hours post-administration

the time of the maximum plasma drug concentration.

t1/2up to 36 hours post-administration

The elimination or terminal half-life

AUCresup to 36 hours post-administration

Residual area

Trial Locations

Locations (1)

QUINTA-ANALYTICA s.r.o.

🇨🇿

Prague, Czechia

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