Bioavailability of a new formulation of losartan Not Applicable
Conditions
Interventions
TEST (T): Losartan potassium 100 mg modified-release tablets, Doppel Farmaceutici S.r.l., Italy
REFERENCE (R): Cozaar®, 100 mg losartan potassium film-coated tablets, Merck Sharp & Doh
Sponsors
DPL Pharma S.p.A.
Eligibility
Sex/Gender
Male
Inclusion criteria
Inclusion criteria: 1. Informed consent: signed written informed consent before inclusion in the study 2. Men, 18-55 years old inclusive 3. Body Mass Index: 18.5-30 kg/m² inclusive 4. Vital signs: systolic blood pressure 100-139 mmHg, diastolic blood pressure 50-89 mmHg, heart rate 50-90 bpm, measured after 5 min at rest in the sitting position 5. Full comprehension: ability to comprehend the full nature and purpose of the study, including possible risks and side effects; ability to co-operate with the Investigator and to comply with the requirements of the entire study
Exclusion criteria
Exclusion criteria: 1. Electrocardiogram (ECG, 12-leads, supine position): clinically significant abnormalities 2. Physical findings: clinically significant abnormal physical findings which could interfere with the objectives of the study 3. Laboratory analyses: clinically significant abnormal laboratory values indicative of physical illness 4. Allergy: ascertained or presumptive hypersensitivity to the active principle and/or formulations' ingredients; history of anaphylaxis to drugs or allergic reactions in general, which the Investigator considers may affect the outcome of the study 5. Diseases: significant history of renal, hepatic, gastrointestinal, cardiovascular, respiratory, skin, haematological, endocrine or neurological diseases that may interfere with the aim of the study. Known renal dysfunction 6. Medications: medications, including over the counter medications and herbal products for 2 weeks before the start of the study 7. Investigative drug studies: participation in the evaluation of any investigational product for 3 months before this study. The 3-month interval is calculated as the time between the first calendar day of the month that follows the last visit of the previous study and the first day of the present study 8. Blood donation: blood donations for 3 months before this study 9. Drug, alcohol, caffeine, tobacco: history of drug, alcohol (>2 drinks/day, defined according to the USDA Dietary Guidelines 2015-2020), caffeine (>5 cups coffee/tea/day) or tobacco abuse (=10 cigarettes/day) 10. Drug test: positive result at the drug test at screening or day -1 (all study periods) 11. Alcohol test: positive alcohol breath test at day -1 (all study periods) 12. Diet: abnormal diets (3500 kcal/day) or substantial changes in eating habits in the 4 weeks before this study; vegetarians
Design outcomes
Primary
| Measure | Time frame |
|---|---|
| Bioavailability of losartan, AUC0-t, Cmax and Tmax of losartan calculated from the relative plasma concentrations after single dose administration of T and R under fasting conditions. Blood samplings were made on Days 1 & 2 of the two study periods at the following timepoints: pre-dose (0), 15, 30, 45 min, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 10, 12, 16 and 24 h post-dose. | — |
Secondary
| Measure | Time frame |
|---|---|
| 1. Plasma renin activity, angiotensin II and aldosterone plasma levels after single dose administration of T and R under fasting conditions. Blood samplings were made on Day1&2 of the two study periods at the following timepoints :pre-dose (0), 3, 6, 9, 12, 16 and 24 h post-dose 2. Safety and tolerability data after single dose administration of T and R under fasting conditions. reatment-emergent adverse events recordings throughout the study duration. 3. Vital signs: subjects blood pressure (BP) and heart rate (HR) were measured by the Investigator or his deputy after 5 min at rest (in sitting position) at: screening visit, day 1 of each period: pre-dose (0), 3, 6, 9, 12 and 16 h post-dose, day 2 of each period: 24 h post-dose. Period 2, 24-h post-dose check was considered as the final study assessment. They were measured at Early Termination Visit, if applicable. 4. Electrocardiograms: 12-Leads ECGs were performed (in supine position) at screening, on day -1 of both study periods and before leaving the clinical centre on day 2 or at ETV in case of premature discontinuation. 5. Body weight: it was recorded at screening and final visit/ETV. BMI was recorded at screening visit only. Subjects were weighed (kg) lightly clothed without shoes. Height was measured at screening only and BMI will be recorded. BMI was calculated as weight [kg]/(height [m] x height [m]). 6. Laboratory parameters: Samples of blood (12.5 mL) and urine were collected. The following laboratory analyses were performed at the screening visit: 6.1 HAEMATOLOGY Leukocytes and leukocyte differential count (percentage values and absolute values), erythrocytes, haemoglobin (conv. units), haemoglobin (IS units), haematocrit, MCV, MCH, MCHC, thrombocytes. 6.2 BLOOD CHEMISTRY Electrolytes: sodium, potassium, calcium, chloride, inorganic phosphorus En | — |
Countries
Italy, Switzerland
Outcome results
None listed