Bioequivalence Study of Two Formulations of Sildenafil Tablet 100 mg in Healthy Male Volunteers Under Fasting Conditions

NCT04882826 | Unknown Phase 1

• 1 other identifier: SLDF-2020-CPI-FRMT
• Study Type: interventional
• Target: 44
• Locations: 1 country
• Sites: 1

Brief Summary

This is an open-labeled (laboratory blinded), randomized, two period, single-center, crossover, comparative study, where each participant will be randomly assigned to the reference (Viagra®, 100 mg film-coated tablets) or the test (Sildenafil, 100 mg film-coated tablets) formulation in each period of study (sequences Test-Reference (TR) or Reference-Test (RT)), in order to evaluate if both formulations are bioequivalent

Conditions

Bioequivalence

Keywords

Sildenafil; Bioequivalence; Viagra

Outcome Measures

Primary Outcomes (2)

• Cmax of sildenafil and N-Desmethyl Sildenafil in plasma after administration of the test and the reference products.

  Maximum observed concentration in plasma.

  Time points 0.00 (prior to each drug administration) and 0.17, 0.33, 0.50, 0.67, 0.83, 1.00, 1.25, 1.50, 1.75, 2.00, 2.33, 2.67, 3.00, 3.50, 4.00, 5.00, 6.00, 8.00, 10.00, 12.00, 16.00, 24.00 hours after each drug administration.

• AUC0-t of sildenafil and N-Desmethyl Sildenafil in plasma after administration of the test and the reference.

  Cumulative area under the concentration time curve calculated from 0 to time of last observed quantifiable concentration (TLQC) using the linear trapezoidal method

  Time points 0.00 (prior to each drug administration) and 0.17, 0.33, 0.50, 0.67, 0.83, 1.00, 1.25, 1.50, 1.75, 2.00, 2.33, 2.67, 3.00, 3.50, 4.00, 5.00, 6.00, 8.00, 10.00, 12.00, 16.00, 24.00 hours after each drug administration.

Secondary Outcomes (8)

• Tmax of sildenafil and N-Desmethyl Sildenafil in plasma after administration of the test and the reference products.

  Time points 0.00 (prior to each drug administration) and 0.17, 0.33, 0.50, 0.67, 0.83, 1.00, 1.25, 1.50, 1.75, 2.00, 2.33, 2.67, 3.00, 3.50, 4.00, 5.00, 6.00, 8.00, 10.00, 12.00, 16.00, 24.00 hours after each drug administration.

• TLQC of sildenafil and N-Desmethyl Sildenafil in plasma after administration of the test and the reference products.

  Time points 0.00 (prior to each drug administration) and 0.17, 0.33, 0.50, 0.67, 0.83, 1.00, 1.25, 1.50, 1.75, 2.00, 2.33, 2.67, 3.00, 3.50, 4.00, 5.00, 6.00, 8.00, 10.00, 12.00, 16.00, 24.00 hours after each drug administration.

• AUC0-INF of sildenafil and N-Desmethyl Sildenafil in plasma after administration of the test and the reference products.

  Time points 0.00 (prior to each drug administration) and 0.17, 0.33, 0.50, 0.67, 0.83, 1.00, 1.25, 1.50, 1.75, 2.00, 2.33, 2.67, 3.00, 3.50, 4.00, 5.00, 6.00, 8.00, 10.00, 12.00, 16.00, 24.00 hours after each drug administration.

• Residual area of sildenafil and N-Desmethyl Sildenafil in plasma after administration of the test and the reference products.

  Time points 0.00 (prior to each drug administration) and 0.17, 0.33, 0.50, 0.67, 0.83, 1.00, 1.25, 1.50, 1.75, 2.00, 2.33, 2.67, 3.00, 3.50, 4.00, 5.00, 6.00, 8.00, 10.00, 12.00, 16.00, 24.00 hours after each drug administration.

• Time point where the log-linear elimination phase begins (TLIN) of sildenafil and N-Desmethyl Sildenafil in plasma after administration of the test and the reference. products.

  Time points 0.00 (prior to each drug administration) and 0.17, 0.33, 0.50, 0.67, 0.83, 1.00, 1.25, 1.50, 1.75, 2.00, 2.33, 2.67, 3.00, 3.50, 4.00, 5.00, 6.00, 8.00, 10.00, 12.00, 16.00, 24.00 hours after each drug administration.

Study Arms (2)

Sequence TR

OTHER

22 subjects assigned to the sequence TR will receive a single 100 mg dose of the test product Sildenafil (1 x 100 mg tablet), marked as T in the sequence, in Period 1 and a single 100 mg dose of the reference product Viagra® (1 x 100 mg tablet), marked as R in the sequence, in period 2. These treatments will be administered orally with approximately 200 mL of water, in the morning, following a 10-hour overnight fast. The tablet must be swallowed whole and must not be chewed or broken.

Drug: Sildenafil film-coated tablet 100 mg; Drug: Viagra® film-coated tablet 100 mg

Sequence RT

OTHER

22 subjects assigned to the sequence RT will receive a single 100 mg dose of the reference product Viagra® (1 x 100 mg tablet), marked as R in the sequence, in Period 1 and a single 100 mg dose of the test product Sildenafil (1 x 100 mg tablet), marked as T in the sequence, in period 2. These treatments will be administered orally with approximately 200 mL of water, in the morning, following a 10-hour overnight fast. The tablet must be swallowed whole and must not be chewed or broken.

Drug: Sildenafil film-coated tablet 100 mg; Drug: Viagra® film-coated tablet 100 mg

Interventions

Sildenafil film-coated tablet 100 mg DRUG

Sildenafil is manufactured by Pharmtechnology LLC, Belarus. Each tablet contains 100 mg of sildenafil.

Also known as: The test product

Sequence RT; Sequence TR

Viagra® film-coated tablet 100 mg DRUG

Viagra® is manufactured by Fareva Amboise, France. Each tablet contains 100 mg of sildenafil.

Also known as: The reference product

Sequence RT; Sequence TR

Eligibility Criteria

• Age: 18 Years - 45 Years
• Sex: male
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Healthy caucasian men aged between 18 to 45 years
• The written consent of the volunteer to be included in the study
• Verified diagnosis "healthy" according to the anamnesis data and the results of standard clinical, laboratory and instrumental examination methods, physical examination and anamnestic examination
• Body mass index 18.5-30 kg/m² according to Quetelet's weight-height index
• The results of an X-ray or fluorographic examination of the chest organs within the normal range (the results of an examination carried out within 12 months before the start of the study may be provided)
• Absence of ophthalmological disease according to the data of the ophthalmological examination
• Consent to use a double barrier method of contraception (condom + spermicide) or sexual continence, as well as consent not to take part in sperm donation from the moment of taking the drug in the first period, during the entire study and within 14 days after taking the drug in the second period research
• Subjects are able to understand the requirements of the study, to sign a written informed consent, and also to accept all the restrictions imposed during the course of the study, and to agree to return for the required investigations

You may not qualify if:

• Burdened allergic history, hypersensitivity to sildenafil or excipients that are part of any of the investigational drugs, or intolerance to these components.
• Lactose intolerance, lactase deficiency, glucose-galactose malabsorption.
• Anatomical deformation of penis (angulation, cavernous fibrosis, or Peyronie's disease).
• History of priapism.
• Hereditary retinitis pigmentosa.
• Episodes of development of anterior non-arteritis ischemic neuropathy of the optic nerve.
• Organic brain damage, a history of increased convulsive readiness.
• Acute or chronic diseases of the cardiovascular, bronchopulmonary, neuroendocrine systems, and also diseases of the gastrointestinal tract, liver, kidneys and blood, eye disease.
• Other diseases that, in the opinion of the researcher, may affect the absorption, distribution, metabolism or excretion of both drugs, or increase the risk of negative consequences for the volunteer.
• The presence of mental disorders, including a history.
• Surgical interventions on the gastrointestinal tract, with the exception of appendectomy.
• Acute infectious diseases that ended less than 4 weeks before taking the drug in the first period.
• Dehydration due to diarrhea, vomiting or other reason within the last 24 hours before taking the drug in the first period of the study, if vomiting or diarrhea wasn't a manifestation of an infectious disease.
• Clinically significant abnormalities on the ECG, the level of systolic blood pressure (SBP) measured in the sitting position at the time of screening \<100 mm Hg or ≥ 130 mm Hg and / or diastolic blood pressure (DBP) \<60 mm Hg or ≥ 85 mm Hg.
• Heart rate less than 60 beats/min or more than 90 beats/min at the time of screening, respiratory rate less than 14 or more than 18 per minute at the time of screening, body temperature below 36.0 ° C or above 37.0 °C at the time of screening.

Sponsors & Collaborators

• Pharmtechnology LLC: lead
• ClinPharmInvest, LLC: collaborator

Study Sites (1)

Private healthcare institution "Clinical Hospital "RZD-Medicine" of the city of Yaroslavl"

Yaroslavl, 150047, Russia

Location

Study Officials

• Alexander Khokhlov

  ClinPharmInvest, LLC

  PRINCIPAL INVESTIGATOR

Central Study Contacts

Veronika Kumpel

CONTACT

80173094418; specialist.fs@ft.by

Andrei Yaremchuk

CONTACT

development@ft.by

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: SINGLE
• Who Masked: OUTCOMES ASSESSOR
• Purpose: OTHER
• Intervention Model: CROSSOVER
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: May 6, 2021
• First Posted: May 12, 2021
• Study Start: May 10, 2021
• Primary Completion: May 30, 2021
• Study Completion: May 30, 2021
• Last Updated: May 12, 2021

Record last verified: 2021-05

Locations

RU (1)