Safety, Tolerability, and Pharmacokinetic Profile of Grammidin With Anesthetic, a Metered Dose Topical Spray in Healthy Volunteers

NCT06857890 | Recruiting Phase 1

• 1 other identifier: GRM-01-07-2024
• Study Type: interventional
• Target: 24
• Locations: 1 country
• Sites: 1

Brief Summary

This study aims to evaluate the safety, tolerability, and pharmacokinetic profile of the Grammidin with anesthetic, a metered dose topical spray, compared to Grammidin with anesthetic neo, lozenges following single administration in healthy volunteers.

Conditions

Pharyngitis

Outcome Measures

Primary Outcomes (11)

• Pharmacokinetics - Cmax

  Maximum plasma concentration (Cmax) of gramicidin S, oxybuprocaine hydrochloride, and cetylpyridinium chloride. The same analytes would be used for other pharmacokinetic measures listed below.

  From 0 to 24 hours after each drug intake.

• Pharmacokinetics - tmax

  Time to reach Cmax (tmax)

  From 0 to 24 hours after each drug intake.

• Pharmacokinetics - AUC0-t

  Area under the plasma concentration-time curve from time 0 to t (AUC0-t)

  From 0 to 24 hours after each drug intake.

• Pharmacokinetics - AUC0-inf

  Area under the plasma concentration-time curve from time 0 to infinity (AUC0-inf)

  From 0 hours after each drug intake (extrapolated to infinity)

• Pharmacokinetics - AUCextr

  Extrapolated AUC defined as (AUC0-inf - AUC0-t)/AUC0-inf

  From 0 hours after each drug intake (extrapolated to infinity)

• Pharmacokinetics - t1/2

  Elimination half-life (t1/2)

  From 0 to 24 hours after each drug intake.

• Pharmacokinetics - kel

  Elimination constant (kel)

  From 0 to 24 hours after each drug intake.

• Pharmacokinetics - MRT

  Mean residence time (MRT)

  From 0 to 24 hours after each drug intake.

• Pharmacokinetics - Vd

  Volume of distribution

  From 0 to 24 hours after each drug intake.

• Pharmacokinetics - CL

  Clearance (CL)

  From 0 to 24 hours after each drug intake.

• Pharmacokinetics - number of terminal timepoints

  Number of points in the terminal logarithmic phase used to estimate the terminal elimination rate constant

  From 0 to 24 hours after each drug intake.

Secondary Outcomes (55)

• Adverse event type

  From screeninig (days -14 to -1) to the end of study (day 15 ± 1)

• Adverse event number

  From screeninig (days -14 to -1) to the end of study (day 15 ± 1)

• Adverse event severety

  From screeninig (days -14 to -1) to the end of study (day 15 ± 1)

• Drop-outs associated with adverse events

  From screeninig (days -14 to -1) to the end of study (day 15 ± 1)

• Safety and Tolerability: volunteer complaints

  From screeninig (days -14 to -1) to the end of study (day 15 ± 1)

Study Arms (2)

RT sequence: Grammidin with anesthetic neo followed by Grammidin with anesthetic

EXPERIMENTAL

RT sequence where R is Grammidin with anesthetic neo, lozenges, and T is Grammidin with anesthetic, a metered dose topical spray

Drug: Grammidin with anesthetic neo; Drug: Grammidin with anesthetic, a metered dose topical spray

TR sequence: Grammidin with anesthetic followed by Grammidin with anesthetic neo

EXPERIMENTAL

TR sequence where T is Grammidin with anesthetic, a metered dose topical spray, and R is Grammidin with anesthetic neo, lozenges

Drug: Grammidin with anesthetic neo; Drug: Grammidin with anesthetic, a metered dose topical spray

Interventions

Grammidin with anesthetic neo DRUG

Grammidin with anesthetic neo, lozenges, 1 lozenge to be taken once under fed conditions.

Also known as: gramicidin s, cetylpyridinium chloride, oxybuprocaine

RT sequence: Grammidin with anesthetic neo followed by Grammidin with anesthetic; TR sequence: Grammidin with anesthetic followed by Grammidin with anesthetic neo

Grammidin with anesthetic, a metered dose topical spray DRUG

Grammidin with anesthetic, a metered dose topical spray, 4 sprays to be taken once under fed conditions

Also known as: gramicidin s, cetylpyridinium chloride, oxybuprocaine

RT sequence: Grammidin with anesthetic neo followed by Grammidin with anesthetic; TR sequence: Grammidin with anesthetic followed by Grammidin with anesthetic neo

Eligibility Criteria

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

You may qualify if:

• Voluntarily and personally signed informed consent form by a healthy volunteer obtained prior to the conduct of any study-related procedure;
• Males and females aged 18 to 45 years (inclusive);
• Verified healthy status as demonstrated by the absence of clinically significant abnormalities in medical history, physical examination, laboratory tests, and other diagnostic procedures specified in the protocol;
• Blood pressure (BP) level: systolic blood pressure (SBP) from 99 to 129 mm Hg (inclusive), diastolic blood pressure (DBP) from 70 to 89 mm Hg (inclusive);
• Heart rate (HR) from 60 to 89 beats per minute (inclusive);
• Respiratory rate (RR) from 12 to 20 breaths per minute (inclusive);
• Body temperature from 36.0°C to 36.9°C (inclusive);
• Body mass index (BMI) between 18.5 kg/m² and 30 kg/m², with a minimum body weight of ≥ 55 kg for men and ≥ 45 kg for women;
• Consent to use adequate contraceptive methods throughout the study and for 30 days after its completion, with a negative urine pregnancy test result for women of childbearing potential.
• Clinically significant allergic history;
• Hypersensitivity to active and/or excipient substances in the investigational drug and comparator drug in the medical history;
• Drug intolerance to active and/or excipient substances in the investigational drug and comparator drug in the medical history;
• Chronic diseases of the kidneys, liver, gastrointestinal tract (GIT), cardiovascular, lymphatic, respiratory, nervous, endocrine, musculoskeletal, urogenital, and immune systems, as well as skin, hematopoietic organs, and the eye;
• Erosive-ulcerative lesions of the oral mucosa (aphthous stomatitis, mechanical trauma due to dental diseases, herpes lesions, and any other condition resulting in compromised integrity of the oral mucosa);
• Surgical interventions on the GIT in the medical history (except for appendectomy performed at least 1 year prior to screening);

You may not qualify if:

• Withdrawal of the volunteer from further participation in the study;
• Non-compliance by the volunteer with the study participation rules (missed study procedures, self-administration of drugs prohibited in the study, violation of dietary and lifestyle restrictions, etc.);
• Emergence of reasons/situations during the study that threaten the safety of the volunteer (e.g., hypersensitivity reactions, etc.);
• Development of a severe adverse event (SAE) in the volunteer during the study;
• The volunteer undergoes or requires treatment that may affect the pharmacokinetic parameters (PKP) of the investigational drugs;
• Missed collection of 2 or more consecutive blood samples or 3 or more blood samples within one study period;
• Occurrence of vomiting/diarrhea within 6 hours after taking the investigational drug;
• Positive urine test for narcotic substances and potent medications;
• Positive breath test for alcohol vapors;
• Positive pregnancy test result in women;
• Positive SARS-CoV-2 test result;
• Emergence of other reasons during the study that prevent conducting the study according to the protocol.

Sponsors & Collaborators

• Valenta Pharm JSC: lead

Study Sites (1)

Separate Medical Unit "CoMed" (LLC "Ligand Research")

Moscow, Russia

RECRUITING

MeSH Terms

Conditions

Pharyngitis

Interventions

Gramicidin; Cetylpyridinium; benoxinate; Anesthetics

Condition Hierarchy (Ancestors)

Respiratory Tract Infections; Infections; Pharyngeal Diseases; Stomatognathic Diseases; Respiratory Tract Diseases; Otorhinolaryngologic Diseases

Intervention Hierarchy (Ancestors)

Tyrothricin; Peptides, Cyclic; Macrocyclic Compounds; Polycyclic Compounds; Peptides; Amino Acids, Peptides, and Proteins; Pore Forming Cytotoxic Proteins; Membrane Proteins; Proteins; Pyridinium Compounds; Pyridines; Heterocyclic Compounds, 1-Ring; Heterocyclic Compounds; Central Nervous System Depressants; Physiological Effects of Drugs; Pharmacologic Actions; Chemical Actions and Uses; Central Nervous System Agents; Therapeutic Uses

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: NONE
• Purpose: OTHER
• Intervention Model: CROSSOVER
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: February 17, 2025
• First Posted: March 5, 2025
• Study Start: December 9, 2024
• Primary Completion (Estimated): December 1, 2026
• Study Completion (Estimated): December 1, 2026
• Last Updated: July 10, 2025

Record last verified: 2025-07

Data Sharing

• IPD Sharing: Will not share

Locations

RU (1)