COMPOSITIONS AND USE OF ANTIMICROBIAL AGENTS FOR LOCAL APPLICATION WITH IMPROVED CHARACTERISTICS AND SAFETY Russian patent published in 2024 - IPC A61K38/16 A61K9/08 A61P31/04 

FIELD: medicine; pharmaceutics.

SUBSTANCE: group of inventions relates to antimicrobial pharmaceutical compositions containing cationic antimicrobial agents and methods of using them for preventing and/or treating infections. Disclosed composition contains an aqueous carrier and at least one antimicrobial synthetic cationic polypeptide dispersed in said aqueous carrier in the concentration range of 0.01–5 wt.% in terms of the total weight of said composition. Said synthetic cationic polypeptide contains at least 40 amino acid residues; plurality of positively charged amino acid residues at neutral pH, where said plurality of amino acid residues at neutral pH is at least 10; additionally contains a plurality of hydrophobic amino acid residues; characterized by viscosity in concentration of 2 wt.% in deionised water at 37 °C equal to 2 centistokes (cSt) or more; comprises a configuration of hydrophobic amino acid residues and positively charged amino acid residues in a sequence configured to facilitate self-assembly of said antimicrobial synthetic cationic polypeptide into multimeric structures. Aqueous carrier containing the above antimicrobial synthetic cationic polypeptide in amount of 2 wt.% is characterized by viscosity at 37 °C, exceeding the viscosity of the aqueous carrier containing 2 wt.% albumin instead of said synthetic cationic polypeptide. Disclosed composition is sterilized using a sterilization method, which enables to obtain a sterilized composition with said antimicrobial synthetic cationic polypeptide having weight average molecular weight and optionally dispersion comparable to those for the antimicrobial synthetic cationic polypeptide of the antimicrobial pharmaceutical composition not sterilized by said sterilization method, and has low toxicity after infusion into the abdominal cavity of a plurality of healthy young adult mice in dose of 50 mg/kg, according to the measurement of the survival rate of mice of 50 % or more after 72 hours. Also disclosed is a method for preventing microbial infection of tissues other than intact healthy skin, and a method for reducing microbial load in tissues or tissues other than intact healthy skin, involving administering said composition. Composition preserves molecular integrity and antimicrobial efficacy after sterilization.

EFFECT: use of the group of inventions provides safe intraperitoneal administration.

36 cl, 63 dwg, 9 ex