Pharmacokinetic investigation of branched oligohexamethyleneguanidine hydrochloride in a liquid composition for the treatment of stomatitis and gingivitis.

Branched oligohexamethyleneguanidine hydrochloride (branched OHMG-HC) possesses high biocidal activity. This study aimed at evaluating the pharmacokinetics of branched OHMG-HC and is mandatory for obtaining permission to conduct clinical studies. The thermal activation method was used to obtain radioactive-labeled drugs for the investigation of substance distribution in various tissues of experimental animals (rats and rabbits). Substance administration was carried out both orally (a dose was split into two equal volumes that were applied to buccal zones of the oral cavities of the animals) and intravenously to get a clear pharmacokinetic profile. In this research, the drug was applied in the concentration of 0.77 mg/kg with the addition of 0.037 mg/kg 3H-OHMG for rats, and 0.42 mg/kg with the addition of 0.015 mg/kg 3H-OHMG for Chinchilla rabbits. The selected samples of blood, organs, and urine underwent alkaline mineralization. A quantitative determination of 3H-OHMG was carried out using a liquid ß-, γ-counter according to the level of scintillation in the sample. Branched OHMG-HC displayed uniform distribution within all main organs and tissues upon oral administration. The highest concentrations were found in liver and kidney tissues, whereas the lowest in blood, cardiac muscle tissue, and brain. The closeness of the fabs values obtained from different animals (24.5% for rats and 29.0% for rabbits) demonstrated the absence of the species specificity in response to the pharmaceutical substance. The main parameters of excretion were established, and the half-life time was estimated to be 15 h.

Preliminary in vitro and in vivo evaluation of specific activity of branched oligohexamethyleneguanidine hydrochloride.

Branched oligohexamethyleneguanidine hydrochloride (OHMG) possesses great potential for the development of novel drugs for the treatment of diseases caused by bacteria. This study aimed at evaluating the antimicrobial activity of OHMG against potential causative agents of oral and pharyngeal mucosa infections, specifically, the activity against 56 clinical strains, 5 of which were antibiotics-resistant. Also, a preliminary in vivo study of the specific activity of OHMG based on a traumatic stomatitis and gingivitis model in rabbits was carried out. In vitro antimicrobial activity of OHMG was determined by testing the minimal inhibitory concentration (MIC). OHMG displayed excellent activity against Streptococcus pneumoniae, Streptococcus pyogenes (MIC was 0.002-0.25 µg/ml), Moraxella catarrhalis (0.03-0.06 µg/ml), Neisseria gonorrhoeae (0.125-2 µg/ml). Almost complete healing of defects in the groups of animals within the 7-day application of 'OHMG hydrochloride' at concentrations of 0.1% and 0.3% after the thermal formation of the stomatitis and gingivitis model was observed.