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

• Published in: Drug development and industrial pharmacy 2021-11, Vol.47 (11), p.1764-1774
• Main Authors: Beliakov, S. V., Shatalov, D. O., Aldobaev, V. N., Ivanov, I. S., Aydakova, A. V., Akhmedova, D. A., Kedik, S. A.
• Format: Article
• Language: English
• Subjects: antimicrobial activity; branched OHMG hydrochloride; drug labeling; guanidine hydrochloride; pathogens; Pharmacokinetics
• ISSN: 0363-9045; 1520-5762
• DOI: 10.1080/03639045.2022.2058012

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 3 H-OHMG for rats, and 0.42 mg/kg with the addition of 0.015 mg/kg 3 H-OHMG for Chinchilla rabbits. The selected samples of blood, organs, and urine underwent alkaline mineralization. A quantitative determination of 3 H-OHMG was carried out using a liquid β-, 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 f abs 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.