Гексэтидин

Химические свойства

Hexetidine is a colorless or faint yellow-colored oily liquid with a characteristic amine odor.

Использование

Hexetidine, mixture of stereoisomers is an antibacterial and antifungal agent. Used in plant-derived composite antimicrobial agent and application thereof in cosmetic.

Методы производства

Hexetidine is prepared by hydrogenation under pressure of 1,3- bis(2-ethylhexyl)-5-methyl-4-nitrohexahydropyriminine at 100°C using Raney nickel as a catalyst.

Общее описание

The effectiveness of a hexetidine mouthwash in reducing supragingival plaque and gingival inflammation has been examined.

Опасность

Combustible.

Фармацевтические приложения

Hexetidine is used as an antimicrobial preservative in cosmetics and nonparenteral pharmaceutical formulations. Therapeutically, hexetidine is mainly used as a 0.1% w/v solution in mouthwash formulations for the prevention and treatment of minor local infections, gingivitis, and mouth ulcers.

Безопасность

Hexetidine is mainly used in mouthwashes as a bactericidal and fungicidal antiseptic. It is also used as an antimicrobial preservative and is generally regarded as a relatively nontoxic and nonirritant material at concentrations up to 0.1% w/v. Allergic contact dermatitis and altered olfactory and taste perception have occasionally been reported. Hexetidine is toxic when administered intravenously.
Solutions of hexetidine in oil at concentrations of 5–10% w/v cause strong primary irritations without sensitization in humans. Long-term toxicological studies of up to 0.1% w/w of hexetidine in food for 1 year do not show any toxic effect. Fetotoxicity, embryotoxicity, and teratogenicity studies in rats of doses up to 50 mg/kg/day exhibit no sign of toxicity.
LD100 (cat, IV): 5–20 mg/kg
LD50 (dog, oral): 1.60 g/kg
LD50 (mouse, IP): 0.142 g/kg
LD50 (mouse, oral): 1.52 g/kg
LD50 (rat, oral): 0.61–1.43 g/kg

хранилище

Hexetidine is stable and should be stored in a well-closed container in a cool, dry place. Brass and copper equipment should not be used for the handling or storage of hexetidine.

Несовместимости

Hexetidine is incompatible with strong oxidizing agents. Salts are formed with mineral and organic acids; strong acids cause opening of the hexahydropyrimidine ring, releasing formaldehyde.

Регуляторный статус

Included in nonparenteral formulations licensed in Europe.