РОЗРОБКА СКЛАДУ НОВОГО ЛІКАРСЬКОГО ЗАСОБУ ДЛЯ МІСЦЕВОГО ЛІКУВАННЯ МІКОЗУ СТОП У ФОРМІ РІДКОГО ПЛАСТИРУ

Анотація

DEVELOPMENT OF COMPOSITION OF NEW DRUG PRODUCT FOR TOPICAL TREATMENT OF FOOT MYCOSIS IN THE FORM OF LIQUID PLASTER
O.O. Vashchenko
Danylo Halytsky Lviv National Medical University, Lviv
Summary: The article represents a brief description of liquid plasters as a dosage form and their advantages compared to other dosage forms for cutaneous application. The results of investigations on the pharmaceutical development of the liquid plaster for topical treatment of foot mycosis are shown. Terbinafine hydrochloride was selected as an active pharmaceutical ingredient. Cellulose acetate butyrate, propylene glycol and ethyl acetate were used to prepare the plaster base.
Key words: foot mycosis, liquid plaster, terbinafine hydrochloride.
Introduction. Fungal infections occupy a dominant position in the structure of skin diseases. Foot mycoses are among the most common types of skin mycoses. Despite the wide arsenal of antifungal drugs, the incidence of mycoses has not reduced. However, the opposite effect is observed: there is a tendency for the formation of the resistant forms of fungal infections, the increasing of their invasiveness, and the decreasing of macroorganism’s resistance. Therefore, the search for new antifungal agents and the development of new highly efficient preparations is a well justified task.
Promising direction in the treatment of foot mycosis is the introduction of drug products in the new dosage forms, i.e. in the form of liquid plasters (LP), into the pharmaceutical and medical practice.
Methods: informative (search, analysis and systematization of the information); physical and physical-chemical (appearance of LP and film, solubility, film thickness); pharmacotechnological (drying time and adhesion of film); mathematical (statistical data processing).
Results and discussion. Application of drug products in the form of LP for topical treatment of foot mycosis is a far-reaching therapeutic approach. LP compared to other dosage forms for cutaneous application has the following advantages: it is applied directly into the affected area; it provides a prolonged release of active pharmaceutical ingredient (API); increasing of API concentration in the film after the solvent evaporation gives rise to a concentration gradient and enhances the drug penetration into the skin; a formed film acts as a barrier to reinfection and restricts the spread of fungal cells.
Terbinafine hydrochloride in the concentration of 1 % was chosen as an API for the pharmaceutical development of LP for treatment of foot mycosis. It is a broad spectrum antifungal agent that also exhibits antibacterial activity. Terbinafine hydrochloride is a highly lipophilic and keratophilic drug and distributes in high concentrations into the skin and nails.
The quality and efficacy of drug product depends not only on the API, but also the performance of excipients. Excipients used in the formulation of LP should provide the homogeneity of solution and the formation of a uniform elastic film with good adhesive properties after the solvent evaporation.
Based on the results of investigations, the following excipients in the quantities needed to achieve the desired quality parameters of drug product were selected for the development of antifungal LP: cellulose acetate butyrate (film-forming agent), propylene glycol (plasticizer with penetrating properties), ethyl acetate (solvent).
Conclusions. Treatment of foot mycosis is a significant problem of the current healthcare system. The introduction of new drug products in various dosage forms, particularly in the form of LP, is a promising solution to the problem. To that end, composition of antifungal LP with terbinafine hydrochloride was theoretically and experimentally substantiated.