N 3 (188) 2024. P. 91–96

DEVELOPMENT OF THE COMPOSITION OF ORALLY DISINTEGRATING ANTIVIRAL TABLETS WITH THIOSULFONATE COMPONENT, ALLYL ESTER OF 4-METHACRYLOYLAMINOBENZENETHIOSULFONIC ACID

L. V. Fizer, Zh. D. Parashchyn, О. Z. Komarovska-Porokhnyavets,
V. I. Lubenets

Lviv Polytechnic National University, Lviv, Ukraine

DOI 10.32782/2226-2008-2024-3-15

The development of the optimal composition of solid dosage forms for using in the oral cavity with new antimicrobial active ingredients has become a particular issue nowadays. Orally disintegrating tablets occupy a special place in the pharmaceutical market, considering the demand from many categories of patients. Compounds with thiosulfonate pharmacophores are promising active pharmaceutical ingredients for the development of new drugs due to their wide range of biological activity and compound stability.

The aim of the study is to develop an optimal composition of orally disintegrating tablets based on allyl ester of 4-methacryloylaminobenzenethiosulfonic acid that has antiviral, antibacterial and antifungal effects, as well as to select excipients to achieve the required pharmaco-technological parameters.

Materials and methods. The target ester was synthesised according to the authors’ method. The structure and individuality of the synthesised compound were confirmed by elemental analysis, IR and NMR spectroscopy. While studying the development of the composition of tablets, tentatively called “Virulin”, the effect of 16 excipients was investigated. Mathematical planning of the experiment was used to obtain the optimal combination. The direct compression method was used to manufacture the tablets.

Results. A new method for the synthesis of the allyl ester of 4-methacryloylaminobenzenethiosulfonic acid has been developed, which involves 3 stages via preparation of 2 important intermediates. The structure and individuality of the compound were confirmed by elemental analysis, IR and NMR spectroscopy. The conducted studies enabled us to determine the impact of excipients on the main pharmaco-technological parameters of powder masses for tableting, as well as tablets based on them, obtained by direct compression. The optimal excipients were selected for the introduction to the dosage form.

Key words: formulation optimization, synthesis, antiviral activity, thiosulfonates, tablets, mathematical planning of the experiment, Virulin.

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