Comparison of parasiticidal activity of fenbendazole compositions modified by various methods

The purpose of the research is obtaining experimental samples of fenbendazole (FBZ) by alternative methods: dissolution and mechanochemistry and comparative evaluation of their physicochemical and anthelmintic properties.

Materials and methods. Experimental FBZ samples with glycyrrhizic acid and its derivatives were obtained in an ethanol medium using dissolution or solid-phase mechanochemistry. The solubility of FBZ samples was evaluated by the method of high-performance liquid chromatography, and other physicochemical properties were studied using UV- and IR-spectroscopy. The biological activity of the obtained samples was determined on the laboratory model of experimental trichinellosis of white mice based on the results of intestinal necropsy. The efficacy was calculated using a "control test".

Results and discussion. Varying degrees of increase in solubility of FBZ samples obtained with different salts and methods were established: from 0.1 to 9.7 times. IR and UV spectral data confirmed the stabilization of FBZ samples obtained by the liquid-phase method due to intermolecular hydrogen bonds. In this study, no obvious correlation was observed between the solubility and efficacy of the obtained FBZ samples. The samples obtained by the solid-phase method demonstrated the highest activity against trichinellosis, in particular, the FBZ sample with uccinic, alkaline and citric acids (72.1%) and FBZ sample with Na2GA (62.8%) at a dose of 3.0 mg/kg of active substance. Samples of supramolecular FBZ with salts, obtained by the liquid-phase method, showed an increase in efficacy by 1.8–3.6 times compared to the basic drug – FBZ substance at a dose of 3.0 mg/kg of active substance.

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