Solid dispersion complex triclabendazole preparations with succinic acid and their fasciolocidal activity

Abstract

The purpose of the research is to test the efficacy of triclafascid and two solid dispersion complex preparations based on the triclabendazole substance against fasciolosis in cattle and sheep. Materials and methods. Complex preparations of triclabendazole (TCB) formulations: Succinic Acid (SA): Polyvinylpyrrolidone (PVP) (1: 1 : 8) and TCB: SA: Arabinogalactan (AG) (1: 1 : 8) were obtained by combined solid-stategrinding of the components in a fiber drum on an LE-101 ball mill at a roll rotation speed of 60 rpm with a process module of 1: 17 for 1 to 6 hours with sampling for analysis (HPLC) for changes in the TCB solubility. A comparative test of the efficacy of triclafascid and new solid dispersions (SD) of TCB complexes with SA against fascioliasis of sheep and cattle was conducted in the North-Eastern Federal District of the Caucasus in March-April 2023. To determine the Fasciola infection rate in animals, fecal samples were individually taken and examined by the Fülleborn methods using saturated aqueous NaCL solution and sequential washing. The drug efficacy was recorded at 25-30 days after deworming in analogy with "critical test". The results were statistically processed by the Student-Fisher method using Microsoft Excel 2007. Results and discussion. The resulting TCB and SA complexes with polymers had an increased solubility (up to 59–70 times) that depended on the polymer nature. The efficacy of new TCB dosage forms against fascioliasis in sheep at a dose of 1.5 mg/kg, i.e. 0.5 mg/kg less than the therapeutic dose as compared with oral triclafascid was 90.0 and 100%, respectively, and 85.7% in cattle at a dose of 2.0 mg/kg for the active substance.

Keywords

• triclabendazole
• succinic acid
• polyvinylpyrrolidone
• arabinogalactan
• mechanochemistry
• solid dispersion
• solubility
• efficacy
• sheep
• cattle