DIALYSIS STUDY OF TRICLABENDAZOLE-BASED DRUGS

Abstract

The research purpose was to study the dialysis of triclabendazole (TCB) and its solid dispersions (SDs) obtained by mechanochemical methods by modifying TCB with polyvinylpyrrolidone (PVP), arabinogalactan (AG) and succinic acid (SA). Solid dispersions of the following compositions were obtained: TCB:AG:PVP (1:4,5:4,5), TCB:SA:AG (1:1:8) and TCB:SA:PVP (1:1:8), which were characterized by their solubility in water. To study the TCB release from the obtained SDs (dialysis), we used a laboratory installation consisting of a thermostated glass with a buffered solution (sodium borate) with pH 9.18 (intestinal environment). The TCB substance concentration in the dialysate was determined by HPLC the data of which determined that the TCB release into the buffered solution at different rates depended on the SD composition. It was found that SA included in the SD composition significantly increased the TCB release rate, apparently due to the buildup of a salt form from TCB (weak base) and SA (weak acid). The following conclusions were drawn: the increase in the TCB solubility in the studied SDs, as well as the increase in the rate of the TCB release from the SDs with succinic acid was consistent with previously obtained data on high antiparasitic activity of these SDs in sheep fascioliasis.