Solid Dispersions of Fenbendazole with Polymers and Succinic Acid Obtained via Methods of Mechanochemistry: Their Chemical Stability and Anthelmintic Efficiencyстатья
Дата последнего поиска статьи во внешних источниках: 19 июня 2024 г.
Аннотация:The substance fenbendazole is included in the composition of many anthelmintic drugs, inwhich the “chemical stability” parameter is one of the main characteristics when obtaining permissionfor the use of drugs in veterinary practice. Fenbendazole is characterized by low solubility in waterand therefore the content of the substance is overestimated in its preparations, which increases thecost of the drug as well as the safety risks of pharmacotherapy. The possibilities of mechanochemicalmodification of fenbendazole were evaluated in order to improve the solubility index. During themechanical processing treatment of the substance in the presence of polymeric substances, soliddispersions are formed, which have increased solubility and high anthelmintic activity. The inclusionin these dispersions of the third component, which is succinic acid, did not significantly change thesolubility of fenbendazole. In all these dispersions, the substance remained unchanged both duringthe preparation of its solid dispersions and during their storage. When fenbendazole is modifiedin an organic solvent medium, the substance is partially converted into oxfendazole, which is oneof its metabolites. The chemical stability of fenbendazole was confirmed via HPLC/MS and NMRspectroscopy. The anthelmintic activity of these compositions was evaluated and it was found thatthey have a high nematicidal activity.
