The Solving of Persistence Problems of Drugs on the Basis of Ivermektin

Abstract

Ivermectin-based preparations that have been intensively used in veterinary practice for more than 30 years have contributed to the development of resistance to drugs based on it, and this problem is very relevant in modern parasitology. One of the ways to solve this problem is the development of combined preparations based both on new ivermectin derivatives and the inclusion of preparations from other class-es of chemical compounds in their composition. We have proposed an alternative method, i.e. the mechanochemical modification of the substance ivermectin using water-soluble polymers. This paper presents the results of modifying the substance of ivermectin with arabinogalactan polysaccharide (AG), isolated from Siberian larch Larix sibirica by joint machining of components in a variable-voltage shred-der activator. During jointly machining ivermectin with samples of arabinogalactan from three alternative sources, compositions of "Ivermectin: AG" (1:10), which have increased solubility (more than 10 times as compared with the original substance of ivermectin), were obtained. The study of the parasiticidal efficacy of the obtained compositions of ivermectin in intestinal helminthiases was carried out on sheep. As a result of the experiments to evaluate the compositions of ivermectin with three samples of AG, it was found that their use of helminthic efficacy did not show the advantage of any of the batches of polysaccharide. To a greater extent, the effective-ness of the compositions of ivermectin was influenced by the dosage of the drug. Biological testing of the obtained compositions of ivermectin showed the possibility of reducing the dosage of ivermectin by 2 or more times while maintaining high ef-ficiency. The obtained data indicate the promising outlook for a mechanochemical approach for modifying the physicochemical and biological properties of prepara-tions based on ivermectin in solving problems of resistance.