FEATURES OF MECHANOCHEMICAL TECHNOLOGY IN THE DEVELOPMENT OF PARASITOCIDES

Abstract

The purpose of the research is to study the features of the mechanochemical modification of medicinal substances with low solubility in water. According to the Biopharmaceutics Classification System, about 6% of medicinal substances belong to the group of insoluble medicinal substances, and about 47%, to practically insoluble medicinal substances, i.e. more than a half substances have problems with solubility, and therefore bioavailability and pharmacological activity. To achieve the therapeutic effect of such substances, it is necessary to deliberately increase the dosage of the substance, which increases the cost of the drug, as well as safety risks of pharmacotherapy. The work evaluated possibilities of mechanochemical modification of a number of known anthelmintic substances with low solubility to increase this parameter. It was shown that during machining of such substances in the presence of polymeric substances, solid dispersions were formed that had increased solubility while maintaining high anthelmintic activity with decreased dosage of the active substance. Preparations in the form of solid dispersions can be used both orally and by a group method to 10-20 animals, mixed with compound feed. For low-melting substances, a liquid-phase machining method is proposed to obtain stable suspension concentrates that are convenient for oral administration. The prospects for obtaining mixed compositions based on two substances are shown, which makes it possible to obtain combined preparations with a wide spectrum of action with the minimized volume and frequency of their use.