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It is impossible to imagine modern agricultural production without using of chemical pesticides (fungicides, insecticides, herbicides, plant growth etc.) to obtain and save agriculture production. This investigation focuses to improve existing pesticides, as well as new compositions and effective active ingredients, the use of which makes it possible not only to obtain high yields of crops, but also to keep their long-term storage. To create such innovative pesticides we used the possibility of mechanochemical technology, which is based on the idea of changing the solubility and bioavailability of the active ingredients, substance of the majority of whom are poor or water-insoluble organic compounds. For example, some of known antifungal drugs based on tebuconazole substance, which has the water solubility as 23 mg / l. Based on using mechanochemical technology we obtained solid dispersions tebuconazole with plant and biosynthetic polysaccharides that form when dissolved in aqueous media intermolecular complexes of the type of “guest-host”. The alternative ways of modifying tebuconazole we used to obtain its solid dispersion with nanostructured amorphous silica. In all cases there is an increase in water solubility of tebuconazole ~ 101-102 times. Comparative tests of officinal and mechanochemically modified products showed the possibility of reducing the rates of the last 1.5-2 times while maintaining efficiency. The proposed technology of mechanochemical modification tebuconazole and ingredients of other pesticides is universal and can be applied to a wide range of biologically active substances.