Development of Antihelminthics of Increased Efficiency on the Basis of Intermolecular Complexes of Active Substances with Water-Soluble Polymers Including Polysaccharides
S. S. KHALIKOV1, YU. S. CHISTYACHENKO2, A. V. DUSHKIN2, E. S. METELEVA2, N. E. POLYAKOV3, I. A. ARKHIPOV4, A. I. VARLAMOVA4, I. I. GLAMAZDIN4 and N. V. DANILEVSKAYA5
1Nesmeyanov Institute of Elementoorganic Compounds, Russian Academy of Sciences, Ul. Vavilova 28, Moscow 119991 (Russia)
2Institute of Solid State Chemistry and Mechanochemistry, Siberian Branch of the Russian Academy of Sciences, Ul. Kutateladze 18, Novosibirsk 630128 (Russia)
3Institute of Chemical Kinetics and Combustion, Siberian Branch of the Russian Academy of Sciences, Ul. Institutskaya 3, Novosibirsk 630090 (Russia)
4Skryabin All-Russian Research Institute of Fundamental and Applied Animal and Plant Parasitology, Russian Academy of Sciences, Ul. B. Cheremushkinskaya 28, Moscow 117218 (Russia)
5Skryabin Moscow State Academy of Veterinary Medicine and Biotechnology, Ul. Akademika Skryabina 23, Moscow 109472 (Russia)
Keywords: механохимия, антигельминтные препараты, Drug Delivery, медамин, альбендазол, фенбендазол, полисахариды, арабиногалактан, межмолекулярные комплексы, растворимость, биодоступность, эффективность, гельминты, mechanochemistry, antihelminthic preparations, Drug Delivery, medamin, albendazol, phenbendazol, polysaccharides, arabinogalactan, intermolecular complexes, solubility, bioavailability, efficiency, helminths
Abstract
Intermolecular complexes of the guest-host type possessing increased water solubility were obtained by means of solid-phase mechanochemical treatment of a number of benzimidazole antihelminthic pharmaceutical substances with water-soluble polymers - polyvinylpyrrolidone, hydroxyethyl starch, arabinogalactan polysaccharide (from wood of
Larix sibirica and
Larix gmelinii ). Physicochemical studies of the complexes were carried out. An increase in antihelminthic activity of the preparations with respect to different laboratory models of helminthes was discovered and confirmed in experiments with sheep spontaneously infested by nematodes of gastrointestinal tract, with a decrease in substance dosage by a factor of 9-10.
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