Innovative anthelmintic based on mechanochemical technology and their efficacy against parasitic infection of sheepsстатья
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Дата последнего поиска статьи во внешних источниках: 17 февраля 2021 г.
Аннотация:ABSTRACTObjective: This work aims to develop a combined preparation based on ivermectin (Iver), fenbendazole (FBZ), triclabendazole (TBZ) by using mechanochemical technology, which allows increasing the solubility of the substances taken for research because such an increase should lead to an increase in the bioavailability and antiparasitic properties of the substances of these drugs. Materials and Methods: Innovative preparations in the form of solid dispersions (SD) were obtained using joint mechanical processing of drug substances with PVP in a LE-101 roller mill. The efficacy of the preparations was studied in 140 sheep spontaneously infected with gastrointestinal Strongylata, Dicrocelium dendriticum, Moniezia expansa and Melophagus ovinus. The preparations were given individually to the sheep in the form of an aqueous suspension orally; their effectiveness was evaluated using methods of intravital and post-mortem parasitological examinations.Results: It was confirmed the increasing of solubility of substances by 13-29 times. The experiments have shown the high efficiency of SD composition FBZ / Iver / PVP (1/1/9) at a dose of FBZ - 3.0, Iver - 0.2 mg / kg b/ w when used against gastrointestinal strongylates and Moniezia expansa (95.8 and 100%), to a lesser extent against Melophagus ovinus (38.5%). The composition SD of TBZ / Iver / PVP (1/1/9) at a dose of TBZ - 3.0, Iver - 0.2 showed high efficacy against gastrointestinal Strongylata and Dicrocelium dendriticum (96.8 and 100%), less activity in against Melophagus ovinus (61.6%). The initial substances FBZ and TBZ showed significantly less activity in animal helminthiases.Conclusion: The high parasiticidal activity of SD based on FBZ, TBZ, Iver in comparison with initial substances is explained by formation of inclusion complexes of these substances with PVP when SD is dissolved in water and synergistic effect of the active substances of the preparations. The resulting complexes have increased solubility in water and bioavailability. The use of such SD suggests the possibility of a significant reduction in the dosages of FBZ and TBZ without loss of parasiticidal activity.