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Anthelmintic efficacy of Fenbendazole and Niclosamide suspensions obtained by liquid phase mechano-chemical treatment
Abstract
The purpose of the research is to study the anthelmintic efficacy of suspensions based on a combined solid dispersion of Fenbendazole and Niclosamide. Materials and methods . Mechanochemistry methods were used to prepare suspensions of Fenbendazole (FBZ) and Niclosamide (NSM) substances, in particular, liquid phase grinding of substances with additives (licorice extract, polyvinylpyrrolidone (PVP)) in water or in aqueous sodium carboxymethylcellulose (NaCMC) solution. The grinding was conducted in LE-101 roller mill at energy intensity of 1 g for 1 hour at a roll rotation speed of 60–70 rpm. The resulting suspension samples of combined FBZ and NSM dispersions were studied for cestodocidal activity on a laboratory model of hymenolepiosis of white mice that were infected at a dose of 200 infective Hymenolepis nana eggs per animal. Results and discussion . The 100% efficacy of a combined NaCMC-based drug suspension containing FBZ 13 mg and NSM 130 mg in 1 g of suspension was achieved at a dose of 20 mg/kg of NSM and 2 mg/kg of FBZ. The suspension based on licorice extract, NaCMC, and dioctyl sulfosuccinate sodium salt containing FBZ 18.6 mg and NSM 186 mg in 1 g of suspension at the same dose, i.e. 20 mg/kg of NSM and 2 mg/kg of FBZ showed 71.43% efficacy against H. nana. The suspension based on licorice extract and NaCMC containing FBZ 24.6 mg and NSM 246 mg in 1 g of suspension at the same dose showed a 62.0% effect against H. nana. The activity of the basic drug, the FBZ and NSM suspension was 28.58% at this dose without using mechano-chemical treatment.
... Возбудителями гельминтозов у лошадей являются ассоциации паразитов Parascaris equorum, Strongyloides westeri, Oxyuris equi и стронгилята, которые локализуются в органах пищеварительного тракта животных [2,4,6,16,20]. ...
The purpose of the research is to assess and economically justify the use of anthelmintics against helminthosis in horses.
Materials and methods. The activity of the anthelmintic action of drugs against helminthosis in horses was studied, and a comparative analysis and cost calculation were performed in 2017 to 2025. One hundred and seventy-six Orlov, Russian trotting, Trakehner, Budyonny, Akhal-Teke, English Sport and local horses of different age and gender category, use, and type were examined. The results were processed statistically using Statistica 6.1 and Microsoft Excel software.
Results and discussion . It was found that a highly effective and least expensive drug used against helminthosis in horses is a Gelmioks composition form that is advantageous in the composition form (no need for additional labor and time costs to calculate a dose per animal) and ease of use.
The purpose of the research is to study the influence of various technological factors on obtaining of complex solid dispersions of anthelmintics with polyvinylpyrrolidone and licorice extract on anthelmintic efficacy in experimental trichinellosis of white mice. Materials and methods . The study of the nematodocidal activity of complex solid dispersions samples based on fenbendazole (FBZ), fenasal (FNS) and praziquantel (PZQ) with polyvinylpyrrolidone (PVP) and licorice extract (LE) obtained by mechanochemical technology at different ratios of components and different exposure times was carried out on 130 white mice experimentally infected with Trichinella spiralis in two experiments. On the 3rd day after infection, the animals were divided into experimental groups of 10 animals each. Samples of various complex solid dispersions of anthelmintics were administered intragastrically to the mice of the experimental groups at a dose of 2 mg/kg according to the active substance. FBZ substance was used as the basic drug at a dose of 2 mg/kg according to the active substance. Animals of the control groups did not receive the drugs. The animals were killed by decapitation on the 4th day after experimental drug samples administration, and the activity of the drugs was counted according to the results of helminthological necropsy of the intestine, the efficacy was calculated by the type of control test. Results and discussion . The efficacy of complex solid dispersions of FBZ and FNS with PVP polymer was higher in comparison with the activity of complexes with LE at the same duration of mechanochemical treatment in a roller mill. The FBZ activity decreased from 67.05 to 37.77% with a decrease in the duration of mechanochemical treatment from 24 h to 5 h and the efficacy of the FBZ : FNS complex with LE turned out to be almost at the level of the basic drug when treated for 1 h. The use of mechanochemical technology for obtaining of a solid dispersion of FBZ : FNS with PVP for targeted delivery makes it possible to increase the anthelmintic efficacy by 2.7 times compared with the activity of the FBZ substance, and with LE by 2.2 times. It was noted that complex solid dispersions of PBZ with PZQ have lower biological activity in comparison with compositions of FBZ with FNS.
The purpose of the research is studying anthelmintic efficacy of fenbendazole solid dispersion obtained by mechanochemical technology with various components for targeted delivery. Materials and methods. The tests were conducted on 80 white mice infected experimentally with Trichinella spiralis and 145 sheep infected spontaneously with gastrointestinal nematodes. In case of each helminthosis, animals in different groups of 8–10 units each were given, orally, as a single dose, a fenbendazole solid dispersion (FSD) with polyvinylpyrrolidone (PVP), arabinogalactan (AG), glycyrrhizinic acid sodium salt (NaGA), dioctylsulphosuccinate sodium (NaDSS), licorice extract (LE) and hydroxyethylstarch (HES) in a dose of 2.0 mg/kg of the active ingredient as compared to fenbendazole drug at 2.0 mg/kg. A group of animals that were not given the drug was a control group. Anthelmintic activity of the preparations was considered based on dissection of the mouse small bowel and data from the sheep coproovoscopic examination carried out by the flotation technique before and 15 days after application of such drugs. Results and discussion. FSD with PVP, AG, NaGA, NaDSS, LE and HES in a dose of 2.0 mg/kg of the active ingredient (fenbendazole) showed 100; 98.7; 99.8; 100; 96.8 and 95.3% activity in mice against T. spiralis respectively; in sheep – 100; 96.3; 98.0; 100; 94.6 and 93.8% effectiveness against Nematodirus spp., and 100; 97.5; 98.6; 100; 97.0 and 96.5% activity against other species of the gastrointestinal Strongylata at 22.6–27.2% effectiveness of the main drug, namely, the active ingredient fenbendazole.
The purpose of the research is to characterize the methods for testing and assessment of efficiency of anthelmintics against trichinellosis and hymenolepidosis in laboratory model.Materials and methods. The literature and own research results have been analyzed as regards testing and efficiency assessment of anthelmintics against trichinellosis and hymenolepidosis in white mouse as a laboratory model weighting 14–16 g that was infected experimentally with Trichinella spiralis larvae in a dose of 200 larvae per specimen and with Hymenolepis nana eggs in a dose of 200 infective eggs per specimen. The medication efficiency was considered subject to the results of a small intestine autopsy on the 2nd and 4th days after the medications were injected to treat trichinellosis and hymenolepidosis in white mice accordingly.Results and discussion. A detailed description has been given for progressive methods to test medication and new chemical compound effect on nematode activity in white mice infected experimentally with T. spiralis, and on cestode activity in white mice infected experimentally with H. nana in a dose of 200 larvae and 100–200 eggs per specimen accordingly. In order to study effectiveness, the test medications were introduced into animals on the 3rd day in the trichinellosis case and on the 13th day in the hymenolepidosis case. Anthelmintic effectiveness was taken into consideration based on helminthologic autopsy of small intestines in animals on the 2nd and 4th days after the medications were given against T. spiralis и H. nana accordingly. The helminthes found in the experimental and control (uncured) animals were counted by a checkup analysis, namely, in comparison with the control animals.
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