The efficacy of complex solid dispersions of anthelmintics against experimental trichinellosis

A. I. Varlamova, S. Khalikov, E. Meteleva, V. I. Evseenko, M. Khalikov, I. Arkhipov
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Abstract

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.
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驱虫药复合固体分散体对实验性旋毛虫病的疗效
本研究的目的是研究以聚乙烯吡啶酮和甘草提取物为原料制备驱虫药复合固体分散体的工艺因素对实验性白鼠旋毛虫病驱虫药药效的影响。材料和方法。采用机械化学法制备的芬苯达唑(FBZ)、fenasal (FNS)、吡喹酮(PZQ)复合固体分散体样品与聚乙烯吡罗烷酮(PVP)、甘草提取物(LE)在不同配比、不同暴露时间下对实验感染旋毛虫的130只小白鼠的杀线虫活性进行了研究。感染后第3天,随机分为实验组,每组10只。实验组小鼠按活性物质2 mg/kg的剂量灌胃驱虫药的各种复合固体分散体样品。以FBZ物质为基础药物,根据活性物质剂量,以2 mg/kg的剂量给药。对照组的动物没有接受药物治疗。实验药样给药后第4天采用断头处死,根据肠道蠕虫解剖结果计算药物活性,采用对照型试验计算药效。结果和讨论。在相同的机械化学处理时间下,FBZ和FNS与PVP聚合物的复合固体分散体的效率高于与LE的配合物的活性。随着机械化学处理时间从24 h缩短至5 h, FBZ活性从67.05下降至37.77%,FBZ: FNS复合物与LE处理1 h时的疗效几乎与基础药物水平相当。与FBZ物质相比,添加PVP靶向给药的FNS的驱虫效果提高了2.7倍,与LE相比,其驱虫效果提高了2.2倍。PBZ - PZQ复合固体分散体的生物活性低于FBZ - FNS组合体。
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38
审稿时长
8 weeks
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