COMPLEXATION OF PRAZIQUANTEL WITH α-, β- AND y-CYCLODEXTRINS IN AQUEOUS-ALCOHOLIC SOLUTIONS

IF 0.2 Q4 CHEMISTRY, MULTIDISCIPLINARY Periodico Tche Quimica Pub Date : 2020-12-20 DOI:10.52571/ptq.v17.n36.2020.317_periodico36_pgs_302_314.pdf
Nurgiza F Ibrakova, G. G. Kutlugildina, Yuriy S. Zimin
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Abstract

Currently, the percentage of infections with invasive (parasitic) diseases is quite large; therefore, the treatment of helminthiases is an urgent problem in veterinary medicine. Parasitic worms inflict significant damage on animal husbandry, leading to the death of animals, shortage of meat, dairy products, and wool. The most common active ingredient in antihelmintics is praziquantel, which is well known as an effective broad-spectrum anthelmintic. At the same time, praziquantel has low solubility in water and a pronounced bitter taste, which represents a significant obstacle in developing liquid forms of drugs that are convenient for administration to animals. One way to solve these problems is the complexation of medicinal substances with various (natural and synthetic) compounds. In this regard, this paper aims to study the complexation of praziquantel with α-, β-, and -cyclodextrins in aqueous-alcoholic solutions. The studies were carried out by the method of ultraviolet spectroscopy. It was found that the addition of cyclodextrins to aqueous-alcoholic solutions of praziquantel leads to spectral changes indicating the presence of intermolecular interactions and complexation. The isomolar series method showed that in dilute solutions, praziquantel forms complex compounds with cyclodextrins 1:1, that is, one molecule of praziquantel falls on one molecule of α-, β- or y-cyclodextrin. The stability constants of the resulting complexes were calculated using the molar ratio method. It is shown that in the range of 296-316 K, the composition of complex compounds remains unchanged (1:1), and their stability decreases with increasing temperature. The study of the temperature dependences of the stability constants made it possible to determine the standard values of changes in the Gibbs energy, enthalpy, and complexation entropy.
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吡喹酮与α-、β-和y-环糊精在水-酒精溶液中的络合作用
目前,感染侵袭性(寄生虫)疾病的比例相当大;因此,寄生虫病的治疗是兽医学亟待解决的问题。寄生虫对畜牧业造成严重损害,导致动物死亡,肉类、奶制品和羊毛短缺。抗寄生虫药中最常见的有效成分是吡喹酮,它是一种众所周知的有效的广谱驱虫药。同时,吡喹酮在水中的溶解度很低,而且有明显的苦味,这是开发便于动物给药的液体药物的一个重大障碍。解决这些问题的一种方法是将药用物质与各种(天然的和合成的)化合物络合。因此,本文旨在研究吡喹酮与α-、β-和-环糊精在水-醇溶液中的络合作用。研究采用紫外光谱法进行。结果表明,环糊精加入吡喹酮的水-醇溶液中会引起光谱变化,表明存在分子间相互作用和络合作用。等摩尔串联法表明,在稀溶液中,吡喹酮与环糊精形成1:1的络合物,即一个吡喹酮分子落在一个α-、β-或y-环糊精分子上。用摩尔比法计算了配合物的稳定性常数。结果表明,在296 ~ 316k范围内,配合物的组成保持不变(1:1),其稳定性随温度的升高而降低。对稳定常数的温度依赖性的研究使得确定吉布斯能、焓和络合熵变化的标准值成为可能。
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Periodico Tche Quimica
Periodico Tche Quimica CHEMISTRY, MULTIDISCIPLINARY-
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期刊介绍: The Journal publishes original research papers, review articles, short communications (scientific publications), book reviews, forum articles, announcements or letters as well as interviews. Researchers from all countries are invited to publish on its pages.
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