Synthesis of a hydrophilic derivative of ecdysterone and development of its water-soluble form

A. Kozhanova, B. S. Temirgaziyev, A. Zhanarbek, B. Tuleuov, T. Seilkhanov, S. Adekenov
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Abstract

The article presents materials on the isolation of ecdysterone substance from medicinal plant raw materials Silene wolgensis (Hornem.) Bess. ex. Spreng (Volga smolyovka). For the first time, the optimization of the method for ecdysterone substance obtaining from the aboveground part of the superconcentrator of phytoecdysteroids of the Silene wolgensis was carried out and based on it a pilot industrial regulation for the isolation of ecdysterone and an encapsulated water-soluble form were developed. It was found, that the interaction of the substrate molecule and the clathrate forms a substance that can dissolve in water and other more polar solvents, thereby solving the problem of bioavailability of the main hydrophobic drug. The method developed for producing the substance ecdysterone and its water-soluble encapsulated with β-cyclodextrin form was implemented into production at the Karaganda pharmaceutical plant. NMR studies of changes in the chemical shifts of protons of substrates and receptors illustrated that ecdysterone interacts with β-cyclodextrin to form supramolecular inclusion complexes with stoichiometric composition of 1:1
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蜕皮酮亲水性衍生物的合成及其水溶性形态的研究
本文介绍了从药用植物原料硅酮中分离蜕皮酮物质的研究进展。贝斯。例:春天(伏尔加河)。首次对从硅酮体外甾体超浓缩物地上部分提取蜕皮酮物质的方法进行了优化,并在此基础上建立了脱皮酮的工业分离中试工艺和包封水溶形式。研究发现,底物分子与包合物相互作用形成一种能溶于水和其他极性更强的溶剂的物质,从而解决了主要疏水药物的生物利用度问题。所建立的以β-环糊精形式包封的蜕皮酮及其水溶性物质的生产方法已在卡拉干达制药厂投入生产。对底物和受体质子化学位移变化的核磁共振研究表明,蜕皮酮与β-环糊精相互作用形成化学计量组成为1:1的超分子包合物
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