On the possibility of obtaining soft dosage forms based on polyanionic polysaccharides with prolonged yield of drugs

IF 2.8 4区工程技术 Q2 POLYMER SCIENCE Macromolecular Research Pub Date : 2023-12-08 DOI:10.1007/s13233-023-00221-x

Anzhela Shurshina, Mariya Afanasyeva, Valentina Chernova, Mariya Lazdina, Elena Kulish

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Abstract

The work is devoted to the creation of liquid and soft gel dosage forms of prolonged action. The main task to be solved in the work was to give certain rheological characteristics (namely, pseudoplastic behaviour and pronounced yield strength) to dosage forms based on solutions of pectin, sodium salt of carboxymethylcellulose and sodium salt of chitosan succinate, namely. The study has found that the effect of prolonging the release of the medicinal substance cefazolin from liquid and soft dosage forms based on polysaccharides is directly related to the rheological characteristics of the system and can manifest itself in two cases. First, it is possible for liquid dosage forms in the area of polymer concentrations in solution lower than the concentration at which the cell of meshes C < C_e is formed. In this case, with an increase in the polymer concentration, there is a decrease in the rate of the drug substance release, due to an increase in the adduct of the polymer-drug reaction Secondly, it is possible for soft gel forms in the region of concentrations greater than the concentration at which the cell of meshes C < C_e is formed, when using additives capable of ionotropic gel formation. Calcium and zinc salts were used as such additives in the work. It is in the case when the modifying additive is capable of forming a “bridging” bond between macromolecules and the gel formation is not accompanied by a decrease in the amount of the complex adduct of the reaction, there is a prolongation effect. If the gel is only formed by increasing the polymer content in the solution without the use of an additive, the compression of macromolecular tangles and the strengthening of intramolecular interaction between the polymer units in a concentrated solution results in a significant decrease in the amount of the polymer-drug reaction adduct and accelerated the drug release from the soft dosage form.

Graphical abstract

Modification of polymer chain

Abstract Image

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基于聚阴离子多糖获得软剂型并延长药物产量的可能性

这项工作的目的是创造具有长期作用的液体和软凝胶剂型。这项工作要解决的主要问题是使基于果胶、羧甲基纤维素钠盐和壳聚糖琥珀酸钠盐溶液的剂型具有一定的流变学特性（即假塑性行为和明显的屈服强度）。研究发现，基于多糖的液体和软性剂型延长头孢唑啉药物释放时间的效果与体系的流变学特性直接相关，可表现为两种情况。首先，液态剂型溶液中的聚合物浓度有可能低于形成网状细胞 C < Ce 的浓度。在这种情况下，随着聚合物浓度的增加，由于聚合物与药物反应的加合物增加，药物的释放速度也会降低。工作中使用了钙盐和锌盐作为此类添加剂。如果改性添加剂能够在大分子之间形成 "桥接 "键，而且凝胶的形成并不伴随着反应中复合加成物数量的减少，那么就会产生延长效应。如果只通过增加溶液中的聚合物含量而不使用添加剂来形成凝胶，那么在浓缩溶液中，大分子缠结的压缩和聚合物单元间分子内相互作用的加强会导致聚合物-药物反应加合物的量显著减少，并加速药物从软质剂型中的释放。

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来源期刊

Macromolecular Research 工程技术-高分子科学

CiteScore

4.70

自引率

8.30%

发文量

100

审稿时长

1.3 months

期刊介绍： Original research on all aspects of polymer science, engineering and technology, including nanotechnology Presents original research articles on all aspects of polymer science, engineering and technology Coverage extends to such topics as nanotechnology, biotechnology and information technology The English-language journal of the Polymer Society of Korea Macromolecular Research is a scientific journal published monthly by the Polymer Society of Korea. Macromolecular Research publishes original researches on all aspects of polymer science, engineering, and technology as well as new emerging technologies using polymeric materials including nanotechnology, biotechnology, and information technology in forms of Articles, Communications, Notes, Reviews, and Feature articles.