The preparation and evaluation of granulated chitosan-catechin tablets with excellent disintegration properties

IF 2.4 3区 化学 Q3 BIOCHEMISTRY & MOLECULAR BIOLOGY
Tomoki Adachi , Yuto Tomita , Yasuyuki Mizukai , Yuji Maezaki , Kazuo Kawano , Kindness L. Commey , Hideaki Nakamura , Keishi Yamasaki , Masaki Otagiri , Makoto Anraku
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Abstract

In this study, we prepared granulated chitosan (G-CS)/catechin tablets with excellent disintegration properties. We then compared their physical properties, dissolution behavior, and pharmacokinetic profile to non-granulated chitosan (N-CS)/catechin tablets. During the tableting process, the G-CS/catechin tablets demonstrated significantly higher compatibility and superior manufacturability, as evidenced by lower ejection and detachment stress than the N-CS/catechin tablets. This resulted in more robust tablets with better physical properties. The dissolution of catechin from the G-CS/catechin tablets occurred significantly faster than from the N-CS/catechin tablets, resulting in a significantly higher 2,2′-azino-bis(3 ethylbenzothiazoline-6-sulfonic acid) (ABTS) radical scavenging capacity. Similarly, the primary catechin components of the tablets, epigallocatechin gallate (EGCG) and caffeine, showed faster dissolution and membrane uptake from the G-CS/catechin tablets. These indicate a more efficient tablet formulation than N-CS/catechin tablets. Furthermore, the absorption and bioavailability of EGCG and caffeine in rats were significantly higher after oral administration of the G-CS/catechin tablets than the N-CS/catechin tablets. These findings suggest that G-CS/catechin tablets, having better disintegration properties than N-CS/catechin tablets, could allow for combination with other supplements, leading to the design of highly efficient supplement combination tablets.

Abstract Image

制备和评估崩解性能优异的壳聚糖儿茶素颗粒片剂。
在这项研究中,我们制备了崩解性能极佳的粒化壳聚糖(G-CS)/儿茶素片剂。然后,我们将其物理性质、溶出行为和药代动力学特征与非粒化壳聚糖(N-CS)/儿茶素片进行了比较。在压片过程中,G-CS/儿茶素片剂的相容性和可制造性明显优于N-CS/儿茶素片剂,这表现在弹射和脱落应力低于N-CS/儿茶素片剂。这使得片剂更坚固,物理性能更好。G-CS/ 儿茶素片剂中儿茶素的溶解速度明显快于 N-CS/ 儿茶素片剂,因此其 2,2'-偶氮-双(3-乙基苯并噻唑啉-6-磺酸)(ABTS)自由基清除能力明显更高。同样,片剂中的儿茶素主要成分表没食子儿茶素没食子酸酯(EGCG)和咖啡因在 G-CS/catechin 片剂中的溶解和膜吸收速度也更快。这表明 G-CS/catechin 片剂比 N-CS/catechin 片剂更有效。此外,大鼠口服 G-CS/儿茶素片剂后,对 EGCG 和咖啡因的吸收率和生物利用率明显高于 N-CS/儿茶素片剂。这些研究结果表明,G-CS/儿茶素片剂比 N-CS/儿茶素片剂具有更好的崩解特性,可以与其他营养补充剂结合使用,从而设计出高效的营养补充剂复合片剂。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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来源期刊
Carbohydrate Research
Carbohydrate Research 化学-生化与分子生物学
CiteScore
5.00
自引率
3.20%
发文量
183
审稿时长
3.6 weeks
期刊介绍: Carbohydrate Research publishes reports of original research in the following areas of carbohydrate science: action of enzymes, analytical chemistry, biochemistry (biosynthesis, degradation, structural and functional biochemistry, conformation, molecular recognition, enzyme mechanisms, carbohydrate-processing enzymes, including glycosidases and glycosyltransferases), chemical synthesis, isolation of natural products, physicochemical studies, reactions and their mechanisms, the study of structures and stereochemistry, and technological aspects. Papers on polysaccharides should have a "molecular" component; that is a paper on new or modified polysaccharides should include structural information and characterization in addition to the usual studies of rheological properties and the like. A paper on a new, naturally occurring polysaccharide should include structural information, defining monosaccharide components and linkage sequence. Papers devoted wholly or partly to X-ray crystallographic studies, or to computational aspects (molecular mechanics or molecular orbital calculations, simulations via molecular dynamics), will be considered if they meet certain criteria. For computational papers the requirements are that the methods used be specified in sufficient detail to permit replication of the results, and that the conclusions be shown to have relevance to experimental observations - the authors'' own data or data from the literature. Specific directions for the presentation of X-ray data are given below under Results and "discussion".
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