利用升华技术设计和评估新型凝胶基浮动基质片剂,用于胃肠道给药

IF 5 3区 化学 Q1 POLYMER SCIENCE
Gels Pub Date : 2024-09-09 DOI:10.3390/gels10090581
Worawut Kriangkrai, Satit Puttipipatkhachorn, Pornsak Sriamornsak, Srisagul Sungthongjeen
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引用次数: 0

摘要

利用升华技术配制并评估了一种凝胶型浮动基质片剂,以增强胃肠道给药效果。以无水茶碱为活性药物成分,结合升华剂和羟丙基甲基纤维素作为凝胶形成聚合物。通过调整羟丙基甲基纤维素的粘度和升华剂(特别是碳酸铵和薄荷醇)的浓度,实现了漂浮行为和药物释放曲线的优化。之所以选择这些升华剂,是因为它们能有效地形成多孔结构,从而降低片剂密度并增强漂浮性。HPMC 粘度越高,浮力越大,药物释放越慢,侵蚀速度越慢,溶胀性能越好。对片剂孔隙率、机械强度和药物释放动力学之间的平衡进行的严格评估表明,与薄荷醇相比,碳酸铵的片剂硬度更高,易碎性更低,有利于控制释放机制。反常(非费克)扩散模型对茶碱的释放动力学进行了最佳描述,表明扩散和侵蚀作用共同作用。这项研究推动了胃保留给药系统的发展,凸显了基于升华的浮动基质片剂在药物持续释放方面的潜力。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Design and Evaluation of New Gel-Based Floating Matrix Tablets Utilizing the Sublimation Technique for Gastroretentive Drug Delivery.

A gel-based floating matrix tablet was formulated and evaluated using the sublimation technique to enhance gastroretentive drug delivery. Anhydrous theophylline was employed as the active pharmaceutical ingredient, combined with sublimation agents and hydroxypropyl methylcellulose as the gel-forming polymer. The resulting tablets exhibited high porosity, immediate floatation, and sustained buoyancy for over 8 h. Optimization of the floating behavior and drug release profiles was achieved by adjusting the viscosity of and hydroxypropyl methylcellulose and the concentration of sublimation agents, specifically ammonium carbonate and menthol. These agents were selected for their effectiveness in creating a porous structure, thus reducing tablet density and enhancing floatation. Higher HPMC viscosity resulted in increased floating force, slower drug release, and improved swelling properties due to a slower erosion rate. A critical assessment of the balance between tablet porosity, mechanical strength, and drug release kinetics indicates that ammonium carbonate provided superior tablet hardness and lower friability compared to menthol, favoring a controlled release mechanism. The release dynamics of theophylline were best described by the anomalous (non-Fickian) diffusion model, suggesting a combined effect of diffusion and erosion. This research advances the development of gastroretentive drug delivery systems, highlighting the potential of sublimation-based floating matrix tablets for sustained drug release.

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来源期刊
Gels
Gels POLYMER SCIENCE-
CiteScore
4.70
自引率
19.60%
发文量
707
审稿时长
11 weeks
期刊介绍: The journal Gels (ISSN 2310-2861) is an international, open access journal on physical (supramolecular) and chemical gel-based materials. Our aim is to encourage scientists to publish their experimental and theoretical results in as much detail as possible. Therefore, there is no restriction on the maximum length of the papers, and full experimental details must be provided so that the results can be reproduced. Short communications, full research papers and review papers are accepted formats for the preparation of the manuscripts. Gels aims to serve as a reference journal with a focus on gel materials for researchers working in both academia and industry. Therefore, papers demonstrating practical applications of these materials are particularly welcome. Occasionally, invited contributions (i.e., original research and review articles) on emerging issues and high-tech applications of gels are published as special issues.
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