Kriangkrai Worawut, Puttipipatkhachorn Satit, Sriamornsak Pornsak, Sungthongjeen Srisagul
Department of Pharmaceutical Technology, Faculty of Pharmaceutical Sciences and Center of Excellence for Innovation in Chemistry, Naresuan University, Phitsanulok 65000, Thailand.
Center of Excellence for Natural Health Product Innovation, Naresuan University, Phitsanulok 65000, Thailand.
Gels. 2024 Sep 9;10(9):581. doi: 10.3390/gels10090581.
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.
采用升华技术制备并评价了一种凝胶型漂浮骨架片，以增强胃滞留药物递送。无水茶碱用作活性药物成分，与升华剂和作为凝胶形成聚合物的羟丙基甲基纤维素相结合。所得片剂具有高孔隙率、立即漂浮和超过8小时的持续浮力。通过调节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。选择这些试剂是因为它们在形成多孔结构方面有效，从而降低片剂密度并增强漂浮性。较高的羟丙基甲基纤维素粘度导致漂浮力增加、药物释放较慢以及由于侵蚀速率较慢而具有改善的溶胀性能。对片剂孔隙率、机械强度和药物释放动力学之间平衡的关键评估表明，与薄荷醇相比，碳酸铵提供了更高的片剂硬度和更低的脆碎度，有利于控释机制。茶碱的释放动力学最好用非菲克扩散模型描述，表明扩散和侵蚀的综合作用。这项研究推动了胃滞留药物递送系统的发展，突出了基于升华的漂浮骨架片用于持续药物释放的潜力。
