Faculty of Pharmacy, PDRC, Al-Ahliyya Amman University, Amman 19328, Jordan.
Faculty of Pharmacy, Al-Zaytoonah University of Jordan, Amman 11733, Jordan.
Molecules. 2024 Sep 29;29(19):4629. doi: 10.3390/molecules29194629.
This study outlines the development of a cost-effective, extended-release febuxostat (FEB) tablet using activated charcoal as an adsorbent to enhance drug release. FEB, a BCS Class II drug, presents formulation challenges due to low solubility and high lipophilicity. We evaluated eight formulations with varying FEB-to-charcoal ratios using FTIR and DSC for physical interactions and followed USP standards for overall assessment. The optimal 1:0.25 FEB-to-charcoal ratio demonstrated a consistent 12 h zero-order release pattern. In vivo studies indicated a significantly extended plasma profile compared to immediate-release tablets. The optimal tablets demonstrated acceptable hardness and disintegration times. This innovative approach enhances patient compliance, improves bioavailability, and reduces production costs, offering a promising solution for controlled FEB delivery.
本研究概述了一种经济高效的非布司他（FEB）延长释放片的开发，该片剂使用活性炭作为吸附剂来增强药物释放。FEB 是一种 BCS 分类 II 药物，由于低溶解度和高亲脂性，存在制剂挑战。我们使用傅里叶变换红外光谱（FTIR）和差示扫描量热法（DSC）评估了八种不同 FEB-活性炭比例的制剂，以评估物理相互作用，并按照 USP 标准进行全面评估。FEB-活性炭比例为 1:0.25 的最佳比例表现出一致的 12 小时零级释放模式。体内研究表明，与速释片剂相比，其血浆特征得到了显著延长。最佳片剂的硬度和崩解时间可接受。这种创新方法提高了患者的顺应性，改善了生物利用度，并降低了生产成本，为控制 FEB 递送提供了有前景的解决方案。
