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微型化费克索芬纳丁化片的配方和生物等价性评估
Woo-Yul Song1,2, Chang-Soo Han1, Won-Sang Yu2
1Department of Pharmacy, Chungbuk National University, Cheongju 28644, Republic of Korea.
Pharmaceutics
|June 27, 2025
概括
开发了一种新的,较小的fexofenadine化 (FEX) 片来解决吞困难. 这种微型化配方保持了生物等价性,并提高了溶解性和稳定性,为过敏性鼻炎治疗提供了更为患者友好的选择.
科学领域:
- 制药科学 制药科学
- 药物输送系统 药物输送系统
- 制定 发展 制定 发展
背景情况:
- 费克索芬纳丁化 (FEX) 由于溶解性,凝聚性和多态不稳定性差,因此存在配方挑战.
- 传统的FEX药片很大,导致患有食障碍的患者难以吞.
- 开发一个小型化的FEX片对于改善患者的服药性和治疗疗效至关重要.
研究的目的:
- 开发一种微型的fexofenadine化片,其可溶性提高,与市场上销售的产品具有生物等价性.
- 为了优化配方参数,并评估商业可行性的扩展可行性.
- 为了评估微型药片配方的稳定性和强度.
主要方法:
- 使用基于有机溶剂的粘合剂和多孔载体来增强FEX的溶解性和流动性.
- 采用了实验设计 (DoE) 方法来优化平板电脑的大小和多孔载体含量.
- 通过基于Froude数的流程优化和加速稳定性测试进行了扩展可行性研究.
主要成果:
- 迷你FEX片显示了与生理pH (4.0和6.8) 的参考产品相似的溶解概况,在酸性pH (1.2) 的溶解速度更快.
- 六个月的稳定性研究显示溶解,晶体结构或杂质水平没有显著变化.
- 在体内生物等价性研究证实,测试配方符合曲线下的面积和Cmax的监管接受标准.
结论:
- 一个小型化的fexofenadine化片 (44%重量,50%体积减少) 成功开发,提供了商业上可行的和患者友好的替代品.
- 使用基于有机溶剂的粘合剂和多孔载体的配方策略提高了制造效率,稳定性和可溶性.
- 这项研究为药物配方策略提供了宝贵的见解,用于减小尺寸,提高溶解度和大规模生产具有挑战性的药物化合物.
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