辅助剂对纤维素平衡溶解度在禁食和饮食模拟肠道液体中的影响,使用实验协议设计进行评估
Bayan E Ainousah1, Ibrahim Khadra2, Gavin W Halbert2
1Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Umm Al-Qura University, Makkah 21955, Saudi Arabia.
助剂在模拟的肠液中显著改变纤维酸的溶解性,影响药物吸收. 配方开发需要仔细考虑辅助剂的类型,度和媒介成分,以获得最佳的生物可用性.
科学领域:
- 制药科学 制药科学
- 药物运输 药物运输 药物运输
- 物理化学 物理化学
背景情况:
- 药物溶解性对于口服吸收至关重要,特别是对于不容易溶解的化合物.
- 肠道介质组成和辅料可以显著影响药物的溶解性,导致生物可用性问题.
- 了解辅助剂对溶解性的影响对于有效的口服剂型开发至关重要.
研究的目的:
- 为了研究各种辅助剂对模拟肠道介质中的费诺纤维酸溶解性的影响.
- 评估介质组成和辅助剂特性对溶解性的影响.
- 为了指导可溶性较差的药物如 fenofibrate 的配方开发.
主要方法:
- 采用小规模实验设计 (DoE) 进行平衡溶解性研究.
- 在模拟的禁食和食肠道介质中评估的纤维酸溶解度,参数不同.
- 评估了不同度和等级的特定辅助剂 (曼尼,PVP,HPMC,奇托) 的作用.
主要成果:
- 只有pH和酸盐在没有辅助剂的空腹介质中显著影响了纤维酸的溶解性.
- 聚烯利 (PVP) 以媒体,等级和度依赖的方式增加了纤维酸的溶解性.
- 基甲基纤维素 (HPMC) 和奇托桑降低溶解度,受介质,等级和度的影响.
结论:
- 辅助剂对纤维酸溶解性的作用是复杂的,取决于介质组成和辅助剂的特性.
- 用相关介质和助剂进行体外溶解性研究对配方开发有价值.
- 这项研究提供了关于优化纤维酸溶解性的见解,以改善口服药物输送.
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