选择一个不相互作用的缓冲器,以α-cyclodextrin含有溶液
Marlene Storm Andersen1, Simon Løv Thomsen1, Christian Schönbeck2
1Department of Physics, Chemistry and Pharmacy, University of Southern Denmark, Campusvej 55, 5230 Odense, Denmark.
International journal of pharmaceutics
|August 8, 2025
概括
缓冲区的选择显著影响循环德克斯 (CD) 药物配方. 一些碳酸缓冲剂干扰α-环氧德素 (α-CD) 复合,而其他缓冲剂的相互作用很小,影响药物的溶解性和稳定性.
科学领域:
- 制药科学 制药科学
- 物理化学 物理化学
- 药物运输 药物运输 药物运输
背景情况:
- 活性药物成分 (API) 的溶解性和稳定性差,挑战了药物配方.
- 循环脱素 (CDs) 通过包含复合物的形成来增强API的溶解性和稳定性.
- 缓冲区选择对于基于CD的配方的pH控制至关重要,但潜在的缓冲区-CD相互作用尚未完全理解.
研究的目的:
- 调查十二种药学相关的缓冲剂对α-cyclodextrin (α-CD) 与1,9-nonanediol的含有复杂化的影响.
- 为了确定缓冲结构和循环德克斯类型对复杂化常数和热力学参数的影响.
主要方法:
- 使用异热定位热量计 (ITC) 来量化复合常数和热力学参数.
- 该研究评估了在各种缓冲系统的存在下α-CD和1,9-nonanediol之间的相互作用.
- 进行的比较分析包括标准α-CD和基化α-cyclopodextrin (HP-α-CD).
主要成果:
- 缓冲物种显著影响了与1,9-nonanediol的α-CD复合.
- 碳酸缓冲剂 (烟酸,酸,酸,酸,酸) 显示出具有竞争力的结合,减少了复杂化.
- 酸盐,MES,Tris和酸显示出最小的干扰;碳酸酸上增加的基组降低了结合亲和力.
结论:
- 缓冲区的选择对于优化基于环氧德克斯的药物配方至关重要.
- 缓冲器-CD相互作用取决于缓冲器的化学结构和CD腔的特性.
- HP-α-CD显示较低的结合常数,可能是由于硬质障碍和改变的腔体水友性.
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