循环二烯对北二烯化的透性和分割的影响
Tatyana Volkova1, Olga Simonova1, German Perlovich1
1G.A. Krestov Institute of Solution Chemistry RAS, 153045 Ivanovo, Russia.
Pharmaceuticals (Basel, Switzerland)
|July 29, 2023
概括
环极素,包括HP-β-CD和SBE-β-CD,降低诺特胺的分布和透性. 由于静电力,SBE-β-CD显示出更强的相互作用,影响药物输送系统.
科学领域:
- 制药科学 制药科学
- 药物输送系统 药物输送系统
- 物理化学 物理化学
背景情况:
- 基于环德的系统通过修改溶解度,分布和膜透来提高药物的生物可用性.
- 诺特氨酸化物 (NTT•HCl) 是一种三环抗抑郁药,其输送可以通过使用环氧来改善.
研究的目的:
- 调查基基-β-环氧化 (HP-β-CD) 和硫基-β-环氧化 (SBE-β-CD) 对北素化 (NTT•HCl) 的分布和透性的影响.
- 阐明环氧二烯度和相互作用在修改药物运输特性中的作用.
主要方法:
- 在1-octanol/buffer和n-hexane/buffer系统中,在不同度的环氧德克斯中确定分布系数.
- 通过纤维素膜和PermeaPad屏障测量透系数,其度不同.
- 对药物 - 环氧素相互作用的分析,包括关联常量.
主要成果:
- HP-β-CD和SBE-β-CD都显著降低了NTT•HCl的分布和透系数,因为环极的度增加.
- SBE-β-CD表现出更明显的下降,归因于电荷对电荷的吸引和与NTT的静电相互作用.
- 在1-octanol/buffer (pH 6.8) 系统和通过PermeaPad屏障观察到类似的分布和透趋势,突出了分布系数在脂友屏障透中的作用.
结论:
- 循环德克斯林复合,特别是与SBE-β-CD复合,有效地降低了诺特里普提林化的分布和透性.
- 静电相互作用在NTT与SBE-β-CD的增强关联和减少传输方面发挥着至关重要的作用.
- 分布系数是预测循环德克斯特林修饰系统中通过脂友性屏障透的关键描述因子.
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