抗骨溶解双酸盐的结构多样性:解读超长控制释放现象中的结构-活性趋势
Maria Vassaki1, Chrystalleni Hadjicharalambous2, Petri A Turhanen3
1Crystal Engineering, Growth and Design Laboratory, Department of Chemistry, University of Crete, Heraklion, Crete GR-71003, Greece.
ACS applied bio materials
|November 20, 2023
概括
研究了从药片中释放的双酸盐 (BP) 药物,发现增加的分子相互作用减缓了释放. 结构特征显著影响BP释放特征,氨基-BPs通常释放速度比基-BPs慢.
科学领域:
- 药理学 药理学是指药理学的学科.
- 材料科学 材料科学 材料科学
- 药物运输 药物运输 药物运输
背景情况:
- 双酸盐 (BPs) 对骨质疏松症等骨疾病至关重要.
- 低的口服生物利用性需要更高的剂量,导致副作用.
- 控制释放策略为改善高血压治疗提供了一个有希望的解决方案.
研究的目的:
- 调查15种双酸盐 (BPs) 及其类型的受控释放特征.
- 为了将BP释放特征与它们的分子和晶格结构相关联.
- 评估结构特征对模拟胃片BP释放的影响.
主要方法:
- 从纤维素/或纤维素/乳糖/片中研究了15个BP (基-BP和氨基-BP) 的受控释放.
- 模拟人类胃的pH值条件,用于药物释放实验.
- 利用1H NMR峰值集成来构建释放曲线 (%BP释放与时间).
主要成果:
- 控制释放配置文件与BP的结构特征相关,包括和金属-氧键.
- 更高的网格相互作用数量与较低的初始BP释放率相关.
- 随着基侧链长度的增加,基-BP的释放速度减慢;氨基-BPs的释放速度比基-BPs慢.
- 在NIH3T3细胞上没有观察到基和氨基BP的细胞毒性.
结论:
- 分子和晶格特征显著决定了BP释放特征.
- 血压释放率与网格相互作用的总数相反相关.
- 了解这些结构-释放关系可以为改进的双酸盐药物递送系统的设计提供信息.
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