分子间相互作用对晶石尺寸在晶体固体分散中的影响
Hua Huang1, Yong Zhang1, Yao Liu1
1Medical College, Qinghai University, Xining 810001, China.
Pharmaceutics
|October 28, 2023
概括
晶体固体分散 (CSD) 通过减少晶体体大小来增强药物溶解. 在黄类药物上增加基团增强了药物聚合物相互作用,进一步提高了CSD中的溶解性和生物可用性.
科学领域:
- 制药科学 制药科学
- 材料科学 材料科学 材料科学
- 物理化学 物理化学
背景情况:
- 晶体固体分散 (CSD) 是先进的制药系统,旨在提高药物的溶解性和生物可用性.
- 具有不同基群数量的黄类药物作为有效的模型来研究CSD中的药物聚合物相互作用.
- 波洛克萨默188 (P188) 用作CSD配方中的载体.
研究的目的:
- 研究药物聚合物相互作用,结晶体大小和CSD溶解行为的关系.
- 探索黄类药物中基群的数量如何影响这些特性.
- 了解药物聚合物相互作用对药物结晶动学的影响.
主要方法:
- 汉森溶解度参数和弗洛里-哈金斯相互作用参数被计算出来,以评估药物-聚合物相互作用.
- 极化光学显微镜和粉末X射线衍射被用来研究结晶运动.
- 粉末X射线衍射和激光粒子大小分析监测了域和晶石大小.
- 在体外溶解研究验证了结晶体大小和药物释放之间的联系.
主要成果:
- 观察到更强的药物聚合物相互作用与增加的基组数量在黄类药物.
- 增强的药物聚合物相互作用降低了CSD系统内药物结晶的可能性.
- 结晶域和结晶体大小的显著减少得到了实现.
- 在减少结晶体大小和增强体外药物溶解之间发现了直接的相关性.
结论:
- 基群的数量是影响CSD中药物聚合物相互作用的关键因素.
- 优化药物聚合物相互作用可以有效控制结晶体大小并增强药物溶解.
- 中心证券交易所提供了一种有希望的策略,可以提高像黄类药物这样溶解不良药物的生物可用性.
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