使用L-氨酸/氨酸和MβCD/HPβCD的二元和三元纳入复合物的制备和比较,使用不同的摩尔比率
Sophia Awais1, Mehwish Afridi1, Azra Batool2
1IBADAT International University, Islamabad, Pakistan.
Pakistan journal of pharmaceutical sciences
|May 15, 2024
概括
这项研究通过使用含氨基酸的环氧德克斯特林纳入复合物增强了阿里皮普拉 (ARI) 的溶解性和稳定性. 甲基-β-环氧德克斯特林与L-阿基因因显著改善了ARI.
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:
- 阿里皮普拉 (ARI) 具有较差的溶解性和稳定性,限制了其治疗疗效.
- 开发先进的配方对于克服ARI的物理化学限制至关重要.
研究的目的:
- 通过形成二元和三元纳入复合物来增强阿里皮普拉 (ARI) 的溶解性和稳定性.
- 评估复杂化疗效,并描述ARI,环极和氨基酸之间的相互作用.
主要方法:
- 使用甲基-β-环极素 (MβCD) 和基基β环极素 (HPβCD) 与L-氨酸 (ARG) 和L-氨酸 (LYS) 形成二进制和三进制纳入复合体.
- 使用减弱总反射里埃变换红外光谱学 (AT-FTIR),X射线粉微波测量 (XRD),差分扫描热度计 (DSC),扫描电子显微镜 (SEM) 和热重力测量分析 (TGA) 的表征.
- 进行溶解测试和相稳定性研究以评估复杂的性能.
主要成果:
- 与二进制复合物相比,三进制包容复合物,特别是与L-氨酸一起的复合物,表现出优越的溶解性增强.
- 通过冷化制备的ARI:MβCD:ARG复合物显示溶解度增加了18倍,超过ARI:HPβCD:ARG复合物 (增加了7倍).
- 鉴定证实了分子相互作用和复合体内的药物形态的显著变化,冷化产生了比溶剂蒸发更好的稳定性结果.
结论:
- 甲基-β-环极 (MβCD) 是一个比HPβCD更有效的载体,可以提高阿里皮拉的溶解性和稳定性.
- 优化的摩尔比率对于保持包容复合物的稳定性和可溶性好处至关重要.
- 解热化是制备稳定和高度溶解的阿里皮普拉三元包容复合物的首选方法.
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