机械合成稳定的盐水合物Allopurinol与增强的溶解,扩散和药理动力学
Richu Bagya Varsa S1, Noopur Pandey2, Animesh Ghosh2
1Department of Chemistry, Faculty of Engineering and Technology, SRM Institute of Science and Technology, Chennai, Tamil Nadu 603203, India.
ACS omega
|September 25, 2023
概括
新的氨醇 (ALO) 盐与酸和酸显著提高了溶解性和透性. 这些新型配方提高了生物可用性,为痛风和结石治疗提供了有希望的替代方案.
科学领域:
- 制药科学 制药科学
- 材料科学 材料科学 材料科学
- 药用化学 医学化学
背景情况:
- 氨醇 (ALO) 是一种BCS IV药物,具有较差的溶解性,透性和生物可用性,限制了其治疗痛风和结石的疗效.
- 由于ALO的物理化学特性,现有的配方在提供足够的治疗水平方面面临挑战.
研究的目的:
- 合成和表征新型的氨醇 (ALO) 盐与酸 (MLE) 和酸 (OXA),以克服其生物制药限制.
- 评估盐形成对ALO溶解性,溶解性,透性和固态稳定性的影响.
主要方法:
- 使用溶剂辅助研磨方法合成ALO-MLE和ALO-OXA盐.
- 鉴定涉及PXRD,DSC,TGA,FT-IR和SEM. 这三种类型的特征都在研究中.
- 结晶结构是使用Rietveld精炼来确定的.
- 溶解性,溶解性和扩散性透性在pH值6.8.8下进行了评估.
主要成果:
- 新型ALO-MLE和ALO-OXA盐水合物已成功合成,具有独特的晶体结构和离子相互作用.
- 与原生ALO相比,有机盐的可溶性和溶解率增加了多达5倍.
- 扩散透性提高了多达12倍,ALO-MLE表现出卓越的性能.
- 盐水合物在特定的储存条件下表现出极好的稳定性.
结论:
- 盐与酸和酸形成有效地提高了allopurinol的可溶性,溶解性和透性.
- ALO-MLE盐水合物是一种有前途的固体剂型,具有改善的药理动力学和生物可用性.
- 这种方法提供了一个可行的策略,用于开发更有效的阿洛普醇配方,可能允许更低的剂量.
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