核酸作为共同形态系统中的新共同形成物:增强溶解率,水溶性和物理稳定性
Xianzhi Liu1, Luyan Shen1, Lin Zhou1
1Chemical Biology Research Center, School of Pharmaceutical Sciences, Wenzhou Medical University, Wenzhou 325035, Zhejiang, China; Wenzhou Institute, University of Chinese Academy of Sciences, Wenzhou 325024, Zhejiang, China.
概括
氨酸单酸和氨酸二酸作为酸性共同形成物具有前景,显著提高了像mebendazole这样水溶性较差的药物的溶解率和物理稳定性.
科学领域:
- 制药科学 制药科学
- 材料科学 材料科学 材料科学
- 药物运输 药物运输 药物运输
背景情况:
- 同形态系统可以改善水溶性较差的药物的溶解.
- 酸性共同形成物是具有挑战性的发展,具有有限的选择,如酸和谷氨酸.
- 需要新的酸性共同形成剂来扩大配方策略.
研究的目的:
- 调查腺单酸盐 (AMP) 和腺二酸盐 (ADP) 作为新型酸性共同形成物.
- 为了提高模型药物的可溶性和溶解率,mebendazole,celecoxib和tadalafil.
- 评估AMP和ADP对无形药物系统物理稳定性的影响.
主要方法:
- 同形态系统是使用球磨制备的.
- 射线粉碎衍射 (XRPD) 证实了共形系统的形成.
- 溶解研究评估了药物的溶解性和溶解率.
- 评估了无形药物的物理稳定性.
主要成果:
- 与AMP和ADP配合的同形系统与纯药物相比显著增加了药物的溶解性和溶解率.
- 使用AMP和ADP作为共同形成剂增强了无形药物的物理稳定性.
- 观察到分子相互作用,积极影响共同形态系统的性能.
- 梅本达和塔达拉菲尔共同形态系统显示出显著的改善.
结论:
- 氨酸单酸和氨酸二酸是有效的酸性共同形成物.
- 这些核酸为开发先进的共形药物系统提供了一个有前途的战略.
- 这些发现扩大了制定水溶性差药物的工具包.
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