通过联合结晶改善黄素的溶解率和生物可用性
Hao Wang1,2, Chenxuan Zheng2,3, Fanyu Tian1,2
1School of Chinese Materia Medica, Nanjing University of Chinese Medicine, 138 Xianlin Avenue, Nanjing 210023, China.
Pharmaceuticals (Basel, Switzerland)
|April 27, 2024
概括
我们开发了一个黄素和L-卡尼丁联合晶体 (CUR-L-CN) 来增强黄素.
科学领域:
- 制药科学 制药科学
- 材料科学 材料科学 材料科学
- 生物化学 生物化学
背景情况:
- 黄素 (CUR) 是一种具有多种药理作用的天然多.
- 较差的水溶性和生物可用性阻碍了CUR的临床使用.
- L-卡尼丁 (L-CN) 是安全的,并用于肝脏保护和动物营养.
研究的目的:
- 为了提高黄素的生物可用性.
- 准备和描述一种新的黄素-L-卡尼丁联合晶体 (CUR-L-CN).
主要方法:
- 使用液体辅助研磨进行共晶制备.
- 共同晶体结构的表征.
- 在模拟的胃和肠液中进行溶解研究.
- 在老鼠中的药理动力学分析.
主要成果:
- 与纯CUR相比,CUR-L-CN显著提高了溶解速率.
- 希尔什菲尔德表面分析和可湿性测试证实了增加的水亲和力.
- 药理动力学研究显示,CUR-L-CN的AUC0-t增加了6.3倍,Cmax增加了10.7倍.
结论:
- 新的CUR-L-CN联合晶体显著改善了黄素的溶解和生物可用性.
- 这种共同晶体配方提供了一种有希望的方法来增强黄素的治疗疗效.
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