乌比金的晶:提高稳定性和生物利用性
Qi Zhang1, Mengyuan Xia1,2, Chenxuan Zheng1,2,3
1Pharmaceutical Analytical & Solid-State Chemistry Research Center, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
Pharmaceutics
|October 28, 2023
概括
研究人员开发了一种稳定的ubiquinol联合晶体与维生素B3尼古丁胺胺. 这种新形式改善了ubiquinol的性能.
科学领域:
- 营养生物化学 营养生物化学
- 制药科学 制药科学
- 材料科学 材料科学 材料科学
背景情况:
- 辅酶Q10 (CoQ10) 存在于ubiquinol (减少) 和ubiquinone (氧化) 形式.
- 乌比金提供了优越的吸收和治疗效益比乌比金.
- 乌比金固有的不稳定性对储存和配方提出了挑战.
研究的目的:
- 设计和合成一种新的,稳定的ubiquinol联合晶体.
- 为了提高ubiquinol的稳定性,溶解性和生物可用性.
- 为了克服ubiquinol的配方和储存限制.
主要方法:
- 在ubiquinol和维生素B3尼古丁胺胺 (UQ-NC) 之间形成晶.
- 在应力条件下的稳定性测试.
- 在模拟肠液 (SIF) 和模拟胃液 (SGF) 中进行体外溶解研究.
- 在体内药理动力学 (PK) 研究.
主要成果:
- 该UQ-NC共晶体表现出卓越的稳定性,优于市场上销售的ubiquinol形式.
- 溶解实验显示,可晶体的最大乌比基诺度显著更高 (12.6x在SIF中,38.3x在SGF中).
- 与市场上销售的形式相比,PK研究显示UQ-NC共晶的最大CoQ10度是2.2倍,AUC是4.5倍.
结论:
- 新的ubiquinol-nicotinamide联合晶体 (UQ-NC) 有效地解决了ubiquinol的稳定性问题.
- UQ-NC表现出显著改善的溶解和生物可用性.
- 这种共晶体代表了基于ubiquinol的疗法和补充剂的有希望的进步.
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