通过固体自我微乳液输送系统增强费洛迪平的口服生物可用性
Ying Zheng1, Lusi Chen2, Yingshu Feng3
1School of Pharmacy and Food Engineering, Wuyi University, Jiangmen, 529000, China.
AAPS PharmSciTech
|February 18, 2026
概括
这项研究开发了一种固体的自我微乳化药物输送系统 (FEL@S-SMEDDS),以提高费洛迪平 (FEL) 口服生物可用性. 新的FEL@S-SMEDDS配方显著提高了大鼠的FEL吸收,为高血压管理提供了一个有前途的方法.
科学领域:
- 制药科学 制药科学
- 药物输送系统 药物输送系统
- 药理动力学 药理动力学
背景情况:
- 费洛迪平 (FEL) 是一线抗高血压药物,其口服生物可用性较低.
- 低水溶性和第一通代谢限制了FEL的治疗疗效.
- 提高FEL口服生物可用性对于有效的高血压管理至关重要.
研究的目的:
- 开发和表征一种固体的自我微乳化药物输送系统 (FEL@S-SMEDDS) 用于费洛迪平.
- 提高FEL的口服生物可用性和治疗疗效.
- 评估开发的FEL@S-SMEDDS的稳定性和体外释放特征.
主要方法:
- 使用响应表面方法 (RSM) 优化液体自我微乳化药物递送系统 (L-SMEDDS).
- 使用Neusilin® US2对优化的L-SMEDDS进行固化,形成FEL@S-SMEDDS.
- 使用SEM,DSC,XRD和稳定性研究进行全面的表征.
- 实验室药物释放研究和大鼠的药物动力学评估.
主要成果:
- 优化的FEL@L-SMEDDS表现出有利的物理化学特性 (例如,粒子大小为27.80 nm,PDI为0.074).
- 在加速条件下,FEL@S-SMEDDS在6个月内表现出极好的稳定性.
- 超过90%的FEL在30分钟内释放,具有pH独立的特征.
- 与商业FEL药片相比,FEL@S-SMEDDS在老鼠中显示Cmax增加2.73倍,AUC0-24h增加1.46倍.
结论:
- FEL@S-SMEDDS是一种稳定且有效的配方,用于增强FEL口服生物可用性.
- 开发的系统显著改善了FEL的吸收和治疗疗效.
- FEL@S-SMEDDS代表了管理高血压的有希望的策略.
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