第三代固体分散通过溶解增强了resveratrol的口服生物可用性
Hugo Almeida1,2,3,4, Bárbara Ferreira1,3,4, Carlos Fernandes-Lopes2
1ICBAS-Instituto de Ciências Biomédicas Abel Salazar, Universidade do Porto,Rua Jorge de Viterbo Ferreira, 228, 4050-313 Porto, Portugal.
ACS pharmacology & translational science
|March 14, 2024
概括
这项研究开发了一种新的resveratrol固体分散 (SD) 使用冷凍化,显著提高其可溶性,溶解性和口服生物利用性. 新配方改善了复星的吸收,可能增加其治疗效益.
科学领域:
- 制药科学 制药科学
- 药物输送系统 药物输送系统
- 生物制药生物制药公司
背景情况:
- 复星 (RES) 具有较低的溶解性和生物可用性,限制了其治疗功效.
- 固体分散 (SDs) 是一种有前途的策略,可以提高 RES.等难溶药物的口服生物可用性.
研究的目的:
- 开发第三代RES固体分散 (SD),使用冷化来提高溶解性,溶解性和口服生物利用性.
- 在SD中描述固态特性和无形转换的RES.
主要方法:
- 使用Eudragit EPO (水友性载体) 和Gelucire 44/14 (表面活性剂) 通过冷化制备第三代RESSD.
- 使用DSC,SEM,FTIR,PLM,XRPD和粒子大小分析进行固态表征.
- 在体外溶解性,溶解性和肠道透性研究 (Caco-2模型).
- 在Wistar大鼠体内口服生物可用性评估.
主要成果:
- 与纯 RES 和物理混合物相比,第三代 SD 显示了显著增加的 RES 溶解度 (8-12 倍) 和溶解率 (pH 6.8 时 5 倍).
- 在Caco-2模型中观察到增强的体外肠道透性 (增加了2.4倍).
- 在体内研究表明,与第二代SD相比,RES口服生物利用率增加了3倍.
结论:
- 软化第三代RES SD有效地提高了溶解性,溶解性和口服生物可用性.
- 增强的生物利用性归因于提高溶解性,溶解性,并可能减少RES代谢和P-gp流量.
- 这种配方策略提供了一种可行的方法,以最大限度地提高复星的治疗潜力.
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