在Mg-Al层叠加的双氧化物中插入的芬伊托因的可溶性,溶解性和生物利用性的提高
Rehab Anwar Bakr1, Sabna Kotta1,2, Hibah Mubarak Aldawsari1,2
1Department of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah, Saudi Arabia.
Frontiers in pharmacology
|August 19, 2024
概括
层状双氧化物 (LDHs) 成功增强了抗发作药物氨酸 (PHT) 的可溶性和生物可用性. 这种MgAl-PHT-LDH配方为改善药物输送和潜在的较低治疗剂量提供了一个有希望的策略.
科学领域:
- 材料科学 材料科学 材料科学
- 制药科学 制药科学
- 纳米技术 纳米技术
背景情况:
- 层状双氧化物 (LDHs) 是多功能药物递送系统,因为它们的间接容量,稳定性和生物相容性.
- 氨酸 (PHT) 是一种抗发作药物,具有较低的水溶性,限制了其生物可用性 (生物制药分类系统II类药物).
研究的目的:
- 使用层状双氧化物 (LDHs) 提高氨酸 (PHT) 的可溶性,溶解率和口服生物可用性.
- 开发和描述MgAl-PHT-LDH纳米复合材料,以改善PHT输送.
主要方法:
- 芬伊托因 (PHT) 在位地被插入到MgAl-LDH中,形成MgAl-PHT-LDH.
- 使用FTIR,PXRD,DSC和TGA对MgAl-PHT-LDH的表征证实了成功的间隔.
- 评估了Sprague Dawley大鼠的颗粒大小,形态,可溶性,溶解性和口服生物利用性.
主要成果:
- 通过各种分析技术证实了纳米结构MgAl-PHT-LDH的成功形成.
- 间隔剂显著增加了PHT和溶解率 (在0.1N HCl中6.57倍,在酸盐缓冲区pH 6.8中10.5倍).
- 与未经加工的PHT片相比,MgAl-PHT-LDH片显示了改善的PHT溶解和130.15%的相对口服生物利用率.
结论:
- MgAl-PHT-LDH配方有效地提高了芬因 (PHT) 的可溶性,溶解性和口服生物利用性.
- 这种纳米结构的LDH方法提供了一种可行的策略,用于改善像PHT这样的溶解不良药物的输送.
- 开发的MgAl-PHT-LDH药片需要进一步的临床评估,以减少PHT剂量有效控制发作.
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