固体分散系统用于增强溶解水溶性较差的坎德沙坦西莱克塞特:体外评估和模拟的药理动力学研究
Israa Saad Mustafa Ali1, Uday Aziz Sajad1,2, Bazigha K Abdul Rasool3
1Pharmaceutics Department, College of Pharmacy, University of Basrah, Basrah, Iraq.
PloS one
|June 6, 2024
概括
这项研究开发了固体分散系统 (SDSs),以增强candesartan cilexetil (CC) 的溶解性和溶解性. 优化的SDS显著改善了CCCC的性能.
科学领域:
- 制药科学 制药科学
- 药物输送系统 药物输送系统
- 材料科学 材料科学 材料科学
背景情况:
- 坎德沙坦西莱克塞特 (CC) 是一种抗高血压药物,具有较差的水溶性和较低的口服生物利用性.
- CC是P-glycoprotein (P-gp) 的基质,导致肠道排泄.
- 提高CC的溶解和生物可用性对于有效的高血压管理至关重要.
研究的目的:
- 通过使用固体分散系统 (SDS) 来增强德沙坦基莱克塞提尔 (CC) 的体外溶解.
- 调查SDS的潜力,以改善CC.的口服生物可用性.
- 描述优化的固体分散系统及其药物聚合物相互作用.
主要方法:
- 使用聚乙烯 (PVP) 和尤德拉吉特E100 (EE100) 制备了固体分散剂 (SDS).
- 在各种介质中进行和可溶性和溶解率研究.
- 优化的系统 (SE-EE5) 使用DSC,XRD,FTIR,FESEM,DLS,TSEM和IVIVC卷积进行了表征.
主要成果:
- 通过SE-EE5 SDS (1:5药物对EE100的比率) 实现了CC可溶性增加的27,037倍.
- 可溶性增强归因于晶体CC的转化为其无形形式和pH5以下的纳米粒子形成.
- 仪器分析证实了良好的药物聚合物兼容性,稳定性研究表明该系统在三个月内保持稳定.
结论:
- 使用Eudragit E100的固体分散技术有效地提高了可溶性和溶解性差的可溶性药物,如CC.
- 开发的SDS显示了显著的潜力,以改善candesartan cilexetil的口服生物利用性.
- 这种方法为制定具有挑战性的疏水性药物提供了一个有希望的策略.
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