定制药物释放从长效避孕药levonorgestrel子宫内系统
Suraj Fanse1, Quanying Bao1, Yuan Zou2
1University of Connecticut, School of Pharmacy, Storrs, CT 06269, USA.
概括
由于聚二甲基 (PDMS) 变种和添加剂,Levonorgestrel 子宫内系统 (LNG-IUSs) 的配方是复杂的. 这项研究阐明了药物释放机制,指导合理的辅助剂选择以提高LNG-IUS性能.
科学领域:
- 聚合物科学和药物输送
- 材料科学 材料科学 材料科学
- 制药技术 制药技术 制药技术
背景情况:
- 由于多种多基甲基 (PDMS) 变种,复杂的添加剂组合以及对药物释放的不完全理解,Levonorgestrel子宫内系统 (LNG-IUSs) 的配方具有挑战性.
- 聚合物及其添加剂的复杂性质需要对它们对LNG-IUS性能的影响进行更深入的研究.
研究的目的:
- 调查辅助剂对LNG-IUS配方属性和体外性能的影响.
- 阐明控制这些系统中levonorgestrel释放的药物释放机制.
- 建立材料-属性-性能关系,以改善产品开发和监管评估.
主要方法:
- 制备LNG-IUS,包括各种添加剂和填充剂.
- 在12个月内进行体外药物释放测试.
- 评估配方属性 (结晶动力学,粘度,微观结构,机械性能) 和药物辅助剂相互作用.
- 释放动力学的建模和与药物物理化学性质 (溶解度,Log P) 的相关性.
主要成果:
- 添加剂显著改变了PDMS结晶,粘度和微观结构,影响了药物释放.
- 增加的矩阵疏水性和阻碍PDMS结晶促进了莱沃诺格斯特雷尔 (LNG) 溶解和透.
- PDMS化学替代和分子量是影响体外性能的关键聚合物属性.
- 第一阶释放速率常数与药物溶解度和Log P有很强的相关性,证实了基于分离和扩散的释放机制.
结论:
- 本研究提供了对液化天然气-IUSs中的材料-属性-性能关系的机制性理解.
- 建立了基于证据的方法,用于合理选择辅助剂和定制药物释放配置文件.
- 这些发现支持开发创新和通用LNG-IUS产品及其监管评估.
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