越多越好?─维生素E TPGS作为利托纳维尔/PVPVA无形固体分散物的释放增强剂
Ineke Fahrig1, Stefanie Walter2, Samuel Kyeremateng2
1Department of Biochemical and Chemical Engineering, Laboratory of Thermodynamics, TU Dortmund University, Emil-Figge-Street 70, Dortmund D-44227, Germany.
Molecular pharmaceutics
|August 15, 2025
概括
将维生素ETPGS表面活性剂添加到无形固体分散剂 (ASD) 中,可以改善利托纳维尔 (RIT) 的药物释放,药物负载高达30%的重量. 然而,较高的负载仍然会导致由于相位分离而导致释放故障.
科学领域:
- 制药科学 制药科学
- 材料科学 材料科学 材料科学
- 药物运输 药物运输 药物运输
背景情况:
- 无形固体分散 (ASDs) 增强水溶性较差的药物的溶性.
- 在自闭症患者中,高剂量药物负载会导致相分离和药物释放失败.
- 里托纳维尔 (RIT) 和聚乙烯基合乙烯酸 (PVPVA) 是常见的ASD成分.
研究的目的:
- 研究维生素ETPGS在减轻高药负载ASD的相分离中的作用.
- 确定维生素ETPGS的最佳度,以增强药物释放.
- 了解维生素ETPGS在稳定ASD中的机制.
主要方法:
- 开发了一种改进的采样协议,以区分溶解和纳米滴释放的ASD组件.
- 配制的ASDs具有不同度的里托纳维尔和维生素ETPGS.
- 分析了药物释放概况和相分离行为.
主要成果:
- 3重%的维生素E TPGS增强了药物释放,达到30重%的药物负载,而没有表面活性剂则是25重%.
- 维生素ETPGS在相隔过程中稳定了RIT丰富的离散域.
- 在40重%的药物负载下,即使是10重%的维生素ETPGS也无法确保完全释放API,这表明稳定机制的故障.
结论:
- 维生素ETPGS通过稳定相隔域,有效地增强高药负载ASD的药物释放.
- 维生素ETPGS的有效性有一个上限,超出这个上限,相分离行为发生变化,导致释放失败.
- 了解这些复杂的释放机制对于设计稳定有效的ASD配方至关重要.
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