在体外脂解过程中的微透析解释了从基于脂的无形固体分散物中增加的印美他辛透
Mikkel Højmark Tønning1, Annette Bauer-Brandl1, Martin Brandl1
1Department of Physics, Chemistry & Pharmacy, University of Southern Denmark, Odense, DK.
概括
基于脂的无形固体分散剂 (基于PL的ASD) 改善药物吸收,特别是在脂解条件下. 微透析采样准确评估了药物释放和配方性能,有助于未来的药物输送设计.
科学领域:
- 制药科学 制药科学
- 生物制药生物制药公司
- 药物输送系统 药物输送系统
背景情况:
- 许多新药具有较差的水溶性,因此需要先进的配方来进行口服.
- 基于脂的无形固体分散 (基于PL的ASD) 通过结合无形固体分散和基于脂的配方的好处,提供了一种有前途的方法.
- 评估基于PL的ASD的生物制药性能是具有挑战性的,因为它与囊和囊等消化部件的复杂相互作用.
研究的目的:
- 通过使用一种新的微透析采样技术,在非脂质和脂质条件下研究基于PL的ASD的生物制药性能.
- 评估脂与药物比对药物释放和透的影响.
- 为了比较微透析采样的疗效与评估基于PL的ASDs的传统方法.
主要方法:
- 在模拟的非脂质和脂质肠道条件下,利用微透析采样来评估印美他辛载荷的PL基ASDs中的药物释放.
- 为了进行比较分析,进行了合溶解/透实验.
- 分析了自由药物度和通过吸收屏障的透.
主要成果:
- 微透析显示,在所有测试的基于PL的ASDs中,在脂溶性条件下,与非脂溶性条件相比,自由药物度更高,透率增加.
- 基于PL的ASDs具有低至中等的脂与药物比率显示显著改善生物制药性能.
- 高脂含量会因为合体被困而影响表现,尽管在高脂水平时脂解效应最为明显.
结论:
- 微透析采样通过精确测量自由药物度,有效地解决了评估基于PL的ASD常规方法的局限性.
- 该研究提供了对基于PL的ASD机制的更深入的理解,突出了脂解和最佳脂与药物比率的积极影响.
- 在模拟的肠道条件下,自由药物度和透性之间的确定的相关性为未来基于PL的ASD设计提供了一个框架.
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