微型TIM肠道液与人类肠道液:它们的成分和溶解能力对不容易溶解的药物的比较
Brecht Goovaerts1, Álvaro López Mármol2, Joachim Brouwers1
1Drug Delivery and Disposition, KU Leuven, Herestraat 49, 3000 Leuven, Belgium.
概括
微型TIM体外系统模拟人体消化过程,用于药物开发. 虽然它看起来有前途,但它的肠液与人体液不同,可能会过度预测药物溶解度.
科学领域:
- 胃肠病学 胃肠病学
- 药品制造 药品制造 药品制造
- 药物运输 药物运输 药物运输
背景情况:
- 微型TIM系统是一个体外平台,旨在模拟人类胃肠道状况.
- 它有助于预测口服药物配方在禁食和食状态下的生物性能.
- 评估微型TIM肠液 (TIF) 的生理相关性对于其在药物开发中的应用至关重要.
研究的目的:
- 分析TIF的组成和溶解能力.
- 将TIF与人类肠道液体 (HIF) 进行比较.
- 调查液体与固体食对TIF特征的影响.
主要方法:
- 对TIF和HIF的组成分析,重点是脂质和胆盐.
- 对TIF和HIF的溶解能力评估.
- 使用液体和固体食条件下的TIF和HIF的比较.
主要成果:
- 在禁食状态下,TIF的脂质较低 (TIF/HIF比率为0.27) 和胆盐较高 (TIF/HIF比率为1.8),而不是HIF.
- 禁食状态TIF通常预测过度HIF的溶解能力.
- 在养状态下,TIF仍然是单相的,胆盐含量较高,导致溶解性增加3.3倍,与HIF相比,溶解性较差的化合物溶解性增加了3.3倍.
结论:
- TIF的成分和溶解能力与HIF不同,特别是在胆盐度方面.
- 微型TIM系统可能会过度预测药物溶解度,特别是在禁食状态下.
- 餐的类型 (液体与固体) 对TIF特征的影响最小.
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