消化是从以超和脂质为基础的I型配方中吸收辛纳的关键因素
Felix Paulus1, Annette Bauer-Brandl2, Jef Stappaerts3
1Janssen Pharmaceutica NV, Turnhoutseweg 30, Beerse 2340, Belgium; Department of Physics, Chemistry and Pharmacy, University of Southern Denmark, Campusvej 55, Odense 5230, Denmark.
概括
超和脂基配方 (LBFs) 显著增强肉麻的吸收. 脂质消化,特别是从长链甘油三酸中消化,对于从I型LBF中改善药物输送至关重要.
科学领域:
- 药理学 药理学是指药理学的学科.
- 药物运输 药物运输 药物运输
- 生物制药生物制药公司
背景情况:
- 基于脂质的配方 (LBF) 对于提供难溶性药物至关重要.
- 过的LBF会增加药物负载,但它们对消化的影响尚不清楚.
- I型LBF仅由脂质组成,具有独特的配方挑战.
研究的目的:
- 为了研究脂质消化对大鼠超和I型LBFs中肉素吸收的影响.
- 评估脂质链长度 (MCT与LCT) 和脂酶抑制对药物吸收的影响.
- 评估Soluplus®作为超和LBF中的沉抑制剂的作用.
主要方法:
- 在老鼠中,预先给出了脂酶抑制剂orlistat,以研究脂质消化效应.
- 用Cinnarizine加载的超和非超和I型LBFs与MCT和LCT一起被管理.
- 血度 (AUC和Cmax) 被测量以确定药物吸收.
- 还评估了Soluplus®对沉和吸收的影响.
主要成果:
- 超和LBF的AUC (2.3-3.3倍) 和Cmax (1.4-2.2倍) 与非超和LBF相比显著更高.
- 欧利斯塔特的脂酶抑制显著降低了LCT配方的Cmax和AUC,表明依赖脂解.
- 长链甘油三 (LCT) 一般导致更好的肉素吸收比中链甘油三 (MCT).
结论:
- 脂解在从超和I型脂基配方中吸收药物的过程中起着至关重要的作用.
- 超和是一种有效的策略,可以增强这些配方的药物吸收.
- 脂类辅助剂的选择 (LCT与MCT) 影响药物吸收,而LCT更依赖于脂解.
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