In vitro digestion kinetics of excipients for lipid-based drug delivery and introduction of a relative lipolysis half life
In vitro digestion kinetics of excipients for lipid-based drug delivery and introduction of a relative lipolysis half life
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DOI：
10.3109/03639045.2011.645834
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发表时间：
2012-10-01
影响因子：
3.4
通讯作者：
Kuentz, Martin
中科院分区：
文献类型：
--
作者：
Arnold, Yvonne E.;Imanidis, Georgios;Kuentz, Martin
背景资料：基于脂质的药物递送系统被广泛用于增强水溶性差的药物在胃肠道中的溶解度。口服摄入后，脂质系统在胃和肠中进行消化。脂解在这里是一个复杂的过程中，在油/水界面，受众多factors.Purpose的影响：研究的消化率的9种赋形剂，经常使用的脂质为基础的药物输送系统。此外，我们引入了一个数学模型来描述体外脂解动力学。一个相对的脂解半衰期被定义为使用参考赋形剂中链triglycerides.Methods：使用pH-stat设备，NaOH消耗量测定在体外脂解assay.Results：我们确定了两类赋形剂。一些添加剂部分水解，而其他赋形剂显示完全脂解。对于后一类，一个简化的数学模型提供了一个很好的第一近似初始脂解kinetic.Conclusions：辅料的消化特性是重要的脂质为基础的输送系统的发展。所应用的动力学模型和相对脂解半衰期的概念似乎是比较体外脂解结果的有前途的工具。
Background: Lipid-based drug delivery systems are widely used for enhancing the solubility of poorly water soluble drugs in the gastro-intestinal tract. Following oral intake, lipid systems undergo digestion in the stomach as well as the intestine. Lipolysis is here a complex process at the oil/water interface, influenced by numerous factors.Purpose: To study the digestibility of nine excipients often used in lipid-based drug delivery systems. In addition, we introduced a mathematical model to describe in vitro lipolysis kinetics. A relative lipolysis half life was defined using the reference excipient medium-chain triglycerides.Methods: Using pH-stat equipment, the NaOH consumption was determined in an in vitro lipolysis assay.Results: We identified two classes of excipients. Some additives were partially hydrolysed, whereas other excipients displayed complete lipolysis. For the latter class, a simplified mathematical model provided a good first approximation of initial lipolysis kinetics.Conclusions: Digestion characterization of excipients is important for the development of lipid-based delivery systems. The applied kinetic model and the concept of a relative lipolysis half life seemed to be promising tools for comparing in vitro lipolysis results.