University of Basel, Division of Pharmaceutical Technology, Basel, Switzerland.
Drug Dev Ind Pharm. 2012 Oct;38(10):1262-9. doi: 10.3109/03639045.2011.645834. Epub 2011 Dec 30.
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.
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.
Using pH-stat equipment, the NaOH consumption was determined in an in vitro lipolysis assay.
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.
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.
脂质给药系统被广泛用于提高胃肠道中难溶性药物的溶解度。口服后，脂质系统在胃和肠道中经历消化。脂肪分解是油/水界面处的一个复杂过程，受许多因素影响。
研究脂质给药系统中常用的九种赋形剂的消化率。此外，我们引入了一个数学模型来描述体外脂肪分解动力学。使用参考赋形剂中链甘油三酯定义相对脂肪分解半衰期。
使用 pH -stat 设备，在体外脂肪分解测定中确定 NaOH 的消耗。
我们确定了两类赋形剂。一些添加剂部分水解，而其他赋形剂则完全分解。对于后者，简化的数学模型为初始脂肪分解动力学提供了良好的初步近似。
赋形剂的消化特性对于脂质给药系统的开发很重要。所应用的动力学模型和相对脂肪分解半衰期的概念似乎是比较体外脂肪分解结果的有前途的工具。
