Ljusberg-Wahren Helena, Seier Nielsen Flemming, Brogård Mattias, Troedsson Emma, Müllertz Anette
Camurus AB, Ideon, Gamma 2, Sölvegatan 41, SE-223 70 Lund, Sweden.
Int J Pharm. 2005 Jul 25;298(2):328-32. doi: 10.1016/j.ijpharm.2005.02.038.
The present work introduces a simple and robust in vitro method for enzymatic characterisation of surface properties of lipid dispersions in aqueous media. The initial lipolysis rate in biorelevant media, using pancreatic lipase and a self-microemulsifying formulation (SMEDDS) containing digestible lipids as substrate, was determined. The impact of incorporating two sparingly water soluble model drugs, probucol and halofantrine, into the SMEDDS was studied. It was found that both model drugs reduced the initial rate of lipolysis compared with the vehicle, probucol having a larger effect than halofantrine. The reduction of initial lipolysis rate indicates that probucol and halofantrine are bound in the water/emulsion interface limiting the substrate availability.
本研究介绍了一种简单且可靠的体外方法，用于酶促表征水性介质中脂质分散体的表面性质。测定了在生物相关介质中，以胰脂肪酶和含有可消化脂质的自微乳化制剂（SMEDDS）为底物时的初始脂解速率。研究了将两种水溶性较差的模型药物普罗布考和卤泛群加入SMEDDS中的影响。结果发现，与载体相比，两种模型药物均降低了初始脂解速率，普罗布考的作用比卤泛群更大。初始脂解速率的降低表明，普罗布考和卤泛群结合在水/乳液界面，限制了底物的可及性。
