Non-digestible lipid-based liquid crystalline formulations, even in dispersed submicron form,provide dramatically sustained plasma concentrations for poorly water soluble drugs

摘要

The ability of non-digestible mesophase forminglipids to improve oral bioavailability of poorly watersoluble drugs has been further investigated. The oralabsorption behaviour of cinnarizine after administration innon-digestible phytantriol as a lipid vehicle or digestibleglyceryl monooleate, in both bulk and dispersed particleforms, was investigated. Phytantriol showed dramaticallyextended time of absorption (>48 hrs) for both the bulkand non-dispersed forms, and was shown to beattributable to extended residence >24 hrs in the stomach,even for the dispersed particles. GMO was poorlyretained in the stomach, likely due to digestion ordegradation, leading to relative short duration ofabsorption. This study is the first to indicate that dispersedliquid crystalline particles may have application as aversatile sustained release delivery system for poorlysoluble drugs.