Prediction of human intestinal absorption using micellar liquid chromatography with an aminopropyl stationary phase.

The extent of human intestinal absorption (HIA) for a drug is considered to be an important pharmacokinetic parameter which must be determined for orally administered drugs. Traditional experimental methods relied upon animal testing and are renowned for being time consuming and expensive as well as being ethically unfavourable. As a result, the development of alternative methods to evaluate a drug's pharmacokinetics is crucial.

The effect of the presence of biosurfactant on the permeation of pharmaceutical compounds through silicone membrane.

The permeation of ten model drugs through silicone membrane was analysed to investigate the effect of the presence of a biosurfactant obtained from corn steep liquor. The ten selected pharmaceutical compounds were chosen to include a diverse range of physicochemical properties, such as variable hydrophobicities, pKa's, molecular masses and degrees of ionisation. When compared with compound permeation alone, the additional inclusion of biosurfactant in the donor phase altered the rate and extent of permeation.

Formation of a Bile Salt-Drug Hydrogel to Predict Human Intestinal Absorption.

The unique character of bile salts to self-assemble into hydrogels in the presence of halide salts was exploited in this work to facilitate the prediction of human intestinal absorption (%HIA) for a set of 25 compounds. This was achieved by firstly incorporating each compound separately within the process of gel formation to create a series of gel-drug membranes. Scanning electron microscopy analysis of the freeze-dried samples of the blank bile salt hydrogels and drug-loaded bile salt hydrogels indicated a unique microstructure made of a network of intertwined fibrils.

Incorporating physiologically relevant mobile phases in micellar liquid chromatography for the prediction of human intestinal absorption.

Micellar liquid chromatography is a popular method used in the determination of a compound's lipophilicity. This study describes the use of the obtained micelle-water partition coefficient (log P ) by such a method in the prediction of human intestinal absorption (HIA). As a result of the close resemblance of the novel composition of the micellar mobile phase to that of physiological intestinal fluid, prediction was deemed to be highly successful.

The Use of Bile Salt Micelles for the Prediction of Human Intestinal Absorption.

Human intestinal absorption (HIA) will dictate biopharmaceutical performance through its influence on absorption, distribution, metabolism, and elimination and can vary significantly depending upon the nature of the compound under consideration. In this study, an in vitro assay method is proposed for the prediction of HIA through the measurement of drug solubility in an aqueous phase containing micellar bile salt, namely sodium deoxycholate. A series of twenty compounds, displaying a range of physicochemical properties and known HIA values, were analyzed using UV spectroscopy to determine a solubilization ratio for each compound.

Predicting human intestinal absorption in the presence of bile salt with micellar liquid chromatography.

Understanding intestinal absorption for pharmaceutical compounds is vital to estimate the bioavailability and therefore the in vivo potential of a drug. This study considers the application of micellar liquid chromatography (MLC) to predict passive intestinal absorption with a selection of model compounds. MLC is already known to aid prediction of absorption using simple surfactant systems; however, with this study the focus was on the presence of a more complex, bile salt surfactant, as would be encountered in the in vivo environment.