Category: Advances in Bioanalytics and Biomarkers

1345-A - Bile salts: The intestinal absorption foretellers

Monday, February 5, 2018
2:00 PM - 3:00 PM

Formulation of the newly released pharmaceutical compounds in the form of orally administered drugs has become abundant due to the convenience of oral administration route. Because of this reason it is important to determine the physicochemical properties of new drug entities (NDE) and determine whether they would be convenient for oral formulation or not. Some drugs can be considered as poor candidates, if having poor aqueous solubility and poor oral bioavailability, and be terminated before reaching final clinical stages of development, otherwise it can cause massive financial losses to pharmaceutical industry. As a result, a growing interest has been given over the last 30 years to predicting biopharmaceutical characteristics of new drug entities (NDE) such as aqueous solubility and intestinal permeability, so there has been a growing number of methods developed for predicting these characteristics, these developed methods included both experimental and mathematical models. Since most of these methods are cost effective and time saving therefore, what would greatly distinguish a good method from another is how well it predicts the biopharmaceutical property under study. Among the most important biopharmaceutical properties which are very important to be studied is drug intestinal permeability. This work describes a number of different methods developed for the prediction of human intestinal absorption. The first one is micellar liquid chromatography using biosurfactants naturally occurring in the body, where the biosurfactants used in this method were different types of bile salts which gave models of high prediction power especially with NaDC and NaTDC, as their developed models gave R2 of prediction of 75 and 91%, respectively. The second developed method was based on using the solubilizing capacity of bile salts as surfactants on the drug under study. Also, this method had a high predictive power of 82%. The last method is a permeation method which used a hydrogel made up of the biosurfactant at a certain concentration with a saturated dose of the drug under study. The permeation method has been conducted using two types of diffusion cells; flow through and Franz diffusion cells to measure the permeation of the studied drug across the hydrogel. The obtained mathematical models had a high predictability of 80% for both techniques. Overall, all the obtained mathematical models from the developed methods in this work had high prediction power which make them valuable methods for prediction of human intestinal absorption.

Dina S. Abdelsamei

Ph.D. Student at the School of Applied Sciences, University of Huddersfield
School of Applied Sciences, University of Huddersfield
Huddersfield, England, United Kingdom

Dina Abdelsamei had her bachelor degree in Pharmacy in 2009 from Ain Shams University then completed her Masters degree in Analytical Chemistry from Cairo University in 2013. Now she is about to finish her PhD as a member of Dr Waters group for finding alternatives to animal testing at Huddersfield University. She worked as a teaching assistant then as an assistant lecturer of Analytical Chemistry at Future University. She produced high quality research that was published in a number of reputed peer reviewed journals and presented her work in six conferences. Dina’s work is focused on developing models for prediction of human intestinal absorption through in vitro-in vivo correlation studies which has economic impact in the pharmaceutical industry field. She developed prediction models from MLC, solubilization and permeation studies where the obtained in vitro data correlated well with the in vivo absorption data and resulted in two recently published papers.