Strategies to address low drug solubility in discovery and development

HD Williams, NL Trevaskis, SA Charman… - Pharmacological …, 2013 - Elsevier
Drugs with low water solubility are predisposed to low and variable oral bioavailability and,
therefore, to variability in clinical response. Despite significant efforts to “design in” …

In vivo methods for drug absorption–comparative physiologies, model selection, correlations with in vitro methods (IVIVC), and applications for formulation/API …

E Sjögren, B Abrahamsson, P Augustijns… - European Journal of …, 2014 - Elsevier
This review summarizes the current knowledge on anatomy and physiology of the human
gastrointestinal tract in comparison with that of common laboratory animals (dog, pig, rat and …

Drug nanocrystals: in vivo performances

L Gao, G Liu, J Ma, X Wang, L Zhou, X Li - Journal of controlled release, 2012 - Elsevier
Over the past few decades, there has been a considerable research interest in drug
nanocrystal system as a pharmaceutical approach for poorly soluble drugs. At the beginning …

Application of drug nanocrystal technologies on oral drug delivery of poorly soluble drugs

L Gao, G Liu, J Ma, X Wang, L Zhou, X Li… - Pharmaceutical …, 2013 - Springer
The limited solubility and dissolution rate exhibited by poorly soluble drugs is major
challenges in the pharmaceutical process. Following oral administration, the poorly soluble …

Pharmaceutical excipients—quality, regulatory and biopharmaceutical considerations

DP Elder, M Kuentz, R Holm - European journal of pharmaceutical …, 2016 - Elsevier
Practically all medications contain excipients, which are added for the purpose of production
enhancement, patient acceptability, improving stability, controlling release etc. Typically …

Pharmaceutical drug transport: the issues and the implications that it is essentially carrier-mediated only

DB Kell, PD Dobson, SG Oliver - Drug discovery today, 2011 - Elsevier
All cells necessarily contain tens, if not hundreds, of carriers for nutrients and intermediary
metabolites, and the human genome codes for more than 1000 carriers of various kinds …

Biopharmaceutical aspects and implications of excipient variability in drug product performance

P Zarmpi, T Flanagan, E Meehan, J Mann… - European Journal of …, 2017 - Elsevier
Abstract Implementation of Quality by Design approaches in pharmaceutical industry
requires a sound understanding of the parameters triggering final product variability …

Toward the Establishment of Standardized in Vitro Tests for Lipid-Based Formulations. 2. The Effect of Bile Salt Concentration and Drug Loading on the Performance of Type I, II …

HD Williams, MU Anby, P Sassene… - Molecular …, 2012 - ACS Publications
The LFCS Consortium was established to develop standardized in vitro tests for lipid-based
formulations (LBFs) and to examine the utility of these tests to probe the fundamental …

Interactions between active pharmaceutical ingredients and excipients affecting bioavailability: impact on bioequivalence

A García-Arieta - European Journal of Pharmaceutical Sciences, 2014 - Elsevier
The aim of the present paper is to illustrate the impact that excipients may have on the
bioavailability of drugs and to review existing US-FDA, WHO and EMA regulatory guidelines …

Toward the establishment of standardized in vitro tests for lipid-based formulations, part 3: understanding supersaturation versus precipitation potential during the in …

HD Williams, P Sassene, K Kleberg, M Calderone… - Pharmaceutical …, 2013 - Springer
Purpose Recent studies have shown that digestion of lipid-based formulations (LBFs) can
stimulate both supersaturation and precipitation. The current study has evaluated the drug …