In-situ intestinal rat perfusions for human Fabs prediction and BCS permeability class determination: Investigation of the single-pass vs. the Doluisio experimental …

I Lozoya-Agullo, M Zur, O Wolk, A Beig… - International journal of …, 2015 - Elsevier
Intestinal drug permeability has been recognized as a critical determinant of the fraction
dose absorbed, with direct influence on bioavailability, bioequivalence and biowaiver. The …

[HTML][HTML] Reliable prediction of Caco-2 permeability by supervised recursive machine learning approaches

G Falcón-Cano, C Molina, MÁ Cabrera-Pérez - Pharmaceutics, 2022 - mdpi.com
The heterogeneity of the Caco-2 cell line and differences in experimental protocols for
permeability assessment using this cell-based method have resulted in the high variability of …

Purely in silico BCS classification: Science based quality standards for the world's drugs

A Dahan, O Wolk, YH Kim… - Molecular …, 2013 - ACS Publications
BCS classification is a vital tool in the development of both generic and innovative drug
products. The purpose of this work was to provisionally classify the world's top selling oral …

Advantageous solubility-permeability interplay when using amorphous solid dispersion (ASD) formulation for the BCS class IV P-gp substrate rifaximin: simultaneous …

A Beig, N Fine-Shamir, D Lindley, JM Miller, A Dahan - The AAPS journal, 2017 - Springer
Rifaximin is a BCS class IV (low-solubility, low-permeability) drug and also a P-gp substrate.
The aims of this work were to assess the efficiency of different rifaximin amorphous solid …

[HTML][HTML] Hydrotropic solubilization of lipophilic drugs for oral delivery: the effects of urea and nicotinamide on carbamazepine solubility–permeability interplay

A Beig, D Lindley, JM Miller, R Agbaria… - Frontiers in …, 2016 - frontiersin.org
Hydrotropy refers to increasing the water solubility of otherwise poorly soluble compound by
the presence of small organic molecules. While it can certainly increase the apparent …

Solubility determination of active pharmaceutical ingredients which have been recently added to the list of essential medicines in the context of the biopharmaceutics …

GF Plöger, MA Hofsäss, JB Dressman - Journal of Pharmaceutical Sciences, 2018 - Elsevier
Since the publication of Lindenberg et al., which classified orally administered active
pharmaceutical ingredients (APIs) on the 2004 Essential Medicines List (EML) of the World …

The low/high BCS permeability class boundary: physicochemical comparison of metoprolol and labetalol

M Zur, M Gasparini, O Wolk, GL Amidon… - Molecular …, 2014 - ACS Publications
Although recognized as overly conservative, metoprolol is currently the common low/high
BCS permeability class boundary reference compound, while labetalol was suggested as a …

Provisional in-silico biopharmaceutics classification (BCS) to guide oral drug product development

O Wolk, R Agbaria, A Dahan - Drug design, development and …, 2014 - Taylor & Francis
The main objective of this work was to investigate in-silico predictions of physicochemical
properties, in order to guide oral drug development by provisional biopharmaceutics …

[HTML][HTML] Processing of polyvinyl acetate phthalate in hot-melt extrusion—preparation of amorphous solid dispersions

M Monschke, K Kayser, KG Wagner - Pharmaceutics, 2020 - mdpi.com
The preparation of amorphous solid dispersions (ASDs) is a suitable approach to overcome
solubility-limited absorption of poorly soluble drugs. In particular, pH-dependent soluble …

Multitasking models for quantitative structure–biological effect relationships: current status and future perspectives to speed up drug discovery

A Speck-Planche, MNDS Cordeiro - Expert opinion on drug …, 2015 - Taylor & Francis
Introduction: Drug discovery is the process of designing new candidate medications for the
treatment of diseases. Over many years, drugs have been identified serendipitously …