Methacrylate-copolymer Eudragit EPO as a solubility-enabling excipient for anionic drugs: investigation of drug solubility, intestinal permeability, and their interplay

N Fine-Shamir, A Dahan - Molecular Pharmaceutics, 2019 - ACS Publications
The purpose of this work was to investigate the use of the dimethylaminoethyl methacrylate-
copolymer Eudragit EPO (EPO) in oral solubility-enabling formulations for anionic lipophilic …

Dose number as a tool to guide lead optimization for orally bioavailable compounds in drug discovery

WP Wuelfing, A El Marrouni, MP Lipert… - Journal of Medicinal …, 2022 - ACS Publications
Small molecule developability challenges have been well documented over the last two
decades. One of these critical developability parameters is aqueous solubility. In general …

The discriminatory power of the BCS-based biowaiver: a retrospective with focus on essential medicines

MA Hofsäss, JB Dressman - Journal of pharmaceutical sciences, 2019 - Elsevier
This article summarizes historic developments, recent expert opinions, and (currently)
unresolved challenges concerning the Biopharmaceutics Classification System (BCS) …

An ex vivo fermentation screening platform to study drug metabolism by human gut microbiota

E van de Steeg, FHJ Schuren, RS Obach… - Drug Metabolism and …, 2018 - ASPET
Colon microbiota-based drug metabolism has received little attention thus far in the process
of drug development, whereas the role of gut microbiota in clinical safety and efficacy of …

[HTML][HTML] Synthesis, molecular docking analysis and in vitro evaluation of new heterocyclic hybrids of 4-aza-podophyllotoxin as potent cytotoxic agents

HT Nguyen, KT Van, J Braire, PH Thi, TA Nguyen… - RSC …, 2024 - pubs.rsc.org
Two different synthetic approaches to novel heterocyclic hybrid compounds of 4-
azapodophyllotoxin were investigated. The obtained products were characterized by …

Investigating drug absorption from the colon: Single-pass vs. Doluisio approaches to in-situ rat large-intestinal perfusion

I Lozoya-Agullo, M Zur, N Fine-Shamir… - International journal of …, 2017 - Elsevier
Traditionally, the colon is considered a secondary intestinal segment in the drug absorption
process. However, in many cases the role of colonic drug permeability cannot be …

Usefulness of optimized human fecal material in simulating the bacterial degradation of sulindac and sulfinpyrazone in the lower intestine

C Kostantini, S Arora, E Söderlind… - Molecular …, 2022 - ACS Publications
The first aim of this study was to evaluate the usefulness of optimized human fecal material
in simulating sulforeductase activity in the lower intestine by assessing bacterial degradation …

Biowaiver or bioequivalence: ambiguity in sildenafil citrate BCS classification

C Miranda, Z Pérez-Rodríguez… - AAPS …, 2018 - Springer
The aim of the present study is to contribute to the scientific characterization of sildenafil
citrate according to the Biopharmaceutics Classification System, following the World Health …

Biowaiver monographs for immediate-release solid oral dosage forms: Codeine phosphate

A Dahan, O Wolk, M Zur, GL Amidon… - Journal of …, 2014 - Elsevier
The present monograph reviews data relevant to applying the biowaiver procedure for the
approval of immediate-release multisource solid dosage forms containing codeine …

Assessing the impacts on fetal dosimetry of the modelling of the placental transfers of xenobiotics in a pregnancy physiologically based pharmacokinetic model

M Codaccioni, C Brochot - Toxicology and Applied Pharmacology, 2020 - Elsevier
The developmental origin of health and diseases theory supports the critical role of the fetal
exposure to children's health. We developed a physiologically based pharmacokinetic …