Investigation of molecular weights and pharmacokinetic characteristics of older and modern small drugs

U Fagerholm - bioRxiv, 2022 - biorxiv.org
Background A shift towards higher molecular weight (MW) of drug candidates is anticipated
to lead to changed pharmacokinetics (PK), including deteriorated absorption. Methods The …

Etoposide encapsulated functionalized mesoporous silica nanoparticles: Synthesis, characterization and effect of functionalization on dissolution kinetics in simulated …

S Saroj, SJ Rajput - Journal of Drug Delivery Science and Technology, 2018 - Elsevier
Abstract Highly ordered hexagonal (MCM-41) mesoporous silica nanoparticles (MSNs)
loaded with etoposide (ETO) were synthesized and functionalized with amino groups (MCM …

Aplicación del Sistema de Clasificación Biofarmacéutica al Cuadro Básico de Medicamentos de Cuba:¿ bioequivalencia in vivo o disolución in vitro?

C Miranda-Pérez de Alejo… - Revista de la …, 2020 - SciELO Espana
El siguiente trabajo tiene como objetivos clasificar los ingredientes farmacéuticos activos
(IFAs) de los sólidos orales de liberación inmediata del Cuadro Básico de Medicamentos de …

Examination of urinary excretion of unchanged drug in humans and preclinical animal models: increasing the predictability of poor metabolism in humans

NO Bamfo, C Hosey-Cojocari, LZ Benet… - Pharmaceutical …, 2021 - Springer
Purpose A dataset of fraction excreted unchanged in the urine (fe) values was developed
and used to evaluate the ability of preclinical animal species to predict high urinary …

Modified nonsink equation for permeability estimation in cell monolayers: Comparison with standard methods

V Mangas-Sanjuan, I Gonzalez-Alvarez… - Molecular …, 2014 - ACS Publications
Cell culture permeability experiments are valuable tools in drug development and candidate
selection, but the monolayer preparation protocols and the calculations procedures can …

An analysis of laboratory variability and thresholds for human in vitro ADME/PK methods

U Fagerholm - BioRxiv, 2022 - biorxiv.org
Introduction Various in vitro methods are used to measure absorption, distribution,
metabolism and excretion/pharmacokinetics (ADME/PK) of candidate drugs and predict and …

Novel hydroxamic acids incorporating 1-((1H-1,2,3-Triazol-4-yl)methyl)-3-hydroxyimino-indolin-2-ones: synthesis, biological evaluation, and SAR analysis

DTM Dung, PT Hai, DT Anh, LTT Huong… - Journal of Chemical …, 2018 - Springer
Abstract A series of seventeen novel hydroxamic acids incorporating 1-((1 H-1, 2, 3-triazol-4-
yl) methyl)-3-hydroxyimino-indolin-2-ones was designed and synthesized. Biological …

Comparing multilabel classification methods for provisional biopharmaceutics class prediction

D Newby, AA Freitas, T Ghafourian - Molecular Pharmaceutics, 2015 - ACS Publications
The biopharmaceutical classification system (BCS) is now well established and utilized for
the development and biowaivers of immediate oral dosage forms. The prediction of BCS …

[HTML][HTML] Using human plasma as an assay medium in Caco-2 studies improves mass balance for lipophilic compounds

K Katneni, T Pham, J Saunders, G Chen, R Patil… - Pharmaceutical …, 2018 - Springer
Purpose To examine the utility of human plasma as an assay medium in Caco-2
permeability studies to overcome poor mass balance and inadequate sink conditions …

Predicting food effects on oral extended-release drug products: a retrospective evaluation

P Zou, J Vaidyanathan, D Tran, K Raines… - The AAPS Journal, 2023 - Springer
Theoretically, the risk of food effects for extended-release (ER) products compared to IR
products may be less because:(1) postprandial physiological changes are usually transient …