Impact of gastric pH variations on the release of amorphous solid dispersion formulations containing a weakly basic drug and enteric polymers

HT Nguyen, T Van Duong, LS Taylor - Molecular Pharmaceutics, 2023 - ACS Publications
Enteric polymers are widely used in amorphous solid dispersion (ASD) formulations. The
aim of the current study was to explore ASD failure mechanisms across a wide range of pH …

[HTML][HTML] Enteric coating of tablets containing an amorphous solid dispersion of an enteric polymer and a weakly basic drug: a strategy to enhance in vitro release

HT Nguyen, T Van Duong, LS Taylor - International Journal of …, 2023 - Elsevier
Recent work has highlighted that amorphous solid dispersions (ASDs) containing
delamanid (DLM) and an enteric polymer, hypromellose phthalate (HPMCP), appear to be …

Insights into the release mechanisms of ITZ: HPMCAS amorphous solid dispersions: the role of drug-rich colloids

PD Nunes, JF Pinto, J Henriques… - Molecular …, 2021 - ACS Publications
Understanding the dissolution mechanisms of amorphous solid dispersions (ASDs) and
being able to link enhanced drug exposure with process parameters are key when …

Dissolution behavior of weakly basic pharmaceuticals from amorphous dispersions stabilized by a poly (dimethylaminoethyl methacrylate) copolymer

DS Frank, P Prasad, L Iuzzolino… - Molecular …, 2022 - ACS Publications
Amorphous solid dispersions (ASDs) are a well-documented formulation approach to
improve the rate and extent of dissolution for hydrophobic pharmaceuticals. However …

Amorphous solid dispersions of weak bases with pH-dependent soluble polymers to overcome limited bioavailability due to gastric pH variability–an in-vitro approach

M Monschke, KG Wagner - International Journal of Pharmaceutics, 2019 - Elsevier
Several drugs are pH-dependent soluble weak bases with a poor solubility in the intestinal
pH range. Additionally a variable gastric pH, which is a common issue in the population …

Improved dissolution of an enteric polymer and its amorphous solid dispersions by polymer salt formation

Q Qi, LS Taylor - International Journal of Pharmaceutics, 2022 - Elsevier
Weakly acidic polymers, historically used as enteric coatings, are increasingly being
employed in solubility-enhancing amorphous solid dispersion (ASD) formulations. However …

Patterns of drug release as a function of drug loading from amorphous solid dispersions: A comparison of five different polymers.

S Saboo, DE Moseson, US Kestur, LS Taylor - European Journal of …, 2020 - Elsevier
To reduce the pill burden associated with amorphous solid dispersions (ASDs), which arises
from the large quantity of polymer used in the formulation, it is of interest to understand the …

Formulating Amorphous solid dispersions: Impact of inorganic salts on drug release from tablets containing itraconazole-HPMC extrudate

R Takano, R Maurer, L Jacob, F Stowasser… - Molecular …, 2019 - ACS Publications
Amorphous solid dispersions (ASD) are increasingly used to improve the oral bioavailability
of poorly water-soluble compounds. However, hydrophilic polymers in ASD have high water …

In Vitro and In Vivo Behaviors of KinetiSol and Spray-Dried Amorphous Solid Dispersions of a Weakly Basic Drug and Ionic Polymer†

SV Jermain, MB Lowinger, DJ Ellenberger… - Molecular …, 2020 - ACS Publications
Oral delivery of poorly water-soluble, weakly basic drugs may be problematic based on the
drugs' intrinsic properties. Many drugs in this subset have overcome barriers to delivery …

Amorphous solid dispersions: Utilization and challenges in preclinical drug development within AstraZeneca

AB Anane-Adjei, E Jacobs, SC Nash, S Askin… - International Journal of …, 2022 - Elsevier
The poor aqueous solubility of many active pharmaceutical ingredients (APIs) dominates
much of the early drug development portfolio and poses a major challenge in …