Guiding excipient selection for amorphous solid dispersions by combining an in vitro-in-silico approach – II: Supersaturation and drug release
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Autor:in (Körperschaft)
Publikationsdatum
15.09.2025
Typ der Arbeit
Studiengang
Typ
01A - Beitrag in wissenschaftlicher Zeitschrift
Herausgeber:innen
Herausgeber:in (Körperschaft)
Betreuer:in
Übergeordnetes Werk
International Journal of Pharmaceutics
Themenheft
DOI der Originalpublikation
Link
Reihe / Serie
Reihennummer
Jahrgang / Band
682
Ausgabe / Nummer
Seiten / Dauer
125976
Patentnummer
Verlag / Herausgebende Institution
Elsevier
Verlagsort / Veranstaltungsort
Auflage
Version
Programmiersprache
Abtretungsempfänger:in
Praxispartner:in/Auftraggeber:in
Zusammenfassung
There is a growing industrial need for quick and early screening of amorphous solid dispersions (ASDs). While new technologies are emerging, including in-silico predictions and high-throughput experimentation, a significant gap exists due to a lack of comparative data. The aim of this work was thus to compare experimental data with calculations obtained by the Conductor like Screening Model for Real Solvents (COSMO-RS). A small-scale high throughput method based on solvent casting was used to evaluate the release behavior and precipitation inhibition capacity of ASDs of griseofulvin and nifedipine in the presence of ten pharmaceutically relevant polymers. COSMO-RS was then used to investigate the interaction strength between drug and polymer by means of drug activity coefficients. A stronger interaction would result in better supersaturation maintenance. This was reflected in our results and a good alignment between calculations and experimental performance was observed. COSMO-RS effectively differentiated between polymers with strong precipitation inhibition (PI) functionality and separated those with weaker efficacy for most of the ASDs studied. This pre-selected list of polymers can serve as a foundation for additional studies on all relevant drug development quality attributes, from stability to manufacturing.
Schlagwörter
ASD dissolution, Precipitation inhibition, High-throughput, COSMO-RS, In vitro/in silico alignment
Fachgebiet (DDC)
Veranstaltung
Startdatum der Ausstellung
Enddatum der Ausstellung
Startdatum der Konferenz
Enddatum der Konferenz
Datum der letzten Prüfung
ISBN
ISSN
0378-5173
1873-3476
1873-3476
Sprache
Englisch
Während FHNW Zugehörigkeit erstellt
Ja
Zukunftsfelder FHNW
Publikationsstatus
Veröffentlicht
Begutachtung
Peer-Review der ganzen Publikation
Open Access-Status
Gold
Lizenz
Zitation
Zeneli, E., Bohets, H., Mebenga, F. N., Tistaert, C., Holm, R., & Kuentz, M. (2025). Guiding excipient selection for amorphous solid dispersions by combining an in vitro-in-silico approach – II: Supersaturation and drug release. International Journal of Pharmaceutics, 682, 125976. https://doi.org/10.1016/j.ijpharm.2025.125976