Towards a better understanding of solid dispersions in aqueous environment by a fluorescence quenching approach

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Autor:innen
Autor:in (Körperschaft)
Publikationsdatum
25.10.2018
Typ der Arbeit
Studiengang
Typ
01A - Beitrag in wissenschaftlicher Zeitschrift
Herausgeber:innen
Herausgeber:in (Körperschaft)
Betreuer:in
Übergeordnetes Werk
International Journal of Pharmaceutics
Themenheft
Link
Reihe / Serie
Reihennummer
Jahrgang / Band
550
Ausgabe / Nummer
1-2
Seiten / Dauer
Patentnummer
Verlag / Herausgebende Institution
Elsevier
Verlagsort / Veranstaltungsort
Auflage
Version
Programmiersprache
Abtretungsempfänger:in
Praxispartner:in/Auftraggeber:in
Zusammenfassung
Solid dispersions (SDs) represent an important formulation technique to achieve supersaturation in gastro-intestinal fluids and to enhance absorption of poorly water-soluble drugs. Extensive research was leading to a rather good understanding of SDs in the dry state, whereas the complex interactions in aqueous medium are still challenging to analyze. This paper introduces a fluorescence quenching approach together with size-exclusion chromatography to study drug and polymer interactions that emerge from SDs release testing in aqueous colloidal phase. Celecoxib was used as a model drug as it is poorly water-soluble and also exhibits native fluorescence so that quenching experiments were enabled. Different pharmaceutical polymers were evaluated by the (modified) Stern-Volmer model, which was complemented by further bulk analytics. Drug accessibility by the quencher and its affinity to celecoxib were studied in physical mixtures as well as with in SDs. The obtained differences enabled important molecular insights into the different formulations. Knowledge of relevant drug-polymer interactions and the amount of drug embedded into polymer aggregates in the aqueous phase is of high relevance for understanding of SD performance. The novel fluorescence quenching approach is highly promising for future research and it can provide guidance in early formulation development.
Schlagwörter
Poorly soluble drug, solid dispersion, amorphous formulation, fluorescence quenching, surface characterization, drug-polymer interaction
Fachgebiet (DDC)
631 - Technologie, Ausrüstung, Materialien
Projekt
Veranstaltung
Startdatum der Ausstellung
Enddatum der Ausstellung
Startdatum der Konferenz
Enddatum der Konferenz
Datum der letzten Prüfung
ISBN
ISSN
0378-5173
1873-3476
Sprache
Englisch
Während FHNW Zugehörigkeit erstellt
Ja
Publikationsstatus
Veröffentlicht
Begutachtung
Peer-Review der ganzen Publikation
Open Access-Status
Lizenz
Zitation
JANKOVIC, Sandra, Martin KUENTZ und Simone ALEANDRI, 2018. Towards a better understanding of solid dispersions in aqueous environment by a fluorescence quenching approach. International Journal of Pharmaceutics. 25 Oktober 2018. Bd. 550, Nr. 1-2. DOI doi.org/10.1016/j.ijpharm.2018.08.029. Verfügbar unter: https://doi.org/10.26041/fhnw-1777