Bile and excipient interactions directing drug pharmacokinetics in rats
Zitieren Sie bitte immer diese URN: urn:nbn:de:bvb:20-opus-296969
- Bile solubilization plays a major role in the absorption of poorly water-soluble drugs. Excipients used in oral drug formulations impact bile-colloidal properties and their molecular interactions. Polymer-induced changes of bile colloids, e.g., by Eudragit E, reduced the flux of the bile interacting drug Perphenazine whereas bile non-interacting Metoprolol was not impacted. This study corroborates these in vitro findings in rats. Eudragit E significantly reduced systemic availability of Perphenazine but not Metoprolol compared to the oralBile solubilization plays a major role in the absorption of poorly water-soluble drugs. Excipients used in oral drug formulations impact bile-colloidal properties and their molecular interactions. Polymer-induced changes of bile colloids, e.g., by Eudragit E, reduced the flux of the bile interacting drug Perphenazine whereas bile non-interacting Metoprolol was not impacted. This study corroborates these in vitro findings in rats. Eudragit E significantly reduced systemic availability of Perphenazine but not Metoprolol compared to the oral administrations without polymer. This study confirms the necessity to carefully select polymers for bile interacting drugs whereas non-bile interacting drugs are more robust in terms of excipient choice for formulation. The perspective of bile interaction may introduce interesting biopharmaceutical leverage for better performing oral formulations of tomorrow.…
Autor(en): | Jonas SchlauersbachORCiD, Simon Hanio, Martina Raschig, Bettina Lenz, Oliver Scherf-Cavel, Lorenz Meinel |
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URN: | urn:nbn:de:bvb:20-opus-296969 |
Dokumentart: | Artikel / Aufsatz in einer Zeitschrift |
Institute der Universität: | Fakultät für Chemie und Pharmazie / Institut für Pharmazie und Lebensmittelchemie |
Sprache der Veröffentlichung: | Englisch |
Titel des übergeordneten Werkes / der Zeitschrift (Englisch): | European Journal of Pharmaceutics and Biopharmaceutics |
Erscheinungsjahr: | 2022 |
Auflage: | accepted version |
Band / Jahrgang: | 178 |
Seitenangabe: | 65-68 |
Originalveröffentlichung / Quelle: | European Journal of Pharmaceutics and Biopharmaceutics (2022) 178, 65-68. https://doi.org/10.1016/j.ejpb.2022.07.016 |
DOI: | https://doi.org/10.1016/j.ejpb.2022.07.016 |
Sonstige beteiligte Institutionen: | Helmholtz Institute for RNA-based Infection Biology (HIRI), Josef-Schneider-Straße 2/D15, DE-9708 Wuerzburg, Germany |
Allgemeine fachliche Zuordnung (DDC-Klassifikation): | 5 Naturwissenschaften und Mathematik / 54 Chemie / 540 Chemie und zugeordnete Wissenschaften |
Freie Schlagwort(e): | bile; excipient; in vitro-in vivo correlation; pharmacokinetics; rat study |
Datum der Freischaltung: | 17.12.2022 |
Embargo-Datum: | 06.08.2023 |
Lizenz (Deutsch): | CC BY-NC-ND: Creative-Commons-Lizenz: Namensnennung, Nicht kommerziell, Keine Bearbeitungen 4.0 International |