Bile and excipient interactions directing drug pharmacokinetics in rats

Please always quote using this 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.show moreshow less
Metadaten
Author: Jonas SchlauersbachORCiD, Simon Hanio, Martina Raschig, Bettina Lenz, Oliver Scherf-Cavel, Lorenz Meinel
URN:urn:nbn:de:bvb:20-opus-296969
Document Type:Journal article
Faculties:Fakultät für Chemie und Pharmazie / Institut für Pharmazie und Lebensmittelchemie
Language:English
Parent Title (English):European Journal of Pharmaceutics and Biopharmaceutics
Year of Completion:2022
Edition:accepted version
Volume:178
Pagenumber:65-68
Source: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
Dewey Decimal Classification:5 Naturwissenschaften und Mathematik / 54 Chemie / 540 Chemie und zugeordnete Wissenschaften
Tag:bile; excipient; in vitro-in vivo correlation; pharmacokinetics; rat study
Release Date:2022/12/17
Embargo Date:2023/08/06
Licence (German):License LogoCC BY-NC-ND: Creative-Commons-Lizenz: Namensnennung, Nicht kommerziell, Keine Bearbeitungen 4.0 International