Using PBPK to Establish In Vitro-In Vivo Relationship for Budesonide Delayed Release Oral Drug Product

Authors: Amaral Silva D, Zhou H, Wu F, Fotaki N, Pereira GG, Lukacova V
Conference: AAPS
Keywords: AAPS2024, gastroplus, In vitro–in vivo relationship (IVIVR), oral drug absorption, pbbm, PBPK
Software: GastroPlus®
Division: PBPK

Purpose

  • Budesonide is a corticosteroid used to treat inflammatory bowel diseases (IBD) (1).
  • Budesonide undergoes extensive intestinal metabolism contributing to its low oral bioavailability (~9%) (2).
  • Controlled-release formulations have been developed to target a drug release at pertinent GI segments.
  • ENTOCORT® is a multi-particulate delayed-release (DR) drug product designed to release budesonide to the terminal ileum segment.
  • Developing DR formulations can be challenging due to the numerous layers of complexity related to their in vivo behavior, rendering it difficult to predict the pharmacokinetic of drugs administered as DR (3).
  • Modeling and simulation can support the development and regulatory assessment of DR formulations

By Daniela Amaral Silva, Haiying Zhou, Fang Wu, Nikoletta Fotaki, Gabriela Garrastazu Pereira, Viera Lukacova

American Association of Pharmaceutical Scientists (AAPS) PharmSci 360, October 20-23, 2024, Salt Lake City, Utah