Screening for Differences in Early Exposure in the Fasted State with in Vitro Methodologies can be Challenging: Experience with the BioGIT System.
Aqueous solution
BioGIT
Chewable tablet
Early exposure
FaSSGF(early)
Nanosized formulation
Journal
Journal of pharmaceutical sciences
ISSN: 1520-6017
Titre abrégé: J Pharm Sci
Pays: United States
ID NLM: 2985195R
Informations de publication
Date de publication:
08 2023
08 2023
Historique:
received:
31
01
2023
revised:
08
03
2023
accepted:
08
03
2023
medline:
17
7
2023
pubmed:
15
3
2023
entrez:
14
3
2023
Statut:
ppublish
Résumé
The Biorelevant Gastrointestinal Transfer (BioGIT) system is a useful screening tool for assessing the impact of dose and/or formulation on early exposure after administration of immediate release or enabling drug products with a glass of water in the fasted state. The objective of this study was to investigate potential limitations. BioGIT experiments were performed with five low solubility active pharmaceutical ingredients with weakly alkaline characteristics: mebendazole (tablet and chewable tablet), Compound E (aqueous solutions, three doses), pazopanib-HCl (Votrient™ tablet, crushed Votrient™ tablet and aqueous suspension), Compound B-diHCl (hard gelatin capsule, three doses) and Compound C (hard gelatin capsule containing nanosized drug and hard gelatin capsule containing micronized drug). For all formulation or dose comparisons the ratio of mean BioGIT AUC
Identifiants
pubmed: 36918113
pii: S0022-3549(23)00101-6
doi: 10.1016/j.xphs.2023.03.004
pii:
doi:
Substances chimiques
Gelatin
9000-70-8
Suspensions
0
Tablets
0
Water
059QF0KO0R
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
2240-2248Informations de copyright
Copyright © 2023 American Pharmacists Association. Published by Elsevier Inc. All rights reserved.
Déclaration de conflit d'intérêts
Declaration of Competing Interest Authors declare no conflict of interest.