Vitamin C Improves Dasatinib Concentrations Under Hypochlorhydric Conditions of the Simulated Stomach Duodenum Model.
Dissolution
In vitro in vivo correlations
Ionization
Oral drug delivery
Proton pump inhibitors
Journal
Pharmaceutical research
ISSN: 1573-904X
Titre abrégé: Pharm Res
Pays: United States
ID NLM: 8406521
Informations de publication
Date de publication:
Sep 2022
Sep 2022
Historique:
received:
30
04
2022
accepted:
19
06
2022
pubmed:
2
7
2022
medline:
12
10
2022
entrez:
1
7
2022
Statut:
ppublish
Résumé
pH-dependent drug-drug interactions (DDIs) with poorly soluble, weakly basic drugs may lead to clinical implications. Dasatinib is a tyrosine kinase inhibitor with reduced absorption in patients on acid-reducing agents (ARAs). The objective of this study is to investigate the influence of gastric pH on dasatinib supersaturation and determine if vitamin C (L-ascorbic acid) can improve dasatinib concentrations under simulated hypochlorhydric gastric conditions. A dynamic, in vitro, multi-compartment, simulated stomach duodenum (SSD) model mimicking fluid volumes and transfer rates was used to investigate the concentration of BCS class IIb drugs versus time curves. Dasatinib and lamotrigine were explored under normal, fasted, simulated gastric fluids (pH 2) (FaSGF), hypochlorhydric simulated gastric fluids (pH 4.5) (FaSGF Significant supersaturation of dasatinib was observed in the duodenum compartment of the SSD model in FaSGF. A 90% reduction in dasatinib AUC The SSD model serves as a good in vitro tool for assessing the effect of pH-dependent DDIs on bioavailability of weakly basic drugs with solubility/ dissolution limited absorption. Vitamin C provides a promising approach for improving bioavailability of poorly soluble, weakly basic drugs in hypochlorhydric patients.
Identifiants
pubmed: 35778632
doi: 10.1007/s11095-022-03321-y
pii: 10.1007/s11095-022-03321-y
doi:
Substances chimiques
Protein Kinase Inhibitors
0
Reducing Agents
0
Ascorbic Acid
PQ6CK8PD0R
Dasatinib
RBZ1571X5H
Lamotrigine
U3H27498KS
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
2217-2226Informations de copyright
© 2022. The Author(s), under exclusive licence to Springer Science+Business Media, LLC, part of Springer Nature.
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