The Influence of Fed State Lipolysis Inhibition on the Intraluminal Behaviour and Absorption of Fenofibrate from a Lipid-Based Formulation.
aspiration
drug absorption
fenofibrate
lipid-based formulation
lipolysis
small intestine
Journal
Pharmaceutics
ISSN: 1999-4923
Titre abrégé: Pharmaceutics
Pays: Switzerland
ID NLM: 101534003
Informations de publication
Date de publication:
04 Jan 2022
04 Jan 2022
Historique:
received:
20
11
2021
revised:
23
12
2021
accepted:
28
12
2021
entrez:
21
1
2022
pubmed:
22
1
2022
medline:
22
1
2022
Statut:
epublish
Résumé
The bioavailability of lipophilic drugs may or may not be increased when administered with food due to increased solubilisation in fed state gastrointestinal (GI) fluids. The in vivo interplay between drug solubilisation, lipid phase digestion and drug absorption is complex and remains poorly understood. This study aimed to investigate the role of fed state GI lipolysis on the intraluminal behaviour and absorption of fenofibrate, formulated as the lipid-based formulation Fenogal. Therefore, a crossover study was performed in healthy volunteers using orlistat as lipase inhibitor. Fenofibrate concentrations were determined in the proximal jejunum and linked to simultaneously assessed systemic fenofibric acid concentrations. Inhibition of lipolysis by orlistat resulted in a faster onset of absorption in 4 out of 6 volunteers, reflected by a decrease in systemic T
Identifiants
pubmed: 35057014
pii: pharmaceutics14010119
doi: 10.3390/pharmaceutics14010119
pmc: PMC8781256
pii:
doi:
Types de publication
Journal Article
Langues
eng
Subventions
Organisme : Research Foundation - Flanders
ID : G078417N
Organisme : SMB (Belgium)
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