Orlistat disposition in the human jejunum and the effect of lipolysis inhibition on bile salt concentrations and composition.
Bile salts
Fed state
Fenofibrate
Intestinal drug absorption
Jejunum
Orlistat
Journal
International journal of pharmaceutics
ISSN: 1873-3476
Titre abrégé: Int J Pharm
Pays: Netherlands
ID NLM: 7804127
Informations de publication
Date de publication:
10 Jun 2022
10 Jun 2022
Historique:
received:
18
02
2022
revised:
30
04
2022
accepted:
02
05
2022
pubmed:
10
5
2022
medline:
7
6
2022
entrez:
9
5
2022
Statut:
ppublish
Résumé
The lipolysis-mediated postprandial small intestinal environment is known to influence the solubilisation and subsequent absorption of lipophilic drugs. In a previously performed small-scale clinical study in healthy volunteers, co-administration of the lipase inhibitor orlistat increased jejunal solubilisation and systemic absorption of fenofibrate after intake of the lipid-based formulation Fenogal. In the present study, the jejunal disposition of the locally acting orlistat was assessed and linked to fenofibrate solubilisation. In addition, the effect of orlistat-induced lipolysis inhibition on bile salt concentrations and composition was evaluated. Orlistat was distributed predominantly in the lipid layer, as indicated by a 5- to 14-fold higher AUC
Identifiants
pubmed: 35533920
pii: S0378-5173(22)00362-3
doi: 10.1016/j.ijpharm.2022.121807
pii:
doi:
Substances chimiques
Bile Acids and Salts
0
Lipids
0
Micelles
0
Orlistat
95M8R751W8
Fenofibrate
U202363UOS
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
121807Informations de copyright
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