Nanocrystal solid dispersion of fuzapladib free acid with improved oral bioavailability.
fuzapladib
hydration property
multi-inlet vortex mixer
nanocrystal solid dispersion
oral bioavailability
Journal
Biopharmaceutics & drug disposition
ISSN: 1099-081X
Titre abrégé: Biopharm Drug Dispos
Pays: England
ID NLM: 7911226
Informations de publication
Date de publication:
Jun 2022
Jun 2022
Historique:
revised:
27
02
2022
received:
09
12
2021
accepted:
21
03
2022
pubmed:
25
3
2022
medline:
30
6
2022
entrez:
24
3
2022
Statut:
ppublish
Résumé
This study aimed to develop an oral nanocrystal solid dispersion (nCSD) of fuzapladib (FZP) with enhanced absorbability for the treatment of acute pancreatitis (AP). The hydration properties of crystalline FZP free acid (crystalline FZP) and FZP sodium salt (FZP/Na) were assessed to select a stable crystal form. The nCSD of FZP free acid (nCSD/FZP) was prepared using a multi-inlet vortex mixer and evaluated in terms of physicochemical and pharmacokinetic properties. The results of X-ray powder diffraction analysis indicated that crystalline FZP was stable as an anhydrate, while FZP/Na was converted to its monohydrate at water activity of above 0.2. The nanocrystals in nCSD/FZP were dispersed in hydroxy propyl cellulose-SSL, and their mean particle size were 160 nm with uniform spherical shape. In dissolution testing, nCSD/FZP exhibited rapid dissolution compared with crystalline FZP and reached a saturated concentration of FZP within initial 30 min. After oral administration (2 mg-FZP/kg) to rats, the maximum plasma concentration and bioavailability were 7.3- and 5.2-fold higher for nCSD/FZP than crystalline FZP, respectively, due to improved dissolution by nanosization. In conclusion, nCSD/FZP may be a novel oral dosage form with enhanced absorbability facilitating potent therapeutic effects of FZP for the treatment of AP in animals.
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
89-97Subventions
Organisme : Japan Society for the Promotion of Science
ID : 20K07158
Organisme : Japan Society for the Promotion of Science
ID : 20K07180
Informations de copyright
© 2022 John Wiley & Sons Ltd.
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