On the Usefulness of Two Small-Scale In Vitro Setups in the Evaluation of Luminal Precipitation of Lipophilic Weak Bases in Early Formulation Development.
PBPK modelling
biorelevant
biphasic dissolution
dissolution-permeation.
in vitro techniques
precipitation
supersaturation
Journal
Pharmaceutics
ISSN: 1999-4923
Titre abrégé: Pharmaceutics
Pays: Switzerland
ID NLM: 101534003
Informations de publication
Date de publication:
16 Mar 2020
16 Mar 2020
Historique:
received:
18
02
2020
revised:
08
03
2020
accepted:
11
03
2020
entrez:
20
3
2020
pubmed:
20
3
2020
medline:
20
3
2020
Statut:
epublish
Résumé
A small-scale biphasic dissolution setup and a small-scale dissolution-permeation (D-P) setup were evaluated for their usefulness in simulating the luminal precipitation of three lipophilic weak bases-dipyridamole, ketoconazole and itraconazole. The transition from the gastric to intestinal environment was incorporated into both experimental procedures. Emulsification during the biphasic dissolution experiments had a minimal impact on the data, when appropriate risk mitigation steps were incorporated. Precipitation parameters estimated from the in vitro data were inputted into the Simcyp® physiologically based pharmacokinetic (PBPK) modelling software and simulated human plasma profiles were compared with previously published pharmacokinetic data. Average C
Identifiants
pubmed: 32188116
pii: pharmaceutics12030272
doi: 10.3390/pharmaceutics12030272
pmc: PMC7151110
pii:
doi:
Types de publication
Journal Article
Langues
eng
Subventions
Organisme : Horizon 2020
ID : 674909
Déclaration de conflit d'intérêts
Karl J. Box is an employee of Pion Inc. (UK) Ltd. The funders/company had no role in the design of the study; in the collection, analyses, or interpretation of data; in the writing of the manuscript, or in the decision to publish the results
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