Titre :

Mechanism for Stabilizing an Amorphous Drug Using Amino Acids within Co-Amorphous Blends

Auteur(s) :

Guinet, Yannick [Auteur]
Unité Matériaux et Transformations (UMET) - UMR 8207
Paccou, Laurent [Auteur]
Unité Matériaux et Transformations (UMET) - UMR 8207
Hedoux, Alain [Auteur]
Unité Matériaux et Transformations (UMET) - UMR 8207

Titre de la revue :

Pharmaceutics

Numéro :

15

Pagination :

337

Éditeur :

MDPI

Date de publication :

2023-01

ISSN :

1999-4923

Mot(s)-clé(s) en anglais :

Raman spectroscopy
glass transition
hydrogen bond
physical stability
cryo-milling

Discipline(s) HAL :

Physique [physics]/Matière Condensée [cond-mat]/Science des matériaux [cond-mat.mtrl-sci]
Physique [physics]/Matière Condensée [cond-mat]/Matière Molle [cond-mat.soft]
Physique [physics]/Matière Condensée [cond-mat]/Systèmes désordonnés et réseaux de neurones [cond-mat.dis-nn]

Résumé en anglais : [en]

Designing co-amorphous formulations is now recognized as a relevant strategy for improving the bioavailability of low-molecular-weight drugs. In order to determine the most suitable low-molecular-weight excipients for ...
Lire la suite >Designing co-amorphous formulations is now recognized as a relevant strategy for improving the bioavailability of low-molecular-weight drugs. In order to determine the most suitable low-molecular-weight excipients for stabilizing the drug in the amorphous state, screening methods were developed mostly using amino acids as co-formers. The present study focused on the analysis of the thermal stability of co-amorphous blends prepared by cryo-milling indomethacin with several amino acids in order to understand the stabilization mechanism of the drug in the amorphous state. Combining low- and mid-frequency Raman investigations has provided information on the relation between the physical properties of the blends and those of the H-bond network of the amorphous drug. This study revealed the surprising capabilities of L-arginine to stiffen the H-bond network in amorphous indomethacin and to drastically improve the stability of its amorphous state. As a consequence, this study suggests that amino acids can be considered as stiffeners of the H-bond network of indomethacin, thereby improving the stability of the amorphous state.Lire moins >

Langue :

Anglais

Comité de lecture :

Oui

Audience :

Internationale

Vulgarisation :

Non

Établissement(s) :

Université de Lille
CNRS
INRAE
ENSCL

Collections :

• Unité Matériaux et Transformations (UMET) - UMR 8207

Équipe(s) de recherche :

Matériaux Moléculaires et Thérapeutiques

Date de dépôt :

2023-02-06T09:18:50Z
2023-02-07T16:20:55Z