Stabilization mechanism of amorphous carbamazepine by transglycosylated rutin, a non-polymeric amorphous additive with a high glass transition temperature.
Amorphous formulation
Differential scanning calorimetry
Drug-excipient interaction
Simulation
Solid-state nuclear magnetic resonance spectroscopy
Journal
International journal of pharmaceutics
ISSN: 1873-3476
Titre abrégé: Int J Pharm
Pays: Netherlands
ID NLM: 7804127
Informations de publication
Date de publication:
01 May 2021
01 May 2021
Historique:
received:
15
12
2020
revised:
24
02
2021
accepted:
10
03
2021
pubmed:
22
3
2021
medline:
22
6
2021
entrez:
21
3
2021
Statut:
ppublish
Résumé
α-Glycosyl rutin (Rutin-G), composed of a flavonol skeleton and sugar groups, is a promising non-polymeric additive for stabilizing amorphous drug formulations. In this study, the mechanism of the stabilization of the amorphous state of carbamazepine (CBZ) by Rutin-G was investigated. In comparison with hypromellose (HPMC), which is commonly used as a crystallization inhibitor for amorphous drugs, Rutin-G significantly stabilized amorphous CBZ. Moreover, the dissolution rate and the resultant supersaturation level of CBZ were significantly improved in the CBZ/Rutin-G spray-dried samples (SPDs) owing to the rapid dissolution property of Rutin-G. Differential scanning calorimetry measurement demonstrated a high glass transition temperature (T
Identifiants
pubmed: 33744450
pii: S0378-5173(21)00296-9
doi: 10.1016/j.ijpharm.2021.120491
pii:
doi:
Substances chimiques
Carbamazepine
33CM23913M
Hypromellose Derivatives
3NXW29V3WO
Rutin
5G06TVY3R7
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
120491Informations de copyright
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