Exploration of the physical states of ...
Document type :
Article dans une revue scientifique: Article original
Permalink :
Title :
Exploration of the physical states of riboflavin (free base) by mechanical milling
Author(s) :
Henaff, Charline [Auteur]
1002334|||Unité Matériaux et Transformations - UMR 8207 [UMET]
Unité Matériaux et Transformations (UMET) - UMR 8207
Siepmann, Juergen [Auteur]
Médicaments et biomatériaux à libération contrôlée: mécanismes et optimisation - Advanced Drug Delivery Systems - U 1008 [MBLC - ADDS]
Advanced Drug Delivery Systems (ADDS) - U1008
Siepmann, Florence [Auteur]
Advanced Drug Delivery Systems (ADDS) - U1008
Danede, Florence [Auteur]
174496|||Unité Matériaux et Transformations - UMR 8207 [UMET]
Unité Matériaux et Transformations (UMET) - UMR 8207
Avettand-Fènoël, Marie-Noëlle [Auteur]
174496|||Unité Matériaux et Transformations - UMR 8207 [UMET]
Unité Matériaux et Transformations (UMET) - UMR 8207
Verin, Jérémy [Auteur]
Médicaments et biomatériaux à libération contrôlée: mécanismes et optimisation - Advanced Drug Delivery Systems - U 1008 [MBLC - ADDS]
Advanced Drug Delivery Systems (ADDS) - U1008
Fadel, Alexandre [Auteur]
Willart, Jean-François [Auteur]
Unité Matériaux et Transformations (UMET) - UMR 8207
1002334|||Unité Matériaux et Transformations - UMR 8207 [UMET]
Unité Matériaux et Transformations (UMET) - UMR 8207
Siepmann, Juergen [Auteur]
Médicaments et biomatériaux à libération contrôlée: mécanismes et optimisation - Advanced Drug Delivery Systems - U 1008 [MBLC - ADDS]
Advanced Drug Delivery Systems (ADDS) - U1008
Siepmann, Florence [Auteur]
Advanced Drug Delivery Systems (ADDS) - U1008
Danede, Florence [Auteur]
174496|||Unité Matériaux et Transformations - UMR 8207 [UMET]
Unité Matériaux et Transformations (UMET) - UMR 8207
Avettand-Fènoël, Marie-Noëlle [Auteur]
174496|||Unité Matériaux et Transformations - UMR 8207 [UMET]
Unité Matériaux et Transformations (UMET) - UMR 8207
Verin, Jérémy [Auteur]
Médicaments et biomatériaux à libération contrôlée: mécanismes et optimisation - Advanced Drug Delivery Systems - U 1008 [MBLC - ADDS]
Advanced Drug Delivery Systems (ADDS) - U1008
Fadel, Alexandre [Auteur]
Willart, Jean-François [Auteur]
Unité Matériaux et Transformations (UMET) - UMR 8207
Journal title :
International journal of pharmaceutics
Volume number :
645
Pages :
123416
Publisher :
Elsevier BV
Publication date :
2023-09
ISSN :
0378-5173
HAL domain(s) :
Physique [physics]/Matière Condensée [cond-mat]/Science des matériaux [cond-mat.mtrl-sci]
Sciences du Vivant [q-bio]
Sciences du Vivant [q-bio]
English abstract : [en]
Amorphous riboflavin (free base) could be produced for the first time via high energy ball milling of a commercial crystalline form (Form I). Importantly, this solid state amorphization process allowed to circumvent chemical ...
Show more >Amorphous riboflavin (free base) could be produced for the first time via high energy ball milling of a commercial crystalline form (Form I). Importantly, this solid state amorphization process allowed to circumvent chemical degradation occurring during melting as well as the lack of suitable solvents, which are required for amorphization via spray- or freeze-drying. The amorphous state of riboflavin was thoroughly characterized, revealing a complex recrystallization pattern upon heating, involving two enantiotropic polymorphic forms (II and III) and a dihydrate. The glass transition temperature (Tg) and heat capacity (Cp) jump of the amorphous form were determined as 144 °C and 0.68 J/g/°C. Moreover, the relative physical stability of the different physical states has been elucidated, e.g., at room temperature: I > II > III. The following rank order was observed for the dissolution rates in water at 37 °C during the first 4 h: amorphous > III ≈ II > I. Afterwards, a dihydrate crystallized from the solutions of amorphous and metastable crystalline riboflavin forms, the solubility of which was well above the solubility of the stable Form I.Show less >
Show more >Amorphous riboflavin (free base) could be produced for the first time via high energy ball milling of a commercial crystalline form (Form I). Importantly, this solid state amorphization process allowed to circumvent chemical degradation occurring during melting as well as the lack of suitable solvents, which are required for amorphization via spray- or freeze-drying. The amorphous state of riboflavin was thoroughly characterized, revealing a complex recrystallization pattern upon heating, involving two enantiotropic polymorphic forms (II and III) and a dihydrate. The glass transition temperature (Tg) and heat capacity (Cp) jump of the amorphous form were determined as 144 °C and 0.68 J/g/°C. Moreover, the relative physical stability of the different physical states has been elucidated, e.g., at room temperature: I > II > III. The following rank order was observed for the dissolution rates in water at 37 °C during the first 4 h: amorphous > III ≈ II > I. Afterwards, a dihydrate crystallized from the solutions of amorphous and metastable crystalline riboflavin forms, the solubility of which was well above the solubility of the stable Form I.Show less >
Language :
Anglais
Peer reviewed article :
Oui
Audience :
Internationale
Popular science :
Non
European Project :
Administrative institution(s) :
Université de Lille
CNRS
INRAE
ENSCL
CNRS
INRAE
ENSCL
Collections :
Research team(s) :
Matériaux Moléculaires et Thérapeutiques
Métallurgie Physique et Génie des Matériaux
Métallurgie Physique et Génie des Matériaux
Submission date :
2023-09-20T07:20:20Z
2023-09-22T08:51:00Z
2023-11-08T16:06:06Z
2023-11-10T13:21:21Z
2023-09-22T08:51:00Z
2023-11-08T16:06:06Z
2023-11-10T13:21:21Z
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