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Article Dans Une Revue International journal of pharmaceutics Année : 2023

Exploration of the physical states of riboflavin (free base) by mechanical milling

Résumé

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.
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Dates et versions

hal-04214667 , version 1 (10-11-2023)

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Charline Henaff, Juergen Siepmann, Florence Siepmann, Florence Danede, Marie-Noëlle Avettand-Fènoël, et al.. Exploration of the physical states of riboflavin (free base) by mechanical milling. International journal of pharmaceutics , 2023, International journal of pharmaceutics, 645, pp.123416. ⟨10.1016/j.ijpharm.2023.123416⟩. ⟨hal-04214667⟩
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