Rivaroxaban lyospheres prepared by a dimethyl sulfoxide-based spray-freeze-drying process.

Spray-freeze-drying (SFD) processes are usually using aqueous solvent systems, which however, exclude the use of SFD for poorly water-soluble drugs/excipients. Here, we evaluated dimethyl sulfoxide for its suitability in formulating SFD particles (lyospheres®). Rivaroxaban was spray-freeze-dried from DMSO solutions containing polyvinyl pyrrolidone (PVP; Kollidon® 25), vinylpyrrolidone-vinyl acetate copolymer (PVP-VA; Kollidon® VA64) or polyvinyl alcohol 4-88 (PVA) forming porous lyospheres® (median particle size 250 to 350 µm). Rivaroxaban was amorphous with all three polymers, which in combination with the high porosity resulted in rapid dissolution in vitro within 10 min. Consequently, this translated in lower T

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Déclaration de conflit d'intérêts

Declaration of Competing Interest The authors declare the following financial interests/personal relationships which may be considered as potential competing interests: Jan Kozak reports financial support was provided by German Academic Exchange Service. Alf Lamprecht reports financial support was provided by French National Research Agency. Jan Kozak reports a relationship with German Academic Exchange Service that includes: funding grants. Alf Lamprecht has patent #WO2021110732 (A1) pending to University of Bonn.