3 years ago

Increase in Solubility of Poorly-Ionizable Pharmaceuticals by Salt Formation: A Case of Agomelatine Sulfonates

Increase in Solubility of Poorly-Ionizable Pharmaceuticals by Salt Formation: A Case of Agomelatine Sulfonates
Lubomír Rulíšek, Josef Beránek, Argyro Chatziadi, Michal Hušák, Pavel Šebek, Jiří Klimeš, Luděk Ridvan, Daniel Bím, Eliška Skořepová, Tereza Boleslavská
We present three novel sulfonate salts of agomelatine: a hydrogensulfate, a mesylate, and a besylate, and for two of them, their respective solvated forms. All crystal structures have been solved and their salt character was confirmed by solid state NMR measurements and DFT calculations. By sulfonate salt formation, up to ∼200-times faster dissolution of agomelatine was achieved.

Publisher URL: http://dx.doi.org/10.1021/acs.cgd.7b00805

DOI: 10.1021/acs.cgd.7b00805

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