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Overcoming the Drawbacks of Sulpiride by Means of New Crystal Forms

Birolo, Rebecca
•
Bravetti, Federica
•
Bordignon, Simone
altro
Gobetto, Roberto
2022
  • journal article

Periodico
PHARMACEUTICS
Abstract
This study aims at developing new multicomponent crystal forms of sulpiride, an antipsychotic drug. The main goal was to improve its solubility since it belongs to class IV of the BCS. Nine new adducts were obtained by combining the active pharmaceutical ingredient with acid coformers: a salt cocrystal and eight molecular salts. In addition, three novel co-drugs, of which two are molecular salts and one is a cocrystal, were also achieved. All samples were characterized in the solid state by complementary techniques (i.e., infrared spectroscopy, powder X-ray diffraction and solid-state NMR). For systems for which it was possible to obtain good-quality single crystals, the structure was solved by single crystal X-ray diffraction (SCXRD). SCXRD combined with solid-state NMR were used to evaluate the ionic or neutral character of the adducts. In vitro dissolution tests of the new crystal forms were performed and all the adducts display remarkable dissolution properties with respect to pure sulpiride.
DOI
10.3390/pharmaceutics14091754
WOS
WOS:000856791800001
Archivio
https://hdl.handle.net/11368/3030764
info:eu-repo/semantics/altIdentifier/scopus/2-s2.0-85138614180
https://www.mdpi.com/1999-4923/14/9/1754
Diritti
open access
license:creative commons
license uri:http://creativecommons.org/licenses/by/4.0/
FVG url
https://arts.units.it/bitstream/11368/3030764/1/pharmaceutics-14-01754-v3.pdf
Soggetti
  • X-ray diffraction

  • cocrystal

  • crystal engineering

  • dissolution test

  • improved solubility

  • molecular salt

  • salt cocrystal

  • solid-state NMR

  • sulpiride

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