New Pharmaceutical Salts of Trazodone

New pharmaceutically acceptable salts of trazodone (trazodone hydrogen bromide and trazodone 1-hydroxy-2-naphthonic acid) for the treatment of central nervous system disorders are synthesized and described. Although trazodone salts are poorly crystalline, single-crystal X-ray diffraction data for tr...

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Bibliographic Details
Published in:Molecules (Basel, Switzerland) Switzerland), 2021-02, Vol.26 (3), p.769
Main Authors: Jaśkowska, Jolanta, Zaręba, Przemysław, Drabczyk, Anna, Kozak, Agnieszka, Madura, Izabela D, Majka, Zbigniew, Pindelska, Edyta
Format: Article
Language:English
Subjects:
Acids
Anions
Bioavailability
Cations
Central nervous system
Crystal structure
dissolution
drug design
Drug dosages
Fourier transforms
GIPAW calculation
Hydrogen bromide
Infrared spectroscopy
Lactose
Magnetic resonance spectroscopy
Magnetic shielding
Mode of action
Models, Molecular
Molecular Conformation
NMR
NMR spectroscopy
Nuclear magnetic resonance
Pharmaceuticals
Physicochemical properties
Physiology
Salts
Salts - chemistry
Serotonin
Single crystals
solid-state NMR (SSNMR) spectroscopy
trazodone
Trazodone - chemistry
X-ray diffraction
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Summary:New pharmaceutically acceptable salts of trazodone (trazodone hydrogen bromide and trazodone 1-hydroxy-2-naphthonic acid) for the treatment of central nervous system disorders are synthesized and described. Although trazodone salts are poorly crystalline, single-crystal X-ray diffraction data for trazodone 1-hydroxy-2-naphthonic acid were collected and analyzed as well as compared to the previously described crystal structure of commercially available trazodone hydrochloride. The powder samples of all new salts were characterized by Fourier transform infrared spectroscopy, X-ray diffraction and C solid-state nuclear magnetic resonance spectroscopy. Spectroscopic studies were supported by gauge including projector augmented wave (GIPAW) calculations of carbon chemical shielding constants. The main goal of our research was to find salts with better physicochemical properties and to make an attempt to associate them with both the anion structure and the most prominent interactions exhibited by the protonated trazodone cation. The dissolution profiles of trazodone from tablets prepared from various salts with lactose monohydrate were investigated. The studies revealed that salts with simple anions show a fast release of the drug while the presence of more complex anion, more strongly interacting with the cation, effects a slow-release profile of the active substance and can be used for the preparation of the tables with a delay or prolonged mode of action.
ISSN:1420-3049
1420-3049
DOI:10.3390/molecules26030769