Publication Type Journal Article
Title Sparfloxacin Multicomponent Crystals: Targeting the Solubility of Problematic Antibiotics
Authors Mariama Djalo Andreia E. S. Cunha Joao P. Luis Silvia Quaresma Auguste Fernandes Vânia André M. Teresa Duarte
Year 2021
Month February
Volume 21
Number 2
Pages 995-1005
Abstract The design of novel pharmaceutical multicomponent crystal forms has been reported as an efficient approach to tailor their physicochemical properties, including solubility. Sparfloxacin is a fluoroquinolone antibiotic widely used mainly in respiratory tract infections, but its safety profile is controversial due to photosensitivity reactions, and therefore the development of alternative forms that may contribute to the intake of lower dosages is desirable. Herein we report five novel molecular salts of sparfloxacin with generally regarded as safe coformers. All of the compounds present the typical S-1(1) (6) intramolecular synthon in SPAR molecules, and a direct interaction between SPAR(+) and the anionic coformers is also verified. Only salts 2 and 5 present a C-1(1) (8) chain due to the direct interaction of SPAR molecules via N-H-NH2,H- SPAR center dot center dot center dot O-COOH,O-SPAR. The new forms have been fully characterized, presenting adequate RH and temperature stability; more importantly, they are more soluble in water than sparfloxacin itself. The observed improvement in the physicochemical properties, in particular the 1 order higher aqueous solubility of the citrate salt, may contribute positively to obtain a better safety profile of the drug, as lower dosages may be possible.
Book Title
ISSN 1528-7483
EISSN 1528-7505
Conference Name
Bibtex ID ISI:000647362200028
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