Design, Synthesis, and Characterization of New 5‑Fluorocytosine
Salts
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Abstract
5-Fluorocytosine
(FC), an antifungal drug and a cytosine derivative,
has a complex solid-state landscape that challenges its development
into a drug product. A total of eight new FC salts, both cytosinium
and hemicytosinium, with four strong acids were prepared by controlling
acid concentration in the crystallization medium. The pharmaceutically
acceptable saccharin salt of FC exhibits superior phase stability
and, hence, has the potential to address the instability problem of
FC associated with hydration