TY - JOUR
T1 - Design, synthesis, and characterization of new 5-fluorocytosine salts
AU - Perumalla, Sathyanarayana R.
AU - Pedireddi, Venkateswara R.
AU - Sun, Changquan C.
PY - 2013/6/3
Y1 - 2013/6/3
N2 - 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.
AB - 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.
KW - 5-fluorocytosine
KW - cytosine protonation
KW - fluocytosine
KW - hemicytosinium duplexes
KW - nucleobase
UR - https://www.scopus.com/pages/publications/84878655258
UR - https://www.scopus.com/pages/publications/84878655258#tab=citedBy
U2 - 10.1021/mp400070a
DO - 10.1021/mp400070a
M3 - Article
C2 - 23631720
AN - SCOPUS:84878655258
SN - 1543-8384
VL - 10
SP - 2462
EP - 2466
JO - Molecular pharmaceutics
JF - Molecular pharmaceutics
IS - 6
ER -