Design, Synthesis, and Characterization of New 5-Fluorocytosine Salts

被引：32

作者：

Perumalla, Sathyanarayana R. ^{[1
]}

Pedireddi, Venkateswara R. ^{[2
]}

Sun, Changquan C. ^{[1
]}

机构：

[1] Univ Minnesota, Coll Pharm, Dept Pharmaceut, Minneapolis, MN 55455 USA

[2] Indian Inst Technol, Sch Basic Sci, Bhubaneswar 751013, Orissa, India

来源：

MOLECULAR PHARMACEUTICS | 2013年 / 10卷 / 06期

关键词：

5-fluorocytosine; fluocytosine; cytosine protonation; hemicytosinium duplexes; nucleobase; I-MOTIF; CO-CRYSTALS; COCRYSTALS; DNA; BIOAVAILABILITY; SOLUBILITY; CAFFEINE; CYTOSINE; DRUG;

D O I：

10.1021/mp400070a

中图分类号：

R-3 [医学研究方法]; R3 [基础医学];

学科分类号：

1001 ;

摘要：

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.

引用

页码：2462 / 2466

页数：5

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