Enabling the Tablet Product Development of 5-Fluorocytosine by Conjugate Acid Base Cocrystals

Sathyanarayana R. Perumalla, Shubhajit Paul, Changquan C. Sun

Research output: Contribution to journalArticlepeer-review

16 Scopus citations


5-Fluorocytosine (FC) is a high-dose antifungal drug that challenges the development of a tablet product due to poor solid-state stability and tabletability. Using 2 pharmaceutically acceptable conjugate acid base (CAB) cocrystals of FC with HCl and acesulfame, we have developed commercially viable high loading FC tablets. The tablets were prepared by direct compression using nano-coated microcrystalline cellulose Avicel PH105 as a tablet binder, which provided both excellent tabletability and good flowability. Commercial manufacturability of formulations based on both CAB cocrystals was verified on a compaction simulator. The results from an expedited friability study were used to set the compaction force, which yielded tablets with sufficient mechanical strength and rapid tablet disintegration. This work demonstrates the potential value of CAB cocrystals in drug product development.

Original languageEnglish (US)
Pages (from-to)1960-1966
Number of pages7
JournalJournal of Pharmaceutical Sciences
Issue number6
StatePublished - Jun 1 2016


  • cocrystals
  • crystal engineering
  • formulation
  • powder technology
  • tablet


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