The influence of co-formers on the dissolution rates of co-amorphous sulfamerazine/excipient systems

Katarzyna Gniado, Korbinian Löbmann, Thomas Rades, Andrea Erxleben

Research output: Contribution to journalJournal articleResearchpeer-review

21 Citations (Scopus)

Abstract

A comprehensive study on the dissolution properties of three co-amorphous sulfamerazine/excipient systems, namely sulfamerazine/deoxycholic acid, sulfamerazine/citric acid and sulfamerazine/sodium taurocholate (SMZ/DA, SMZ/CA and SMZ/NaTC; 1:1 molar ratio), is reported. While all three co-formers stabilize the amorphous state during storage, only co-amorphization with NaTC provides a dissolution advantage over crystalline SMZ and the reasons for this were analyzed. In the case of SMZ/DA extensive gelation of DA protects the amorphous phase from crystallization upon contact with buffer, but at the same time prevents the release of SMZ into solution. Disk dissolution studies showed an improved dissolution behavior of SMZ/CA compared to crystalline SMZ. However, enhanced dissolution properties were not seen in powder dissolution testing due to poor dispersibility. Co-amorphization of SMZ and NaTC resulted in a significant increase in dissolution rate, both in powder and disk dissolution studies.

Original languageEnglish
JournalInternational Journal of Pharmaceutics
Volume504
Issue number1-2
Pages (from-to)20-6
Number of pages7
ISSN0378-5173
DOIs
Publication statusPublished - 17 May 2016

Keywords

  • Journal Article
  • Research Support, Non-U.S. Gov't

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