Overcoming the Challenges of Low Drug Solubility in the Intravenous Formulation of Solithromycin

Daniel Evans, Samuel H Yalkowsky, Sara Wu, David Pereira, Prabha Fernandes

Research output: Contribution to journalArticle

1 Scopus citations

Abstract

Solithromycin is a fluoro-ketolide (a fourth-generation macrolide) antibiotic that has been undergoing clinical trials for the treatment of community-acquired bacterial pneumonia. In this study, development of the tri-amino acid–buffered solithromycin intravenous (IV) formulation was performed to minimize the occurrence of infusion-associated local adverse events (infusion-site pain or phlebitis) observed in patients who received the tartaric acid–buffered IV formulation with a lower buffered capacity during phase I clinical trials. Development of the tri-amino acids–buffered solithromycin IV formulation was achieved using a dynamic in vitro precipitation model. Computational modeling also supports the superiority of the amino acid-buffered formulation over the tartaric aid–buffered formulation.

Original languageEnglish (US)
Pages (from-to)412-418
Number of pages7
JournalJournal of Pharmaceutical Sciences
Volume107
Issue number1
DOIs
StatePublished - Jan 1 2018

Keywords

  • acid-base equilibria
  • formulation
  • in vitro models
  • injectables
  • precipitation

ASJC Scopus subject areas

  • Pharmaceutical Science

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