The role of SeDeM for characterizing the active substance and polyvinyilpyrrolidone eliminating metastable forms in an oral lyophilizate-A preformulation study

PLoS One. 2018 Apr 24;13(4):e0196049. doi: 10.1371/journal.pone.0196049. eCollection 2018.

Abstract

A preformulation study of an oral lyophilisate with cetirizine dihydrochloride (CTZ) as active ingredient, mannitol and PVP K30 as bulking agents is presented. CTZ shown a humidity content of 0.150% and a spontaneous hygroscopicity of 0.200% (both determined by SeDeM diagram), demonstrating an adequate stability behavior in solid form. A design of experiments (DoE) performed with both mannitol and PVP K30, followed by a simple factorial design (32) has determined the optimum combination of excipients and CTZ, and showed that a higher proportion of PVP K30 was able to prevent metastable forms generated by mannitol.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Oral
  • Calorimetry, Differential Scanning
  • Cetirizine / administration & dosage
  • Cetirizine / chemistry*
  • Drug Compounding
  • Freeze Drying
  • Mannitol / chemistry*
  • Powders
  • Pyrrolidinones / chemistry*
  • Tablets
  • Wettability

Substances

  • Powders
  • Pyrrolidinones
  • Tablets
  • Mannitol
  • Cetirizine

Grants and funding

The author received no specific funding for the work. The author (myself) received no specific funding for the work, nor grant. All the fees and tuition of the University of Barcelona were paid with my salary working in Reig Jofre. I did my PhD thesis part time, which helped me accomplish both work and PhD thesis. The funder provided support in the form of salaries for authors PFB and EJ but did not have any additional role in the study design, data collection and analysis, decision to publish, or preparation of the manuscript. The specific roles of the authors are articulated in the ‘Authors contributions’ section.