Prilling of API/fatty acid suspensions: Screening of additives for drug release modification

Elien De Coninck, V. Vanhoorne, M. Boone, G. Van Assche, B. G. De Geest, T. De Beer, C. Vervaet

Research output: Contribution to journalArticlepeer-review

1 Citation (Scopus)

Abstract

Current study screened additives which could modify the drug release from prills made of an active pharmaceutical ingredient/fatty acid (API/FA) suspension, without negatively influencing the processability and/or stability of the formulation. Therefore, 11 additives (i.e. emulsifiers, pore-formers and FA-based lubricants) were added in a 20% concentration to a paracetamol/behenic acid formulation. Two additives, Kolliphor® P338 and P407 provided complete drug release in less than 1 h, as their thermoreversible gel formation resulted in a disintegration of the prills. Lower Kolliphor® P338 or P407 concentrations (2.5–10%) resulted in a complete but slower drug release in 24 h as the prills no longer disintegrated and the release mechanism was dominated by pore-formation. Prills with a robust drug release profile (i.e. independent of pH and surfactant concentration of the dissolution medium) were obtained after the addition of ≥5% Kolliphor® P338 or P407 to the FA-based formulation. Based on a 6-month stability study, it was concluded that Kolliphor® P407 was a suitable additive to modify the drug release profile of API/FA suspension-based prills when formulations were stored below 25 °C at low relative humidity.
Original languageEnglish
Article number119022
JournalInternational Journal of Pharmaceutics
Volume576
DOIs
Publication statusPublished - 25 Feb 2020

Bibliographical note

Funding Information:
The authors would like to acknowledge BASF (Ludwigshafen, Germany) for supplying the screened additives. E. De Coninck acknowledges the Special Research Fund of Ghent University for a PhD scholarship.

Funding Information:
The authors would like to acknowledge BASF (Ludwigshafen, Germany) for supplying the screened additives. E. De Coninck acknowledges the Special Research Fund of Ghent University for a PhD scholarship.

Publisher Copyright:
© 2020 Elsevier B.V.

Copyright:
Copyright 2020 Elsevier B.V., All rights reserved.

Keywords

  • Prilling
  • Controlled release
  • Multiparticulate dosage forms
  • Fatty acids
  • Paracetamol
  • Poloxamers

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