Effect of drug-carrier interaction on the dissolution behavior of solid dispersion tablets

Parinda Srinarong*, Sander Kouwen, Marinella R Visser, Wouter L J Hinrichs, Henderik W Frijlink

*Corresponding author for this work

Research output: Contribution to journalArticleAcademicpeer-review

21 Citations (Scopus)

Abstract

The objective of this study was to compare the dissolution behavior of tablets prepared from solid dispersions with and without drug-carrier interactions. Diazepam and nifedipine were used as model drugs. Two types of carriers were used; polyvinylpyrrolidone (PVP K12, K30 and K60) and saccharides (inulin 1.8kDa, 4kDa and 6.5kDa). Solid dispersions with various drug loads were prepared by lyophilization. It was found that the drug solubility in aqueous PVP solutions was significantly increased indicating the presence of drug-carrier interaction while the drug solubility was not affected by the saccharides indicating absence of drug-carrier interaction. X-ray powder diffraction and modulated differential scanning calorimetry revealed that all solid dispersions were fully amorphous. Dissolution behavior of solid dispersion tablets based on either the PVPs or saccharides was governed by both dissolution of the carrier and drug load. It was shown that a fast drug dissolution of solid dispersions with a high drug load could be obtained with carrier that showed interaction with the drug. © 2010 Informa Healthcare USA, Inc.
Original languageEnglish
Pages (from-to)460-468
Number of pages9
JournalPharmaceutical development and technology
Volume15
Issue number5
DOIs
Publication statusPublished - 26-Aug-2010

Keywords

  • Amorphous solid dispersions
  • Dissolution
  • Inulin
  • Lipophilic drugs
  • Lyophilization
  • Polyvinylpyrrolidone
  • carbohydrate
  • diazepam
  • inulin
  • nifedipine
  • povidone
  • article
  • differential scanning calorimetry
  • dispersion
  • dissolution
  • drug solubility
  • freeze drying
  • molecular interaction
  • priority journal
  • solid
  • tablet
  • X ray powder diffraction

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