Correlation between the release characteristics of theophylline and the free volume of polyvinylpyrrolidone

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Abstract

The purpose of this work was to study the drug-release properties of an amorphous polymer, polyvinylpyrrolidone applied conventionally as a binder in tablets. In order to gain data on the wearing properties of tablets, they were stored for a 30 days period under different humidity conditions before the drug-release measurements. The active material chosen for the release study was theophylline. An exponential relationship was found, with good correlation, between the relative humidity of the storage medium and the mean dissolution time of theophylline from polyvinylpyrrolidone tablets and the size of free volume holes. Positron annihilation lifetime spectroscopy (PALS) measurements, performed parallel with the theophylline release study, showed that the main reason for this correlation is the rearrangement of the pore structure of PVP. The results suggest that the water-induced glassy to rubbery transition of the polymer plays a significant role in the drug-release characteristics.

Original languageEnglish
Pages (from-to)351-354
Number of pages4
JournalEuropean Journal of Pharmaceutical Sciences
Volume24
Issue number4
DOIs
Publication statusPublished - Mar 2005

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Keywords

  • Free volume
  • Glassy to rubbery transition
  • Mean dissolution time
  • Polyvinylpyrrolidone
  • Positron lifetime measurement
  • Theophylline

ASJC Scopus subject areas

  • Pharmaceutical Science

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