Modifying matrix micro-environmental pH to achieve sustained drug release from highly laminating alginate matrices

Ai Ling Ching, Celine Valeria Liew, Lai Wah Chan, Paul Wan Sia Heng

Research output: Contribution to journalArticleResearchpeer-review

32 Citations (Scopus)

Abstract

Lamination of alginate matrix tablet at acidic pH can compromise its function as a sustained release carrier. This phenomenon is associated with the conversion of sodium alginate to alginic acid. An innovative approach for controlling the release of a highly water-soluble drug from such matrices is presented in this paper. Inclusion of pH-modifiers was employed to raise the micro-environmental pH within matrices undergoing dissolution at gastric pH. The changes in micro-environmental pH of hydrating alginate matrices were visualized with the aid of a pH-indicator and subsequently quantified using image analysis. Transient elevation in micro-environmental pH impeded alginate protonation and minimized or prevented matrix lamination, contributing to preservation of drug diffusion barrier. Significant reduction in the rate of drug release at pH 1.2 was achieved in the presence of such additives. The action of pH-modifiers was synergistically enhanced in the presence of a carbon dioxide barrier formed by effervescing sodium bicarbonate, reducing drug release in the acidic medium from 60 to 20%. Further insight into the influence of lamination on drug release from alginate compacts was given.

Original languageEnglish
Pages (from-to)361-370
Number of pages10
JournalEuropean Journal of Pharmaceutical Sciences
Volume33
Issue number4-5
DOIs
Publication statusPublished - 23 Apr 2008
Externally publishedYes

Keywords

  • Lamination
  • Micro-environmental pH
  • pH-sensitive polymer
  • Sustained release

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