Alginate ester: New moisture-scavenging excipients for direct compressible pharmaceutical tableting

Carbohydr Polym. 2022 Dec 1:297:120063. doi: 10.1016/j.carbpol.2022.120063. Epub 2022 Aug 31.

Abstract

The objective of this work is to evaluate methyl ester alginates and alginic acid (AA) as moisture-scavenging excipients for the formulation of aspirin tablets obtained by direct compression. The tablets were stored at accelerated conditions (40 °C/75 % RH) and assessed for changes in tensile strength, mass, thickness and disintegration time. While moisture caused a reduction in the hardness of MCC and AA tablets, hardness of the tablets made from methylated materials was virtually unaffected. The physical stability of alginate ester tablets was found to be related to their increased plastic deformation leading to extended interparticle contact with less impact on tablet porosity. Finally, the combination of higher moisture affinity and lower water dissociation exhibited by alginates esters resulted in tablets with the lowest aspirin degradation. These findings suggest that excipients with high water retention can act as moisture-scavengers without losing their functional properties and reducing the degradation of moisture-sensitive drugs.

Keywords: Alginic acid; Aspirin degradation; Degree of methylation; Direct compression; Moisture; Tablet stability.

MeSH terms

  • Alginates*
  • Alginic Acid
  • Aspirin
  • Drug Compounding
  • Esters
  • Excipients*
  • Plastics
  • Tablets
  • Tensile Strength
  • Water

Substances

  • Alginates
  • Esters
  • Excipients
  • Plastics
  • Tablets
  • Water
  • Alginic Acid
  • Aspirin