Alginate ester: New moisture-scavenging excipients for direct compressible pharmaceutical tableting. (1st December 2022)

• Record Type: Journal Article
• Authors: Sanchez-Ballester, Noelia M.; Trens, Philippe; Rossi, Jean-Christophe; Soulairol, Ian
• Is Part Of: Carbohydrate polymers. Volume 297(2022)
• Publication Date: 2022-12-01
• Subjects: AA alginic acid -- MCC cellulose microcrystalline -- MeA methyl alginate -- RH relative humidity -- DM degree of methylation -- DT disintegration time -- TS tensile strength; Alginic acid -- Degree of methylation -- Direct compression -- Moisture -- Tablet stability -- Aspirin degradation; Polysaccharides -- Periodicals; Polysaccharides -- Periodicals; Polysaccharides -- Périodiques; Electronic journals; 547.78
• DOI: 10.1016/j.carbpol.2022.120063
• Languages: English
• ISSNs: 0144-8617

Abstract

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. Graphical abstract: Unlabelled Image Highlights: First evaluation of AA and its methyl-ester derivatives as moisture-scavenging excipients for DC. Degree of methylation did not affect the adsorption mode of the modified alginates, both in terms of quantities and kinetics While moisture produced a softening of MCC and AA tablets, alginate esters tablets preserved their hardness and functionality. Medium- and high-methylated alginates presented a lower percentage of ASA degradation compared to MCC making these materials DC moisture-scavenging candidates.