Alginates as tablet disintegrants: Understanding disintegration mechanisms and defining ranges of applications. 2021

Alberto Berardi, and Sonja Bauhuber, and Obada Sawafta, and Gernot Warnke
Department of Pharmaceutical Sciences and Pharmaceutics, Faculty of Pharmacy, Applied Science Private University, Amman 11931, Jordan. Electronic address: a_berardi@asu.edu.jo.

Alginates are biopolymers that have been investigated for their use in food and medical fields. Minimal information is available regarding their potential application as tablet superdisintegrants. Here we studied the disintegration action of sodium alginate (SA), calcium alginate (CA) and alginic acid (AA). Initially, we characterised the swelling and wicking abilities and the disintegration mechanism of pure disintegrants. We found that the liquid uptake of both CA and AA is more swelling-driven in phosphate buffer and more wicking-driven in hydrochloric acid and water. CA acts by shape-recovery, AA by a combination of swelling and shape-recovery mechanisms. SA cannot be used as disintegrant due to gelling. In the second part of the paper, the disintegration time of formulations with different physico-chemical properties and different alginate concentrations (i.e. 4% and 10%) was measured, thus delivering a direct readout for the ranges of application of alginates as tablets disintegrants. The main observations are: i) CA and AA often provide very rapid disintegration, similarly to the superdisintegrants used as controls; ii) the action of CA is more susceptible to the medium conditions than AA; iii) CA underperforms in hard tablets containing a binder; iv) both CA and AA have slightly slower disintegration than other superdisintegrants in tablets containing a hydrophobic component. While the suitability of CA as a disintegrant is formulation- and medium- dependent, AA appears as a promising tablet superdisintegrant, particularly for the development of uncomplicated hydrophilic formulations for the nutraceutical and supplement industry, where natural ingredients are favoured.

UI MeSH Term Description Entries
D005079 Excipients Usually inert substances added to a prescription in order to provide suitable consistency to the dosage form. These include binders, matrix, base or diluent in pills, tablets, creams, salves, etc. Excipient,Stabilizing Agent,Stabilizing Agents,Suspending Agent,Suspending Agents,Agent, Stabilizing,Agent, Suspending,Agents, Stabilizing,Agents, Suspending
D000464 Alginates Salts and esters of ALGINIC ACID that are used as HYDROGELS; DENTAL IMPRESSION MATERIALS, and as absorbent materials for surgical dressings (BANDAGES, HYDROCOLLOID). They are also used to manufacture MICROSPHERES and NANOPARTICLES for DIAGNOSTIC REAGENT KITS and DRUG DELIVERY SYSTEMS. Alginate,Alginic Acid, Barium Salt,Alginic Acid, Calcium Salt,Alginic Acid, Copper Salt,Alginic Acid, Potassium Salt,Alginic Acid, Sodium Salt,Alloid G,Barium Alginate,Calcium Alginate,Calginat,Copper Alginate,Kalrostat,Kalrostat 2,Kaltostat,Potassium Alginate,Sodium Alginate,Sodium Calcium Alginate,Vocoloid,Xantalgin,poly(Mannuronic Acid), Sodium Salt,Alginate, Barium,Alginate, Calcium,Alginate, Copper,Alginate, Potassium,Alginate, Sodium,Alginate, Sodium Calcium,Calcium Alginate, Sodium
D012995 Solubility The ability of a substance to be dissolved, i.e. to form a solution with another substance. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 6th ed) Solubilities
D013607 Tablets Solid dosage forms, of varying weight, size, and shape, which may be molded or compressed, and which contain a medicinal substance in pure or diluted form. (Dorland, 28th ed) Tablet
D057927 Hydrophobic and Hydrophilic Interactions The thermodynamic interaction between a substance and WATER. Hydrophilic Interactions,Hydrophilic and Hydrophobic Interactions,Hydrophilicity,Hydrophobic Interactions,Hydrophobicity,Hydrophilic Interaction,Hydrophilicities,Hydrophobic Interaction,Hydrophobicities,Interaction, Hydrophilic,Interaction, Hydrophobic,Interactions, Hydrophilic,Interactions, Hydrophobic

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