Formulation Strategies to Improve the Stability and Handling of Oral Solid Dosage Forms of Highly Hygroscopic Pharmaceuticals and Nutraceuticals

Abstract

Highly hygroscopic pharmaceutical and nutraceutical solids are prone to significant changes in their physicochemical properties due to chemical degradation and/or solid-state transition, resulting in adverse effects on their therapeutic performances and shelf life. Moisture absorption also leads to excessive wetting of the solids, causing their difficult handling during manufacturing. In this review, four formulation strategies that have been employed to tackle hygroscopicity issues in oral solid dosage forms of pharmaceuticals/nutraceuticals were discussed. The four strategies are (1) film coating, (2) encapsulation by spray drying or coacervation, (3) co-processing with excipients, and (4) crystal engineering by co-crystallization. Film coating and encapsulation work by acting as barriers between the hygroscopic active ingredients in the core and the environment, whereas co-processing with excipients works mainly by adding excipients that deflect moisture away from the active ingredients. Co-crystallization works by altering the crystal packing arrangements by introducing stabilizing co-formers. For hygroscopic pharmaceuticals, coating and co-crystallization are the most commonly employed strategies, whereas coating and encapsulation are popular for hygroscopic nutraceuticals (e.g., medicinal herbs, protein hydrolysates). Encapsulation is rarely applied on hygroscopic pharmaceuticals, just as co-crystallization is rarely used for hygroscopic nutraceuticals. Therefore, there is potential for improved hygroscopicity reduction by exploring beyond the traditionally used strategy.

Evaluation of Film-Coated Tablets of Ethyl Acetate Fraction of Uncaria gambir (Hunter) Roxb

“…The polyvinyl alcohol polymer molecule absorbs water and binds it with hydrogen bonds, preventing it from penetrating the core tablet. 30 Catechin dissolves well in the acid medium at pH 1.2 and buffer 4.5, although it dissolves slower in buffer medium at pH 6.8. This demonstrates that the pH of the dissolution medium affects the catechin's dissolution rate.…”

Fabrication and Characterization of Microcapsules Containing Eel Fish Oil (Anguilla marmorata (Q.) GAIMARD)

“…Spray drying is frequently employed in food and pharmaceutical industries, to turn liquid materials into dried powders, and it has been extensively utilized to create omega-3 PUFA microcapsules [7]. Compared to other drying techniques like freeze drying, extrusion, and complex coacervation, spray drying has some benefits, such as relatively low costs, the ability to work with heat-sensitive materials, easily accessible equipment, reliable efficiency, and the capability to manage the average particle size of the powders for spray dried emulsions [8]. In light of this background, eel fish oil is microencapsulated using a variety of binding agents to preserve its quality.…”

Effect of storage age and containers on the physicochemical degradation of guggul oleo-resin

“…Product development involves processing 13 , mixing of various ingredients 14 and even heating. Combination index 15 in drug formulation is vital for effectiveness and stability 16 , 17 . Quality deterioration of any natural product, including guggul during storage and transit is an important point for consideration 18 , on account of the loss of aromatic oils and bio-active compounds 7 .…”