Co-proccessed excipients with enhanced direct compression functionality for improved tableting performance

Abstract

It is necessary to have excipients with excellent functional properties to compensate for the poor mechanical properties and low aqueous solubility of the emerging active ingredients. Therefore, around 80% of the current drugs are not suitable for direct compression and more advanced excipients are required. Further, conventional grades of excipients cannot accommodate the technologically advanced high speed rotary tablet presses which require a powder with excellent flow, good compressibility, compactibility, particle size distribution and homogeneity of the ingredients. Co-processed excipients have been created to enhance the functional properties of the excipients and reduce their drawbacks. Co-processing is defined as the combination of two or more excipients by a physical process. Co-processed excipients are adequate for direct compression since they become multifunctional and thus, their dilution potential is high eliminating the need for many excipients in a formulation. In some cases, they are able to hold up to 50% of the drug in a formulation rendering compacts of good tableting properties. This study describes and discusses the functionality enhancement of commercial and investigational excipients through co-processing.

Novel application of hydroxypropyl methylcellulose to improving direct compaction properties of tablet fillers by co-spray drying

“…A majority of commercially available co-processed excipients are produced by spray drying. [3][4][5][6] Co-spray drying uses a one-step continuous process to dry and agglomerate multi-component powders, which reduces the number of unit operations and thus improves These features altogether offer obvious benefits for the development of co-processed excipients.…”

Choice of excipients for gelly-like pulp prepared ex tempore “on a spoon”– “placebo” and with sartans

“…While dissolving upon contact with water, lactose creates free cavities in powder facilitating, thereby, the penetration of humidity within the entire carrier volume. To achieve fast swelling, various disintegrants were applied as commercial mixtures of co-processed auxiliary substances 23,24 . Co-processed excipients are usually proposed as a good option not only for easier manufacturing but also due to their enhanced organoleptic properties, including taste, smell, texture and mouth feel.…”

Comparative analysis of co-processed starches prepared by three different methods

“…A combination of a plastic and brittle deforming material produces a co-processed excipient with desirable attributes for tableting (Wang et al, 2015). Many co-processing methods have been employed, including spray drying (Chauhan et al, 2016;Rojas and Kumar, 2011;Sharma et al, 2015), codrying (Mshelia et al, 2015;Olowosulu et al, 2011) wet massing, spheronisation, melt extrusion (Goyanes et al, 2011), co-precipitation (Kittipongpatana and Kittipongpatana 2011), co-grinding (Adeoye and Alebiowu, 2014a;Katsuno et al, 2013), wet-, dry-and spray-granulation (Daraghmeh et al, 2010) and coprocessing by crystal coating (Vanhoorne et al, 2014) among which spray drying is the most widely used and successful strategy (Rojas et al, 2012).…”

“…The outcome of this intervention has led to the development of a single-bodied composite excipient with improved functionalities like compressibility, flowability, dilution potential etc. (Nachaegari and Bansal 2004;Rojas et al, 2012). A combination of a plastic and brittle deforming material produces a co-processed excipient with desirable attributes for tableting (Wang et al, 2015).…”