Development and Characterization of Multifunctional Directly Compressible Co-processed Excipient by Spray Drying Method

Abstract

The present investigation was carried out to develop and characterize a multifunctional co-processed excipient for improving the compressibility of poorly compressible drugs. Etodolac was used as a model drug. Microcrystalline cellulose (MCC), lactose monohydrate (lactose), and StarCap 1500 (StarCap) were selected as components of the co-processed excipient. The spray drying method was used for co-processing of excipients. D-optimal mixture design was applied to optimize the proportion of component excipients. Statistical analysis of the D-optimal mixture design revealed that all response variables were significantly affected by the independent variables (p value < 0.05). Optimized composition was obtained from the desirability function. The optimized composition of the co-processed excipient was found to be 30% MCC, 25% lactose, and 45% StarCap. This optimized batch was evaluated for flow properties, compressibility parameters such as Kawakita's and Kuno's equation and Heckel's equation, and dilution potential. Evaluation parameters for flow properties (angle of repose, Carr's index, and Hausner's ratio) suggested excellent flow character. The parameters of Kawakita's and Kuno's equation and Heckel's equation suggested improvement in the compressibility of the model drug. Dilution potential was found to be 40%, and based on that, tablets of the model drug were formulated and evaluated for general evaluation parameters of tablets. All the parameters were found to be within the acceptance criteria which concluded that the multifunctional directly compressible co-processed excipient was prepared successfully that improved the compressibility of the poorly compressible model drug etodolac along with spray drying as an efficient method for the preparation of co-processed excipient.

Impact of binder as a formulation variable on the material and tableting properties of developed co-processed excipients

“…Research into co-processing of excipients has yielded products with diverse functionalities and performance attributes. These functionalities include orally disintegrating ability [6,7], improved dilution potential [8], rapid disintegration [9], enhanced direct compression functionality [10], multifunctional excipient [4,8], improved tabletability [11], and improved dispersibility [12].…”

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“…Melt granulation 10, 12, 15 , co-precipitation 16 , solvent evaporation method 6,17,18 , freeze-thaw technique, kneading method 19 , melt fusion method 14 , Spray-drying 7,9,20,21 , wet granulation [22][23] , spheronization 5 , co-milling 8,24 , and co-crystallization can be used for coprocessing. Melt granulation method include first melting of meltable polymer and add blend in it mixed properly followed by sieving of hot mass and then cooling.…”

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).…”

“…Hence, the method of co-processing influenced the outcome of the particle size of the generated co-processed excipients. Coprocessing by spray-drying has yielded a significant increase in particle size compared to other methods (Chauhan et al, 2016;Rojas and Kumar 2011;Sharma et al, 2015;Vanhoorne et al, 2014). Engineering the particle size during co-processing plays a key role in defining the functionality of the co-processed excipient.…”

“…Dilution potential is a measure of the material's ability to compress large amounts of a poorly compressible drug and still retain its compressibility (Adeoye and Alebiowu 2014;Camargo, 2011;Chauhan et al, 2016). The dilution potential of a material gives us an insight into the tablet formula and how much of the poorly compressible drug can be loaded to give robust tablets with the DC excipient.…”