The aim of this study was to investigate the functionality of two disintegrants (crospovidone and croscarmellose sodium) in tablet formulations processed via roll compaction and subsequent tableting. The influence of different fillers and the effect of sodium lauryl sulfate on the disintegration process were studied using full factorial design. For a direct comparison of disintegrant functionality, the center point formulations were manufactured via direct compression. Tablet characteristics, such as tensile strength, solid fraction, disintegration time and mechanism, and dissolution profile were determined. The results allow the conclusion that the functionality of the disintegrants is impaired by dry granulation. Both the disintegration mechanism and the disintegration time were different when comparing tablets made after dry granulation and by direct compression. The effect was more pronounced on the functionality of crospovidone than on that of croscarmellose sodium. In addition, sodium lauryl sulfate showed a notable influence on all tablet properties due to its lubricating effect. The variation of the filler also had a remarkable effect on the tablet characteristics. The results link excipient functionality to drug product properties depending on the applied manufacturing process and could contribute to extend the Manufacturing Classification System to excipient characteristics.
Keywords: Direct compression; Dry granulation; Excipients; Manufacturing Classification System; Tablet disintegration.
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