Functionality of wet-granulated disintegrant in comparison to directly incorporated disintegrant in a poorly water-soluble tablet matrix

Tablet disintegration is crucial for drug release and subsequent systemic absorption. Although factors affecting the disintegrant’s functionality have been extensively studied, the impact of wet granulation on the performance of disintegrants in a poorly water-soluble matrix has received much less attention. In this study, the disintegrants, crospovidone (XPVP), croscarmellose sodium (CCS) and sodium starch glycolate (SSG), were wet-granulated with dibasic calcium phosphate dihydrate as the poorly water-soluble matrix and polyvinylpyrrolidone as the binder.

Highlights

• Wet granulation affected the functionality of disintegrants to a different extent.
• The disintegrant’s disintegration mechanism affected its sensitivity to wet granulation.
• A swelling disintegrant was more affected by wet granulation.

The effect of wet granulation was studied by evaluating tablet tensile strength and disintegratability. Comparison between tablets with granulated or ungranulated disintegrants as well those without disintegrants were also made. Different formulations showed different degrees of sensitivity to changes in tablet tensile strength and disintegratability post-wet granulation. Tablet tensile strength decreased for tablets with granulated disintegrant XPVP or CCS, but to a smaller extent for SSG.

While tablets with granulated XPVP or CCS had increased disintegration time, the increment was lesser than for SSG, suggesting that wet granulation impacted a swelling disintegrant more. The findings showed that tablets with wet-granulated disintegrant had altered the disintegrant’s functionality. These findings could provide better insights into changes in the disintegrant’s functionality after wet granulation.

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Materials

The disintegrants investigated were crospovidone (XPVP; Kollidon CL, BASF, Germany), croscarmellose sodium (CCS; Ac-Di-Sol, FMC BioPolymer, USA) and sodium starch glycolate (SSG; Primojel, DFE Pharma, Germany). DCP (Di-Cafos D9, Budenheim, Germany) and polyvinylpyrrolidone (Kollidon 25, BASF, Germany) were used as the diluent and binder, respectively. Magnesium stearate (MgSt; M−125, Productos Metalest S.L., Spain) was used as a lubricant in tableting.

Natalia Veronica, Erinn Si Min Lee, Paul Wan Sia Heng, Celine Valeria Liew, Functionality of wet-granulated disintegrant in comparison to directly incorporated disintegrant in a poorly water-soluble tablet matrix, International Journal of Pharmaceutics, Volume 661, 2024, 124467, ISSN 0378-5173, https://doi.org/10.1016/j.ijpharm.2024.124467.

Read also our introduction article on “Disintegrants“ here: