Surface dissolution UV imaging for characterization of superdisintegrants and their impact on drug dissolution.

Superdisintegrants are a key excipient used in immediate release formulations to promote fast tablet disintegration, therefore understanding the impact of superdisintegrant variability on product performance is important. The current study examined the impact of superdisintegrant critical material attributes (viscosity for sodium starch glycolate (SSG), particle size distribution (PSD) for croscarmellose sodium (CCS)) on their performance (swelling) and on drug dissolution using surface dissolution UV imaging. Acidic and basic pharmacopoeia (compendial) media were used to assess the role of varying pH on superdisintegrant performance and its effect on drug dissolution. A highly soluble (paracetamol) and a poorly soluble (carbamazepine) drug were used as model compounds and drug compacts and drug-excipient compacts were prepared for the dissolution experiments. The presence of a swelled SSG or CCS layer on the compact surface, due to the fast excipient hydration capacity, upon contact with dissolution medium was visualized. The swelling behaviour of superdisintegrants depended on excipient critical material attributes and the pH of the medium. Drug dissolution was faster in presence compared to superdisintegrant absence due to improved compact wetting or compact disintegration. The improvement in drug dissolution was less pronounced with increasing SSG viscosity or CCS particle size. Drug dissolution was slightly more complete in basic compared to acidic conditions in presence of the studied superdisintegrants for the highly soluble drug attributed to the increased excipient hydration capacity and the fast drug release through the swelled excipient structure. The opposite was observed for the poorly soluble drug as potentially the improvement in drug dissolution was compromised by drug release from the highly swelled structure. The use of multivariate data analysis revealed the influential role of excipient and drug properties on the impact of excipient variability on drug dissolution.

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Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.