Development of orally disintegrating tablets containing solid dispersion of a poorly soluble drug for enhanced dissolution: In-vitro optimization/in-vivo evaluation

Shahinaze A Fouad, Fady A Malaak, Mohamed A El-Nabarawi and Khalid Abu Zeid

PLOS ONE, 2020, vol. 15, issue 12, 1-17

Abstract: Diacerein (DCN), a potent anti-inflammatory API used to treat osteoarthritis yet, it suffers from poor water solubility which affects its oral absorption. Unabsorbed colonic DCN is converted into rhein, which is responsible for laxation as a main side effect of DCN treatment. Therefore, in this study orally disintegrating tablets (ODTs) loaded with optimized DCN solid dispersion system were prepared using different co-processed excipients (Prosolv® ODT, Pharmaburst® 500 and F-melt®), aiming to achieve improved solubility, rapid absorption and consequently limited amount of rhein reaching the colon. Prepared ODTs were evaluated for physical characteristics, in-vitro drug release, disintegration and wetting times. Dissolution parameters; dissolution efficiency percent at 10 (DE (10 min)%) and 30 (DE (30 min)%) min and mean dissolution time (MDT) were determined. The optimized ODT showed 1.50 and 1.12 fold increase in DE (10 min)% and DE (30 min)%, respectively and 2 fold decrease in MDT, compared to Diacerein® capsules. In-vivo anti-inflammatory effect of optimized ODT, using rat paw edema revealed significant increase in edema inhibition (p

Date: 2020
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Persistent link: https://EconPapers.repec.org/RePEc:plo:pone00:0244646

DOI: 10.1371/journal.pone.0244646

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