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 < 0.0465) and promoted onset of action compared to Diacerein® capsules at 0.5 hr. It could be concluded that optimized ODT could be promising for enhanced dissolution and rapid absorption of DCN from the oral cavity.
Highlights
Osteoarthritis (OA) is the most commonly known type of arthritis affecting middle aged and elderly populations worldwide
Hardness of orally disintegrating tablets (ODTs) is preferable to range between 2–8 Kg [24], where it provides sufficient mechanical strength and preserved porosity for quick disintegration and wetting times
ODTs loaded with optimized DCN-SDs were successfully prepared by the direct compression method and in-vitro evaluated
Summary
Osteoarthritis (OA) is the most commonly known type of arthritis affecting middle aged and elderly populations worldwide. It is the predominant cause of joint pain and one of the most leading reasons for disability; as it affects joints of the hands, feet, knees, hips and spine [1]. OA is progressive and worsens over time, often resulting in chronic joint pain and stiffness which can become severe enough to make daily tasks difficult [2]. It is treated clinically via analgesia including both topical and oral non-.
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