ArticlePloS one2021
Preparation of solid dispersion systems for enhanced dissolution of poorly water soluble diacerein: In-vitro evaluation, optimization and physiologically based pharmacokinetic modeling.
Article in PloS one, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Who cites it
17 citing papers in PubMed, 35 citations in OpenAlex.
- Pluronic F-127/Propylene Glycol Binary Building Blocks for Novel Solid Dispersion Matrix: Industrial and Ecological Paradigm to Enhance Dissolution Profile of Dapagliflozin.Pharmaceutics · 2026Article
- Advances in Drug Delivery Science for Diacerein: Strategies to Enhance Solubility, Bioavailability, and Pharmacokinetic Performance.Pharmaceutics · 2025Review
- How Do Cryo-Milling and Lyophilization Affect the Properties of Solid Dispersions with Etodolac?Pharmaceutics · 2025Article
- Newly designed curcumin-loaded hybrid nanoparticles: a multifunctional strategy for combating oxidative stress, inflammation, and infections to accelerate wound healing and tissue regeneration.BMC biotechnology · 2025Article
- Formulation Strategy of BCS-II Drugs by Coupling Mechanistic In-Vitro and Nonclinical In-Vivo Data with PBPK: Fundamentals of Absorption-Dissolution to Parameterization of Modelling and Simulation.AAPS PharmSciTech · 2025Review
- An Investigation into the Effect of Maltitol, Sorbitol, and Xylitol on the Formation of Carbamazepine Solid Dispersions Through Thermal Processing.Pharmaceutics · 2025Article
- Solid Dispersions Obtained by Ball Milling as Delivery Platform of Etodolac, a Model Poorly Soluble Drug.Materials (Basel, Switzerland) · 2024Article
- Dissolution enhancement of Gefitinib by solid dispersion and complexation with β-cyclodextrins: In vitro testing, cytotoxic activity, and tablet formulation.Saudi pharmaceutical journal : SPJ : the official publication of the Saudi Pharmaceutical Society · 2024Article
- InvestigatingHeliyon · 2024Article
- Assessment of formulation variables of poor water soluble diacerein for its improved loading and anti-inflammatory activity.Drug delivery and translational research · 2023Article
- How to Improve Solubility and Dissolution of Irbesartan by Fabricating Ternary Solid Dispersions: Optimization and In-Vitro Characterization.Pharmaceutics · 2022Article
- Enhancing Atorvastatin In Vivo Oral Bioavailability in the Presence of Inflammatory Bowel Disease and Irritable Bowel Syndrome Using Supercritical Fluid Technology Guided by wbPBPK Modeling in Rat and Human.AAPS PharmSciTech · 2022Article
- Solubility and Permeability Enhancement of Oleanolic Acid by Solid Dispersion in Poloxamers and γ-CD.Molecules (Basel, Switzerland) · 2022Article
- Improved solubility and corneal permeation of PEGylated curcumin complex used for the treatment of ophthalmic bacterial infections.PloS one · 2022Article
- Long-term stability of clopidogrel solid dispersions-Importance of in vitro dissolution test.PloS one · 2022Article
- Article
- An Update of Anthraquinone Derivatives Emodin, Diacerein, and Catenarin in Diabetes.Evidence-based complementary and alternative medicine : eCAM · 2021Review
Corrections and comments
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Authors and funding
5 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Diacerein (DCN), a BCS II compound, suffers from poor aqueous solubility and limited bioavailability. Solid dispersion systems (SD) of DCN were prepared by solvent evaporation, using hydrophilic polymers. In-vitro dissolution studies were performed and dissolution parameters were evaluated. I-Optimal factorial design was employed to study the effect of formulation variables (drug:polymer ratio and polymer type) on the measured responses including; drug content (DC) (%), dissolution efficiency at 15 min (DE (15 min)%) and 60 min (DE (60 min)%) and mean dissolution time (MDT) (min). The optimized SD was selected, prepared and evaluated, allowing 10.83 and 3.42 fold increase in DE (15 min)%, DE (60 min)%, respectively and 6.07 decrease in MDT, compared to plain drug. DSC, XRD analysis and SEM micrographs confirmed complete amorphization of DCN within the optimized SD. Physiologically based pharmacokinetic (PBPK) modeling was employed to predict PK parameters of DCN in middle aged healthy adults and geriatrics. Simcyp® software established in-vivo plasma concentration time curves of the optimized SD, compared to plain DCN. Relative bioavailability of the optimized SD compared to plain drug was 229.52% and 262.02% in healthy adults and geriatrics, respectively. Our study reports the utility of PBPK modeling for formulation development of BCS II APIs, via predicting their oral bio-performance.
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