Deferasirox Tablet Formulation Using Polysorbate 80

The patent employs a composite material approach by combining Deferasirox with specific excipients including hydroxypropyl cellulose (HPC), microcrystalline cellulose (MCC), and polysorbate 80. This composite formulation creates a matrix that enhances the dissolution properties of the poorly soluble active ingredient while maintaining its pharmacokinetic advantages. The HPC forms a gel matrix that controls drug release, MCC provides disintegration and absorption enhancement, and polysorbate 80 acts as a surfactant to improve wetting and dissolution of the hydrophobic drug particles.

The patent applies parameter changes by carefully optimizing the ratios and amounts of each excipient in the formulation. Specifically, it uses HPC in amounts of 5-20% w/w, MCC in 60-80% w/w, and polysorbate 80 in 0.5-5% w/w. The processing parameters are also optimized: granulation with 3-10% w/w binder solution, drying at controlled temperatures, and specific granule size ranges (0.5-2.0 mm). These parameter optimizations enhance dissolution rate and bioavailability while maintaining manufacturing feasibility through standard pharmaceutical equipment and processes.

The patent uses hydroxypropyl cellulose as an intermediary substance that mediates between the poorly soluble Deferasirox and the aqueous gastrointestinal environment. HPC forms a hydrophilic gel matrix around the drug particles, facilitating their interaction with gastrointestinal fluids. Polysorbate 80 acts as a surfactant intermediary that reduces surface tension and improves wetting of drug particles. These intermediary substances bridge the solubility gap, enabling adequate absorption and reliable therapeutic effect without requiring changes to the active ingredient itself.