Solubility enhancement, formulation development and evaluation of extended-release tablets of BCS class IV drugs ticagrelor
Abstract
Objective: The study was done to make extended-release tablets of Ticagrelor, a BCS Class IV drug that has low solubility and poor bioavailability. The goal was to improve solubility using hydrotropic solid dispersions and to achieve sustained release for longer drug action. Methods: A A ternary mixture of nicotinamide, sodium salicylate and resorcinol in 1:1:2 ratio was used to increase solubility. Solid dispersions were prepared by solvent evaporation and compressed into tablets with HPMC K100M and ethyl cellulose. A 3² factorial design was used for optimization, with hardness and 12-hour drug release as the main responses. Results: Solubility of Ticagrelor in water was 9.43 µg/mL, while the ternary hydrotrope gave 225.8 ± 11.4 µg/mL (23.94 times higher). The optimized batch TF5 with 75 mg HPMC K100M and 35 mg ethyl cellulose showed hardness of 8.6 ± 0.3 kg/cm² and 95.8 ± 3.7% release at 12 h. Model predictions were close to experimental values with prediction errors of +1.06% for hardness and +0.23% for drug release). Stability studies for 6 months showed no major changes in hardness, friability, drug content or dissolution. Conclusion: The optimized tablets improved solubility and gave controlled release for 12 h. This may help in reducing dosing frequency and improving patient compliance in cardiovascular therapy. Further in vivo studies are required to confirm the effect.
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