Formulation and in Vitro Evaluation of Ibrutinib Extended-Release Matrix Tablets

Abstract

The present study was aimed at the formulation and in vitro evaluation of Ibrutinib extended-release matrix tablets using different polymers in varying ratios to achieve a controlled and prolonged drug release profile. Extended-release formulations offer several advantages, including reduced dosing frequency, improved patient compliance, and maintenance of therapeutic drug levels over an extended period.

A series of Ibrutinib matrix tablet formulations (F1–F9) were prepared using suitable hydrophilic polymers at different concentrations by direct compression method. The prepared powder blends were evaluated for pre-compression parameters such as angle of repose, bulk density, tapped density, Carr's index, and Hausner's ratio. The compressed tablets were further assessed for post-compression parameters including hardness, thickness, weight variation, friability, and drug content uniformity. All formulations exhibited satisfactory pre-compression and post-compression characteristics and were found to be within the limits specified by the Indian Pharmacopoeia (IP).

The in vitro dissolution studies were carried out to evaluate the drug release behaviour of the formulated tablets. The results indicated that the type and concentration of polymers significantly influenced the release pattern of Ibrutinib. Among all the formulations, formulation F6 demonstrated the most desirable extended-release profile and was considered the optimized formulation. F6 showed a cumulative drug release of 99.96% over a period of 12 hours, providing a controlled and sustained release pattern compared to the other formulations.

The findings of the study suggest that the optimized formulation (F6) is a promising extended-release matrix tablet of Ibrutinib with acceptable physicochemical properties and excellent in vitro drug release characteristics. Therefore, the developed formulation has the potential to improve therapeutic efficacy and patient compliance.