FORMULATION AND IN VITRO EVALUATION OF COMBINED FLOATING-BIOADHESIVE TABLETS OF IMATINIB MESYLATE

Objective: Gastro retentive drug delivery system (GRDDS) pertaining to its attributes like gastric retention time and the extended drug release profile has significantly improved patient compliance. The objective of the present study is to formulate and evaluate a stomach-specific floating-bioadhesive tablet of imatinib mesylate for prolonged residence in the stomach in the treatment of gastrointestinal stromal tumors (GIST).Methods: All the tablets were prepared with hydroxypropylmethylcellulose (HPMC), guar gum, sodium alginate, and carbopol using direct compression technique. Physical characterization, in vitro dissolution, the mucoadhesive force along with data analysis was done on each tablet. Results: The pre-compression characteristics of powder mixtures found to be satisfactory for all formulation batches. The results of physical evaluation for all batches were complying with pharmacopeia specification. The swelling index for all formulation batches was approximately 100% after 8 hours. The bioadhesive force (mean ± SD) reported in a range of 0.05 ± 0.09 to 0.18 ± 0.06 N/m2. It was observed that the release rate of tablets was decreased when the viscosity and concentration of the polymer were increased. Formulation batches IB1, IB2, IB4, IB5, IB6, IB9, IB10, IB11, and IB13 follows Higuchi Matrix model kinetics; whereas IB3, IB7, IB8, and IB12 follows Korsmeyer- Peppas model kinetics.Conclusion: Formulation batch IB9 reported a considerable swelling index, floating behavior, more bioadhesive strength with uniform drug release pattern. Therefore formulation batch IB9 was selected as optimized batch and were kept for further evaluation studies