FORMULATION AND EVALUATION OF BUCCAL TABLETS OF POORLY SOLUBLE DRUG ZALEPLON

In the present investigation, an attempt was made to formulate mucoadhesive buccal tablets containing Zaleplon for the treatment of insomnia. The tablets were prepared by direct compression method using sodium CMC, crospovidone, and other excipients. The buccal route was selected to enhance bioavailability, absorption and patient compliance while bypassing first-pass metabolism and providing a faster onset of action. The formulation was optimized using Central Composite Design by selecting sodium CMC and crospovidone as independent variables and mucoadhesive strength and % drug release as dependent variables. Various formulations were prepared by altering polymer and superdisintegrant concentrations along with binder, lubricant, glidant and diluent. The powder blend was evaluated for pre- compression parameters and the compressed tablets were tested for post-compression parameters such as weight variation, thickness, hardness, friability, drug content, swelling index, mucoadhesive strength and In-vitro drug release. The optimized formulation (OPT-F) showed a mucoadhesive strength of 13.62 g and 93.15% drug release within 30 minutes. The results of the evaluation tests obtained were within Pharmacopoeial limits. Stability studies indicated no significant change in physical or chemical parameters. Hence, Zaleplon buccal tablets were successfully developed for immediate release with enhanced bioavailability and improved patient compliance.