FORMULATION AND EVALUATION OF ORALLY DISINTEGRATION TABLET OF DOLASETRON MESYLATE

Rushikesh Nikam*, Prof. Vinayak Munde

The present study aimed to formulate and evaluate orally disintegrating tablets (ODTs) of dolasetron mesylate, a selective serotonin 5-HT3 receptor antagonist used for the prevention and treatment of nausea and vomiting associated with chemotherapy, radiotherapy and postoperative conditions. Conventional oral dosage forms may be difficult to administer in nauseated, pediatric, geriatric, dysphagic or bedridden patients, and they may delay onset because of the time required for disintegration and dissolution. Therefore, the study focused on developing a patient-friendly solid oral dosage form capable of rapid disintegration without water, adequate mechanical strength and improved dissolution performance. Dolasetron mesylate ODTs were prepared by the direct compression method using crospovidone, croscarmellose sodium and sodium starch glycolate as superdisintegrants, with mannitol and microcrystalline cellulose as diluent and compressibility-improving excipients. Preformulation studies confirmed that the drug was white to off-white, odorless, crystalline and freely soluble in water, methanol and 1N hydrochloric acid. UV spectrophotometry showed lambda max at 281 nm, and the calibration curve was linear over 2-10 µg/mL with the regression equation y = 0.0503x - 0.0035. FTIR and DSC compatibility studies showed retention of characteristic drug peaks and no evidence of significant drug-excipient interaction. A 3-level factorial design was applied to study the influence of crospovidone and croscarmellose sodium on disintegration time, tablet hardness, drug release and wetting time. The optimized formulation showed acceptable weight variation, friability below 1%, rapid disintegration, drug content of 98% and 95.33% cumulative drug release within 5 min. Stability data for three months indicated minimal changes in drug content, disintegration time, dissolution, hardness, wetting time and friability. The findings demonstrate that dolasetron mesylate can be successfully developed as an ODT using direct compression and optimized superdisintegrant concentrations.