Formulation and Evaluation of Mizolastine Fast-Dissolving Tablets by Direct Compression

Abstract

Fast-dissolving tablets are patient-oriented oral dosage forms designed to disintegrate rapidly in the oral cavity with minimal or no requirement for water. They are particularly useful for patients who experience difficulty swallowing conventional tablets and may improve convenience and acceptability of oral drug administration. Mizolastine is a second-generation selective histamine H1-receptor antagonist used for the symptomatic management of allergic rhinitis and chronic idiopathic urticaria. The present study was undertaken to formulate and optimize Mizolastine fast-dissolving tablets using the direct-compression technique. Preliminary formulation trials were performed using different superdisintegrants, including Indion 414, Kyron T-314, croscarmellose sodium (CCS), and sodium starch glycolate (SSG). Based on preliminary performance, CCS and SSG were selected for further formulation optimization, while microcrystalline cellulose (MCC) was used as a directly compressible diluent and binder. Nine formulations (F1–F9) were prepared according to a 3² factorial design by varying CCS and SSG concentrations at three levels. The prepared formulations were evaluated for pre-compression flow properties and post-compression parameters including thickness, diameter, weight, crushing strength, friability, wetting time, disintegration time, drug content, and in-vitro drug release. FT-IR spectroscopy was used to assess drug–excipient compatibility. The analytical method showed a linear response for Mizolastine in phosphate buffer pH 6.8 at 288 nm, with an R² value of 0.999. FT-IR analysis indicated the absence of significant chemical interaction between Mizolastine and the selected excipients. Among the factorial batches, F9 exhibited the most favorable overall performance, with a disintegration time of 18 ± 0.6 s, wetting time of 21 ± 0.7 s, drug content of 98.88 ± 0.22%, friability of 0.39 ± 0.02%, crushing strength of 4.0 ± 0.1 kg/cm², and cumulative in-vitro drug release of 97.61 ± 0.25%. The findings demonstrate that appropriate combinations of superdisintegrants and directly compressible excipients can successfully produce Mizolastine fast-dissolving tablets with rapid disintegration, satisfactory mechanical strength, and efficient drug release.