FORMULATION AND EVALUATION OF EZETIMIBE LOADED CHEWABLE TABLETS IN THE TREATMENT OF HYPERLIPIDEMIA

Arya Modi* and Bansi Zalavadia

ABSTRACT

The study aimed to develop and evaluate chewable tablets of Ezetimibe to improve its solubility and patient compliance. A β-Cyclodextrin (β-CD) inclusion complex was prepared in three different molar ratios to enhance the drug‟s aqueous solubility, with the 1:1 ratio showing the highest solubility improvement. This was confirmed by DSC and pXRD analyses, which indicated reduced crystallinity, while FTIR confirmed no significant drug–excipient interactions. Tablets were formulated using direct compression, incorporating the optimized inclusion complex. A 3² full factorial design was employed to optimize the formulation, using HPMC K100 as a binder (X1) and Croscarmellose Sodium as a superdisintegrant (X2), with tablet hardness (Y1) and cumulative drug release (%CDR) (Y2) as dependent variables. The tablets were evaluated for both pre- and post-compression parameters. Among all batches, Batch F6 exhibited the best results, with a hardness of 6.2 kg/cm² and 99.48% drug release, complying with pharmacopeial standards. Stability testing under ICH guidelines confirmed the formulation‟s physical and chemical stability. Overall, the study successfully developed a stable and effective chewable tablet formulation of Ezetimibe.

Keywords: Ezetimibe, ?-Cyclodextrin, 32factorial design, solubility enhancement, inclusion complex, FTIR, DSC, 3² Full factorial design, CDI.