Abstract

DESIGN AND EVALUATION OF NOVAL LEVOCETRIZINE ORODISPERSIBLE TABLETS USING DUAL SUPERDISINTEGRANT

Abdullah A. A. Ali*, Thamer H. S. Odhah, Esmail, T. N. Al-gaolbi, Abdullah S. A. Ahmed, Nagmi H. M. A. Anaam, Issa H. Y. Aqlan, Moein Y. Q. Al-shami, Mohammed G. A. Al-saidi and Qeis M. A. Alsamwi

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Abstract

Background: Fast-dissolving tablets (FDTs) have emerged as an innovative and patient-friendly drug delivery system, particularly beneficial for individuals who experience difficulties swallowing conventional tablets, such as pediatric, geriatric, and psychiatric patients. This study focuses on the development and optimization of FDTs for Levocetirizine dihydrochloride, a second-generation antihistamine used for the treatment of allergic rhinitis and chronic idiopathic urticaria. The primary objective was to enhance the drug's therapeutic efficacy, improve bioavailability, and ensure a rapid onset of action by optimizing the disintegration and dissolution properties of the tablets. Method: A total of eight formulations (F1–F8) were prepared using the direct compression method, incorporating various superdisintegrants such as sodium starch glycolate (SSG), crospovidone, and croscarmellose sodium in different concentrations and combinations. The formulations were evaluated based on their pre-compression properties (angle of repose, bulk density, compressibility index) and post-compression parameters (tablet hardness, friability, weight variation, disintegration time, wetting time, and drug content). In addition, in vitro dissolution studies were conducted to assess drug release profiles. Result: The results demonstrated that all formulations met the basic quality criteria for FDTs, but significant differences were observed in their performance. Formulation F1, which combined sodium starch glycolate (6%) and crospovidone (5%), was identified as the most promising due to its superior characteristics. It exhibited the shortest wetting time (12 seconds) and disintegration time (6 seconds), alongside a high dissolution rate, releasing 95% of the drug within the first few minutes of testing. These properties ensure a rapid onset of therapeutic action, making it ideal for patients requiring immediate relief. Conclusion: the development of Levocetirizine FDTs using advanced superdisintegrants presents a valuable alternative for improving patient compliance and drug efficacy. Formulation F1 was determined to be the best among the tested formulations, combining excellent disintegration, fast dissolution, and robust mechanical properties. This study underscores the potential of FDTs in addressing the needs of diverse patient populations and sets a benchmark for further research in the field of antihistamine delivery systems.

Keywords: Evaluation, Formulation, Fast-dissolving tablets, Levocetirizine dihydrochloride.