FORMULATION, OPTIMIZATION, AND IN-VITRO EVALUATION OF GASTRORETENTIVE FLOATING TABLETS OF LAFUTIDINE USING NATURAL POLYMERS
Author
Mohin Khan, Dr. Gurpreet Singh, Dr. Rajesh Sharma, Dr. Praveen Goyal
Abstract
This study aims to design, develop, and evaluate gastroretentive floating tablets of lafutidine a potent anti-ulcer drug to prolong gastric residence time and enhance therapeutic efficacy. Preformulation characterization confirmed the identity, purity, and appropriate lipophilicity (log P = 3.8) of lafutidine. Tablets containing 10 mg of lafutidine were prepared via wet granulation using varying concentrations of synthetic (HPMC K100) and natural (chitosan) hydrophilic swellable polymers. Pre-compression evaluations demonstrated excellent flow properties for all powder blends. Post-compression parameters confirmed compliance with official pharmacopeial specifications regarding weight variation, hardness (4.8-6.5kp), friability (< 0.6%), floating lag time (32–82 sec), total floating time (> 12 hours for optimized batches), and drug content uniformity (97.9–100.2%). In-vitro dissolution studies over 12 hours in 0.1 N HCl (pH 1.2) identified batch F4 (50 mg HPMC K100) and batch F7 (30 mg Chitosan) as optimal configurations, achieving cumulative drug releases of 84.56% and 98.25%, respectively. Kinetic modeling of the optimized batch F7 revealed that drug release followed the Higuchi model (R2 = 0.942), indicating diffusion-controlled matrix release. Accelerated stability testing for 90 days) established the robustness and stability of the formulation, with similarity factors (F2) remaining above 50.
Keywords
Lafutidine, Floating Drug Delivery System (FDDS), HPMC K100, Chitosan, Release Kinetics, Gastroretentive.
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References
Gastroretentive floating tablets of lafutidine were successfully formulated using HPMC K100 and chitosan. Batch F4 (containing 50 mg HPMC K100) and batch F7 (containing 30 mg Chitosan) exhibited ideal buoyancy, excellent mechanical properties, and extended release profiles over 12 hours. With superior release kinetics obeying the Higuchi diffusion model and proven accelerated stability, the optimized chitosan-based floating matrix tablet demonstrates strong potential for improved clinical efficacy in anti-ulcer therapy.