Formulation And Evaluation of Rebamipide Gastroretentive Floating In-Situ Gelling System for An Oral Controlled-Release Dosage Form (Research Article)

Author(s): M. Rajesh, B. Rahul, and Shayeda*

Abstract: This study focuses on developing a novel floating in-situ gel system for the controlled delivery of Rebamipide (REB), a gastroprotective agent used to treat ulcers and gastritis. REB has a short half-life of 1.5 hours, requires 100 mg thrice daily, and shows low oral bioavailability (<10%) as a BCS class IV drug. To enhance gastric residence time and modulate drug release, a gastro-retentive floating in-situ gel was formulated. These polymeric systems remain in solution before administration and undergo gelation in the acidic stomach environment; sodium citrate was incorporated to prevent premature gelation. Thirteen formulations (F1-F13) were developed using varying concentrations of sodium alginate, gellan gum, HPMC K4M, and HPMC K100M. Among them, formulation F12 showed optimal performance, achieving 97.9% drug release over 5 hours and containing 1% w/v sodium alginate, 0.5% gellan gum and 1.5% w/v HPMC K4M. FTIR analysis confirmed the compatibility and interaction profile of the drug with the selected excipients. F12 was optimised based on drug release, gel strength, floating behaviour, buoyancy, density and swelling index, all of which showed satisfactory results. Dissolution data fitted the Korsmeyer-Peppas model (R2+=0.982), with an n value of 0.765, indicating that the optimised formulation pattern of release was preceded by Fickian diffusion. Stability studies of F12 revealed no changes in appearance, viscosity, drug content or floating time throughout the storage period.

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