PREPARATION AND EVALUATION OF ONCE-DAILY FLOATING GMO-ALGINATE MICROSPHERES CONTAINING FAMOTIDINE

Objective: In this work, a gastro-retentive floating microsphere delivery system composed of Drug/Glyceryl mono-oleate (GMO) embedded in Ca-alginate gas-generated matrix was designed to improve the bioavailability slightly-soluble model drug Famotidine. Methods: The water/Oil emulsion method used prepare Famotidine floatable microspheres, and formulation variables such as Alginate: GMO ratio, bicarbonates concentration, loading concentration were investigated. Conventional techniques, including DSC, XRD FTIR performed confirm compatibility with Alginate polymers. Real-Time X-ray Radiography for vivo imaging microspheres using rabbits an animal model. HPLC spectroscopic technique determine plasma after oral administration Alginate-GMO loaded microspheres. Results: Floating (0.75:1:0.25) w/w/w showed remarkable entrapment efficiency (>98%), good buoyancy (>84) prolonged vitro release properties (>24 hours). XRD, techniques no evidence interaction between or GMO. Imaging that capsules containing Famotidine-Alginate not detected 3 h administration, while Famotidine-GMO-Alginate can be more than 12 h, indicating superior gastric retention properties. pharmacokinetic parameters calculated Famotidine: GMO-Alginate, alginate compared plain over 24 period. GMO-Alginate exhibited controlled absorption Tmax 6.0 vs. 3.0 2.0 h; Cmax 124.9±0.9 323.7±0.4and 458.6±0.5 ng/ml; AUC0-24 2153.025±6.7 1650.4±1.9 1110.725±2.1 ng/ml drug, respectively, reflecting increase formulations free drug. Conclusion: Prolonged time sustained GMO-alginate suggest it could provide valuable dosage form drugs.