Hydrodynamically balanced bilayer tablets of glycerol monooleate coated amoxicillin trihydrate: a novel approach to prolong the local action by gastric retention.

Abstract

This investigation describes the development of an intragastric drug-delivery system for Amoxicillin trihydrate for treatment of Helicobacter pylori. Gram-negative bacterium Helicobacter pylori are found in colonized gastric mucosa or adherent to the epithelial of the stomach associated with a lifelong extracellular persistence of the microorganism. Bilayer tablets were prepared by direct compression technique using polymers hydroxypropylmethyl cellulose (Methocel K4M), Carbopol 971P and other standard excipients. Calcium carbonate was incorporated as a gas-generating agent. The effect of polymers, diluents (lactose & microcrystalline cellulose) on drug release profile, floating properties were investigated. The tablets were evaluated for thickness, hardness, friability, swelling index, mucoadhesion and in vitro drug release. Polymer with lower viscosity (hydroxyl propyl methyl cellulose K4M) was found to be beneficial than higher viscosity polymer (Carbopol 971P) in improving the release properties of gastric floating drug delivery system. Incorporation of Carbopol in formulation helped in maintaining buoyancy of system. The mechanism of drug release was found to follow Higuchi matrix order release. The formulation A4 was optimized based on floating time and in vitro drug release (97.60 %). In conclusion, the prolonged gastrointestinal residence time and prolonged release might make contribution to H.Pylori clearance.