Ph Sensitive In-Situ Gelling Gastro-Retentive Drug Delivery System Of Esomeprazole For Management Of Peptic Ulcer Disease

Abstract

Esomeprazole, a proton pump inhibitor recommended for the treatment of gastroesophageal reflux disease-related erosive esophagitis, is one of the frequently prescribed drugs for the treatment of peptic ulcer diseases. Owing to the poor oral bioavailability and half life of less than 2 hrs, the current work was aimed to formulate an in situ floating system for the delivery of Esomeprazole in a sustained manner using Xanthan Gum, Gelrite along with Calcium carbonate and citric acid with 3² factorial design. Xanthan gum, Gelrite and calcium carbonate were selected as independent variables. The prepared formulations were evaluated for viscosity, clarity, gelling strength, floating time, drug release and in-vivo gelation and floating study. All the batches have shown pH around 8 and good gelling capacity except E₁, E₂ and E₃. Viscosity and drug content of Raft formulation varied from 1343.33 to 7034.66 CP, 96.24 to 101.52 % respectively. The viscosity is positively influenced by concentration of Xanthan gum and Gelrite. Floating time differed from 5 seconds to 5 minutes where all formulations showed total floating time more than 12 hours except E₁, E₂ and E₃. In-situ gelation was observed at acidic pH with good gastric retention which was confirmed by gelation study conducted on Albino rats. X-Ray radiograph authenticated in-vivo gastric retention after administration of prepared in-situ gel. The release study indicates that present DDS delivers drug over a period of more than 12 hours. The factorial equation proved Xanthan Gum and Gelrite’s concentration is dominant causing drug release retardation while concentration of Calcium carbonate is not having any effect on drug release.