FORMULATION AND TECHNOLOGY OF ENTERIC AND FOAM-FORMING RABEPRAZOLE TABLETS

Abstract

              Helicobacter pylori (H. pylori) is considered the main cause of gastroduodenal diseases. For the eradication of Helicobacter, triple therapy is actively used, the so-called "Gold standard", which combines antibiotics and proton pump inhibitors. Among the innovative delivery systems for the gastroenterological drug formulationsfoams appear to be of particular interest.Foams are light systems. Unlike solid medicationforms, theyare not simply depositedin the gastrointestinal mucosa, on the contrary, they grow in volume,have a large contact surface, completely cover the mucous membrane, and penetrate it. Targeted delivery, enteric-soluble and foam-forming tablets have been developed from the "Gold standard"ingredients with a significant amount of antacids. The study aimed to determine the composition of enteric-coated and foam-forming rabeprazole sodium tablets and process  their  technology. Based on biopharmaceutical research, the optimal composition of foam-forming powder has beenformulated as an auxiliary substance for the preparation of foam-forming tablets, with the following composition: sodium lauryl sulfate, lecithin, and METHOCEL™ E6 PLV (0.75:1.25:5) 7%, Xanthan, and guar gum in a ratio of  1:1 - 2%, Isomalt 10%. Based on biopharmaceutical studies, the formulations of enteric-soluble and foam-forming core,tabletcoating composition, and manufacturing technologyof rabeprazolehave beendrawn up. The physical, chemical, and technological properties of foam-forming and enteric-coated rabeprazole tablets have been studied. And, we have ascertainedthat the technology appliedfor their manufacturing meets the quality requirements of this medication: its appearance, dosing accuracy, mechanical strength, solubility, foaming, stability, etc. The dissolution profile of rabeprazole tablets, generated at pH 1.2 and 6.8,has been studied. We have ascertainedthat Active Pharmaceutical Ingredient (API)is almost 100% resistant to the acidic environment: the amount of API released during 2 hours in the acid area is insignificant and varies within 3%. The API of the tablet is completely released within 30 min at pH 6.