Preparation and Evaluation of Mucoadhesive Microspheres of Amoxicillin Trihydrate and Potassium Clavulanate to Eradicate H. Pylori in Treatment of Gastric Ulcer

摘要

Mucoadhesive microspheres which are referred to as the Adhesive Micromatrix System and which consist of a drug and an adhesive polymer powder such as a cross-linked polyacrylic acid derivative dispersed in a waxy base. It has been confirmed that these mucoadhesive microspheres have the ability to adhere to the stomach wall and thereby remain in the gastrointestinal tract for an extended period. It is expected that mucoadhesive microspheres containing anti-H.pylori agents will provide potent anti-H.pylori activity. The Amoxicillin mucoadhesive microspheres, Potassium Clavulanate mucoadhesive microspheres were prepared by an emulsification/evaporation method. In this accurately weighed quantity of ethyl cellulose was dissolved in acetone; drug and carbopol 93 4P powder were added to the ethyl cellulose solution under magnetic stirring and the mixture was blended. Then the suspension was slowly dispersed liquid paraffin containing Span 80 at a stirring rate of 600 rpm using propeller. After emulsification, acetone was evaporated gradually and microspheres were formed. The purpose of this study was to design mucoadhesive microspheres containing amoxicillin and potassium Clavulanate as an anti-H. pylori agent and to evaluate the effectiveness of the mucoadhesive microspheres for H. pylori eradication therapy.Mucoadhesive microspheres can be tailored to adhere to any mucosal tissue including those found in eye, nasal cavity, urinary and gastrointestinal tract, thus offering the possibilities of localised aswell as systemic controlled release of drugs. Application of bioadhesive microspheres to the mucosal tissues of ocular cavity, gastric and colonic epithelium is used for administration of drugs for localised action. Prolonged release of drugs and a reduction in frequency of drug administration can highly improve by this system that increases the patient compliance.