Formulation and characterization of Gastroretentive drug delivery system

Abstract

newlineGastroretentive drug delivery system (GRDDS) is among the novel approaches in the newlineoral sustained release dosage forms. Drugs which have short biological half-life and are newlinesimply absorbed through GIT often require frequent dosing to attain therapeutic activity newlinebecause of quick elimination from body. This limitation can be overcome by developing newlineoral sustained release GRDDS. It maintains therapeutic concentration over an extended newlineduration by releasing drug slowly in GIT. Post oral administration GRDDS is retained newlinein gastric region and release drug in sustained fashion. Because of inferior absorption of newlinenumerous API in the lower part of GIT, it is required that controlled release DDS to be newlinepositioned in upper part of GIT. These DDS bear two diversities: short retention time of newlineDDS in stomach and small stomach emptying time which may result in incomplete newlinerelease in absorption window resulting in reduced efficacy. newlineIn present work Gastroretentive drug delivery system of captopril and simvastatin is newlineprepared by amalgamating novel drug delivery technologies like chitosan microparticles newlineand SMEDDS with gastroretentive delivery system newlineCaptopril is an angiotensin converting enzyme inhibitor, usually prescribed in newlinetreatment of hypertension and require long term use for its therapeutic benefit. It newlinebelongs to BCS class III i.e. high solubility and low permeability. So once a daily newlinecaptopril oral formulation would be significant in reducing the fluctuations in blood newlineconcentration and increasing patient compliance. Chitosan microparticles were newlinedeveloped with aim to improve the permeability and it was further incorporated in the newlinegastroretentive floating mini tablets. Chitosan microparticles were systemically newlinedeveloped by applying Plackett Burman design for screening different formulation newlinefactors. Total 11 factors were screened at two levels considering % entrapment newlineefficiency as the response. Chitosan concentration, TPP concentration and speed of newlinestirring were the significant factors out of total 11 factors screened.