title: Development of HPMC and Eudragit S100 blended microparticles containing sodium pantoprazole.
abstract: Pantoprazole is used in the treatment of acid related disorders and Helicobacter pylori infections. It is activated inside gastric parietal cells binding irreversibly to the H+/K(+)-ATPase. In this way, pantoprazole must be absorbed intact in gastro-intestinal tract, indicating that enteric delivery systems are required. The purpose of this study was to prepare pantoprazole-loaded microparticles by spray-drying using a blend of Eudragit S100 and HPMC, which can provide gastro-resistance and controlled release. Microparticles presented acceptable drug loading (120.4 mgg(-1)), encapsulation efficiency (92.3%), surface area (49.0 m2g(-1)), and particle size (11.3 microm). DSC analyses showed that the drug is molecularly dispersed in the microparticles, and in vivo anti-ulcer evaluation demonstrated that microparticles were effective in protecting stomach against ulceration. Microparticles were successfully tabletted using magnesium stearate. In vitro gastro-resistance study showed that microparticles stabilized pantoprazole in 62.0% and tablets in 97.5% and provided a controlled release of the drug.
authors.affiliation: Programa de Pós-Graduação em Ciências Farmacêuticas, Instituto de Química, Universidade Federal do Rio Grande do Sul, Porto Alegre, RS, Brazil.
authors.forename: R P
authors.initials: RP
authors.lastname: Raffin
authors.forename: L M
authors.initials: LM
authors.lastname: Colomé
authors.forename: S E
authors.initials: SE
authors.lastname: Haas
authors.forename: D S
authors.initials: DS
authors.lastname: Jornada
authors.forename: A R
authors.initials: AR
authors.lastname: Pohlmann
authors.forename: S S
authors.initials: SS
authors.lastname: Guterres
mesh_terms: D053799:2-Pyridinylmethylsulfinylbenzimidazoles / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology; D000180:Acrylic Resins / Q000737:chemistry*; D000818:Animals; D000897:Anti-Ulcer Agents / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology; D002152:Calorimetry, Differential Scanning; D002626:Chemistry, Pharmaceutical; D002851:Chromatography, High Pressure Liquid; D003692:Delayed-Action Preparations; D003890:Desiccation; D004339:Drug Compounding; D000431:Ethanol; D005079:Excipients; D065347:Hypromellose Derivatives; D008747:Methylcellulose / Q000031:analogs & derivatives* / Q000737:chemistry; D008855:Microscopy, Electron, Scanning; D053758:Nanoparticles; D000077402:Pantoprazole; D010316:Particle Size; D016062:Porosity; D051381:Rats; D012997:Solvents; D013276:Stomach Ulcer / Q000139:chemically induced / Q000473:pathology / Q000517:prevention & control; D013499:Surface Properties
chemical_list: D053799:2-Pyridinylmethylsulfinylbenzimidazoles; D000180:Acrylic Resins; D000897:Anti-Ulcer Agents; D003692:Delayed-Action Preparations; D005079:Excipients; D012997:Solvents; C050528:Eudragit RS; D000431:Ethanol; D065347:Hypromellose Derivatives; D008747:Methylcellulose; D000077402:Pantoprazole