Development of HPMC and Eudragit S100 blended microparticles containing sodium pantoprazole.
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.
Raffin
R P
RP
Programa de Pós-Graduação em Ciências Farmacêuticas, Instituto de Química, Universidade Federal do Rio Grande do Sul, Porto Alegre, RS, Brazil.
Colomé
L M
LM
Haas
S E
SE
Jornada
D S
DS
Pohlmann
A R
AR
Guterres
S S
SS
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
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