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.
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