Soft agglomerates of pantoprazole gastro-resistant microparticles for oral administration and intestinal release

Soft agglomerates containing pantoprazole gastro-resistant microparticles were prepared for an oral delayed-release solid dosage form. A new technique was used to agglomerate the microparticles: enteric microparticles of pantoprazole, non-agglomerating per se, were blended with mannitol/lecithin spray-dried microparticles, i.e. excipient microparticles. The blend was agglomerated by tumbling or sieve vibration. In order to elucidate the agglomerate formation, the effect of factors such as the amount of lecithin in the excipient microparticles, the ratio between pantoprazole and excipient microparticles and the agglomeration method were investigated by factorial design. Twelve batches of agglomerates presenting differing yield, drug loading, morphology, mechanical and release properties were prepared. The concentration of lecithin in the excipient microparticles was crucial for the agglomeration process. The biopharmaceutical characteristics of pantoprazole microparticles, i.e. their delayed-release properties, were not affected by the agglomeration process