This work was aimed at the use of dissolution testing and similarity factor to assess the\nlevel of damage taken by active drug microspheres during compression in tablet dosage form.\nTo achieve that, combinations of suitable excipients were used to protect drug microspheres\nduring compression. The excipients were used in the form of powders, granules or placebo\npellets prepared by extrusion-spheronization technology. The excipients were evaluated alone,\nin combinations and post-compression into compacts. Preliminary experiments included\nassessing density, hardness, friability and disintegration of all the selected excipients. Based on\nsuch experiments it was found that the flowability of combination of powders was more\nacceptable than individual excipients. Two combinations of microcrystalline -starch and\nmicrocrystalline cellulose -calcium carbonate granules were selected to be compressed with\npellets of the active pharmaceutical ingredient ketoprofen. In all the combinations used there\nwas a significant amount of damage to drug pellets. The kinetics of drug release appears to\nfollow the zero-order rate, which remained unchanged even when a significant degree of\ndamage to pellets occurs. It was found that a high level of excipients is required in order to\nprepare microspheres as a rapid disintegrating tablet.
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