Abstract
In the second part of this publication the differing interactions of micronized glibenclamide during mixing with four filler/binders for direct compression were studied. The excipients used were: Ludipress, Cellactose, Avicel PH 200 and Karion Instant. In order to prepare interactive mixtures, increasing amounts of micronized glibenclamide were blended with filler/binder fractions of 125 to 500 μm. The degree of interactivity was determined by air jet sifting of the mixes, comparing drug content in the mixes before and after sieving. Cellactose showed the highest adhesion tendency for glibenclamide due to the large cavities in the particles, leading to a reagglomeration within these cavities. Tablets containing 1.75, 3.50, 5.00 and 10.00 mg of glibenclamide per tablet were compressed with Cellactose and Ludipress. As previously reported (1) for Cellactose based placebo tablets, Cellactose also showed a tremendous increase in disintegration time and a prolonged dissolution rate at compaction pressures above 100 MPa. The corresponding values of Ludipress were not influenced. Therefore in terms of a multipurpose-excipient, Ludipress should be given preference in the formulation of low dosed drugs.