Novel Co-Processed Excipients of Mannitol and Microcrystalline Cellulose for Preparing Fast Dissolving Tablets of Glipizide

摘要

Co-processed particles of microcrystalline cellulose and mannitol were fabricated by spray drying technique to be used as a direct compression excipient in fast dissolving tablet formulation. Microcrystalline cellulose passed through sieve no.80, having a volumetric mean diameter (d_(50)) of 28.35 um, was used to form composite particles with powdered mannitol which was previously passed through sieve no. 80, in various mixing ratios. The composite particles were evaluated for their powder and compression properties. An increase in the microcrystalline cellulose proportion imparted greater compressibility to the composite particles, but the flowability of these mixtures was decreased. Although microcrystalline cellulose and mannitol have been extensively used in the formulation of fast dissolving tablets, the non-wetting property of the hard compact central core may delay the disintegration time. Optimized co-processed formulation containing mannitol and microcrystalline cellulose in the ratio of 1.25:1 was found to have optimized powder and compressibility characteristics with fast disintegrating property (<15 s). Photomicrographs have shown that the mannitol crystals are fine and uniformly distributed in the microcrystalline matrix in spray dried form compared to physical mixture of the same combination. The fast disintegration may be due to the partial amorphization and formation of submicron particles of mannitol. These results indicated that improved fast dissolving tablets could be prepared by the co-processed mixture of microcrystalline cellulose and mannitol. Finally fast dissolving tablets of glipizide were prepared by blending with other excipients and compressed into tablets. Sensory study on disintegration time and mouth feel attributes ranked the present formulation based on grittiness, chalkiness and overall preference as the best.