Particle Design of Aceclofenac-Disintegrant Agglomerates for Direct Compression by Crystallo-Co-Agglomeration Technique

The purpose of present research was to obtain aceclofenac-disintegrant agglomerates with improved solubility, flow and compression characteristics by a novel crystallo-co-agglomeration (CCA) technique. Aceclofenac agglomerates were prepared by using a three solvent system comprising of acetone: DCM: water. Acetone-water containing PEG 6000, HPC and disintegrants like sodiumstarch glycolate (SSG), crospovidone (CP) and croscarmellose sodium (CCS) in different concentrations were used as the crystallization medium. The agglomerates were characterized by FTIR, DSC, PXRD, SEM studies and were evaluated for flow, packing and tableting properties and drug release. The growth of particle size and the spherical form of the agglomerates resulted in formation of products with good flow and packing properties. The improved compaction properties of the agglomerated crystals were due to their fragmentation occurred during compression. DSC and XRPD studies showed that aceclofenac particles, crystallized in the presence of HPC, PEG 6000 and disintegrant did not undergo structural modifications. The dissolution rate of aceclofenac from the agglomerates could be controlled by the amount of included disintegrant, being enhanced as the latter was increased. This was attributed to an increase in the surface area of the practically water insoluble drug is exposed to the dissolution medium. Among all the formulations studied, F-9 prepared by incorporation of CP (18.43%) had shown short disintegration time (18.03 sec) and maximum drug release.