Spherical Crystallization of Zaltoprofen for Enhancement of Micromeritic Properties and Dissolution Rate

The present work deals with the spherical crystallization process by Spherical agglomeration method applied to Zaltoprofen, a novel NSAID drug. The object of present study was to prepare and characterize the spherical agglomeration of water insoluble non-steroidal anti-inflammatory drug. Zaltoprofen spherical agglomerates prepared with poly ethylene glycol, which is hydrophilic polymer by using simple spherical agglomeration technique for enhancing micromeritic properties and dissolution rate. The prepared zaltoprofen spherical agglomerates were examined in terms of flow properties, particle size analysis, compression and dissolution behavior. Physical characters of the crystals were studied for the morphology of crystals using scanning electron microscope (SEM), identification of polymorphism done by x-ray powder diffraction (XPRD) and for thermo dynamic properties using differential scanning colorimetry (DSC). The prepared agglomerates were improved the micromeritic properties, packability, wettability, solubility and compaction behavior, as well as dissolution behavior in comparison to pure Zaltoprofen drug. INTRODUCTION: The conventional tableting method used involves first making granules and then compressing into tablets by way of direct (granule) tableting, but the need in recent years for process validation, GMP and automation of production processes has focused renewal of attention on the direct tableting, which involves few steps. The direct compression is a modern technique in the tablet manufacturing, many processing steps are limited in direct compression and also wet granulation cannot be used with sensitive drugs . Spherical agglomeration is a modern technique for development of directly compressible drugs where the drug crystals are converted to spherical form to improve flowability, compressibility, packability and to enhance dissolution rate characteristics of poorly water insoluble drug. Also direct tableting of pharmaceutical drugs is desirable to reduce the cost of production . Spherical crystallization technique directly transforms the fine particles produced in the crystallization or in the reaction process into a spherical shape . Agglomerates exhibit improved secondary characteristic like flowability and compressibility so that direct tableting is possible without further processing. The literature citation reveals that spherical crystals can be made in various ways such as Simple crystallization, Ammonia diffusion system method, Emulsion solvent diffusion method and Neutralization method. Out of these methods available to prepare spherical agglomerates, simple spherical crystallization is very easy, common and faster relative to other methods .