Abstract
Ebastine (EBS) is a poorly water-soluble antihistaminic drug; it belongs to the class II group according to the biopharmaceutical classification system (BCS). The aim of the present work was to enhance the solubility, dissolution rate and micromeritic properties of the drug, by formulating it as spherical crystal agglomerates by Quasi Emulsion Solvent Diffusion (QESD) method.
 Spherical crystal agglomerates (SCAs) were prepared in presence of three solvents dichloromethane (DCM), water and chloroform as a good solvent, poor solvent and bridging solvent respectively. Agglomeration of EBS involved the use of some hydrophilic polymers like polyethylene glycol 4000 (PEG 4000), polyvinyl pyrrolidine K30 (PVP K30), D-?-tocopheryl polyethylene glycol 1000 succinate (TPGS) and ?. cyclodextrin. The pure drug (EBS) and its agglomerates with and without polymers were characterized for their drug content, percentage yield, solubility, in vitro drug release study and micromeritic property as well as by optical microscope, Scanning Electron Microscopy (SEM), FTIR spectroscopic studies, Differential Scanning Calorimetry (DSC) and X-ray Diffraction (XRD). The results of this work showed that there was a marketed enhancement in the solubility with improvement in dissolution rate, physiochemical properties, decrease in crystallinity and alteration in the crystal habit of the drug especially in presence of polymers. The best results were obtained with formula prepared by the combination of PEG 4000 and B. cyclodextrin in the agglomeration process of (EBS).
Highlights
The oral route of drug administration is the most common and preferred one over the other routes due to its convenience and ease of administration
Spherical crystal agglomeration (SCAs) prepared by emulsion solvent diffusion method. 2g EBS was dissolved in 10ml good solvent (DCM), this solution was poured drop by drop in to 100ml distilled water containing either no, single or combination of polymers in presence of 0.1 g Aerocil 200; stirred by mechanical stirrer
When the organic drug solution was added to the stirring water, emulsion droplets were formed due to the interfacial tension between the two solvents, the good solvent gradually diffuses out of the emulsion droplets into the outer poor solvent phase, and the poor solvent diffuses into droplets, which reduced the solubility and eventually caused drug crystallization inside the droplets [30], the bridging liquid would wet the precipitated crystals
Summary
The oral route of drug administration is the most common and preferred one over the other routes due to its convenience and ease of administration. It is important to increase bioavailability of the drug by improving the solubility of the bulk drug powder [3].Spherical crystal agglomeration (SCAs) method directly transforms the fine particles produced in the crystallization process into a spherical shape [4]. ; it improves the secondary characteristics like flowability and compressibility so that direct tableting is possible without further processing [5]. It is the particle engineering technique by which crystallization and agglomeration can be carried out simultaneously in one step to transform crystals directly into compacted spherical form which has been successfully utilized for improvement of solubility and dissolution
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