Formulation and In- Vitro Evaluation of Spherical Crystal Agglomerates of Ebastine by Quasi Emulsion Solvent Diffusion Method

[摘要] Ebastine (EBS) is a poorly water-soluble antihistaminic drug; it belongs to the class II group according to the biopharmaceutical classification system (BCS). This work aims to enhance the solubility, dissolution rate and micrometric properties of EBS, by formulating it as spherical crystal agglomerates by Quasi Emulsion Solvent Diffusion (QESD) method. Spherical crystal agglomerates (SCAs) were prepared in the presence of 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-α-tocopheryl polyethylene glycol 1000 succinate (TPGS) and β. cyclodextrin. (EBS) and its agglomerates (with and without polymers) were characterize d 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), Fourier Transform Infrared Spectroscopy (FTIR), Differential Scanning Calorimetry (DSC) and X-ray Diffraction (XRD). The results showed that there was a marked enhancement in the solubility with improvement in dissolution rate, physiochemical properties, and decrease in crystallinity and alteration in the crystal habit of the drug especially in the presence of polymers. The best results were obtained with formula prepared by the combination of PEG 4000 and β. cyclodextrin in the agglomeration process of (EBS).

[学科分类] 计算机网络和通讯

[关键词] Ebastine;Spherical crystal agglomerates;Quasi emulsion solvent diffusion method.