Crystallo-co-Agglomeration Technique for Improving Physicochemical Properties, Compressibility and Solubility Characteristics of Metronidazole

Abstract

The objective of this study is to develop crystallo-co-agglomeratesof metronidazole having improved physicochemical, compressibility andsolubility properties. The process of agglomeration employed the use ofdichloromethane (good solvent), ethanol (bridging liquid) and distilled water (poorsolvent). Micromeritic properties of the metronidazole co-agglomerates werestudied in terms of bulk density, tapped density, Carr's index, Hausner’sratio, and angle of repose. Co-agglomerates were also subjected to compactionstudies using the Heckel and Kawakita compaction models. Characterisation ofthe agglomerates was studied using Scanning electronic microscopy, Fourier-transformed infrared spectroscopy, and X-ray diffraction. The co-agglomerateswere further evaluated for drug release profile. The micrometric properties anddissolution characteristics of metronidazole co-agglomerates were significantlyimproved when compared to pure metronidazole. The angle of repose formetronidazole co-agglomerates was found to be 29.77°±1.09, Carr’s index was13.60±0.35, and Hausner’s ratio was 1.15±0.06, indicating good flow ability. Thedrug released over a period of 30 min was 102.61%, this shows better drugrelease than the pure drug, this could be due to the solubilization of the drug inpresence of hydrophilic polymers. It can be concludedthat metronidazole was successfully prepared using the crystallo-co-agglomeration technique with improved micrometric properties, excellentcompressibility, and improved solubility characteristics.