Preparation of novel optimum liquisolid compacts via incorporating water granulation process to enhance the powder characterizations and dissolution behavior of a poorly soluble drug: Norfloxacin

摘要

The aim of this work is to investigate the addition of wet granulation technique into liquisolid process in order to enhance the characterizations of liquisolid compacts, such as flowability, compressibility and the percentage of drug release (using norfloxacin as a model of poorly soluble-permeable drug) in neutral dissolution medium. The water in the liquisolid formulations works as a liquid binder to the carrier and coating particles, creating a wider space inside their structure, which allows the amount of the liquid vehicle (PEG200 or Synperonic (TM) PE/L-61) to increase inside the formulations. This feature reflects positively on: the flowability (decreasing the angle of the slide up to 10 degrees), the compressibility (increasing the load factor from 0.2 to >0.4 in PEG200 liquisolid compacts and from 0.14 to 0.29 in the case of Synperonic (TM) PE/L-61iquisolid compacts) and the dissolution behaviour of norfloxacin (increasing drug release). The applied accelerated stability study on the water granulated liquisolid compacts showed no significant differences in the dissolution profiles. Also, the DSC thermographs indicated that the water granulated liquisolid compacts resist the applied stressful conditions. As a consequence, the positive outcomes of the combination between liquisolid and water granulation process open the door for robust tablet production on a large scale in pharmaceutical industries. (C) 2019 Elsevier B.V. All rights reserved.