Preparation of cefixime liquisolid formulation for enhancing its dissolution rate

Abstract

Introduction: Cefixome is one of the water-insoluble drugs which its oral absorption is limited by its lower dissolution rate. So by increasing its dissolution rate, enhanced bioavailability is expected. Aim: Liquisolid technique is a promise way to speed up the dissolution rate of poorly water soluble drugs which has been considered in this study. Methods: For preparation of liquisolid compacts, microcrystalline cellulose and colloidal silicon dioxide (Silica) were used as a carrier and coating material, respectively. Furthermore, in order to prepare liquid medication, PEG 300 were employed as a nonvolatile solvent and additive, respectively. The effect of various ratios of drug: PEG400, carrier: coating material and aging on dissolution rate were also studied. Physicochemical properties of all samples were evaluated using X-ray diffraction crystallography (XRD) and differential scanning calorimetery (DSC) analyses. Results: The results showed that the amount of load factor was increased significantly in the presence of additive. Liquisolid formulations, displayed significantly higher drug dissolution rates compared to the compacts prepared by the direct compression technique. Additionally, increasing of the nonvolatile solvent ratio: drug in liquid medication caused a remarkable enhancement in dissolution rate. The dissolution profile and hardness of liquisolid tablets were not significantly affected by storing the tablets at 25 oC in a relative humidity of 75% for a period of 6 months. The DSC and XRD data were not revealed any changes in crystallinity of the drug and interaction between drug and excipients during the process. Conclusion: With the proposed liquisolid process it is possible to obtain flowable, compactible liquisolid powders of high dose poorly- water soluble cefixime with the enhanced dissolution rate from the compacts.