Formulation and Evaluation of Ezetimibe Liquisolid Tablets: An Approach to Enhance the Dissolution Rate

Background and the Purpose of the Study: Liquisolid compacts’ using poorly water soluble drugs is considering as one of the novel pharmaceutical formulation technologies to improve the dissolution rate. This study was intended to improve the dissolution rate of ezetimibe by preparing liquisolid tablets.

Methods: In the preparation of liquisolid tablets, the following materials are used as carrier powder; polyethylene glycol (PEG) 400, tween 80 and propylene glycol as solvent, Avicel PH102 or starch or HPMC or PEG 4000 or PEG 6000 and Aerosil 200 are used as coating material. The interaction between drug and excipients was examined by differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FTIR). In vitro drug release studies of liquisolid and conventional tablets (control) were conducted and compared the both to study the improvement in dissolution rate. Then the best formulation was subjected to stability studies.

Results and Discussion: The results of DSC and FTIR studies revealed that there are no possible drug-excipient interactions. The percentage drug release of ezetimibe at 10 min (Q10) and dissolution efficiency were increased from 23.86±1.08% and 11.61 for conventional tablet to 92.57±1.12% and 60.30 for the liquisolid formulation. From the stability studies, the similarity factor was found as above 50 that revealed the stability of the formulation.

Conclusion: In conclusion, the liquisolid technique was believed as a capable approach to enhance the ezetimibe dissolution rate.