FABRICATION AND CHARACTERIZATION OF EZETIMIBE SOLID DISPERSION FOR SOLUBILITY ENHANCEMENT

Abstract

Objective: The objective of the present study was to formulate solid dispersions (SD) of Ezetimibe to improve the solubility and dissolution rate to facilitate faster onset of action. Ezetimibe is poorly water soluble BCS class II drug and used as a hypolipidemic agent. It has poor bioavailability (35-65%) due to its low dissolution profile in gastro intestinal tract.

Methods: In the present study, eight solid dispersion formulations of Ezetimibe with polymers PEG-4000 and PEG-6000 were prepared by solvent evaporation and fusion methods.  Solid dispersion formulations were characterized by content uniformity, flow properties and in vitro dissolution studies.

Results: The solubility of Ezetimibe powder in distilled water at 37±0.5°C was 2.37±0.14 µg/ml, whereas solubility of the solid dispersion formulations was in the range of 322.43-37.48 µg/ml. Percent yield of eight solid dispersion formulations of Ezetimibe lies in range of 98.20 to 99.42% w/w. 

Conclusion: Present study concluded that the Ezetimibe solid dispersion formulations are a suitable approach to improve the solubility and dissolution rate of ezetimibe than pure form of drug.

Peer Review History:

Received 8 December 2016;   Revised 12 January 2017; Accepted 14 February, Available online 15 March 2017

Academic Editor: Dr. Ali Abdullah Al-yahawi, Al-Razi university, Department of Pharmacy, Yemen, alyahawipharm@yahoo.com

Received file:        Reviewer's Comments:

Average Peer review marks at initial stage: 4.0/10

Average Peer review marks at publication stage: 8.0/10

Reviewer(s) detail:

Dr.  Murtaza M. Tambuwala, Ulster University, Ireland, m.tambuwala@ulster.ac.uk

Dr. Masoumeh Divar, Shiraz University, Shiraz, Iran, zhaledivar@gmail.com