ENHANCEMENT OF SOLUBILITY AND DISSOLUTION RATE OF EZETIMIBE THROUGH LIQUISOLID TECHNIQUE

The present study enlightens to enhance the dissolution profile, absorption efficiency and bioavailability of water insoluble drug like Ezetimibe. It is a poorly soluble, highly permeable drug and the rate of its oral absorption is often controlled by the dissolution rate in the gastrointestinal tract. There are several techniques to enhance the dissolution of poorly soluble drugs, in which the “liquisolid compacts” is a promising technique. Different formulations were prepared by using polyethylene glycol-400 as a non-volatile liquid vehicle, with drug and vehicle ratios of 1:5 and 1:7.5, microcrystalline cellulose (Avicel PH 102), starch were used as carrier materials and nm-sized silica gel (Aerosil-200) was used as coating materials. The empirical method introduced by Spireas and Bolton was applied to calculate the amounts of coating and carrier materials required to prepare Ezetimibe liquisolid tablets. Based upon this method, improved flow characteristics and hardness of the formulation has been achieved by changing the proportion of carrier and coating material ratio from 20:1 to 5:1. They were characterized for different physical parameters to comply with pharmacopoeial limits. In vitro dissolution profiles of the liquisolid formulations were studied and compared with conventional formulation in pH 4.5 acetate buffer. It was found that liquisolid tablets formulated with microcrystalline cellulose produced high dissolution profile and they showed significant higher drug release rates than conventional tablets due to increase in wetting properties and surface of drug available for dissolution. FTIR spectral studies showed that there is no interaction between the drug and excipients. Aging studies indicates that, there is no significant effect on dissolution rate and hardness of the formulation of fresh and stored at 40±2⁰C/ 75±5% relative humidity for 45days. In conclusion, development of ezetimibe liquisolid tablets is a good approach to enhance the dissolution rate to improve bioavailability