Revista estadounidense de administración avanzada de fármacos Acceso abierto

Abstracto

Ezetimibe Solid Dispersions: Formulation, Development and In vitro Evaluation

Chaitanya P, Jyothi Penta, Venkat Ratnam Devadasu, Raj Kumar Venisetty and Sateesh Kumar Vemula

Development of solid dispersions of poorly water soluble drugs is one of the most widely used approaches to enhance the solubility as well as dissolution rate. In the current investigation, ezetimibe is selected as model drug to improve the solubility and dissolution rate by solid dispersion method. Solid dispersions were prepared using solvent evaporation method by incorporating polyethylene glycol 4000, polyethylene glycol 6000 and gelucire 44/14 as carriers in different ratios and evaluated for solubility studies, drug-carrier compatibility studies and in vitro dissolution studies. Based on the solubility and drug release studies, formulations F4, F8 and F11 were selected to prepare in the form of tablets and compared with conventional tablets. From the in vitro dissolution study, tablets containing gelucire 44/14 showed almost complete drug release within the 15 min. The percent drug release in 15 min (Q15) and initial dissolution rate for formulation F11 was 94.22±1.08%, 9.26%/min. These were very much higher compared to conventional tablets containing pure drug (23.87±1.13%, 2.38%/min). The relative dissolution rate was found to be 2.14 and dissolution efficiency was found to be 67.52 and it is increased by 4.0 fold with F11 formulation compared to conventional tablets. Thus, it is concluded that the formulation of gelucire 44/14 solid dispersions is a suitable approach to improve the solubility and dissolution rate of ezetimibe than pure form of drug.