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THE PHARMA REVIEW (SEPTEMBER - OCTOBER 2013)

Influence of Diluents on Dissolution Rate of Ezetimibe Tablets

P. Gouthami Choudary1 & Dr.T.E.G.K.Murthy2

Introduction: Ezetimibe,1-(4-fluorophenyl)-3(R)-[3-(4-fluorophenyl)-3(S)-hydroxypropyl]-4(S)-(4-hydroxyphenyl)-2-azetidinone, is the first lipid-lowering drug that inhibits intestinal uptake of dietary and biliary cholesterol without affecting the absorption of fat-soluble nutrients. The estimated terminal half-life of ezetimibe is 19-30 hours. Consistent with the elimination half-life of ezetimibe, an approximate 2-fold accumulation is observed upon repeated once-daily administration. The recommended dose of ezetimibe (10 mg/day) can be administered in the morning or evening without regard to food. The bitter taste of ezetimibe and its solubility becomes a hurdle for formulating. Hence there is a need to explore techniques to enhance its solubility and simultaneously masking its taste2. 

 

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