SOLUBILITY ENHANCEMENT AND DEVELOPMENT OF DISPERSIBLE TABLET OF CANDESARTAN CILEXITILAbstract
Candesartan Cilexitil is an angiotensin II receptor antagonist used mainly for the treatment of hypertension. Candesartan cilexitil is a BCS class II drug having low solubility and high permeability. Candesartan Cilexitil is a prodrug which is rapidly converted to the active drug, Candesartan, by ester hydrolysis during absorption from the gastrointestinal tract. The bioavailability of Candesartan Cilexitil is approximately 15% after an oral administration. To increase bioavailability of such drug, solubility and dissolution are important parameters. To increase solubility of candesartan cilexitil, spray drying technique was incorporated with use of Fluidised Bed Processor. Also dissolution rate was improved with the use of appropriate superdisintegrants. Superdisintegrants used are Croscarmellose sodium, Crospovidone and Sodium starch glycolate. Dissolution rate of Candesartan Cilexitil from prepared dispersible tablet was compared with marketed formulation. Results have shown that solubility of Candesartan Cilexitil has been increased and dissolution rate was improved significantly. The transformation of Candesartan Cilexitil from crystalline to amorphous state by spray drying and the use of superdisintegrants are considered among the factors which contributed in improvement of Candesartan Cilexitil dissolution.
A. V. Shrirao and S. Bhilegaonkar *
Department of Pharmaceutics, PES’s Rajaram and Tarabai Bandekar College of Pharmacy, Ponda, Goa, India.
05 May, 2016
10 August, 2016
22 August, 2016
01 October 2016