Abstract

IMPROVEMENT OF SOLUBILITY AND DISSOLUTION RATE OF CANDESARTAN CILEXETIL BY EMPLOYING SOLID DISPERSION TECHNIQUE USING HYDROPHILIC POLYMERS

Jayendra Chunduru*, Pavankumar Chadalawada, Ranjith Kumar Nadipalli, Govada Kishore Babu and Srinivasa Babu Puttagunta

ABSTRACT

Candesartan Cilexetil is a prodrug that is hydrolyzed to its active form, candesartan, during gastrointestinal absorption. As a selective AT1 subtype angiotensin II receptor antagonist, Candesartan plays a critical role in managing hypertension. However, its therapeutic effectiveness is limited by poor aqueous solubility, which significantly impacts its bioavailability. In this study, we aimed to enhance the solubility and dissolution profile of Candesartan Cilexetil through solid dispersion techniques using the hydrophilic polymers Poloxamer 407 and PEG 4000. Solid dispersions were prepared in different ratios through physical mixing, hot melt agglomeration, co-evaporation, and co-precipitation methods. The dissolution profiles were evaluated, and dissolution efficiencies were calculated using model-independent approaches, including the f2 similarity factor and DE30 values. Our findings indicate that both PEG 4000 and Poloxamer 407 are effective carriers for enhancing the dissolution of Candesartan Cilexetil, with thehot melt agglomeration method demonstrating the most promising results. These results suggest that the optimized formulations could significantly improve the bioavailability of Candesartan Cilexetil, providing a basis for further development and scale-up in pharmaceutical applications.

Keywords: Candesartan Cilexetil, hydrophilic polymers, Poloxamer 407, PEG 4000, solid dispersions, Solubility, Dissolution Rate.