PREFORMULATION STUDY FOR CANDESARTAN CILEXETIL BUCCAL (EFFERVESCENT) TABLET

Candesartan cilexetil is a novel, potent, and highly selective non-peptide angiotensin II type 1 receptor blocker. It is a hydrophobic drug that belongs to the BCS Class II drug. For enhancement, the bioavailability and quick systemic action of Candesartan cilexetil a novel formulation of buccal (effervescent) tablet, was designed.  Preformulation is an important step in the rational formulation of an active pharmaceutical ingredient (API). Micromeritics properties: Bulk density (du), Tapped density (db), Compressibility Index (% C) and sieve analysis was performed in order to determine the best excipients to be used in the formulation development of Candesartan cilexetil (effervescent) tablets. Results show that Candesartan Cilexetil has a fair flow and compressibility properties (du 0.8 g/mL, db 0.7 g/mL, % C 12.5, and sieve analysis time 4.5 min. HPLC method for estimation of Candesartan cilexetil shows linearity ( R² = 1) and specific with no interference of excipients. Solubility studies reveal that it soluble at pH 6.8 and 7.5 in phosphate buffer. The ability of a material to absorb water (Hygroscopicity) was found 0.1% after 24 H at 80% Relative Humidity. Melting point range from 161-165 °C. There was no drug excipient interaction observed when analyzed through FTIR and DSC. There was no change in appearance after 15days at 40°C and 75% Relative humidity. These results lead to the better development of Candesartan cilexetil buccal (effervescent) tablet.