Formulation and Development of Candesartan Cilexetil Fast Dissolving Tablets by Sublimation Technique

[摘要] Candesartan cilexetil is a prodrug of candesartan – a compound that inhibits binding of angiotensin II to the AT1 – receptor. It is mainly used in the treatment of hypertension. In the present work attempts were mase to prepare fast dissolving tablets of candesartan cilexetil by sublimation technique. The prepared formulations were evaluated for pre-compressional and postcompressional parameters. The compatibility of drug with other ingredients was checked by FTIR studies, these results revealed that there was no interaction between dug and other excipients. The values of pre-compressional parameters were within prescribed limits and indicated good free flowing properties. In all the formulations the hardness test indicates good mechanical strength. Friability of all formulations was less than 1. Drug content was found to be high (≥ 100.27%) and uniform in all the formulations. The tablet thickness was found to be 3.14 – 3.47. The weight variation results revealed that average percentage deviation was less then ± 7.5 %, which provides good uniformity in all formulations. The disintegration time of the tablets decreased significantly with increase in the concentration of subliming agent. The formulations CSC3, CSM3, CSA3, and CSU3 50 % of drug released in 1.38, 2.55, 4.00 and 3.57 min, and 90 % of drug released in 3.39, 6.04, 7.50 and 7.18 min. The formulation CS (control) released 42.16 % in 60 min. Stability study carried out as per ICH guidelines for three months and results revealed that upon storage disintegration time of tablets decreased significantly (p<0.05). The results concluded that by adopting a systemic formulation approach, an optimum point could be reached in the shortest time with minimum efforts. Sublimation technique would be an effective alternative approach compared with the use of more expensive adjuvants in the formulations of fast dissolving tablets.

[学科分类] 药学

[关键词] Candesartan cilexetil;Fast dissolving tablets;sublimation technique;Croscarmillose Sodium.