Formulation and evaluation of rapid disintegrating tablet of candesartan cilexetil for the management of hypertension

Lokesh Kumar, Rakesh Kumar Mee

Abstract

Candesartan is water insoluble oral antihypertensive agent, with problems of variable bioavailability and bioequivalence related to its water insolubility. Candesartan is a highly potent, long-acting and selective angiotensin II type 1 (AT) receptor blocker. It is administered orally as the inactive prodrug Candesartan Cilexetil which is rapidly and completely converted to Candesartan during gastrointestinal absorption. Candesartan Cilexetil should be administrated orally once or twice daily for a total daily dosage of 4 to 32 mg. In this investigation rapid disintegrating tablet were prepared by using super disintegrating agent crospovidone, croscaremellose sodium, sodium starch glycolate in concentration 8%, 9%, 10%. Sweeteners and flavors were used to enhance the organoleptic properties of tablet. Tablets were prepared by direct compression technique. Prepared tablets were evaluated for thickness, uniformity of weight, hardness, friability, wetting time, in-vitro disintegration time, drug content and in vitro drug release. Disintegration time and drug release were taken as the basis to optimize the rapidly disintegrating tablet. All the formulations were evaluated for the influence of disintegrates and their concentrations on the characteristics of rapid disintegrating tablets mainly in terms of disintegration time and dissolution studies. The disintegration time of all formulation showed less than 37 seconds. Among the three superdisintegrants used, Crospovidone showed less disintegrating time followed by croscarmellose sodium and sodium starch glycolate. The relative efficiency of different superdisintegrants to improve the drug rate of tablets was in order, crospovidone> Croscarmellose sodium >sodium starch glycolate. The optimized formulation was found as F6, which have been made by use of crospovidone as superdisintegrant. And it show less disintegration time, better drug release profile as well as optimize drug content as compared to other excipients formulations.