Abstract

FORMULATION AND OPTIMIZATION OF SUBLINGUAL TABLETS OF TELMISARTAN

Shailesh T. Prajapati*, Shefali I. Modh and Chaganbhai N. Patel

Abstract

The patients with sudden increase blood pressure have rapid onset of action is require. So the patient would be benefited from acute treatment by using Sublingual drug delivery system. Telmisartan is an angiotensin II receptor antagonist (ARB) used in the hypertension. Its bioavailability is less than 42% due to its high hepatic first pass metabolism. It is a BCS class II drug which is insoluble in water. Telmisartan has poor and pH dependent solubility. The drug may be slowly or incompletely dissolves in the gastro-intestinal tract, to enhance its dissolution different alkalizers were used. Diverse water soluble carriers viz. Polyethylene glycols (PEG 4000, 6000), Chitosan, Poloxamer (188, 407) Na.CMC and β‐cyclodextrin, PVP K30 were used for this purpose. Phase solubility studies revealed an increase in drug solubility with PVP K30, Poloxamer 407, and β‐cyclodextrin. Solid dispersion of Telmisartan With PVP K30, Poloxamer 407 and β‐cyclodextrin carried out in order to determine the potential effect on solubility of Telmisartan. Solid dispersion was evaluated by DSC. DSC studies showed that the Drug polymer complex formed by solid dispersion. Results show that maximum increase in solubility was found for Telmisartan with solid dispersion using PVP K30 in 1:2 drug to polymer ratio solvent evaporation method. Prepared solid dispersion was further compressed into as sublingual tablet by direct compression method. The prepared tablets were evaluated for the drug content, weight variation, wetting time, in vitro disintegration, hardness, friability, thickness and in vitro dissolution.

Keywords: Telmisartan, Solid Dispersion, Sublingual Tablet, PVP K 30.