A Review on: Telmisartan

Telmisartan is a potent, long-lasting, nonpeptide antagonist of the angiotensin II type-1 (AT1) receptor that is indicated for the treatment of essential hypertension. It selectively inhibits stimulation of the AT1 receptor by angiotensin II without affecting other receptor systems involved in cardiovascular regulation. Very high lipophilicity a unique feature of telmisartan coupled with a high volume of distribution indicate that the compound offers the clinically important advantage of good tissue penetration. It also activates peroxisome proliferator–activated receptor c (PPAR-c) and increase adiponectin protein content in adipocytes. By this means they may improve insulin sensitivity. It belongs to a class II drug in BCS classification i.e. low solubility and high permeability. One of the major problems with this drug is its low solubility in biological fluids which results into poor bioavailability after oral administration to improve the aqueous solubility and dissolution rate of the telmisartan solid dispersions of drug using different methods were prepared and investigated. Enhancement of solubility of Telmisartan was observed with solid dispersion of drug using carriers such as Poly vinyl pyrrolidonek30, Poly ethylene glycol-4000 and βeta –Cyclodextrin, poly ethylene glycol 6000, alkalizers, Gelucire 43/01, Poloxamer 407, PVP K30 and HPMC E4 , PEG 6000 and NaHCO3. The observed results showed the solid dispersion of drug greater than the pure drug.