RECENT ADVANCES IN THE SYNTHESIS OF TELMISARTAN: A REVIEW

Premchand Patil, Deepak V. Nagarale, and Dr. Bhata R. Chaudhari*

ABSTRACT

Telmisartan is an effective, 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 attached 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. As a result they may develop insulin sensitivity. It belongs to a class II drug in BCS categorization i.e. low solubility and high permeability. One of the major troubles 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.

Keywords: Telmisartan was discovered and commercialized by Boehringer Ingelheim.