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Solubility Enhancement of Telmisartan as Solid Dispersion by Different Methods

Hiba A. Aziz
Department of Pharmaceutics, College of Pharmacy, University of Baghdad, Baghdad, Iraq.
Entidhar J. Al-Akkam
Department of Pharmaceutics, College of Pharmacy, University of Baghdad, Baghdad, Iraq.

Abstract

Background Telmisartanis an antihypertensive angiotensin II receptor antagonist drug commonly used to treat hypertension. It’s a BCS Class II poorly soluble drug in the Biopharmaceutical Classification System (BCS). Objective To increase the solubility and rate of dissolution of Telmisartan utilizing a solid dispersion method. Methods Two methods were obtained to prepare solid dispersion ofTelmisartan: solvent evaporation and kneading method. Each method used different polymersusing soluplus, poloxamer (188,407), and polyethylene glycol (4000,6000) as hydrophiliccarriersin different ratiosof 1%, 2%, and 3%. Results It was observed that the solid dispersion showsan increase in solubility in comparison to its pure drug. The best formula was obtained withthe formula (Telmisartan, soluplus at a 1:3 ratio) Conclusion By preparingTelmisartanas asolid dispersion via the solvent evaporation method, its solubility, and dissolution have been improved. Using a 1:3 ratio of hydrophilic carriers (drug: carrier). Its enhanced wettability and decreased crystallinity result in enhanced drug solubility and dissolution.

Keywords: Poloxamer, Polyethylene glycol, solid dispersion, soluplus,Telmisartan ,

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