ENHANCEMENT OF AQUEOUS SOLUBILITY AND DISSOLUTION OF TELMISARTAN USING SOLID DISPERSION TECHNIQUEAbstract
The present study was aimed to improve the water solubility and bioavailability of telmisartan by solid dispersion technique. Telmisartan is 4′-[(1,4′-dimethyl-2′-propyl[2,6′-bi-1H-benzimidazol]-1 ‘- yl) methyl]- [1, 1’-biphenyl]- 2- carboxylic acid. Telmisartan is practically insoluble in water. Telmisartan is an angiotensin II receptor antagonist (ARB), used in the management of hypertension. Solid dispersions of telmisartan were prepared by using polyethylene glycol 4000 and mannitol as hydrophilic carriers in different weight ratios by a solvent evaporation method. The drug and the solid dispersions were characterized by saturation solubility studies, in-vitro dissolution study, Fourier-transform infrared spectroscopy, differential scanning calorimetry, drug content estimation, and stability study. Based on physical characters and drug release pattern, formulation F2 (1 g drug, 4 g PEG 4000 and 1 g mannitol) exhibited the best results. The carriers, polyethylene glycol 4000 and mannitol, were found to be effective in increasing the aqueous solubility and dissolution rate of telmisartan in solid dispersions when compared to the pure drug.
A. Dubey *, A. A. Kharia and D. P. Chatterjee
Oriental College of Pharmacy, Department of Pharmaceutics, Thakral Nagar, Bhopal, Madhya Pradesh, India.
03 April 2014
28 May 2014
17 July, 2014
01 October 2014