Abstract 06 V2 I4

Azilsartan medoxomil is [(5-methyl-2-oxo-1, 3-dioxol-4-yl) methyl 2-ethoxy-1-{[2'-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)biphenyl-4- yl]methyl}-1H-benzimidazole-7-carboxylate] with a molecular weight of 568.5 g/mol. It is a selective AT1 subtype angiotensin II receptor blocker and is indicated for the treatment of mild to moderate essential hypertension. It is having stumpy aqueous solubility, so the aim is to augment the solubility of azilsartan by solid dispersion and complexation methods. Further fabricate them into tablets by direct compression method.

Solid dispersion and inclusion complex were fabricated following solvent evaporation method using poloxamer-407 and methyl β-cyclodextrin as a carrier. The equipped formulations were characterized for compatibility by differential scanning calorimetry (DSC), X-ray diffraction (PXRD) studies and Fourier-transform infrared spectroscopy (FTIR). FT-IR study revealed no interaction between drug and excipients. Among all methods, solid dispersion ASD2 containing active pharmaceutical ingredient: poloxamer 407 in the ratio of 1:3 showed quick and high drug release (89.42% within 40 min).

The tablets formulated using ASD2 solid dispersion and AC2 inclusion complex were characterized for both precompression and postcompression parameters. All the data gathered from the precompression and postcompression parameters accomplish the official requirements of tablets.

The % drug release from the AF1 batch tablet is higher 86.85% than the AF2 batch tablets 73.56% within 40 minutes. Stability studies of AF1 batch tablets showed no noteworthy alteration in formulation during study period. Thus, it can be recapitulated that the formulation was unwavering.

Keywords: Bioavailability, Azilsartan, Poloxamer-407, Stability studies, PXRD.