Abstract

PREPARATION AND CHARACTERIZATION OF IRBESARTAN HYDROTROPIC SOLID DISPERSION TABLET

Pooja R. Gawandar* and Amrapali B. Jadhav

ABSTRACT

Oral bioavailability of Irbesartan (IRB) is only 60% due to its poor aqueous solubility and dissolution rate. The present research work was aimed for improvement of dissolution of IRB by hydrotropic solid dispersion technique which is supposed to improve oral bioavailability. Solid dispersions of IRB were prepared using various hydrotropic agents (Sodium Salicylate, Urea, Sodium Citrate and Sodium alginate) in different ratios. Quantitative solubility of selected formulations were evaluated after a trial of physical solubility study of all the formulations. Formulation G [Sodium Salicylate 10% + Urea 10%+Sodium citrate 10%] and formulation I[Sodium Salicylate 15% + Sodium citrate 15%] were taken for solid dispersion. Formulation G and I have been characterized by instrumental study such as XRD (D8 Advanced model of Brukar Axs Company in the 30-800 2 Theta scale) FTIR Shimadzu (IR Prestige 21). Formulation G and I have been tableted (each tablet contains 150mg IRB) using Micro Crystalline Cellulose (MCC 102), as major filler by direct compression applying 100-120 N pressure. Solubility of G and I have been improved to 3.4 (0.043mg/ml) times and 3.8 (0.048mg/ml) times respectively compared to pure drug (0.012mg/ml). IRB dissolution of tablet A has been improved to 71.76% in SGF (0.1N HCl) and amorphization of drug in Solid dispersions (decreased intensity of XRD and is appearance of endothermic peak of crystalline drug) have brought about improved dissolution.

Keywords: Irbesartan, solubility enhancement, hydrotropic agents, solid dispersion.