Formulation development and characterization of eplerenone insitu oralgels

Abstract

Gastro retentive drug delivery systems have been widely used to prolong the retention of dosage forms in the stomach. Among the various approaches, the floating in-situ gelling formulation offers sustained drug release as well as prolonged gastric retention, along with the added advantage of the liquid oral dosage form. The present study was an attempt to formulate and evaluate floating in situ gel of Eplerenone by using various polymers like Xanthan gum, Carbopol, HPMC K100M, and Karaya gum which undergoes pH dependant sol-gel transition at gastric pH, thereby prolonging the retention of the system in the stomach. Sodium alginate a natural polymer was employed as a gelling agent where Gelation is triggered by the source of calcium ions in the form of calcium carbonate. Drug and polymers were subjected for compatibility study using FTIR studies, which revealed that there was no interaction between drugs and polymers. The evaluation was carried out for invitro parameters such as gelling nature, Total floating time, drug content, viscosity, & in vitro dissolution studies. Among all the formulations, the F12 formulation containing HPMC K100M was chosen as an optimized formulation that shows maximum drug release by the end of 12hrs and has excellent floating characteristics and gastric retention. From kinetic studies, the optimized formulation shows zero-order release with super case II transport mechanism.