Formulation and Evaluation of Torsemide Granules (Sustained Release)

Abstract

The aim of study was to design development and optimize a controlled release system of Torsemide. to increase its bioavailability by increasing the residence time in the stomach without contact with the mucosa, and was achieved through the preparation of floating granules by melt granulation techniques. Torsemide; a loop diuretic used in the treatment of congestive heart failure and edema was chosen as the drug candidate to be formulated as gastro retentive multiparticulate system as it is a weakly basic drug with a short half life of 2-3 hrs. Gelucire 43/01 was selected as a lipid carrier in different ratio (1:0.5, 1:1, 1:1.5) along with drug. The formulation F₁ to F₆ were prepared and evaluated for dependent variable (in vitro floating ability) and formulations F₄ to F₆ were selected as preliminary optimized formulation. The preliminary optimized formulation F₄ to F₆ were evaluated for micromeritic properties, drug content and percentage yield, in-vitro drug release,  percentage in-vitro floating ability and formulation F₄ was selected as optimized formulation that exhibited good floating ability and zero order drug release (85.95 %) at the end of 8 hours. Aging effect on storage was evaluated using In-vitro drug release. The In-vitro drug release study of the aged sample showed increase in release behaviour, it may be due to phase transformation of Gelucire. In conclusion, hydrophobic lipid, Gelucire 43/01 can be considered as an effective carrier for design of a multi-unit floating drug delivery system of Torsemide.

Keywords: Torsemide, Floating granules, Gelucire, In-vitro release study.