Clinical Investigation of Valsartan Sustained-Release Matrix Tablets: Formulation Design and Performance Evaluation

Abstract

The primary objective of this main study is to develop and assess the sustained-release matrix tablets containing Valsartan, an angiotensin II receptor type 1 antagonist. The powder mixtures underwent a thorough examination of pre-compression parameters and observed angle of repose, bulk density, tapped density, and Carr’s index, all of which exhibited satisfactory results. Following compression, the tablets were subjected to post-compression evaluations, including weight variation, thickness, hardness, friability, drug content, in-vitro dissolution, and stability studies. In-vitro dissolution investigations are conducted over 24 hours, employing 0.1 N HCL for the initial 2 hours and pH 6.8 phosphate buffer for the subsequent 24 hours. Notably, formulations F4 and F7 demonstrated promising dissolution profiles, effectively controlling the release of the drug. These formulations, enriched with higher concentrations of chitosan and sodium alginate in addition to other polymers, successfully sustained the drug release for the entire 24-hour duration. The compatibility of the drug, polymers, and other excipients was meticulously assessed using FT-IR Spectroscopy, affirming the harmonious interaction among these components. Further analysis involved fitting the release data to various mathematical models, including Zero-order, First-order, Higuchi equation, and Korsmeyer-Peppas model, to ascertain the kinetics and mechanisms governing drug release. Results indicated that the drug release adhered to first-order kinetics, with a non-Fickian mechanism prevailing. Stability studies conducted for 3 months provided reassurance regarding the stability of the selected formulations (F4 and F7), bolstering confidence in their potential for sustained release of Valsartan.