Formulation development and characterization of Sustained release tablets of nicardipine
Keywords:
Nicardipine, sustained-release tablets, Xanthum gum, Guar gumAbstract
The aim of this study was to develop and characterize sustained-release tablets of nicardipine hydrochloride, a calcium channel blocker used to treat hypertension and angina. Sustained-release formulations improve patient compliance by reducing dosing frequency and maintaining stable plasma drug concentrations. Nicardipine short half-life and high first-pass metabolism make it an ideal candidate for sustained-release delivery systems. The tablets were prepared using the wet granulation technique, employing various hydrophilic and hydrophobic polymers such as Xanthum gum, Guar gum as release-controlling agents. Formulations were optimized by evaluating pre-compression parameters like bulk density, tapped density, compressibility, and angle of repose, as well as post-compression characteristics such as hardness, friability, drug content, weight variation, and in vitro dissolution profiles. In vitro drug release studies were conducted in simulated gastric fluid (pH 1.2) for the initial 2 hours, followed by simulated intestinal fluid (pH 6.8) for 10 hours, using USP Type II dissolution apparatus. The release data were analyzed using kinetic models such as zero-order, first-order, Higuchi, and Korsmeyer-Peppas to determine the release mechanism. The optimized formulation demonstrated sustained drug release for up to 12 hours, following a non-Fickian diffusion mechanism. The results suggest that the combination of Xanthum gum, Guar gum provides effective control over drug release, ensuring prolonged therapeutic effects. Stability studies conducted as per ICH guidelines confirmed the robustness of the formulation. This study highlights the potential of sustained-release nicardipine tablets in improving treatment outcomes and patient adherence.