Development of Nifedipine sublingual tablets using disintegrants as release modifiers

Abstract

The current study mainly focused on treating cardiovascular diseases such as angina pectoris and chronic hypertension by modifying the existing commercial tablet available for Nifedipine. The limitation of Nifedipine is poor solubility, which comes under BCS class II drug category, which needs improvement in formulation to achieve better bioavailability. The objective of this research work is to enhance the oral bioavailability (first-pass metabolism in the liver (42–56%)) of Nifedipine by improving dissolution property. Sublingual fast dissolving tablets of Nifedipine formulated by sublimation method, designed to increase its disintegration time in the presence of saliva. This formulation is helpful for paediatric and geriatric patients who are unable to swallow the conventional tablet. Sublimation of camphor makes the tablet more porous and improve disintegration time as well. The direct compression method is used with different ratio of Croscarmellose Sodium (CS) and Sodium Starch Glycolate (SSG) as super disintegrants to formulate Nifedipine loaded Sublingual tablets. All formulations contain various ratio between super disintegrants and camphor, followed by the sublimation method. FTIR and DSC studies were conducted to investigate compatibility between drugs and disintegrants. Formulated tablets were subjected for precompression parameters, e.g., bulk density, tapped density, Carr’s index, Hausner’s ratio, angle of repose and for post-compression parameters, e.g. weight variation, thickness, hardness, friability, drug content, wetting time, disintegration time followed by dissolution study and found satisfactory as per IP.