Development and in vivo evaluation of solid dispersions containing nifedipine

Abstract

The main aim of this investigation was to develop and in vivo evaluation solid dispersions of Nifedipine which has low aqueous solubility and bioavailability. Preliminary solubility studies were carried out using various hydrophilic polymers. Formulation with 1:4:2 ratios of Nifedipine, Labrosol and SLS was found to be the best as it possessed better drug release properties compared to pure drug and other physical mixtures. The optimized formulation SD12 was found to have better drug release of 98.74±5.19% in 90 minutes. From FTIR studies no interaction was takes place between drug and polymers. XRD peaks indicate the successful transformation of drug from crystalline to amorphous form. From in vivo bioavailability studies, Cmax of the optimized formulation SD12 was 4.14±0.06ng /ml, was significantly higher as compared to pure drug suspension, i.e., 2.88±0.32ng/ml. Tmax  of optimized formulation was decreased significantly when compared with pure drug (1.00±0.04hr, 2.00±0.05hr), AUC0-inf  and AUC0-t  for optimized solid dispersion formulation was significantly higher (p<0.05) as compared to pure drug suspension. The present study demonstrated that formulation of Nifedipine solid dispersion by solvent evaporation technique is a highly effective strategy for enhancing the bioavailability of poorly water soluble Nifedipine.