Abstract

PREPARATION AND CHARACTERIZATION OF SOLID DISPERSIONS FOR SOLUBILITY ENHANCEMENT OF BCS CLASS II DRUG

Dr. Monica R.P. Rao* and Pranoti A. Chandanshive

ABSTRACT

Budesonide is BCS class II drug (solubility 0.0457 mg/ml) with oral bioavailability of 10-20%. Solid dispersions of budesonide was prepared by solvent evaporation technique using Soluplus® in different ratios. These were characterized by infrared spectroscopy, differential scanning calorimeter, scanning electron microscopy and powder x-ray diffraction studies. FTIR studies confirmed the lack of interaction between drug and Soluplus®. Saturation solubility studies in different media such as water, 0.1 N HCl and phosphate buffer pH 7.4 were performed. A 9 fold increase in solubility in phosphate buffer was observed. Invitro dissolution studies revealed 90 % release whereas plain drug showed 38.75% release in 90 min. Polyethylene glycol (PEG) rectal suppositories were prepared using the solid dispersion bymoulding technique and compared with plain drug suppositories. The suppositories were examined for various properties. The dissolution time at 37°C was found to be 12 min and softening time was 10-12 min. The breaking test revealed that the suppositories had sufficient mechanical strength. The suppositories with solid dispersion exhibited 92 % release in 90 min in phosphate buffer pH 7.4 while plain drug suppositories displayed 68 % release. Thus we may conclude that improved saturation solubility and invitro dissolution of budesonide in presence of Soluplus® will result in its improved bioavailability.

Keywords: Budesonide, Soluplus®, Solid dispersion, Rectal suppositories.