Journal of Bioequivalence & Bioavailability

Formulation development and evaluation of rapid disintegrating tablet of racecadotril with enhanced In-Vitro dissolution using solid dispersion technique

3^rd World Congress Bioavailability & Bioequivalence

March 26-28, 2012 Marriott Hotel & Convention Centre, Hyderabad, India

Gautham Gampa, Gautam Singhvi, Shweta Sharma and Manish Goyal

Posters: J Bioequiv Availab

Abstract:

R acecadotril is an antidiarrheal drug which acts as a peripherally acting enkephalinase inhibitor. It is a BCS class ІІ compound thus the bioavailability can be improved by increasing its aqueous solubility. Solid dispersion is one of the most promising of the many approaches for solubility enhancement because of the greatly enhanced surface area. Solid dispersions of racecadotril were prepared using polymers β-cyclodextrin, poloxamer 188 (Lutrol F 68) and poloxamer 407 (Lutrol F127) in different proportions (1:1, 1:3, 1:5 and 1:10). Solvent evaporation method was employed using methanol as solvent. Solubility studies were carried out using shake flask method at 270C for 24hrs. The pure drug showed aqueous solubility of 18.89μg/ml while the solid dispersions with poloxamer 188 and poloxamer 407 in ratios 1:5 showed solubility of 70.75μg/ml and 58.07μg/ml. There was a 3 fold increase in drug solubility and t-test confirms the superior solubility incase of solid dispersions. The solid dispersion complexes were also characterized using FT-IR spectroscopy and Differential Scanning Calorimetry. The optimized dispersions were formulated into fast disintegrating tablets by wet granulation technique using sodium starch glycolate as disintegrant. The mean dissolution time of the formulated tablet was compared with the marketed formulation by performing dissolution study in USP Type II apparatus operated at 37 0 C and 75rpm. The t 90% for the formulated tablet was found to be lesser than marketed formulation. Thus the formulated tablets have superior dissolution characteristics compared to the marketed tablets and may be beneficial in improving the bioavailability of the drug