Formulation and Evaluation of Solid Dispersion of Felodipine by Hot Melt Extrusion for Enhancement of Solubility

Abstract

ABSTRACT Background: Felodipine (BCS Class II) undergoes extensive first-pass metabolism with bioavailability of about 15% that creates problem in therapeutic efficacy after oral administration. Objective: Immediate release formulation of felodipine was developed using hot-melt extrusion (HME) technique in an attempt to improve solubility and dissolution of felodipine through the solid dispersion technique. Materials and Methods: The solid dispersion was prepared using Eudragit EPO, NE30D as a carrier with different drug polymer ratios using the HME technique. The optimized batch was made into tablets. The solid dispersion was characterized by solubility studies, drug content, and in vitro dissolution rate studies. Results: From the cumulative dissolution profile, it was observed that the drug and Eudragit EPO alone have the highest percentage of drug release compared to the other combinations of drug and Eudragit EPO, NE30D. It is also evident from the dissolution profile that with increase in the concentration of Eudragit NE30D, there is a decrease in the dissolution rate. There was a significant decrease in drug release even with increase in stabilizer in a smaller ratio. The dissolution profile showed that there is not much variation in the release profile of the solid dispersion alone and the solid dispersion tablets. Conclusions: Solid dispersion by the HME technique is an effective method to increase the dissolution rate of felodipine.