Design and Development of Fenofibrate Solid Dispersions for Solubility Enhancement

Abstract

This research work designed to overcome the problems associated with poorly aqueous soluble drug. Fenofibrate (FENO) being BCS Class II drug shows low solubility but permeability is high. Compatibility of the drug and polymer studies was done by FTIR. Physical mixtures (PM) of the drug and polymer HPMCAS were prepared by trituration method. Fenofibrate solid dispersions (SD) were prepared by common solvent technique ascribed feasibility in laboratory scale. Physical state of formulations was characterized by powder XRD, TGA. Solubility of pure drug (FENO), Physical mixture and SD found to be 0.3, 0.78±0.15 to 1.15±0.28 and 2.17±0.37 to 3.25±0.14 mg/ml respectively. Percentage yield and percentage drug content were determined and found within satisfactory range. The maximum cumulative percentage of drug release from pure drug (FENO), Physical mixture and SD found to be 34.5%, 72.1 and 97.2% respectively at 60 minutes. Microscopy (SEM) study was found that the prepared solid dispersion has porous morphology. The present study establishes the increased bioavailability of the optimized batch when compared with the pure FENO. There was significant (50%) increase in absorption of Fenofibrate observed from the in vitro everted gut sac model. SD of FENO was developed successfully. The solubility of FENO was ameliorated significantly while compared with API (pure FENO). This research work found formulation of SD preferable technique to enhance solubility and enhance dissolution of lipophilic drugs.

Investigating the Influence of Processing Conditions on Dissolution and Physical Stability of Solid Dispersions with Fenofibrate and Mesoporous Silica

“…Diffractograms of crystalline FF, PM-30, Syloid, and SDs with 30% FF prepared under different conditions are shown in Figures 5 and 6. While Syloid does not give any distinct peaks, crystalline FF shows distinct Bragg peaks at 2θ 14.3, 16.6, 17.8, 20.8, 22.2, 24.6, and 29.0, which is in line with the published literature [32,34,35]. PM-30 also shows distinct peaks at most of these values, implying that FF is present in crystalline form, as was already postulated with DSC.…”