Abstract:
Diosmin is one of the most widely used phlebotonic drugs, but its poor bioavailability has restricted its usage.
The aim of this study was to formulate a complex Diosmin with phospholipids (75% in PC, in 1:2 molar ratios) and to evaluate for solubility, drug content, X-ray diffraction (XRD), differential scanning calorimetry (DSC) and in vitro dissolution study. Further to test the bioavailability of both the complex and Alvenor® in beagle dogs and compare pharmacokinetic parameters. Diosmin herbosome was found to be more soluble than both pure diosmin and Alvenor® The complex contained 71.94% drug content. DSC thermograms and XRD also proved the claim of the complexation. The dissolution profile of diosmin herbosome and Alvenor® in water-ethanol medium showed an increase of the dissolution for diosmin herbosome. Comparison of plasma concentration and main pharmacokinetic parameters of diosmin herbosome treated and Alvenor® treated dogs showed a higher Cmax for the complex with longer elimination half-life. The complexation of diosmin with phospholipids can be potentially used in enhancing the absorption and solubility, consequently increasing the bioavailability of the drug.
