In Vitro and in vivo studies on the complexes of vinpocetine with hydroxypropyl-β-cyclodextrin

摘要: The purpose of this study was to evaluate complexes vinpocetine (VIN), a poorly water-soluble base type drug, with hydroxypropyl-β-cyclodextrin (HP-β-CD) in aqueous environment and solid state, or without citric acid (CA) as an acidifier the complexation medium. apparent stability constant (Kc) calculated by phase solubility 282 M-1 solution structurally characterized by1H-NMR which showed VIN likely fit into cyclodextrin cavity its phenyl ring ethyl ester bond. Solid HP-β-CD were prepared kneading (KE), co-evaporating (CE) freeze-drying (FD) methods. Physical mixtures for comparison. state included differential scanning calorimetry (DSC), X-ray diffractometry (XRD) infrared absorption spectroscopy (IR). From these analyses, CE FD products found amorphous allowing conclusion strong evidences inclusion complex formation. However, dissolution test that only VIN/HP-β-CD+CA method could provide satisfying behavior (rapid, complete lasting) when compared VIN/HP-β-CD complexes. Interestingly, addition CA significantly decrease amount needed solubilize same thereby reducing formulation bulk. Furthermore, in-vivo revealed bioavailability after oral administration rabbits (n=6) improved complex.