Fenazinel Dihydrochloride

This paper aims to investigate the protective effect of fenazinel dihydrochloride(FD) on focal cerebral ischemia injury in rats and to explore its possible mechanism.Middle cerebral artery occlusion (MCAO) was used to induce focal cerebral ischemia model.After 24 h ischemia, the infarct area was determined by the method of TTC staining, and the ischemia brains of some other rats were used for measurements of superoxide dismutase (SOD) activity, malondialdehyde (MDA) content, lactic acid (LA) content and the histopathol. change.Cortical neurons of fetal rats were cultured in vitro.The protective effects of FD on injuries by treating cells with FBS retraction medium and with N-methyl-D-aspartic acid (NMDA) were observed by determinations of cell death rate, activity of SOD and change of MAD/LA level.FD decreased the infarct area in MCAO model, increased the activity of SOD in brain, lowed the MDA/LA level, and protected against the brain histol. injury.In neuron cells, FD not only increased neuron survival rate and activity of SOD, but also downregulated the MDA/LA level.FD is able to protect cerebral ischemia with involvement of decreasing NMDA level, attenuating oxygen-derived free radicals and improving energy metabolism

The formulation of fenazinel dihydrochloride injection was optimized with appearance, color, pH, drug content and related substances as the indexes.Sodium bisulfite was used as the stabilizer, and the pH value of injection should be controlled within 3.0-4.0.The prepared product was stable when stored at room temperature in a light-resistant container for 18 mo or mixed with 0.9% sodium chloride injection or 5% glucose injection within 24 h.