| Pyritinol Hydrochloride (Py-Hy) has two molecules of VB6 which connected by disulfide bridge Although its chemical structure is similar to that of VB6 ; Py-Hy does not have the effects of vitamins or antivitamins. Py-Hy is a neurodynamic agent used for improving the loss of memory due to advanced age, nervous exhaustion etc. Py-Hy has proved to show excellent activity. Because of the construction features which have thiol group and phenolic hydroxyl group and lower of the pH value of the common injection of the clinical used, it has very irritation when it injected. Recent years, the reports of initiation serious phlebophlogosis are more and more. In this study, we used two methods to decent irritation and elevate compliance in clinical. One is to develop less-painful formulations utilized hydro soluble metal salts of two adicity as masking agent. The other one is to develop the submicron emulsions ,in which the oil phase or the surfactant layer were assignment as the main drug loading position during the preparation investigation..Meanwhile the physical-chemical properties and stability were also investigated. Py-Hy can be applied to the less-painful the freeze-dried powder and submicron emulsions for intravenous administration. The pharmacokinetics of the formulations was examined.HPLC method was developed for the assay of Py-Hy in vitro. The method is simple, rapid, acute, sensitive, reproducible and suitable for the quality control of Py-Hy freeze-dried powder and submicron emulsions. Liner calibration curve was obtained by plotting concentrate vs. peak area ratio over the rang 2-100 μg · ml-1 The solubility depresses and and the coefficient of oil-water distribution increases with increasing of pH. The in vitro degradation kinetics of Py-Hy was studied. Py-Hy was sensitive to pH and temperature of the system and was easily hydrolyzed by base catalysis.According to the results of pre-formulation study, the stability and the irritant were the main...
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