Studies On The Preparation Of Xingnaojing Parenreral Emulsion

The Compendium of Materia Medica records that aromatic traditional Chinese drugs such as corn mint, borneol and musk have the effectiveness of waking up mind, guiding drugs to move upwards, and animal experiments have testified that they can enter into the brain via the inter-endothelial cell close-up conjunction of blood-brain barrier, heightening the permeability of blood-brain barrier; The nanoemulsion drops in blood circulation can get into brain by being phagocytized by endothelial cell in blood-brain barrier. According to the Chinese traditional medicine recipe of Xingnaojing injection (XNJI), Xingnaojing parenteral emulsion (XNJPE) would be prepared by the optimization of Chinese crude drug extraction processes and screening of emulsion formula and preparation technics. We expect XNJPE could target brain relatively and treat center coma such as aural obstruction, coma and hyperthermy more efficiently after intravenous injection.TLC method was used to identify muscone, gardenoside and volatile oil; Gas chromatography (GC) method was set up to determine the concentration of muscone and borneol; The method of gradient elution high performance liquid chromatography (HPLC) was established to determine the content of curcumin and gardenoside simultaneously.The best extraction technics of musk, fructus gardeniae and radix curcumae were gained by single factor investigation and orthogonal experiment, when effective component contents were as detection index. The result of verification experiment indicated it was efficient and reproducible.Effects of fatty oil, emulsifier, stabilizer, and antioxidant were studied by single factor test, and based on these we found the best formula by orthogonal design when refining soybean oil, emulsifier and stabilizer were as consideration factors, K_e as investigation index. Effects of emulsification temperature, nanomizer working pressure, cycle times and emulsification time were also investigated by single factor test, and then the orthogonal design was adopted to obtain the optimized preparation procedure.The physicochemical properties of XNJPE were studied. The microphotograph showed that most of emulsion drops were round in shape. Gaussian Volume-Wt diameter, zeta-potential, viscosity and pH value is 127±20nm, -32.49mV, 1.243×10^-3Pa·s, 7.20 respectively, and the osmotic pressure was high in a sort.The results of accelerating and long-term stability tests indicated the physical and chemical stability of XNJPE were fine and in compliance with the requirement of preparation stability, but it should be tightly preserved from light and heat. There was no creaming after XNJPE was centrifugated at speed of 4000r/min for 15 minutes, and freezing-heating experiment showed...