Coenzyme Q <sub> 10 </ Sub> Intravenous Emulsion Development

CoenzymeQ₁₀ (CoQ₁₀) is widely distributed in humans and several other mammalian species. In human body concentrations of CoQ₁₀ in heart, liver, kidney, muscle, thyroid and pancreas are higher than the other organs. Total concentration is 0.5～1.5mg. Studies on epidemiology indicate that the concentration of CoQ₁₀ of human being is beginning to descend gradually when we 20 years old. The concentrations of CoQ₁₀ in patient and affection tissues are lower than normal. Many kinds of disease caused by CoQ₁₀ deficiency are hazard human's health.As a liposoluble endogeny antioxidant, hydrogen carrier of mitochondrial respiratory chain and reactivator of cell-metabolism, CoQ₁₀ is widely applied in clinical.At present, there are injection, tablet, capsule and lipid on sale. The price of CoQ10 is too high and it is hardly dissoluble, but it can dissolve in oil, We test the dissolubility, apparent oil/water distribute coefficient (P) and examine the stabilities under the high temperature, oxidation, strong acid, strong base and strong light therefore this article choose the intravenous injection emulsion to be the dosage form of CoQ₁₀.After investigate the basic physico-chemical properties of CoQ₁₀, the pseudo-ternary phase diagrams were obtained, and the best proportion and total dosage were decided. Soybean phospholipid and pluronic F-68 were choose as emulsifiers. Therefore, we frame the recipe of CoQ₁₀ intravenous injection emulsion (2.0mg/ml) . Establish quality evaluation and content determination method of CoQ₁₀ intravenous injection emulsion by HPLC to test the physico-chemical stabilities. One is physical stability, it is about osmotic pressure and stability when mixed with dilutions, it will affect the safety character, when we inject. So we use the CoQ₁₀ intravenous injection emulsion mixed with glucose injection with the ratio of 1:4. The other is chemic stability, we use HPLC to test the concentrationg changes under high temperature, strong light and accelerated test.Establish quality evaluation and content determination method of CoQ₁₀ of rat blood plasma, The CoQ₁₀ intravenous injection emulsion release kinetics of rats is complied with the second order model and solution is mono-order model according to results of B APP2.0. The CoQ₁₀ intravenous injection emulsion we had studied on the formulation and preparation technique, steady physicochemical properties, pharmacokinetics and it will have a good future.