Preparation Of Scutellaria Baicalensis Extract-phospholipid Complex And The Initial Pharmacodynamics Research

Scutellaria Baicalensis is commonly used in china, and has been used as a traditional Chinese folk medicine for a long time,only contained in "Shen Nong’s Materia Medica". The main effective component of Scutellaria baicalensis flavones, has a variety of pharmacological effects, widely used in the treatment of various diseases. Researches recently find out that Scutellaria baicalensis flavones has positive effects against cerebral edema and cerebral ischemia. However, its liposolubility, water solubility and mucosal permeability are all very poor, which lead to the low concentration in brain and poor bioavailability by oral or intravenous injective administration. Therefore, the drug’s effects against cerebral edema and cerebral ischemia cannot be fully produced. This limited the application of Scutellaria baicalensis flavones. To solve the above problems, we established a new drug carrier system--phospholipid complex, and the phospholipid complex quality standard and stability study, through the preliminary pharmacodynamics experiment to determine the intranasal administration of rationality and validity. Main research contents are as follows:In this paper,in the establishment of Scutellaria baicalensis phospholipid preparation evaluation indexes, through solubility experiment to determine the best solvent composite rate determination In different solvents, the amount of solvent screening to determine the optimum dosage of solvent and Composite rate determination method. Combination of Scutellaria baicalensis phospholipid complex method for the determination, eventually developed an evaluating standard of preparation technology. The final value is Composite rate and baicalin phospholipid complex content as the index of evaluation.two weight, the weight coefficient is0.7, which is a0.3.Through the influence of composite reaction solvent,different PC (phosphatidyl choline) content of soybean lecithin,the reaction temperature, reaction time, concentration of drug, reaction of lipid drug, Magnetic stirring speed7factors single factor study. Consider the economic cost, production feasibility factors. Ultimately determine the main effect factors for the concentration of complex reaction, reaction of lipid drug,the reaction temperature. The total value of evaluation index,using central composite design and response surface methodology to optimize the best process. And in the process of verification, the results show that the process is stable, reliable. The best technique for:With a certain quantity of Scutellaria baicalensis extract and PC content of80%soybean lecithin, the weight ratio of1:2, adding proper amount of dehydration of ethanol, extract drug concentration is3.5mg/ml, In the constant temperature water bath at50℃for2hours in a magnetic stirring which keeping120r/min, recovering solvent, vacuum drying, that is Scutellaria baicalensis phospholipid complex.In this paper,the baicalin phospholipid complex trait, Moisture, TLC, drug content and related substances determination of analysis, establishment of baicalin phospholipid complex quality standards. Through the light, humidity, temperature factors for initial stability study. Determine the storage of baicalin phospholipid complex conditions:In the light of less than40℃, the humidity below37%dry and ventilating place save.In this paper, the method for preparing the rat models of cerebral ischemia reperfusion injury, the neurological function score and infarct rate as evaluation indexes. To phospholipid composition for nasal administration, intraperitoneal dosing, intragastric administration,Screening out three administration routes in the best way for nasal administration;through to the high to low doses of phospholipid complex nasal drug discovery screening, high dose group was significantly better than the low dose group. In the neurological function score, high dose group and model group have significant difference in Statistics, cerebral infarction rate in high dose group and model group had no significant difference,but the trend is clear. Overall consideration phospholipid complex itself loading and rats administrated with the maximum dose limit,t, the determination of effective dose of drug concentration is40mg/ml.