Resveratrol Glucoside Liposomes And Its Pharmacokinetics

As the development of people's social life, people's life has beening damagedby cardiovascular disease day by day. Cardiovascular disease is one of the disease thatdisease incidence and deathe rate are the highest in the world. Nowadays, there aremore than about 13 million people sufferd from cardiovascular disease and with thegrowth rate of 10% every year. According to some information, the diseaseincidence of cardiovascular disease in our country is that: high blood pressure is18.8%, coronary heart disease is 10%, fore-cardiopathia is 3%, wind-cardiopathia is1%, acute myocardial infarction is 15.4 per 100 thousand. Adding to the fast growingof aging of the polulation, cardiovascular disease has gone up sharply and the trend isthat many young people has began to suffered the disease year by year. Protectionagainst Cardiovascular disease has become a common problem for all the people inthe world. As an important ingredient of Giant Knotweed Rhizome, Polydatin has anobvious effection against Cardiovascular disease. It is against thromb, therosclerosis,myocardial ischemia, hyperlipemia and has the effection of nervous protection,anti-inflammatory, elieving cough and wheeze, improving minicirculation,therapeutic shock and so on. It has a significant value in clinic and has been focusedin recent years. Liposome is a kind of single or multiple membrane ves which formedby phospholipids dispersing in water, it can envelope liposolubility andwater-solubility medicine. Its structure is just like biological membrane. The liposomemedicine with the carrier of lipsome has a good targeted efficiency and many strongpoints such as improving and extending therapeutic effect, moderating its side effects,avoiding drug resistance and changing medinice's given pathway.The subject optimized the dissolvent, method and so on by cross experiment.Using the technique of macroporous resin and chromatography extracted GiantKnotweed Rhizome's effective part, Polydatin. Then making sure what we haved gotis Polydatin by light spectrum.Using modern liposome technique made liposome which has the efficacy of promoting blood flow, removing blood stasis, dredging themeridian passage and alleviating pain.Its main use is to cure heart and Cerebralvessels disease and supply special chinese new medicine.Methods and results:1 The orthogonal design was used for selecting the best solvent and method, theresult shows that the best technique is 70% ethanol, 12 times ethanol, extracted byrecirculating, 3 times, 2 hours each time.The transfer rate of Polydatin is93.23±2.90%.2 To study 7 different kinds of macroreticular resin's static adsorption action, theresult shows that SP850 resin is the best.3 We adopted SP850 resin to purify Polydatin, the result shows that when theconcentration of sophora extract is 0.20 g/mL, the flow rate is 1 BV/h and theethanol concentration is 40%. The static adsorbtion capacity and elutive ratio weregood. The transfer rate of Polydatin is 78.32±1.44%.4 Adopting the techqique of silica gel column chromatography to purify Polydatinand ethanol and acetylacetic ether are the condition of elution.The structure wascheck by light spectrum.5 The content of Polydatin was determinedby Ultraviolet-Visible spectrophotometryand study on the methodology. According to pharmacopoeia(2005), the methods ofenvelopment ratio was established.6 Studing the membrane material purchased in the market by oxidizing indexmethod, the result shows that the soybean phosphatide fulfills the requirement. Theliposomes were prepared by the following methods: TFV, REV(reverse-phaseevaporation vesicle method), technique of ethanol infusion and aether infusion.The result indicats the encapsulation of liposomes prepared by TFV is the highest.7 The orthogonal design was used for selecting the best technique, and the best isthat the ratio between Lecithin and Cholesterol is 1: 1, the pH of PBS buffer salt is7.0, and the volume is 30 mL. 8 The quality of Polydatin lipsomes were evaluated. The lipsomes shape was sphericalor ellipsoidal, and their size range was 146-505 nm by TEM. The surface charge oflipsomes was negative by electrophoresis and pH=6.68±0.13. The encapsulation ratioof Polydatin in lipsomes was 61.77%. The lipsomes was stored in 3-5℃.9 To prepare the Polydatin liposomes orl liquid and study the programe of metabolismin rat. The pharmacokinetic parameters were computed by software program 3P87and comformed to two compartment model.Conclusion1 We choosed four factors such as the content and the dosage of ethanol, the numberof times and time of extracting and three level to carry out the orthogonal design, andthe reasonable technical method was set.2 SP850 resin has a good effect on the adsorption and desorption of piceid fromPolygonum cuspidatum.3 The method of Ultraviolet-Visible spectrophotometry was sensitive, convenienceand reliable.4 The prepration of Polydatin liposome supplies foundation for the clinic use ofPolydatin.5 Comparison of the pharmacokinetics showed that Polydatin liposomes was rapidlydistributed than Polydatin. It was more effective. The duration was long.