The Preliminary Study On Total Saponins Of Astragalus Sustained-released Tablets

OBJECTIVE: To optimize the technology of Total Saponins of Astragalus(TSA) extracted and purified from Radix Astragal and obtain the TSA raw material with high purity; To prepare the TSA sustained-released tablets and establish the quality control standard of TSA raw material and sustained-released tablets; To investigate the preliminary stability of them.METHODS: The extraction and purification technology of TSA were studied by orthogonal test design and compare experiments selecting the three factors which can affect the extraction process and different methods for purification. The content of TSA and astragaloside IV were controlled by UV spectrophotometry and HPLC. Using blood viscosity, plasma viscosity, hematocrit, thrombin time and blood hemaleucin quantity as the detection index, the precaution and therapeutical effect of TSA raw material on blood stasis rats were studied. Using HPMC and EC as sustained-release framework materials and MCC as quick-release materials, the factors' effective on dissolution was explored. Uniform Design method was applied to optimize prescription of TSA sustained-released tablets. Using TSA and astragaloside IV as the detection index , the standard of TSA quality control was established by UV and HPLC. The preliminary stability of them studied and the influencing factors include the high temperature and the high humidity were observed.RESULTS: The optimum extractive condition of TSA was the slices of Radix Astragal refluxed with 8 times amount of 70% alcohol for 1. 5 hours and then with 6 times amount of 70% alcohol for 1 hour; D₁₀₁ macroreticular resin was used to adsorb and purify the TSA with 70% alcohol to elutriate and four multiples of column volume was best, the purity quotient of TSA was up to 73. 5%. So defined the purity of TSA not less then 70% and the content of astragaloside IV not less than 3%. Raw TSA was stable at high temperature and high humidity, but it was easy to absorb water and must be stored in a dry place with being sealed. Differentdosage, low, middle, high, all had effective on blood stasis rats. All could cut down blood viscosity and plasma viscosity, lengthen prothrombin time and degrad blood fibrinous quantity. HPMC, EC, MCC were the major factors on dissolution of TSA sustained-released tablet. When the principal agent was 150mg, the HPMC was 56mg, EC was 84mg, MCC was 75mg, the prescription was the best. Purity quotient of TSA was defined not less than 90mg and content of astragaloside IV not less than 4. Omg. Preliminary stability indicated that TSA was stable at high temperature and high humidity except absorbing water easily and the tablets must store in dry air.CONCLUSION: The method of using alcohol and Djoi macroreticular resin could adsorb and purify TSA best. TCL, UV, HPLC were qualitative and quantitative methods for TSA raw material and TSA sustained-released tablets. TSA could cut down blood viscosity and prevent thrombotic. Uniform Design could be used to optimize the TSA sustained-released tablets. Preliminary stability indicated that TSA raw material and TSA sustained-released tablets are stablilty.