Extraction Of Active Constituents And Its Correlative Foundation Studies

The dry fruit of Cornusofficinalis Sieb. et Zucc. is a traditional Chinese herb used for nourishing liver and kidney. It has been increasingly paid much attention as one of the most popular and cherish herbal medicine in clinic in the world and can be used for medicine, hygienic food and cosmetic due to its biological and pharmacyological actives such as anti-inflammation, anti-virous and anti-oxidation and so on. There is the largest Cornusofficinalis Sieb. et Zucc. production base which has acquired GAP authentication in He'nan Province. Therefore, it is of important social significance and commercial values to investingate extraction of its useful components, its exploitation and utilization.With occurring the upsurge of savageness, nitrition and returning to nature all over the world, supercritical fluid extraction technology holds prominent ststus in the domain of extraction of natureal products as a kind of effective and clean separateion technology. The feasibility and the optimal conditions of extracting volatile oil and total saponins with supercritical CO₂ from Cornusofficinalis Sieb. et Zucc. grown in Nanyang, He'nan Province were investingated.Firstly, three volatile oil samples were prepared with steam distillation(SD) and supercritical CO₂ extraction(SFE) in different experimental conditions respectively and analysised by GC-MS. It is found that SD sample's colour, purfume and chemical components different greatly from that of the two SFE Samples. 52 kinds of substances were found and the content of hydrocarbon is high up to 27.83% in SD sample. However the two SFE samples posses 24 and 14 substances and the approximately samemain consition, 1 , 2-Benzenedicarboxylic acid, mono (2-ethylhexyl) ester high up to48.31% and 45.50% respectively. Their content of hydrocarbon reduced greatly. The results demonstrated the selectivity of SFE is much higher.The process of extracting total saponins was further studied from the remains after extracting oil from Cornus officinalis Sieb. et Zucc with supercritical CO₂. The effects of extraction temperature, pressure, the kinds and dosage of entrainers, granularity, time and flow rate of CO₂ on the extraction yield of saponins were studied, and the optimum parameters and conditions were finally achieved. The experiment results shows: under optimum conditions eg. Granularity 0.2-0.3mm, pressure 35Mpa, temperature 55℃, absolute ethyl alcohol(v/w 0.75) as entrainer, flow rate of CO₂ Skg·hr^-1, time 3.5h, the content of total saponons is 2.87mg·g^-1. Compared with the conventional extraction technology, it has evident advantages to extract saponins with supercritical CO₂. In addition, it is proved that the results of lab-scale experiments can be successfully blown up and the supercritical fluid extraction technology of saponins has excellent foreground.Diethyl ether, ethyl acetate and methanol as extracting solvents respectively, 10 batches of Cornus officinalis Sieb. et Zucc were soxhet extracted and extracted solution were analysized by HPLC fingerprint with the gradient elution mode, acetontrile-methanol-water as flow phase. The result shows: llpeaks were co-possesed by each batch and the area of the co-possesed peaks is above 90% of total areas. The establishment of technical parameters of fingerprint for the liposoluble components from Cornus Officinalis by HPLC affords basic data for the quality control of Cornus Officinalis drugs.Large quantity of OLA was separated from supercritical extract of Cornus officinalis Sieb. et Zucc. OLA is used to treat acute icterohepatitis and toxic hepatitis in clinical. But the lower solubility and the siower dissolution rate of OLA in water make for the lower biotic utilization ratio . To enhance the dissolution rate of OLA, the solid dispersion systems consisting of oleanolic acid and polyviny pyrrolidone (PV P) were made by solvent evaporation method. DSC shows the transition of crystal form of OLA with addition of carrier PVPk-30. IR spectrum proved the formation of hydrogen bond between OLA and PVPk-30. The solubility experiment in vitro reveals the dissolution of OLA solid dispersion systems is near seven times than the that of OLA standard 100minutes. The results demonstrate OLA solid dispersion systems can dramaticly improve the solubility of OLA in water.The solubility of oleanolic acid in supercritical CO₂ was measured by static method. An Chrastil's association model with three constants, an inproved Chrastil's association model with four constants and another association model with definite physics meaning were employed to correlate the solubility data of oleanolic acid in supercritical CO₂ respectively. The averagee relative deviations of the three association models are 7.01 %,16.99%,2.32%, which shows the third models has much better correalated accuracy than the other two. The correalated parameters can be explained reasonably.