Extraction And Separation Of Active Components From Tripterygium Wilfordii And Microspheres Preparation

Tripterygium Wilfordii Hook.f. (T. Wilfordii) is a traditional Chinese herb which has many pharmacological effects such as anti-inflammation, antibacterial effect, immunosuppression, antifertility, anti-tumor and so on. So far most of products from T. Wilfordiii are crude extracts,in which triptolide is considered to have great curative effect on rheumatoid arthritis, but tripterine has been considered to have toxicity and side effects. It is a problem all long that how to reduce the tripterine and how to increase the content of effective triptolide in the extracts. Recently tripterine was found to be a effective anti-tumor in spite of its toxicity. The purpose of this paper is to extract and isolate triptolide and tripterine by advanced extraction and separation technologies, which has important values for developing new medicines.The pretreatment method for analysis of tripterine in raw material was improved. With the raw material was first carried out by ultrasonic extraction in methanol, and then treated by acid precipitation and extraction with ethyl acetate, the yield can be increased by 34% with RSD of 2.65%. This improved method is simple, rapid and accurate.Supercritical carbon dioxide extraction was used to extract both triptolide and tripterine effectively under the investigated optimal conditions. Then a valid purification process of acidification–alkalization–organic solvent extraction was further employed to separate triptolide and tripterine. The analytical results show that the content of tripterine in the product of triptolide is close to zero, while the content of triptolide in the product of tripterine is also reduced to 0.05%. The yield of triptolide is 2.71×10-3% and the content of triptolide in its products is 0.75%, both of which are much higher than the literature reported values. The content of tripterine in its product is high up to 35.76%.The preparation of microspheres of the tripterine product was studied. The influences of the concentration of PLGA, the concentration of PVA, the ratio of drug to PLGA and the rotate speed on the encapsulation efficiency were investigated. Under the reasonable conditions, round smooth and even particle size microspheres with the encapsulation efficiency of about 80% can be obtained.