The Preparation Of Low Toxicity And High Efficiency Tripterygitium Wilfordill Hook.f.and ?-cyclodextrin Inclusion Complex

Tripterygium wilfordii Hook.f.is mainly used in the treatment of rheumatoid arthritis,glomerulonephritis,nephrotic syndrome,lupus erythematosus and other diseases.But its adverse reactions can not be ignored.The main causes of adverse reaction of the chemical constituents of Tripterygium wilfordii complex and its pharmacodynamics,toxic substance basis is not clear,the lack of scientific and effective quality evaluation and control methods of extraction and purification of diversity,lead to Tripterygium preparations from different manufacturers efficacy and side effects of big differences,the lack of clinical guidelines.Most of the active components in Tripterygium wilfordii were difficult to dissolve in water,which reduced the bioavailability of Tripterygium wilfordii hook.On the basis of previous studies,the present study was to optimize the chromatographic conditions of HPLC,and to establish the fingerprint of 8 batches of different kinds of Chinese crude drugs.HPLC-MS analysis was performed to identify the chromatographic peaks in the fingerprint by using reference and literature comparison,19 constituents in 35 characteristic peaks were identified,including 7 two terpenoids,6 three terpenoids and 5 alkaloids.Based on the experimental results,the partial least square method was used to construct the spectral relationship.The spectrum effect analysis as a guide,in accordance with reserving "major components",controlling "efficacy and toxic components",removing the" toxic ingredients,using macroporous resin and silica gel chromatography,preparation of different proportion of components,and then through the HPLC analysis,Combining with other researchers of the pharmacology experiment results carries on these components of selecting and efficacy,safety verification,screening of high efficiency and low toxicity extract groups were T3-3 components,for the preparation of T3-3:taking the amount of the crude extract,adding methanol dissolved,according to 1:1 adding silica gel(100-200 mesh)stir,with 10 times the amount silica gel(100-200 mesh)packed columns,using dichloromethane-methanol(80:1)solvent elution(10 times the column volume),collecting the eluent,reducing pressure concentration recovery of organic reagent,getting extract,vacuum drying,obtaining.Establishing in viron analysis method of Tripterygium wilfordii Hook.f.of low toxicity and high efficient extraction,using the quality control of Tripterygium wilfordii Hook.f.of low toxicity and high efficient extraction.the extract of low toxicity and high efficiency of Tripterygium wilfordii Hook.f.was packed with beta cyclodextrin,and carring on the single factor test:testing the preparation method of inclusion compound,the feed ratio of inclusion compound,the time of inclusion and the amount of water added.Preliminary determined the high efficiency and low toxicity of Tripterygium wilfordii Hook.f.preparation process of inclusion compound was the grinding method,adding to 2 times amount of water(purified water:beta cyclodextrin =2:1)the feed ratio(cyclodextrin:high efficiency and low toxicity of Tripterygium wilfordii Hook.f.extract)is 10:1,after grinding 1 h drying 24 h.using SEM,X-ray diffraction and DSC were used to identify the low toxicity and high efficiency inclusion compound of Tripterygium wilfordii Hook.f.verifing the formation of inclusions.At the same time,Packet equilibrium solubility complexes were determined.The results show that Tripterygium wilfordii extract will be made from the extract of inclusion compounds,its effective component solubility was significantly increased in distilled water:the solubility of triptolide is improved about 3 times,the solubility of triptonide is improved about 46 times,the solubility of tripterine increased about 3 times,the solubility of wilforlide A is improved 2 times,the time base solubility was significantly improved.The dissolution rate of inclusion compound was determined.Compared with the extract of Tripterygium wilfordii,the solubility of the active components of the extract was significantly improved when the extract of Tripterygium wilfordii was made into inclusion compound.