Study On Anti-osteoporosis Of Saponins Of Sulfate Dipsacus And Preparation Of Slow-release Skeletal Pellets

Dipsacus asper is the dry root of dipsacaceae species' Dipsacus asper Wall.ex Henry.Its main distribution for China's Jiangxi,Hubei,Hunan,Guangxi,Sichuan and other places.Due to Dipsacus can “continue to fold bone”and named.Dipsacus micro-temperature,taste bitter,into the liver,kidney by.Autumn digging,remove the root and the fibrous roots,with micro-fire bake to the semi-dry,stacked "sweat" to the internal dark green,and then bake to near dry.The chemical composition is complex and diverse,including saponins(triterpenoid saponins),iridoid terpenes,alkaloids,volatile oils and other ingredients.Dipsacus as orthopedic and gynecological commonly used traditional Chinese medicine,clinical mainly used in Yaoxisuanruan,rheumatism Bitong,bruises,uterine bleeding,fetal leakage.Modern pharmacology proved that Sichuan continued with anti-osteoporosis,promote bone healing,anti-inflammatory,anti-aging,anti-premature birth,abortion,and other pharmacological effects.In this paper,the total saponins and the content of saponin? were used as evaluation indexes.First,two methods were established.For the test sample by adding the new preparation of5% vanillin-glacial acetic acid 0.4ml,perchloric acid 1.6ml,dense shaking.Placed in 60 ? water bath after 20 min to stop the reaction,remove immediately after the ice bath into the cooling,and then fine into the ice acetic acid 10 ml,shake.The absorbance was measured at 540 nm to calculate the total saponin content.The results showed that the concentration of methanol,ultrasonic time and solvent were three main factors.The comprehensive evaluation of the content of total saponins and the content of saponin ? was the final evaluation index,and the orthogonal test was designed.The extraction process of total saponins,That is,plus 10 times the amount of 75% methanol ultrasonic extraction twice,each 30 min.The results showed that the RSD of the total saponins was 1.12% and the RSD of the sapogenin was 0.62%.The results showed that the best extraction process was simple and feasible.The crude extracts of the total saponins were degreased first with petroleum ether and water saturated n-butanol,and then the purification process of total saponins of D101 macroporous resin was investigated.The optimum purification process was as follows: the loading concentration was 0.2g / ml(crude drug)by 2BV / h wet sample loading,the sample volume was 1BV,finally 6BV,70% ethanol at 1BV/ h flow rate elution.The average saponin purity was 98.86% and the RSD was 0.64%.The average saponin transfer rate was 83.35% and the RSD was 1.05%,indicating that the optimal process was stable and could be used for the total saponin Separation and purification.In this experiment,the contents of target components in Kidney Dipsacus were determined.The results showed that the average content of saponin ?,loganin,oleanolic acid and ursolic acid were66.327,2.240,0.157,0.564 mg / g.The experiment also established the HPLC fingerprint of 70% ethanol elution site.The results showed that there were 13 common peaks in the matched peaks.All the common peaks peaked in 20 ~50min,the peak type was stable and the peakcould be well separated.The results showed that the similarity of the total saponin purification system was good,and the quality control of the total saponin was the reference value.The effects of total saponins on the proliferation of osteoblasts,the effect of ALP on the expression of OPG and the expression of OPG and RANKL mRNA were investigated.The results showed that the effect of total saponins on the osteoporosis,Three indicators have shown a certain degree of promotion.Experiments were carried out with the main powder of total saponin as the main drug,and microcrystalline cellulose,ethyl cellulose and stearic acid were used as skeleton materials.Orthogonal test is preferably composed of 10% MCC content,the ratio of ethyl cellulose to stearic acid is 2: 1,and the dosage of lactose is 3%.The optimum process is: the extrusion speed is 25 r / min,the roll speed is 950 r / min,the spheronization time is 3 min.It is proved that the powder and in vitro release of the three batches of pellets are in good agreement with each other.The results showed that the drug release mechanism of Diposide Saponins Sustained Skeleton Pellets was the most consistent with Higuchi equation,which indicated that the drug release was mainly carried out by diffusion mechanism.