| Plants of Polygala (Polygala tenuifolia willd) or polygala sibirica (polygalasibirica L.) roots, with tranquilizer puzzle, expectorant, swelling of thefunction, multi-compound compatibility for the clinical treatment of heartpalpitations, insomnia, forgetfulness, etc. disease. In recent years, manyscholars have found polygala as a single product also has a strong sedative andhypnotic effects, and its main active ingredient is polygala saponins. Currently,the roots have been isolated from Polygala get Tenuigenin (Onjisaponin) manysaponins A, B, C, D, E, F, G and so on. The results of previous studies by ourgroup showed Tenuigenin B is one of the sedative and hypnotic Polygala mainactive ingredient, but also one which produces toxic ingredients.Currentedition of "Chinese Pharmacopoeia"(2010edition) Polygala herbs under itssaponins are hydrolyzate Tenuigenin-the Tenuifolin as quality controlindicators, and fine herbs in Tenuifolin in Polygala there is no detectioncoverage, so its not a comprehensive indicator for the quality control ofmedicines to control the quality of Polygala. Tenuigenin B as the activeingredient is toxic ingredients, explore the in vivo pharmacokinetics of law toguide the clinical application of the medicine has an important significance.This thesis Tenuigenin B for the study, conducted content analysis of kineticsand pharmacokinetic Polygala herbs in Tenuigenin B, in order to furtherimprove the quality standards of Polygala herbs, interpretation and guidance polygala concocted attenuation to provide a scientific basis for clinicalapplication. In this paper, the main research work done:（1）Polygala established HPLC determination of the content ofTenuigenin B method for improving the quality control of herbs Polygalastandards provide a scientific basis. Experimental results show that thedetermination of five different commercial origin of the content of six batchesof Radix Polygala Tenuigenin B is between1.62%~2.26%, which producedcontent Hebei Polygala highest medicinal Tenuigenin B, while the other fourlittle difference between the origin of the content of herbs.（2）The effects of the commonly used four different processing methodsfor Polygala Pieces Tenuigenin B content. Experimental results show that thecontent of the polygala using honey Tenuigenin B decreased significantly,suggesting Tenuigenin B levels decline may be one of the causes than the rawhoney Polygala Polygala low toxicity; several other processing methods forTenuigenin B does not affect content large, but for other saponins containedPolygala affect whether further study.（3）Discusses Tenuigenin B metabolism rules in rats. Select male SDrats as test animals were divided into high and low two-dose (80mg/kg,40mg/kg) conducted pharmacokinetic studies Tenuigenin B’s. Gavage using asingle method, orbital blood ways, at different time points to determine theconcentration of plasma Tenuigenin B’s; using LC/MS/MS plasma sampleswith high sensitivity and high specificity of detection; DAS software to handlefitting the data to calculate the pharmacokinetic parameters related. The resultsshowed that after a single oral administration of high dose group was the mainpharmacokinetic parameters: Cmax of67.081ug·L-1, Tmax was240min, AUC(0-t) is38513.44ug·L-1·min AUMC (0-t) is18980972.28, t1/2z to441.02min;low-dose group was the main pharmacokinetic parameters: Cmax of43.834ug·L-1·min, Tmax was360min, AUC (0-t) is26270.73ug·L-1·min, AUMC (0-t) was12807100.76, t1/2z is391.695min. The results showed thathigh doses of B Tenuigenin faster absorption and metabolism in thegastrointestinal tract.（4）Preliminary analysis of the Tenuigenin B metabolites in rats. UsingLC/MS method for detecting drug-containing plasma to the theoreticalprediction and experimental results and methods of combiningdrug-containing plasma and blank plasma contrast, were initially rats after oralgavage Tenuigenin B in rats research metabolites. The results showed thatTenuigenin B metabolism in the rat, easy off the end of the partiallyglycosylated, produced at least three kinds of possible metabolites. |
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