Compound Xueshuantong Capsule Pharmacokinetics Main Active Ingredient Of Dynamics

Research background:Fufang Xueshuantong capsule is a kind of pure traditional Chinese medicine which is jointly developed by the Department of Ophthalmology center of Zhongshan and Guangdong Zhongsheng Pharmaceutical Co., Ltd. At persent, the compound is commonly used in the clinical treatment of various eye diseases, especially has significant curative effect for the treatment of diabetic retinopathy (DR). Currently, with the market lacking of the drugs for treatment DR, because of it’s observably effective function,Fufang Xueshuantong capsule possess an extensive clinical application market in the future and the value of re-development.Thus, to achieve this goal, that clarifying the pharmacodynamic constituents and laying the foundation is significat for the compound.Aim:The Subject based on the previous research, through the studies of serum pharmacochemistry and pharmacokinetic for main effective components to discovery and clarify the material basis of Fufang Xueshuantong capsule.Contents and methods:In the serum medicinal chemistry research, using of ion trap mass spectrometer analysis, we compared the difference of the main effective components in the rat plasma after oral administration Fufang Xueshuantong capsule,in70%methanol extract of capsules and in the standard.In the Pharmacokinetic study,we used a triple quadrupole mass spectrometer to establish the analytical method to simultaneously determinate notoginsenosideR1, ginsenosideRg1, ginsenosideRb1, ginsenosideRe, ginsenosideRd, tanshinoneI(TSA), astragaloside IV (AIV) and harpagoside in of Fufang Xueshuantong capsule in rat plasma. According to the clinical dose of Fufang Xueshuantong, the research calculated the high (4200mg/kg), middle(2100mg/kg) and low(1050mg/kg) dosage to ig the rat.Results:We found that notoginsenosideR1, ginsenosideRg1, ginsenosideRb1, ginsenosideRe, ginsenosideRd, tanshinonel(TSA), astragaloside IV (AIV) and harpagosidein would entrance the plasma after oral administration Fufang Xueshuantong capsule. Determinated the change of concentration the mian effective compounds (notoginsenosideR1, ginsenosideRg1, ginsenosideRb1) wich is from monarch drug Panax notoginseng (Burk.) F.H. in the plasma after rat oral administration. With plasma concentration-time profiles, the study achived the main pharmacokinetic parameters of notoginsenoside R1, ginsenosideRg1, ginsenosideRb1to reflect the pharmacokinetic process of Fufang Xueshuantong capsule in rat. Conclusion: We found that notoginsenosideRi, ginsenosideRgi, ginsenosideRb1, ginsenosideRe, ginsenosideRd, tanshinonel(TSA), astragaloside IV (AFV) and harpagosidein would entrance the plasma after oral administration Fufang Xueshuantong capsule. The result which obtained by non-compartmental model showed that three components have multiple absorption peak and non-linear dynamics of relationships is within the range of high (4200mg/kg), middle (2100mg/kg) and low (1050mg/kg) dose. Absorption, notoginsenosideRi, ginsenosideRgi, ginsenosideRbi rapidly absorbed by rats after ig Fufang Xuanshuantong capusle, have multi-time peaks phenomenon and Tmax is0.17h,0.17h,0.5h hour. Distribution, notoginsenosideRi and ginsenosideRgi distributed immediately after the Cmax, while ginsenoside Rbi shows slow distribution.The three components have widely distributed in rat tissues.Digestion, notoginsenosideRi, ginsenosideRgi, ginsenosideRbi were slowly digested.In addition, T1/2and Ke were calculate by analysis of variance,p>0.05, no significant difference between high (4200mg/kg), middle (2100mg/kg) and low (1050mg/kg) dose, constant ratio to eliminate.