NATURAL PRODUCT RESEARCH AND DEVELOPMENT ›› 2018, Vol. 30 ›› Issue (4): 554-558.doi: 10.16333/j.1001-6880.2018.4.004

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Study on The PK-PD Model of Apigenin-7-O-glucronide Based on The Cerebral Ischemia-Reperfusion Injury Model Rats

GONG Zi-peng1,2,3,4, LI Mei1,2,3,4, HU Jian-chun1,2,3,4, WU Lin-lin1,2,3,4, LI Yue-ting1,2,3,4, LI Yong-jun1,2,3,4, WANG Ai-min1,2,3,4*   

  1. 1Guizhou Provincial Key Laboratory of Pharmaceutics,Guizhou Medical University; 2Engineering Research Center for the Development and Application of Ethnic Medicine and TCM (Ministry of Education),Guizhou Medical University; 3School of Pharmacy,Guizhou Medical University; 4National Engineering Research Center of Miao’s Medicines,Guiyang 550004,China
  • Online:2018-05-07 Published:2018-05-07

Abstract: To establish the pharmacokinetic-pharmacodynamic(PK-PD) model of apigenin-7-O-glucronide in Xinshao formula .Firstly,in order to get the concentration-time curve of apigenin-7-O-glucronide in Xinshao formula in plasma collected from different time points of a disease model animal,whose concentration were determined by the method of UPLC-MS.At the same time,two kinds of indexes(SOD and LDH) in the plasma samples of different time points were determined by the kit for time-effect curve.Then the pharmacokinetic software was used to fit the pharmacokinetic parameters of apigenin-7-O-glucronide with the compartmental model and to get PK parameters.After that,the pharmacokinetic parameters were fixed,and the time effect relationship were fitted to get the relevant PD parameters.According to the PD parameters,the PK-PD model of apigenin-7-O-glucronide has been established.When SOD was used as the index of efficacy,the PK-PD model of apigenin-7-O-glucronide was obtained as E= 20.67+(1.22×Ce)/(Ce+5.58);When LDH was used as the index of efficacy,the PK-PD model of apigenin-7-O-glucronide was obtained as E= 214.17-(32.72×Ce)/(Ce+0.08).The PK-PD model of apigenin-7-O-glucronide in the formula showed that the concentration of SOD and LDH was correlated with the concentration of apigenin-7-O-glucronide.The formula and its main active compound apigenin-7-O-glucronide could protect cerebral ischemia reperfusion injury by increasing SOD and decreasing LDH.

Key words: Cerebral Ischemia-Reperfusion Injury Model Rats, Xinshao formula, apigenin-7-O-glucronide, PK-PD model

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