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Abstract
Pharmaceutical Care and Research: 2018; 18(1):21-25
DOI: 10.5428/pcar20180105
Enterohepatic circulation of mycophenolic acid in rat models
1. XIA Qin1(1.Department of Pharmacy,Ruijin Hospital Affiliated to School of Medicine,Shanghai Jiaotong University,Shanghai 200025,China 2.Department of Physiology,School of Medicine,Shanghai Jiaotong University,Shanghai 200025,China xiaqin_@126.com)
2. JIANG HuiTing1(1.Department of Pharmacy,Ruijin Hospital Affiliated to School of Medicine,Shanghai Jiaotong University,Shanghai 200025,China 2.Department of Physiology,School of Medicine,Shanghai Jiaotong University,Shanghai 200025,China )
3. ZHI JianMing2(1.Department of Pharmacy,Ruijin Hospital Affiliated to School of Medicine,Shanghai Jiaotong University,Shanghai 200025,China 2.Department of Physiology,School of Medicine,Shanghai Jiaotong University,Shanghai 200025,China )
4. CHEN Bing1(1.Department of Pharmacy,Ruijin Hospital Affiliated to School of Medicine,Shanghai Jiaotong University,Shanghai 200025,China 2.Department of Physiology,School of Medicine,Shanghai Jiaotong University,Shanghai 200025,China chenchenbing@163.com)
ABSTRACT  Objective: To study the enterohepatic circulation of mycophenolic acid (MPA) in rats.Methods: Five male SD rats were intravenously injected with MPA.Whole blood samples 0-12 h after medication was collected,and plasma concentrations of MPA were determined.Five male SD rats were intravenously injected with MPA,the bile samples 0-12 h later were collected,and concentrations of MPA and 7-O-glucuronide conjugate of MPA(MPAG) were determined.The rat model of enterohepatic circulation was established by using 10 pairs of male SD rats and MPA plasma concentrations of donor and recipient rats 0-12 h later were also determined.Results: The AUC0-12 h of MPA was (43.3±20.4) μg·h·ml-1 after intravenous injection of MPA 20 mg/kg.There was a peak at hour 8 after MPA administration.In the rat bile test,the excretion rates of MPA from bile were 0.078,0.077,0.049,0.062,0.079,0.114,0.120,0.073 mg respectively at the time points of 0 to 0.33 h, 0.33 to 0.67 h,0.67 to 1 h,1 to 1.5 h,1.5 to 2 h,2 to 4 h,4 to 8 h,8 to 12 h.AUC0-12 h of MPA for bile-donor rats and bile-recipient rats were (42.3±27.1) and (4.28±3.05) μg·h·ml-1, respectively.There was a peak concentration of MPA in recipient rats at hour 8 after bile transferred.Conclusion: About 10% of MPA was reabsorbed in enterohepatic circulation,which is consistent with the process in the human body.The peak value of MPA in enterohepatic circulation in the rat model was 6-8 h after administration of MPA.
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XIA Qin1,JIANG HuiTing1,ZHI JianMing2,CHEN Bing1,. Enterohepatic circulation of mycophenolic acid in rat models[J]. Pharmaceutical Care and Research / yao xue fu wu yu yan jiu. 2018; 18(1): 21-25.
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