Nonlinear relationship between enteric-coated mycophenolate sodium dose and mycophenolic acid exposure in Han kidney transplantation recipients

The aim of the research was to investigate the pharmacokinetics (PK) of enteric-coated mycophenolate sodium (EC-MPS) by quantification of the active metabolite of mycophenolic acid (MPA) after multiple escalating oral doses in Han kidney transplant recipients. A total of 28 Han postoperative kidney...

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Main Authors: Jun Zhang (Author), Mengmeng Jia (Author), Lihua Zuo (Author), Na Li (Author), Yonggang Luo (Author), Zhi Sun (Author), Xiaojian Zhang (Author), Zhenfeng Zhu (Author)
Format: Book
Published: Elsevier, 2017-05-01T00:00:00Z.
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Summary:The aim of the research was to investigate the pharmacokinetics (PK) of enteric-coated mycophenolate sodium (EC-MPS) by quantification of the active metabolite of mycophenolic acid (MPA) after multiple escalating oral doses in Han kidney transplant recipients. A total of 28 Han postoperative kidney transplant recipients were given a multiple-dose of 540, 720 or 900 mg of EC-MPS two times a day in combination with tacrolimus for 6 days. Blood specimens were collected at each time point from 0 to 12 h after EC-MPS administration. MPA plasma concentrations were measured by UPLCUV. The relationship between the EC-MPS dose and its PK parameters was assessed. In the range from 540 to 900 mg, Cmax and AUC012h did not increase with dose escalation. The AUC012h, Cmax, C0 and Tmax for the 540 720 and 900 mg doses were not significantly different, respectively (P >0.05). AUC012 h and Cmax were increased less than proportionally with increasing EC-MPS dose levels. Inter-individual variability in AUC012h, Cmax and C0 were considerable. Nonlinear PK relationships were found from the doses of 540-900 mg of EC-MPS.
Item Description:2211-3835
2211-3843
10.1016/j.apsb.2016.11.003