Pharmacokinetics of mycophenolate mofetil in adult Chinese patients with autoimmune disease
10.13699/j.cnki.1001-6821.2015.02.007
- VernacularTitle:吗替麦考酚酯在自身免疫性疾病患者体内的药代动力学研究
- Author:
Hong-Jun CHEN
1
;
Zi-Cheng YU
;
Rong ZHOU
;
Jie SHEN
;
Zhi-Bin GAN
;
Yuan-Jun TANG
Author Information
1. 同济大学 附属杨浦医院 临床药学与药理学研究室
- Keywords:
mycophenolate mofetil;
mycophenolic acid;
mycophenolic acid glucuronide;
autoimmune disease;
pharmacokinetics
- From:
The Chinese Journal of Clinical Pharmacology
2015;(2):102-105
- CountryChina
- Language:Chinese
-
Abstract:
Objective To investigate the pharmacokinetics of mycophe-nolate mofetil ( MMF) in Chinese adult patients with autoimmune disea-ses.Methods Fourteen patients with autoimmune disease were included in this study.Oral dose ( MMF 0.75 g, q12 h) was given for the first time and 7 days later steady -state.Serum concentrations of the myco-phenolic acid ( MPA) , an active metabolite of the pro -drug MMF, and its phenol glucuronide metabolite ( MPAG ) were determined by HPLC method.Pharmacokinetic parameters of MPA and MPAG were calculated and influences of renal function on MPA drug exposure and MPAG drug exposure in steady -state were investigated.Results The main pharma-cokinetic parameters of MPA after first -dose and steady -state were as follows: Cmax were ( 8.45 ±7.54 ) , ( 10.89 ±4.37 ) mg · L-1 , AUC0-12 h were (41.07 ±49.26 ), (55.09 ±41.74 ) mg· h· L-1 and the main pharmacokinetic parameters of MPAG after first -dose and steady-state were as follows: Cmax were (41.24 ±28.57 ), (67.63 ± 36.98) mg · L-1, AUC0-12h were (487.25 ±326.53 ), (720.79 ± 413.86 ) mg· h· L-1.A large variability existed in pharmacokinetic parameters of MPA and MPAG.The differences in pharmacokinetic parameters are larger between individual patient of the two groups , the AUC0-12h of steady -state compared with the first administration were both obviously greater ( P<0.05 ).There was an obviously inverse relation-ship between MPAG drug exposure and renal function ( P<0.05 ) , however , MPA drug exposure was less affected by renal function ( P>0.05 ).Conclusion In patients with autoimmune disease receiving a fixed MMF dose , there is a large inter-individual variability of MMF pharmacokinetics and accumulation of MPA and MPAG drug exposure .In addition, a significant accumulated phenomenon was found.
