文章摘要
朱婷婷,薛源,赵宇蕾,过怿赟,孙胜利,芮建中,周国华.咪唑立宾在中国肾病患儿中的药代动力学研究[J].药学与临床研究,2019,27(6):411~415
咪唑立宾在中国肾病患儿中的药代动力学研究
Pharmacokinetics of Mizoribine in Children with Nephropathy in China
投稿时间:2019-04-30  修订日期:2019-12-06
DOI:
中文关键词: 咪唑立宾  儿童肾病  高效液相色谱法  血药浓度  药代动力学
英文关键词: Mizoribine  Children with nephropathy  High performance liquid chromatography  Serum concentration  Pharmacokinetics
基金项目:南京军区南京总医院院管课题(2011058)
作者单位E-mail
朱婷婷 东部战区总医院药理科 zhutingting00790@126.com 
薛源 东部战区总医院药理科  
赵宇蕾 东部战区总医院药理科  
过怿赟 皖南医学院弋矶山医院药学部  
孙胜利 东部战区总医院药理科  
芮建中 东部战区总医院药理科 ruijianzhong@126.com 
周国华 东部战区总医院药理科  
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中文摘要:
      目的:测定肾病患儿口服咪唑立宾后体内血清药物浓度,研究咪唑立宾在中国肾病患儿中的药代动力学特征。方法:14例肾病患儿,口服咪唑立宾片达到稳态,分别在服药前(0 h)以及服药后2、3、4、6、8、12 h采血,共86个采血点。采用高效液相色谱法测定药物浓度数据,分别用非房室模型法和一房室模型法进行药代动力学参数拟合。结果:非房室模型法的主要药代动力学参数Tmax为(2.5±0.52) h、Cmax为(3.33±1.75) mg·L-1、AUC0-t为(18.05±10.43) h·mg·L-1、AUC0-∞为19.23±11.47 h·mg·L-1、V为(42.06±27.73) L、CL为(12.72±8.63) L·h-1、t1/2为(2.36±0.47) h,MRT0-t为(4.45±0.45) h。一房室模型法的药代动力学参数为Tmax为(2.1±0.65) h、Cmax为(2.91±1.42) mg·L-1、AUC0-t为(18.86±10.80) h·mg·L-1、AUC0-∞为(20.04±11.89) h·mg·L-1、V为(37.94±23.26) L、CL为(12.23±6.93) L·h-1、t1/2为(2.17±0.47) h。结论:本研究测定人血清中咪唑立宾浓度简便准确,初步建立咪唑立宾在中国肾病患儿中的药代动力学模型,可以针对Tmax、Cmax和AUC等药代动力学参数调整用药剂量,提高用药安全性和有效性。
英文摘要:
      Objective: To study the pharmacokinetic characteristics of mizoribine in children with nephropathy by measuring its serum concentrations in vivo. Methods: Chinese children with nephropathy were treated with mizoribine tablets to achieve steady state, then blood samples were collected at time points before (0 h) and 2, 3, 4, 6, 8 and 12 hours after administration to determine serum mizoribine concentrations by high performance liquid chromatography. The pharmacokinetic parameters of mizoribine were fitted based on 86 sampling points from 14 children by a non-compartment model and a one-compartment model, respectively, with the Phoenix WinNonlin 8.0 software. Results: The main pharmacokinetic parameters for mizoribine by the non-compartment model were as follows: Tmax (2.5±0.52) h, Cmax (3.33±1.75) mg·L-1, AUC0-t (18.05±10.43) h·mg·L-1, AUC0-∞ (19.23±11.47) h·mg·L-1, V (42.06±27.73) L, CL (12.72±8.63) L·h-1, t1/2 (2.36±0.47) h and MRT0-t (4.45±0.45) h. Those by the one-compartment model were as follows: Tmax (2.1±0.65) h, Cmax (2.91±1.42) mg·L-1, AUC0-t (18.86±10.80) h·mg·L-1, AUC0-∞ (20.04±11.89) h·mg·L-1, V (37.94±23.26) L, CL (12.23±6.93) L·h-1 and t1/2 (2.17±0.47) h. Conclusions: This study is simple and accurate to determine the concentrations of mizoribine in human serum. The pharmacokinetic characteristics of mizoribine in children with nephropathy in China are preliminarily clarified. The dosage of mizoribine can be adjusted according to the pharmacokinetic parameters of Tmax , Cmax and AUC, so as to improve the safety and effectiveness of the drug.
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