中国临床药理学杂志2011，Vol.27Issue(9)：696-700,5.
比较他克莫司缓释制剂与普通制剂在中国肾移植患者的药代动力学
Comparison the pharmacokinetics of tacrolimus in Chinese kidney transplant patients after repeated-dose of modified release and immediate release preparations
张逸凡 1陈笑艳 1戴晓健 1敖建华 2钟大放1
作者信息
- 1. 中国科学院,上海药物研究所,上海,201203
- 2. 中国人民解放军总医院,北京,100853
- 折叠
摘要
Abstract
Objective To compare the pharmacokinetics of tacrolimus in kidney transplant patients treated with modified release and immediate release preparations . Methods It was a multi - centre, open label, 1:1 randomized, parallel, repeated - dose study. Adult kidney transplant recipients aged from 18-70 years were randomized into modified release group once daily (qd) and immediate release group twice a day (bid). A validated LC/MS/MS method was used to determine blood concentrations of tacrolimus. Results The mean daily dose for modified release (re = 17) was (0. 12 ±0. 05) mg ? Kg-1on day 56, and that for immediate release (re = 15) was (0. 10 ±0. 04) mg ? Kg-1. The parameters of tacrolimus for the two formulations at steady state were as follows; Cmax was (13. 20 ±4. 20) ng ? mL"'at (3. 10 ±3.00)h for modified release and (11.80±3.80) ng ? mL"'at (1.80 ±0.90) h for immediate release, Cmwas (4.40 ± 1.30) and (4.50 ± 1.20) ng ? mL-1, and AUCo.^was (171.70 ±49.90) and(145.10 ±29. 30) ng ? mL-1 ? H, respectively. The coefficient between AUC0 _M and CM was 0. 87 for modified release, and was 0. 62 for immediate release, respectively. Conclusion In patients undergoing primary kidney transplantation, daily doseof modified release tacrolimus increases 23% compared with that of immediate release on day 56 after operation, and the systemic exposure to tacrolimus over the 24 - hour interval is 16% higher. There is a good correlation between C24 and AUC0_24 for the modified release tacrolimus.关键词
他克莫司缓释制剂/药代动力学/肾移植Key words
modified release tacrolimus/ pharmacokinetics/ kidney transplantation分类
医药卫生引用本文复制引用
张逸凡,陈笑艳,戴晓健,敖建华,钟大放..比较他克莫司缓释制剂与普通制剂在中国肾移植患者的药代动力学[J].中国临床药理学杂志,2011,27(9):696-700,5.
