吗替麦考酚酯分散片人体药动学和生物等效性研究  

Pharmacokinetics and Bioequivalence of Mycophenolate Mofetil Dispersible Tablets in Healthy Volunteers

作　　者：师少军[1] 李忠芳[2] 万元胜[1] 陈华庭[1] 曾繁典[3] 

机构地区：[1]华中科技大学同济医学院附属协和医院药剂科,武汉430022 [2]华中科技大学同济医学院附属协和医院妇产科,武汉430022 [3]华中科技大学同济医学院临床药理研究所,武汉430030

出　　处：《中国药学杂志》2008年第10期776-779,共4页Chinese Pharmaceutical Journal

摘　　要：目的研究吗替麦考酚酯分散片在健康人体的药动学和相对生物利用度并求证其生物等效性。方法男性健康志愿者20名,随机交叉单剂量口服吗替麦考酚酯受试分散片和参比胶囊各1.0g,采用反相高效液相色谱法测定血浆中其活性代谢物霉酚酸浓度。应用DAS软件计算药动学参数和相对生物利用度,评价其生物等效性。结果口服受试和参比制剂后的主要药动学参数:t1/2分别为(16.26±3.79)和(16.85±3.97)h;tmax分别为(0.67±0.22)和(0.78±0.29)h;ρmax分别为(24.07±7.04)和(25.58±9.02)mg.L-1;AUC0-48分别为(56.84±12.81)和(59.06±15.96)mg.h.L-1;AUC0-∞分别为(62.25±12.63)和(64.58±15.28)mg.h.L-1。受试制剂与参比制剂比较的相对生物利用度F0-48为(97.95±13.73)%。结论两制剂具有生物等效性。OBJECTIVE To study the pharmacokinetics and relative bioavailability of mycophenolate motetil （MMF） dispersible tablets in healthy volunteers and to evaluate the bioequivalence. METHODS A single oral dose of 1. 0 g MMF test dispersible tablets and reference capsules was given to 20 male healthy volunteers in a randomized, two-way crossover study. Myeophenolic acid （MPA） , the active constitute of MMF was determined by RP-HPLC method. The pharmacokinetic parameters and relative bioavailability were calculated with DAS software to evaluate the bioequlvalence of the two preparations. RESULTS The main pharmacokinetic parame- ters of test and reference preparations were as follows ： t1/2were（ 16. 26 ±3.79） and （ 16. 85 ± 3.97） h ; tmax were （0. 67 ± 0. 22） and （0.78±0.29）h;ρmax were（24.07 ±7.04）and （25.58 ±9.02）mg·L^-1; AUC0-48 were （ 56. 84 ± 12.81）and（59.06 ± 15.96）mg·h·L^-1 ; AUC0-∞ were（62. 25± 12. 63）and （64. 58 ±15.28）mg·h·L^-1 , respectively. The differences of the major pharmaco- kinetic parameters between test and reference tablets were not significant. The relative bloavailability of F0-48 was（97.95 ± 13.73）%. CONCLUSION The statistical analysis of the results show that the two preparations are bioequivalent.

关 键 词：吗替麦考酚酯 霉酚酸 高效液相色谱法 药动学 生物等效性 

分 类 号：R944[医药卫生—药剂学]