HPLC-MS/MS法测定人血浆中瑞舒伐他汀钙的浓度及生物等效性研究  

HPLC-MS/MS study on determination of rosuvastatin calcium in human plasma and its bioequivalence

作　　者：严方[1] 狄斌[1] 张宏文[2] 孙桂斌 杭太俊[1] 

机构地区：[1]中国药科大学药学院,南京210009 [2]南京医科大学第一附属医院临床药物研究室,南京210029 [3]南京正大天晴制药有限公司,南京210018

出　　处：《药物分析杂志》2010年第11期2012-2016,共5页Chinese Journal of Pharmaceutical Analysis

摘　　要：目的:建立人血浆中瑞舒伐他汀钙的高效液相色谱-质谱(LC-MS/MS)测定方法,并评价瑞舒伐他汀钙片剂的药动学和人体生物等效性。方法:20名男性健康志愿者随机交叉口服瑞舒伐他汀钙片受试制剂和参比制剂各10mg,采用HPLC-MS/MS测定血药浓度,以BAPP2.0软件计算其药动学参数,考察其生物等效性。结果:受试制剂与参比制剂瑞舒伐他汀钙t1/2分别为(7.6±1.0)h和(7.8±1.1)h,tmax分别为(4.0±2.1)h和(4.2±1.6)h,Cmax分别为(15.7±7.8)ng·mL-1和(16.7±9.4)ng·mL-1,用梯形法计算所得的AUC0-72分别为(145±83)ng·mL-1·h-1和(142±67)ng·mL-1·h-1,AUC0-分别为(147±84)ng·mL-1·h-1和(144±70)ng·mL-1·h-1,以AUC0-72计受试制剂相对参比制剂生物利用度为(102±40)%。结论:该方法重复性好,灵敏度高,瑞舒伐他汀钙片受试制剂和参比制剂具有生物等效性。Objective：To establish an HPLC-MS/MS method for the determination of rosuvastatin calcium in human plasma,and to study the pharmacokinetics and bioequivalence of rosuvastatin calcium tablets in human volunteers.Methods：A single oral dose of 10 mg test or reference tablets was given to 20 male healthy volunteers in a randomized cross-over design.The concentration of rosuvastatin calcium in plasma was determined by HPLC-MS/MS.Pharmacokinetic parameters were calculated by BAPP 2.0 software.Results：The main pharmacokinetic parameters of test and reference rosuvastatin calcium were as followings：t1/2（7.6±1.0）h and（7.8±1.1）h,tmax（4.0±2.1）h and（4.2±1.6）h,Cmax（15.7±7.8）ng·mL^-1 and（16.7±9.4）ng·mL^-1,AUC0-72（145±83）ng·mL^-1·h^-1 and（142±67）ng·mL^-1·h^-1,AUC0-∞（147±84）ng·mL^-1·h^-1 and（144±70）ng·mL^-1·h^-1.The relative bioavailability of test to reference preparation was（102±40）% according to AUC0-72.Conclusion：The method is repeatable and sensitive.The test and reference formulations were bioequivalent.

关 键 词：瑞舒伐他汀钙 血药浓度 生物等效性 高效液相色谱-串联质谱 

分 类 号：R917[医药卫生—药物分析学]