【摘要】 目的:建立测定血浆中苯磺酸左氨氯地平质量浓度的高效液相色谱-串联质谱(HPLC-MS/MS)法,研究苯磺酸左氨氯地平片的相对生物利用度及其生物等效性。方法:按照两制剂、双周期、自身对照、交叉试验设计,20例健康男性志愿者单剂量口服试验试剂或参比试剂,采用LC-MS/MS法测定血浆中苯磺酸左氨氯地平的药物质量浓度,使用WinNonlin 6.1软件的NCA模块计算药动学参数,并评价2种制剂的生物等效性。结果:受试试剂及参比试剂的主要药代动力学参数如下:峰浓度(Cmax)分别为(3.37!0.9)、(3.50!1.39)μg.L-1;峰时间(Tmax)分别为(4.7±2.1)、(5.7±2.8)h;AUClast(AUC0-t)分别为(146.3±53.5)、(144.1±43.3)μg.h-1.L-1;AUCinf(AUC0-∞)分别为(167.9±64.8)、(165.1±52.3)μg.h-1.L-1;AUClast/AUCinf分别为(87.8±6.1)%、(87.8±6.1)%;MRTlast(MRT0-t)分别为(40.4±4.4)、(40.0±3.6)h;MRTinf(MRT0-∞)分别为(57.5±13.6)、(57.1±12.5)h;血浆半衰期(t1/2)分别为(38.6±9.4)、(38.8±9.4)h。受试试剂的相对生物利用度:Flast为(101.3±15.7)%,Finf为(101.2±15.9)%。结论:受试试剂和参比试剂具有生物等效性。更多还原

【Abstract】 OBJECTIVE:To establish HPLC-MS/MS method for determination of levamlodipine besylate tablets in human plasma and study the relative bioavailability and bioequivalence of levamlodipine besylate tablets.METHODS:By a two-preparation double-cycle own control crossover design,a single dose of test or reference preparation of levamlodipine besylate tablets was given to 20 healthy volunteers respectively.The mass concentration of levamlodipine was determined by HPLC-MS/MS.The pharmacokinetic parameters were calculated using NCA module of WinNonlin 6.1 software.The bioequivalence of the test vs.reference preparation of levamlodipine besylate tablets was evaluated as well.RESULTS:The main pharmacokinetic parameters of test vs.reference levamlodipine besylate tablets were stated as follows: Cmax:(3.37±0.9) vs.(3.50±1.39) μg·L-1;Tmax:(4.7±2.1) vs.(5.7±2.8) hrs;AUClast(AUC0-t):(146.3±53.5) vs.(144.1±43.3) μg·h-1·L-1AUCinf(AUC0-∞):(167.9±64.8) vs.(165.1±52.3)μg·h-1·L-1;AUClast/AUCinf:(87.8%±6.1%) vs.(87.8%±6.1%);MRTlast(MRT0-t):(40.4±4.4) vs.(40.0±3.6)hMRTinf(MRT0-∞):(57.5±13.6) and(57.1±12.5) hrs;t1/2:(38.6±9.4) vs.(38.8±9.4) hrs.The relative bioavailability of test preparation was as follows:Flast stood at(101.3%±15.7%) and Finf stood at(101.2%±15.9%).CONCLUSION:The tested preparation of levamlodipine besylate tablets was bioequivalent to the reference preparation.更多还原