尼索地平片人体相对生物利用度研究  

Relative Bioavailabflity of Nisoldipine Tablets in Human Subjects

作　　者：宋兴发[1] 曹晓梅[2] 李金恒[2] 孙增先[1] 

机构地区：[1]江苏连云港市第一人民医院药学部,连云港222002 [2]南京军区南京总医院药理科,南京210002

出　　处：《海峡药学》2017年第2期273-275,共3页Strait Pharmaceutical Journal

摘　　要：目的比较两种国产尼索地平片的人体相对生物利用度。方法用随机双周期自身交叉对照试验方案,20名健康男性受试者口服单剂量试验与参比制剂20mg,用液相色谱-质谱法测定血浆中尼索地平的浓度,计算两药的药代动力学参数。结果单剂量口服试验与参比制剂后尼索地平的达峰浓度Cmax分别为5.84和5.64μg·L^(-1);达峰时间tmax分别为1.4h和1.5h;半衰期t_(1/2)分别为4.74h和5.04h;曲线下面积AUC0-t分别为22.85和22.46μg/(h·L);试验制剂的相对生物利用度为(101.7±15.8)%。结论试验与参比制剂具有生物等效性。OBJECTIVE To study the pharmacokinetics and bioavailability of test and reference of nisoldipine in human subjects.METHODS A single oral administration of 20 mg test and reference tablets were given to 20 healthy male volunteers according to a randomized dual-period self crossover control trial design.The concentrations of nisoldipine in plasma were determined by a LC/MS（high-pressure liquid chromatographic-mass） method.The pharmacokinetic parameters and bioavailability of test tablets were compared with those of reference tablets.RESULTS After a single oral administration of 20 mg test and reference tablets,the pharmacokinetic parameters were as follows：Cmaxwere 5.84 and 5.64μg·L（-1）;tmaxwere 1.4 and 1.5h;t_（1/2） were 4.74 and 5.04h;AUC_（0-t） were 22.85 and 22.46μg/（h·L） for test and reference tablets,respectively.The relative bioavailability of test tablets was（101.7 ± 15.8） %.CONCLUSION The two preparations were bioequivalent.

关 键 词：尼索地平 相对生物利用度 药代动力学 生物等效性 液相色谱-质谱 

分 类 号：R96[医药卫生—药理学]