尼索地平片人体相对生物利用度研究

摘要

OBJECTIVE To study the pharmacokinetics and bioavailability of test and reference of nisoldipine in human subjects.METHODS A single oral administration of 20mg test and reference tablets were given to 20 h ealthy male volunteers according to a randomized dual-period self crossover con trol trial design.The concentrations of nisoldipine in plasma were determined b y a LC/MS (high-pressure liquid chromatographic-mass) method.The pharmacokine tic parameters and bioavailability of test tablets were compared with those of r eference tablets.RESULTS After a single oral administration of20mg test and reference tablets,the pharmacokinetic parameters were as follows:Cmax were 5.84 and 5.64μg·L-1;tmax were 1.4 and 1.5h;t1/2 were 4.74 and 5.04h;AUC0-t were 22.85 and 22.46μg/(h·L) for test and reference tablets,respectively.The relative bioavailability of test t ablets was (101.7±15.8)%.CONCLUSION The two preparations we re bioequivalent.%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t1/2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.