硝苯地平缓释片与普通片在健康人体内药动学的比较

Compare of pharmacokinetics of nifedipine sustained release tablets and nifedipine tablets in healthy volunteers

目的比较硝苯地平缓释片与硝苯地平普通片在健康人体内药动学。方法 12名男性健康志愿者平均分为2组,分别单剂量口服硝苯地平缓释片与硝苯地平普通片20 mg,用高效液相色谱法检测硝苯地平的血药浓度,并用DAS 2.1软件进行数据处理。结果硝苯地平缓释片与硝苯地平普通片主要药动学参数ρmax分别为(1 247.8±78.4)μg.L-1和(1 896.7±109.2)μg.L-1,tmax分别为(4.6±0.7)h和(2.6±0.9)h,t1/2分别为(8.6±2.8)h和(4.8±1.5)h,AUC0-∞分别为(5 879.3±176.2)μg.h.L-1和(3 724.9±121.3)μg.h.L-1,AUC0-t分别为(4 427.8±131.7)μg.h.L-1和(2 936.5±75.4)μg.h.L-1。结论硝苯地平缓释片的tmax、t1/2长于普通片,AUC0-t、AUC0-∞高于普通片,而ρmax低于普通片,说明硝苯地平缓释片具有良好的缓释效果。

AIM To compare the pharmacokinetics of nifedipine sustained release tablets and nifedipine tablets in healthy volunteers. METHODS Twelve healthy male volunteers were divided into two groups, and received a single oral dose of nifedipine sustained release tablets and nifedipine tablets 20 mg, respectively. The plasma concentrations of nifedipine were determined by HPLC, and the pharmacokinetic parameters were calculated by DAS 2.1 software. RESULTS The pharmacokinetic parameters of nifedipine sustained release tablets and nifedipine tablets were as follows： pax were （1 247.8± 78.4） μg·L-1 and （1 896.7 ± 109.2）μg·L-1, tax were （4.6 ± 0.7） b and （2.6 ± 0.9） h, tl/2 were （8.6 ± 2.8） b and （4.8 ± 1.5） h, AUC0-∞ were （5 879.3 ± 176.2）μg·h·L-1 and （3 724.9 ± 121.3）μg·h·L-1, AUC0-t, were （4 427.8 ± 131.7） μg·h·L-1 and （2 936.5 ± 75.4） μg·h·L-1 respectively. The tax and t1/2 of nifedipine sustained release tablets were significantly longer than that of nifedipine tablets, AUC0-t and AUC0-∞ were significantly higher than that of the nifedipine tablets, and pax was significantly lower than that of nifedipine tablets. CONCLUSION The nifedipine sustained release tablets have the sustained-release characteristics.