尼莫地平片的药动学及生物等效性

The pharmacokinetics and bioequivalence study of nimodipine tablets

目的 :研究尼莫地平片的药动学和相对生物利用度 ,验证该制剂与进口尼莫地平片的生物等效性。方法 :采用HPLC法测定 2 4名健康男性志愿者自身交叉单剂量口服国产尼莫地平片和进口尼莫地平片 12 0mg的经时血药浓度 ,计算主要药动学参数以及受试制剂的生物利用度。结果 :国产尼莫地平片和进口尼莫地平片的血药浓度 时间曲线符合一室模型 ,其主要药动学参数 :Cmax分别为 (83.9± 15 .4) μg·L-1与 (83.5± 12 .8) μg·L-1,Tmax分别为 (0 .5 7± 0 .0 6 )h与 (0 .6 7± 0 .0 8)h ,T1/2ke分别为 (1.80± 0 .16 )h与 (1.6 9± 0 .17)h ,AUC0 -t分别为 (16 0 .9± 15 .8) μg·h·L-1与 (15 6 .2± 18.7) μg·h·L-1。国产尼莫地平片对进口尼莫地平片的相对生物利用度为 (10 8.0± 7.2 ) %。结论

OBJECTIVE To study the pharmacokinetics and relative bioavailability of nimodipine tablets, and to evaluate the bioequivalence.METHODS A single dose 120 mg of domestic or imported nimodipine tablets was given to 24 healthy volunteers in a randomized crossover study. The concentrations of nimodipine in serum were determined by HPLC. The pharmacokinetic parameters as well as relative bioavailability were measured.RESULTS The concentration-time curves of nimodipine were confirmed to one-compartment model. The main pharmacokinetic parameters of domestic and imported nimodipine were as follows: C max were ( 83.9± 15.4) μg·L -1 and ( 83.5± 12.8) μg·L -1,T max were ( 0.57± 0.06) h and ( 0.67± 0.08) h,T 1/2kewere ( 1.80± 0.16) h and ( 1.69± 0.17) h,AUC 0-t were ( 160.9± 15.8) μg·h·L -1 and ( 156.2± 18.7) μg·h·L -1, respectively. The relative bioavailability of domestic nimodipine tablet was ( 108.0± 7.2)%.CONCLUSIONS The results of the statistical analysis showed that the two formulations were bioequivalent.