摘要
目的:研究单剂量口服硝苯地平缓释片在人体内的药动学特点和国产硝苯地平缓释片的生物等效性。方法:22名健康男性志愿者采用双周期交叉、自身对照试验设计。以尼群地平为内标,采用高效液相色谱-大气压化学源-质谱联用(HPLC-MS)的方法,测定人血浆中硝苯地平的浓度。结果:单剂量口服20mg受试和参比制剂后血浆中硝苯地平的Cmax分别为(52.9±31.5)μg·L-1和(52.1±35.6)μg·L-1,Tmax分别为(4.1±1.2)h和(4.7±1.9)h,t1/2分别为(6.9±3.5)h和(7.7±4.5)h,AUC0-36h分别为(410.7±188.1)μg·h·L-1和(440.4±271.7)μg·h·L-1,AUC0-∞分别为(437.6±206.8)μg·h·L-1和(477.9±290.4)μg·h·L-1。将22名受试者的经时血药浓度录入DAS(ver1.0)程序,Tmax进行非参数秩和检验,CmaxAUC0-36h、AUC0-∞、t1/2经对数转换后做方差分析,并经双向单侧t检验,两制剂的tmax、Cmax、AUC0-36h、AUC0-∞、t1/2差异均无显著性,两种制剂的相对生物利用度为(104.4±40.1%)(AUC0-36h,T/AUC0-36h,R×100%)。结论:两种制剂具有生物等效性。
OBJECTIVE To investigate the pharmacokinetics properties and bioequiavailability of nifedipine sustained-release tablets after a single dose administration in healthy volunteers. METHODS The study was designed in a two-treatment, twoperiod, two-sequence randomized cross-over trial Nitrendipine was used as the internal standard and the concentrations of nifedipine in plasma were determined by HPLC - APCI-MS method. RESULTS The pharmacokinetics parameters were calculated by DAS（ver 1.0）program and the bioequivalence were compared. The pharmacokinetics parameters were as follows： Cmax- （52.9 ±31.5）μg·L^-1 and（52.1 ± 35.6）μg·L^-1 Tmax-（4.1±1.16）h and（4.7±1.9）h; t1/2-（6.9±3.5）h and（7.7±4.5）h ; AUC0-36 h-（410.7± 188.1）μg·L^-1 and （440.4±271.7）μg·L^-1 , AUC0-∞-（437. 6 ± 206. 8）μg·L^-1 and（477. 9 ± 290. 4）μg·L^-1 for tested and reference preparations, respectively. There were no significant differences（P〉0.05） in AUC0-t, Tmax, Cmax and t1/2 between two preparations. The relative bioavailability of tested tablets was（ 104.4±40.1）%. CONCLUSlON The test and reference preparations are bioequivalent.
出处
《中国医院药学杂志》
CAS
CSCD
北大核心
2006年第8期970-973,共4页
Chinese Journal of Hospital Pharmacy
