【摘要】 目的:研究尼莫地平乳剂型注射剂、注射剂在动物体内的药动学特征及生物等效性。方法:采用双周期二制剂交叉试验设计,高效液相色谱法测定犬的血药浓度,DAS软件计算药动学参数。结果:静脉注射尼莫地平乳剂型注射剂和尼莫地平注射液的AUC0-5h分别为(355.8±114.6),(338.9±83.0)h.μg.L-1;AUC0-∞分别为(356.8±114.5),(339.9±82.9)h.μg.L-1;t1/2α分别为(0.32±0.19),(0.27±0.17)h;t1/2β为(1.6±0.5),(1.46±0.27)h。方差分析结果表明,二制剂的主要药动学参数之间差异无显著性。试验制剂相对生物利用度为(103.7±11.2)%。结论:二种制剂生物等效,但乳剂型注射剂安全性高于注射剂。更多还原

【Abstract】 OBJECTIVE To investigate the pharmacokinetics properties and bioequiavailence of two dosage forms of nimodipine（NM） in dogs.METHODS Single dose of NM was given to beagles in an open randomized cross-over design to study the pharmacokinetic parameters of NM.NM concentrations in plasma were determined by HPLC.RESULTS The pharmacokinetic parameters of NM emulsion for injection and injection were as follows: AUC_{0-5 h}（（355.8）±（114.6））,（（338.9）±（83.0）） h·μg·L^-1,AUC_0-∞（（356.8）±（114.5））,（（339.9）±（82.9）） h·μg·L^-1,t_1/2α（（0.32）±（0.19））,（（0.27）±（0.17）） h,t_1/2β（（1.57）±（0.48））,（（1.46）±（0.27）） h,respectively.The statistical analysis results showed that there was no significant difference between the two formulations.The relative bioavailability of the test formulation was（（103.7）±（11.2））%.CONCLUSION The two formulations were bioequivalent and the emulsion for injection was superior to the injection in safety.更多还原