盐酸金刚乙胺颗粒人体生物等效性研究

 目的用高效液相色谱-质谱法(LC-MS)测定受试者口服盐酸金刚乙胺制剂后的血药浓度,估算受试制剂和参比制剂的药动学参数,评价两种制剂的生物等效性和相对生物利用度。方法采用随机二交叉设计试验,20例男性健康志愿受试者,单剂量口服受试制剂盐酸金刚乙胺颗粒和参比制剂盐酸金刚乙胺片。以LC-MS测定血浆中金刚乙胺的浓度。采用BAPP3.0软件处理计算主要药动学参数。结果受试制剂和参比制剂血浆中金刚乙胺的t_1/2分别为(26.46±4.48)和(27.41±4.42)h;ρ_max分别为(84.5±17.7)和(93.1±17.8)μg·L^-1;t_max分别为(4.08±2.86)和(4.70±3.59)h;AUC_0-120h分别为(3204±691)和(3450±724)μg·h·L^-1;AUC_0-∞分别为(3395±767)和(3661±820)μg·h·L^-1;人体相对生物利用度为(93.4±10.8)%。结论2种制剂在健康人体内具有生物等效性。

Bioequivalence Study of Rimantadine Hydrochloride Granules in Chinese Healthy Volunteers

OBJECTIVE To evaluate the relative bioequivalence of two rimantadine hydrochloride preparations in Chinese healthy volunteers by LC-MS.METHODS A single oral dose of two preparations was given to 20 healthy male volunteers according to a randomized crossover design. Plasma drug concentrations were determined by LC-MS. The pharmacokinetic parameters were calculated by BAPP3.0. RESULTS The main pharmacokinetic parameters of rimantadine in test and reference preparations were as follows:t_1/2 (26.46±4.48) and (27.41±4.42) h,ρ_max (84.5±17.7) and (93.1±17.8) μg·L^-1,t_max(4.08±2.86) and (4.70±3.59) h,AUC_{0-120 h}(3 204±691) and (3 450±724) μg·h·L^-1,AUC_0-∞(3 395±767) and (3 661±820) μg·h·L^-1,respectively. The relative bioavailability of test preparation was (93.4±10.8) %. CONCLUSION The two formulations were bioequivalent in human body.