两种西尼地平制剂在中国健康志愿者体内的生物等效性  

Bioequivalence of Two Cilnidipine Formulations in Healthy Chinese Volunteers

作　　者：李晓光[1] 赵荣生[1] 张现化[1] 佘飞[2] 翟所迪[1] 陈凤荣[2] 李海燕[2] 

机构地区：[1]北京大学第三医院药剂科,北京100191 [2]北京大学第三医院心内科,北京100191

出　　处：《中国药学杂志》2010年第5期381-384,共4页Chinese Pharmaceutical Journal

摘　　要：目的评价国产西尼地平胶囊与国产上市西尼地平片剂在中国健康人体内的生物等效性。方法入选20名男性健康志愿者,随机交叉单剂量口服西尼地平胶囊或西尼地平片剂10mg,液质联用测定血浆中西尼地平浓度。结果西尼地平胶囊及片剂的药动学参数分别如下:ρmax分别为(11.08±4.42)和(2.94±3.44)μg.L-1;tmax分别为(1.30±0.56)和(2.21±1.25)h;t1/2分别为(3.99±1.90)和(4.55±1.75)h,AUC0-t分别为(35.28±14.63)和(13.22±12.44)μg.h.L-1,AUC0-∞分别为(38.05±16.49)和(15.43±13.59)μg.h.L-1。2种制剂的ρmax、tmax、AUC0-t、AUC0-∞均存在显著差异(P<0.01)。结论国产西尼地平胶囊与国产上市西尼地平片剂生物不等效。OBJECTIVE To evaluate the bioequivalence of domestic cilnidipine capsules and commercially available cilnidipine tablets in healthy Chinese volunteers.METHODS Twenty healthy male Chinese volunteers were enrolled and orally administrated 10 mg cilnidipine capsules or tablets randomly and the concentrations of cilnidipine in plasma were determined by HPLC-MS/MS.RESULTS The pharmacokinetic parameters of two cilnidipine productions were as following：ρmax（11.08±4.42）and（2.94±3.44）μg·L^-1,tmax（1.30±0.56）and（2.21±1.25）h,t1/2（3.99±1.90）and（4.55±1.75）h,AUC0-16 h（35.28±14.63）and（13.22±12.44）μg·h·L^-1,AUC0-∞（38.05±16.49）and（15.43±13.59）μg·h·L^-1,respectively.There were significant differences in ρmax,tmax,AUC0-t and AUC0-∞ between the two formulations.CONCLUSION The domestic cilnidipine capsules were not bioequivalent to the marketed cilnidipine tablets in China.

关 键 词：西尼地平 药动学 生物等效性 

分 类 号：R969.1[医药卫生—药理学]