西布曲明胶囊在中国人体内的生物等效性  

Bioequivalence of sibutramine capsule in Chinese healthy volunteers

作　　者：李中东[1] 施孝金[1] 胡敏[1] 钟明康[1] 黄文辉 刘罡一[3] 余琛[3] 

机构地区：[1]复旦大学附属华山医院临床药学研究室,上海200040 [2]上海雅虎制药有限公司,上海200040 [3]上海市徐汇区中心医院中心实验室,上海200031

出　　处：《中国临床药学杂志》2004年第2期87-89,共3页Chinese Journal of Clinical Pharmacy

摘　　要：目的 :研究西布曲明 (SBT)胶囊在中国人体内的生物利用度。方法 :采用随机交叉试验设计 ,2 0名健康志愿者单剂量口服受试制剂SBT胶囊与参比制剂SBT片各 2 0mg后 ,在规定时间取血 ,用HPLC MS/MS法测定血药浓度 ,梯形法计算AUC。结果 :受试制剂和参比制剂的药动学参数分别为 :AUC0→∞(2 4 4 0 3± 113 10 ) ,(2 33 77± 91 74 ) μg·h·L-1;AUC0→ 72 (2 2 3 4 6±10 5 12 ) ,(2 2 0 5 6± 87 98) μg·h·L-1;tmax(3 0 8± 1 5 7) ,(3 0 0± 1 19)h ;cmax(14 80± 6 6 4 ) ,(14 98± 5 32 ) μg·L-1;MRT/F(18 14± 1 39) ,(18 4 9± 1 6 8)h ;T1/2 (2 0 4 9± 3 14 ) ,(2 0 2 3± 3 4 3)h ;药动学参数差异无显著意义。相对生物利用度 (F) =(10 0 11± 12 0 6 ) %。结论 :西布曲明AIM: To study the bioequivalence of sibutramine capsules after oral single dose of 20 mg in 20 healthy Chinese volunteers. METHODS: The active metabolites of sibutramine,N-di-desmethylsibutramine concentrations in serum were determined by HPLC-MS/MS following an oral dose of 20 mg. The pharmacokinetic parameters were calculated using 3P87 software. RESULTS: The average of pharmacokinetic parameters after oral single dose of the test drug or reference one were as follows, respectively: AUC 0→∞:(244.03±113.10),(233.77±91.74) μg·h·L -1;AUC 0→72:(223.46±105.12),(220.56±87.98) μg·h·L -1;t max:(3.08±1.57),(3.00±1.19) h;c max:(14.80±6.64),(14.98±5.32) μg·L -1;MRT/F:(18.14±1.39),(18.49±1.68) h;T 1/2:(20.49±3.14),(20.23±3.43) h; There was no significant difference of pharmacokinetic parameters between 2 preparations. The relative bioavailability of was (100.11±12.06)%. CONCLUSION: The 2 preparations are bioequivalent.

关 键 词：西布曲明胶囊 中国 人体 生物等效性 生物利用度 减肥药 

分 类 号：R96[医药卫生—药理学]