摘要
目的:研究盐酸西布曲明滴丸在健康人体的药动学和相对生物利用度并求证其生物等效性。方法:男性健康志愿者20名,随机交叉单剂量口服受试制剂盐酸西布曲明滴丸和参比制剂盐酸西布曲明胶囊各15mg,采用高效液相色谱-质谱联用法测定血浆中西布曲明的活性代谢产物之一双去甲基西布曲明的浓度。计算药动学参数和相对生物利用度,评价其生物等效性。结果:口服受试和参比制剂后的主要药动学参数经统计矩参数计算:试验制剂t1/2为(20.8±6.0)h和(21.2±6.2)h;tmax为(4.2±1.0)h和(4.8±1.2)h;Cmax为(7.3±2.1)μg.L-1和(7.6±2.0)μg.L-1;AUC0-96h为(159.5±56.4)μg.h.L-1和(168.4±57.3)μg.h.L-1。受试制剂与参比制剂比较的相对生物利用度F为(96.4±18.2)%。结论:两制剂具有生物等效性。
OBJECtiVE To investigate the pharmacokinetics and relative bioavailability of sibutramine dripping pills and capsules in healthy volunteers and evaluate the bioequivalence. METHODS A single oral dose of 15 mg test and reference sibutramine dripping pills or capsules was given to 20 male healthy volunteers in a randomized, two-way crossover study. The concentration of one of active metabolite of sibutrarnine in plasma was determined by LC-MS/MS. The pharmacokinetics parameters and relative bioavailability were calculated with DAS 2. 0 software to evaluate the bioequivalence of the two preparations. RESULTS The main pharmacokinetics parameters of test and reference preparations were as follows： t1/2 （20. 8 ± 6. 0） h and （21.2±6.2）h;tmax（4.2±1.0） h and（4.8±1. 2）h;Cmax（7.3±2.1）μg·L^-1 and（7.6±2.0）μg·L^- 1 AUC0-96h（159.5±56.4） μg·h·L^-1 and（168. 4 ± 57. 3）μg·h· L^-1, respectively. The differences of the major pharmacokinetics parameters between test and reference granules were not significant. The relative bioavailability of F was（96. 4± 18. 2） %. CONCLUSION The statistical analysis of the results shows that the two preparations are bioequivalent.
出处
《中国医院药学杂志》
CAS
CSCD
北大核心
2009年第14期1161-1165,共5页
Chinese Journal of Hospital Pharmacy
