【摘要】 目的　研究西布曲明主要药理活性代谢产物N 去二甲基西布曲明 (BTS 5 4 5 0 5 )在中国志愿者体内的药代动力学。方法　 2 0名健康中国志愿者采用随机交叉自身对照的方式 ,单剂量po盐酸西布曲明胶囊 2 0mg。给药后 ,连续采集血样至 72h。分离得到的血浆 ,采用高效液相色谱 电喷雾 二级质谱分析BTS 5 4 5 0 5的血药浓度。结果　国产和进口胶囊剂的体内药代动力学参数AUC0 t,AUC0 ∞ ,Cmax,Tmax,T1 2 ,Kelm 和MRT均与文献报道相似。结论　国产和进口胶囊剂生物等效更多还原

【Abstract】 Aim To evaluate the pharmacokinetic profiles of the pharmacologically active primary amine metabolite of sibutramine, N-di-desmethyl sibutramine (BTS 54505) in Chinese origin. Methods According to a randomized cross-over design,a single oral dose of 20 mg of sibutramine hydrochloride capsule was given to 20 healthy Chinese young volunteers. After dosing, serial blood samples were collected for a period of 72 h. BTS 54505 concentration in plasma was analyzed by high-performance liquid chromatography-electrospray ionization-tandem mass spectrometry. Results Various pharmacokinetic parameters including AUC 0-t, AUC 0-∞, C max, T max, T 1/2, K elm and MRT were determined for both test and reference capsules and found to be in good agreement with literature values. Conclusion The test and reference sibutramine capsules were bioequivalent.更多还原