盐酸西布曲明在中国志愿者体内的药代动力学

Pharmacokinetics of sibutramine hydrochloride in Chinese healthy volunteersPharmacokinetics of sibutramine hydrochloride in Chinese healthy volunteers

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 54505）在中国志愿者体内的药代动力学。方法20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20 mg。给药后，连续采集血样至72 h。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 54505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AUC_0-t，AUC_0-∞，C_max，T_max,T_1/2,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。

Abstract: AimTo evaluate the pharmacokinetic profiles of the pharmacologically active primary amine metabolite of sibutramine, N-di-desmethyl sibutramine (BTS 54505) in Chinese origin. MethodsAccording 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. ResultsVarious pharmacokinetic parameters including AUC_0-t, AUC_0-∞,　C_max, T_max, T_1/2, K_elmand MRT were determined for both test and reference capsules and found to be in good agreement with literature values. ConclusionThe test and reference sibutramine capsules were bioequivalent.