Pharmacokinetics of sibutramine hydrochloride in Chinese healthy volunteers.

Author(s): Chen J, Lu W, Jiang XG, Rong ZX, Huang X, Chen HZ

Affiliation(s): Department of Pharmaceutics, School of Pharmacy, Fudan University, Shanghai 200032, China.

Publication date & source: 2003-11, Yao Xue Xue Bao., 38(11):850-3.

Publication type: Clinical Trial; Randomized Controlled Trial

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 AUC0-t, AUC0-infinity, Cmax, Tmax, T1/2, Kelm 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.