Pharmacokinetics of sibutramine hydrochloride in Chinese healthy volunteers.
OBJECTIVE
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.


CONCLUSIONS
The test and reference sibutramine capsules were bioequivalent.
Chen
Jun
J
Department of Pharmaceutics, School of Pharmacy, Fudan University, Shanghai 200032, China.
Lu
Wei
W
Jiang
Xin-guo
XG
Rong
Zheng-xing
ZX
Huang
Xia
X
Chen
Hong-zhuan
HZ
D000284:Administration, Oral; D000328:Adult; D019540:Area Under Curve; D001682:Biological Availability; D002851:Chromatography, High Pressure Liquid / Q000379:methods; D018592:Cross-Over Studies; D003503:Cyclobutanes / Q000008:administration & dosage / Q000097:blood* / Q000493:pharmacokinetics*; D006801:Humans; D008297:Male; D017367:Selective Serotonin Reuptake Inhibitors / Q000008:administration & dosage / Q000493:pharmacokinetics*; D021241:Spectrometry, Mass, Electrospray Ionization
D003503:Cyclobutanes; D017367:Selective Serotonin Reuptake Inhibitors; C087851:BTS 54 505; C058254:sibutramine