Purpose: The purpose of this study was to characterize the food effect on the pharmacokinetics of sibutramine and its pharmacologically active metabolites.
Methods: This was an open label, single dose, crossover study completed by six healthy males. A single dose of sibutramine 15 mg was administered orally under fasting and fed conditions. Plasma concentrations of sibutramine and its metabolites were determined by LC/MS/MS: Non-compartmental pharmacokinetics and statistical analysis were performed using SAS.
Results: The food intake increased significantly AUCs and C(max) of sibutramine and its M1 metabolite, but did not affect M2 metabolite. When sibutramine was administered with food, the T(max) was delayed by 2 to 4 hours for sibutramine, M1 and M2 metabolites as stated in the literature.
Conclusions: The results of this study indicate that sibutramine is measurable using a sensitive bioanalytical method. In contrast with what is reported in the product monograph, this study demonstrated that the bioavailability of sibutramine and M1 metabolite was significantly increased with administration with food. The results confirmed lack of food effect on the pharmacokinetics of M2 metabolite. These relatively large food effect observed for sibutramine and M1 metabolite, could have implication for the efficacy and safety of the drug.
Download full-text PDF |
Source |
|---|
Publication Analysis
Top Keywords
Similar Publications
Cardiogenic shock in a 28-year-old woman associated with sibutramine use.
Int J Legal Med
May 2024
Department of Forensic Medicine, Tongji Medical College, Huazhong University of Science and Technology, No. 13 Hangkong Road, Wuhan, 430030, People's Republic of China.
A 28-year-old woman collapsed in her home, and her companion rushed to call emergency services. Upon arrival, a physician performed CPR and endotracheal intubation, successfully restoring her voluntary heart rhythm. However, while en route to the hospital, ventricular fibrillation recurred.
View Article and Find Full Text PDFNotifications and Health Consequences of Unauthorized Pharmaceuticals in Food Supplements.
Pharmacy (Basel)
September 2023
Department of Pharmacy, Faculty of Medicine, University of Novi Sad, Hajduk Veljkova 3, 21000 Novi Sad, Serbia.
Health concerns associated with the consumption of food supplements rise in parallel with the rise in the popularity and market availability of these products. In pursuit of data related to the unauthorized presence of pharmaceuticals in food supplements, the Rapid Alert System for Food and Feed (RASFF) database was searched for the 2011-2022 period. The most "popular" pharmaceuticals for the adulteration of food supplements were phosphodiesterase-5 inhibitors (235 records); anorexics and laxatives (76), including sibutramine and its active metabolite N-didesmethyl sibutramine, phenolphthalein and 2,4-dinitrophenol; stimulants, among which 1,3-dimethylamine (97), and synephrine (53) were the most numerous; nootropic drugs (24); anabolics and prohormones (16); and cannabinoid cannabidiol (14) (pending authorization as a novel food ingredient).
View Article and Find Full Text PDFHighly resistant and sensitive colorimetric immunochromatographic assay for sibutramine (SBT) illegally adulterated into diet food based on PDA/AuNP labelling.
Analyst
October 2023
Jiangsu Key Laboratory for Food Quality and Safety-State Key Laboratory Cultivation Base of Ministry of Science and Technology, Institute of Food Safety and Nutrition, Jiangsu Academy of Agricultural Sciences, Nanjing 210014, PR China.
A gold nanoparticle (AuNP) based immunochromatographic assay strip is a valuable tool for monitoring chemicals in foods. However, the sensitive ICA strip for SBT is rarely reported due to the fact that monoclonal antibodies (mAbs) against SBT with high affinity are commercially unavailable. Herein, a monoclonal antibody against SBT was prepared through a designed hapten with a carboxyl end-capped space arm.
View Article and Find Full Text PDFMetabolic analysis of the illegal analogues of anti-obesity drugs using LC-Q-TOF-MS/MS.
J Chromatogr B Analyt Technol Biomed Life Sci
January 2021
College of Pharmacy, Kyungsung University, Busan 48434, Republic of Korea. Electronic address:
With an increase in the obese population, the indiscriminate demand for anti-obesity drugs for rapid weight loss or maintenance has grown. As a result, illegal substances that could induce unexpected negative health effects or fatal side effects are being produced and mixed into consumer products. In the present study, the metabolites of five major illegal anti-obesity drugs are analyzed for the first time.
View Article and Find Full Text PDFDevelopment of a liquid chromatography Q Exactive high resolution mass spectrometry method by the Box-Behnken design for the investigation of sibutramine urinary metabolites.
J Chromatogr B Analyt Technol Biomed Life Sci
September 2019
Federal University of Rio de Janeiro, Institute of Chemistry, LBCD - LADETEC, Rio de Janeiro, Brazil.
Sibutramine is cited by the World Anti-Doping Agency as a stimulant. According to the literature, sibutramine is extensively metabolized into N-desmethyl-sibutramine (M1), N-bisdesmethyl-sibutramine (M2) and monohydroxy derivatives of M1 and M2. Therefore, it is important to verify new sibutramine metabolites through current analytical methodologies, such as liquid chromatography coupled to high resolution mass spectrometry (LC-HRMS).
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!