A Review of Analytical Methods for the Determination of Tibolone: Pharmacokinetics and Pharmaceutical Formulations Analysis and Application in Doping Control

Background: Tibolone is a synthetic steroid commercialized by Organon under the brand name Livial (Org OD14), which is used in hormone therapy for menopause management and treatment of postmenopausal osteoporosis. Tibolone is defined as a selective tissue estrogenic activity regulator (STEAR) demonstrating tissue-specific effects on several organs such as brain, breast, urogenital tract, endometrium, bone and cardiovascular system. Aims: This work aims to (1) present an overview of important published literature on existing methods for the analysis of tibolone and/or its metabolites in pharmaceutical formulations and biological fluids and (2) to conduct a critical comparison of the analytical methods used in doping control, pharmacokinetics and pharmaceutical formulations analysis of tibolone and its metabolites. Results and Conclusion: The major analytical method described for the analysis of tibolone in pharmaceutical formulations is High Pressure Liquid Chromatography (HPLC) coupled with ultraviolet (UV) detection, while Liquid Chromatography (LC) or Gas Chromatography (GC) used in combination with Mass Spectrometry (MS) or tandem mass spectrometry (MS/MS) is employed for the analysis of tibolone and/or its metabolites in biological fluids.