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.