Quantifying Isotibolone in Raw Materials of Tibolone
作者机构：Departamento de Físico-QuímicaInstituto de QuímicaUniversidade Estadual PaulistaAraraquaraBrazil Department of PhysicsUniversity of GuelphGuelphCanada Centro de Ciencias Naturais e HumanasUniversidade Federal do ABCSanto AndreBrazil Faculty of Pharmaceutical SciencesDepartment of PharmacyUniversity of Sao PauloSao PauloBrazil
出 版 物：《Pharmacology & Pharmacy》 (药理与制药（英文）)
年 卷 期：2013年第4卷第3期
页 面：283-287页
学科分类：1002[医学-临床医学] 100214[医学-肿瘤学] 10[医学]
基 金：the financial support of FAPESP(proc.nos.2008/10537-3,2010/06849-0) CAPES and CNPq(proc.nos.476335/2008-6,309811/2009-0,306293/2009-9 and 477296/2011-4)and the LNLS(Brazilian Synchrotron Light Laboratory)for beam time
主 题：Hormones Rietveld Method X-Ray Powder Diffractometry Synchrotron Radiation Quantitative Phase Analysis
摘 要：Tibolone, a synthetic steroid, is used in the treatment of natural or surgical menopause disturbs resultant of estrogenic deficiency. Isotibolone (Δ4-tibolone) is one of the three active metabolic degradation products of tibolone that displays progestagenic effects on carcinoma cell growth and gene regulation. Isotibolone can be present in raw material of tibolone due to some inadequate synthesis or storage. Its presence is necessary to be identified and quantified in active pharmaceutical ingredients (API), before its use in the manufacturing of medicines. After a recent study on the crystal structure determination of isotibolone, quantitative phase analyses of both tibolone and isotibolone in raw materials and tablets became possible to be conducted. X-ray powder diffraction is one recommended tool for this purpose, but it can be highly frustrating due to the extreme peak overlap when conventional laboratory equipments are used. In this work we show that the use of Brazilian Synchrotron Light Source X-ray powder diffraction data and the Rietveld method can be successfully applied to identify and quantify the isotibolone in two samples of tibolone raw materials.
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