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RECRYSTALLIZATION OF TIBOLONE TO PRODUCE MORE STABLE AND HIGHLY BIOLOGICALLY ACTIVE TIBOLONE
RECRYSTALLIZATION OF TIBOLONE TO PRODUCE MORE STABLE AND HIGHLY BIOLOGICALLY ACTIVE TIBOLONE
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机译:替勃龙重结晶以产生更稳定和高度生物活性的替勃龙
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摘要
PURPOSE: A process for recrystallization of tibolone is provided to produce tibolone which has more stability and higher biological activity using isopropanol or mixed solvent of isopropanol and acetone. CONSTITUTION: The process comprises the steps of: dissolving 1 part by weight of tibolone polymorph compound to 10 to 30 parts by weight of isopropanol or mixed solvent of isopropanol and acetone at room temperature, cooling the mixed solvent to -20 to -14 deg.C to precipitate tibolone crystals, then washing the obtained crystals with mixed solvent of isopropanol and acetone, raising the temperature to 30 to 40 deg.C and drying at reduced pressure to up to 0.2 atm. The mixed solvent of isopropanol and acetone comprises 0.01 to 0.2 part by weight of acetone per part by weight of isopropanol. The angle of diffraction of X-ray of recrystallized tibolone is 8.49, 15.11, 17.33, 18.35, 21.85, 24.07, 26.03, 27.64, 29.17, 35.25, 37.49, 39.47, 44.51.
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