26-10-2017 дата публикации
Номер: US20170305958A1
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The present invention relates to four crystalline forms (crystalline forms A, B, C and D) of 5α-androstane-3β,5,6β-triol (YC-6) and preparation methods therefor. The four crystalline forms have significant difference in their lattice parameters, 2θ values and intensity in X-ray power diffraction, and melting points, etc. The study on its polymorphism is very important for further studying its effect, bioavailability and stability. 19-. (canceled)105. A crystalline form of o-androstane-3β ,5 ,6β-triol ,{'b': 2', '2', '2, 'sub': 1', '1', '1, 'wherein the crystalline form is a transparent column-shaped crystal, and belongs to orthorhombic crystal system and space group P, and'}wherein the crystalline form is characterized by lattice parameters of a=6.3±0.2 Å, b=12,6±0,2 Å, c=26.7±0.2 Å, α=90.0°, β=90°, γ=90.0°; and characterized by diffraction peaks at diffraction angle 2θ values of 4,0±0.2, 8.1±0.2, 8.5+0.2, 9,4±0.2, 12.5±0.2, 14.0±0,2, 14.9±0.2, 15.5±0.2, 16.4±0.2, 17.1 ±0.2, 18.3±0.2, 19.5±0.2, 20.5±0.2, 20.9±0.2, 21.5±0.2 degrees; and characterized by an endothermic transition temperature of 226±2° C.11. A method for preparing the crystalline form of claim 10 , comprising:dissolving 5α-androstane-3β,5,6β-triol in tetrahydrofuran at room temperature, with a ratio of the 5α-androstane-3β,5,6β-triol to the tetrahydrofuran being 1 g : 10˜30 mL;adding tetrahydrofuran in a ratio of 0˜5:1 to dilute; andallowing to form a crystalline precipitate. The present invention relates to crystalline forms of 5α-androstane-3β,5,6β-triol (also known as 5α-androst-3β,5,6β-triol). The present invention also relates to preparation methods for the crystalline forms of 5α-androstane-3β,5,6β-triol.Polymorphism is common in solid drugs, and drug compounds in different crystalline forms have different physical and chemical properties. Polymorphism is one of important factors that have influence on the effect and quality of solid drugs. Different crystalline forms may differ by several times ...
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