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SOLID FORMS CONTAINING (-) - O-DESMETHYLVENLAFXIN, AND THEIR APPLICATIONS

机译:包含(-)-O-去甲甲基文拉芬辛的固体形态及其应用

摘要

1. The crystalline form of the hydrochloride salt of a stereomerically pure compound of formula (I):! ! 2. The crystalline form of the stereomerically pure hydrochloride salt of (-) - O-desmethylvenlafaxine. ! 3. The crystalline form of the stereomerically pure hydrochloride salt of (-) - 1- [2- (dimethylamino) -1- (4-hydroxyphenyl) ethyl] cyclohexanol. ! 4. The crystalline form according to claim 1, 2 or 3, which contains water. ! 5. The crystalline form according to claim 4, which is a form A.! 6. The crystalline form according to claim 5, in which the molar ratio of water to hydrochloride salt of (-) - O-desmethylvenlafaxine is approximately one to one. ! 7. The crystalline form according to claim 5, in which water is present in an amount of from about 4 to about 8% of the total weight of the sample. ! 8. The crystalline form according to claim 4, which is characterized by mass loss during thermal gravimetric analysis from about 4 to about 8% of the total mass of the sample when heated from about 25 to about 110 ° C. ! 9. The crystalline form according to claim 4, which is characterized by an endothermic effect in differential scanning calorimetry with a temperature of the onset of the effect from about 50 to about 125 ° C. ! 10. The crystalline form according to claim 4, which has a dehydration temperature of from about 50 to about 125 ° C. ! 11. The crystalline form according to claim 4, which has a peak powder x-ray at a position of approximately 21.35 ° 2θ. ! 12. The crystalline form according to claim 11, which has peaks of an X-ray powder diffraction pattern at positions of about 14.48, 19.05, and 22.96 ° 2θ. ! 13. The crystalline form according to claim 5, which is obtained by crystallization of the hydrochloride salt of the compounds of formula (I) from water or a mixture of solvents containing water. ! 14. The crystalline form according to claim 4, which
机译:1.式(I)的立体异构纯的化合物的盐酸盐的晶体形式: ! 2。(-)-O-去甲基文拉法辛的立体异构纯的盐酸盐的晶体形式。 ! 3。(-)-1-[[2-(二甲基氨基)-1-(4-羟基苯基)乙基]环己醇的立体异构纯的盐酸盐的晶体形式。 ! 4.根据权利要求1、2或3的结晶形式,其含有水。 ! 5.根据权利要求4的结晶形式,其为A形式。 6.根据权利要求5的结晶形式,其中水与(-)-O-去甲基文拉法辛的盐酸盐的摩尔比为约1比1。 ! 7.根据权利要求5的晶型,其中水以样品总重量的约4-约8%的量存在。 ! 8.根据权利要求4所述的晶型,其特征在于,当从约25℃至约110℃加热时,在热重量分析期间的质量损失为样品总质量的约4%至约8%。 9.根据权利要求4的晶型,其特征在于在差示扫描量热法中的吸热效应,该效应的起始温度为约50至约125℃。 10.根据权利要求4所述的晶型,其具有约50至约125℃的脱水温度。 11.根据权利要求4的晶体形式,其在大约21.35°2θ的位置具有峰粉末X射线。 ! 12.根据权利要求11所述的晶形,其在大约14.48、19.05和22.96°2θ的位置处具有X射线粉末衍射图的峰。 ! 13.根据权利要求5的晶型,其是通过从水或含有水的溶剂混合物中使式(I)的化合物的盐酸盐结晶而获得的。 ! 14.根据权利要求4的结晶形式,其中

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