16-11-2017 дата публикации
Номер: US20170327467A1
The present invention relates to a new type of eutectic crystal of lorcaserin hydrochloride and benzoic acid. Compared with the prior art, the eutectic crystal has the improved properties of good stability, low solubility, and being suitable for the application of controlled-release preparation. The present invention also relates to a method for preparing the eutectic crystal, a pharmaceutical composition thereof and the use thereof in the manufacture of drugs for treating and/or preventing diseases associated with 5HT. 2. The cocrystal of lorcaserin hydrochloride and benzoic acid according to claim 1 , wherein measured using Cu—Kα radiation claim 1 , the X-ray powder diffraction pattern of the cocrystal claim 1 , expressed as 2θ angles claim 1 , has the following characteristic peaks: 4.5±0.2° claim 1 , 9.0±0.2° claim 1 , 12.3±0.2° claim 1 , 18.0±0.2° claim 1 , 19.4±0.2° and 23.0±0.2°.3. The cocrystal of lorcaserin hydrochloride and benzoic acid according to claim 2 , wherein the X-ray powder diffraction pattern of the cocrystal claim 2 , expressed as 2θ angles claim 2 , has the following characteristic peaks: 4.5±0.2° claim 2 , 9.0±0.2° claim 2 , 11.7±0.2° claim 2 , 12.3±0.2° claim 2 , 13.5±0.2° claim 2 , 16.9±0.2° claim 2 , 18.0±0.2° claim 2 , 19.4±0.2° claim 2 , 20.4±0.2° claim 2 , 22.6±0.2° claim 2 , 23.0±0.2° and 23.5±0.2°.5. The cocrystal of lorcaserin hydrochloride and benzoic acid according to claim 1 , wherein measured at 100K in temperature claim 1 , has the following single-crystal unit cell parameters: axial length: a=6.1734(6) Å claim 1 , b=7.6376(5) Å claim 1 , c=39.233(4) Å; dihedral angle: α=90° claim 1 , β=90° claim 1 , γ=90°; space group: P 1 1 2.6. The cocrystal of lorcaserin hydrochloride and benzoic acid according to claim 2 , wherein the Fourier transform infrared spectrum of the cocrystal has characteristic peaks at wave numbers of 3384 claim 2 , 2971 claim 2 , 2861 claim 2 , 2524 claim 2 , 2362 claim 2 , 1700 claim 2 , 1595 claim 2 , 1315 ...
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