A kind of prodrug crystal form suitable for medicine, preparation method and pharmaceutical composition
A precursor compound and crystal form technology, applied in the field of medicinal chemistry, can solve the problems of controllable quality and safety of unfavorable drugs, low hygroscopicity and stability of propofol precursor series compounds, etc.
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Embodiment 1
[0053] In the Chinese patent document whose publication number is CN101845057, 13.0 g of a sample with a water content of 6% is added to 104 ml of water / isopropanol (V / V=20:1) and stirred at room temperature to fully dissolve, and after fully dissolved, an appropriate amount of activated carbon is added for decolorization for 15 minutes ,filter. The filtrate was placed in a material tray and pre-frozen in a freeze dryer at -5°C for 2 hours; then cooled to -25°C and kept for 4 hours; cooled to -55°C within 1 hour and kept for 4 hours. Maintain a vacuum of 15 Pa, raise the temperature to -15°C, and dry for 22 hours; then raise the temperature to -5°C, and dry for 10 hours; finally raise the temperature to 25°C, and dry for 4 hours to obtain 12.29 g of white crystals, which contain The amount of water is 5.5% by weight.
[0054] Sample 1 was decomposed by combustion, converted quantitatively, and detected by ElementaVarioELIII elemental analyzer to obtain the percentage content ...
Embodiment 2
[0058] In the Chinese patent document whose publication number is CN101845057, 13.0 g of a sample with a water content of 10% is added to 104 ml of water / ethanol (V / V=10:1) and stirred at room temperature to dissolve completely, after fully dissolve, add an appropriate amount of active carbon for decolorization for 15 minutes, filter . The filtrate was placed in a material tray and pre-frozen in a freeze dryer at -5°C for 2 hours; then cooled to -25°C and kept for 4 hours; cooled to -55°C within 1 hour and kept for 4 hours. Maintain a vacuum of 15 Pa, raise the temperature to -15°C, and dry for 22 hours; then raise the temperature to -5°C, and dry for 10 hours; finally raise the temperature to 25°C, and dry for 4 hours to obtain 10.32 g of white crystals, which contain The amount of water is 5.6% by weight.
Embodiment 3
[0060] In the Chinese patent document whose publication number is CN101845057, 13.0 g of a sample with a water content of 21%, add 130 ml of water / acetone (V / V=20:1) and stir at room temperature to dissolve completely, add an appropriate amount of activated carbon to decolorize for 15 minutes after fully dissolve, filter . The filtrate was placed in a material tray and pre-frozen in a freeze dryer at -8°C for 1.5 hours; then cooled to -30°C and kept for 2.5 hours; cooled to -60°C within 1 hour and kept for 3 hours. Maintain a vacuum of 20 Pa, raise the temperature to -20°C, and dry for 22 hours; then raise the temperature to -5°C, and dry for 10 hours; finally raise the temperature to 25°C, and dry for 4 hours to obtain 10.32 g of white crystals, which contain The amount of water is 5.5% by weight.
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